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www.MedChemExpress.com 1 Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com Cell Cycle/DNA Damage Cell Cycle includes many processes necessary for successful self-replication, and consists of DNA synthesis (S) and mitosis (M) phases separated by gap phases in the order G1–S–G2–M. S phase and M phase are usually separated by gap phases called G1 and G2, when cell-cycle progression can be regulated by various intracellular and extracellular signals. In order to move from one phase of its life cycle to the next, a cell must pass through numerous checkpoints. At each checkpoint, specialized proteins determine whether the necessary conditions exist. Progression through G1 phase is controlled by pRB proteins, and phosphorylation of pRB proteins by CDKs releases E2F factors, promoting the transition to S phase. The G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition, many proteins, such Wee1, PLK1 and cdc25, is involved the regulation of this process. The best-understood checkpoints are those activated by DNA damage and problems with DNA replication. DNA damage response (DDR) is a series of regulatory events including DNA damage, cell-cycle arrest, regulation of DNA replication, and repair or bypass of DNA damage to ensure the maintenance of genomic stability and cell viability. Genome instability arises if cells initiate mitosis when chromosomes are only partially replicated or are damaged by a double-strand DNA break (DSB). To prevent cells with damaged DNA from entering mitosis, ATR inhibits cyclin B/Cdk1 activation by stimulating the Cdk1 inhibitory kinase Wee1 and inhibiting Cdc25C via Chk1, besides, ATM and ATR also initiate DNA repair by phosphorylating several other substrates. In cancer cells, the cell cycle regulators as well as other elements of the DDR pathway have been found to protect tumor cells from different stresses and to promote tumor progression. Thus, cell cycle proteins that directly regulate cell cycle progression (such as CDKs), as well as checkpoint kinases, Aurora kinases and PLKs, are promising targets in cancer therapy. References: [1] Rhind N, et al. Cold Spring Harb Perspect Biol. 2012 Oct; 4(10): a005942. [2] Duronio RJ, et al. Cold Spring Harb Perspect Biol. 2013 Mar; 5(3): a008904. [3] Liu W, et al. Mol Cancer. 2017 Mar 14;16(1):60.
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Page 1: Cell Cycle/DNA Damage - MedchemExpress.com · 2019. 7. 2. · G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition,

wwwMedChemExpresscom 1

Inhibitors Agonists Screening LibrarieswwwMedChemExpresscom

Cell CycleDNA Damage

Cell Cycle includes many processes necessary for successful self-replication and consists of DNA synthesis (S) and mitosis(M) phases separated by gap phases in the order G1ndashSndashG2ndashM S phase and M phase are usually separated by gap phasescalled G1 and G2 when cell-cycle progression can be regulated by various intracellular and extracellular signals In orderto move from one phase of its life cycle to the next a cell must pass through numerous checkpoints At each checkpointspecialized proteins determine whether the necessary conditions exist Progression through G1 phase is controlled by pRBproteins and phosphorylation of pRB proteins by CDKs releases E2F factors promoting the transition to S phase TheG2M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1S transitionmany proteins such Wee1 PLK1 and cdc25 is involved the regulation of this process The best-understood checkpointsare those activated by DNA damage and problems with DNA replicationDNA damage response (DDR) is a series of regulatory events including DNA damage cell-cycle arrest regulation of DNAreplication and repair or bypass of DNA damage to ensure the maintenance of genomic stability and cell viabilityGenome instability arises if cells initiate mitosis when chromosomes are only partially replicated or are damaged by adouble-strand DNA break (DSB) To prevent cells with damaged DNA from entering mitosis ATR inhibits cyclin BCdk1activation by stimulating the Cdk1 inhibitory kinase Wee1 and inhibiting Cdc25C via Chk1 besides ATM and ATR alsoinitiate DNA repair by phosphorylating several other substratesIn cancer cells the cell cycle regulators as well as other elements of the DDR pathway have been found to protect tumorcells from different stresses and to promote tumor progression Thus cell cycle proteins that directly regulate cell cycleprogression (such as CDKs) as well as checkpoint kinases Aurora kinases and PLKs are promising targets in cancertherapy References[1] Rhind N et al Cold Spring Harb Perspect Biol 2012 Oct 4(10) a005942[2] Duronio RJ et al Cold Spring Harb Perspect Biol 2013 Mar 5(3) a008904[3] Liu W et al Mol Cancer 2017 Mar 1416(1)60

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bull Nucleoside AntimetaboliteAnalog 104

bull p97 111

bull PAK 113

bull PARP 116

bull PERK 122

bull Polo-like Kinase (PLK) 124

bull PPAR 128

bull RAD51 137

bull ROCK 139

bull Sirtuin 144

bull SRPK 149

bull Telomerase 151

bull TOPK 153

bull Topoisomerase 155

bull Wee1 163

bull Antifolate 3

bull APC 7

bull ATMATR 9

bull Aurora Kinase 12

bull Casein Kinase 17

bull CDK 20

bull Checkpoint Kinase (Chk) 34

bull CRISPRCas9 37

bull Deubiquitinase 39

bull DNA AlkylatorCrosslinker 43

bull DNA-PK 48

bull DNARNA Synthesis 52

bull Eukaryotic Initiation Factor (eIF) 60

bull G-quadruplex 62

bull Haspin Kinase 64

bull HDAC 66

bull HSP 77

bull IRE1 83

bull Kinesin 86

bull LIM Kinase (LIMK) 89

bull MicrotubuleTubulin 91

bull Mps1 101

Inhibitors Agonists Screening LibrarieswwwMedChemExpresscom

Target List in Cell CycleDNA Damage

Antifolate

Antifolates are compounds that antagonise the actions of folic acid(vitamin B9) Folic acids primary function in the body is as a cofactorto various methyltransferases involved in serine methioninethymidine and purine biosynthesis Consequently antifolates inhibitcell division DNARNA synthesis and repair and protein synthesisSome such as Proguanil Pyrimethamine and Trimethoprim selectivelyinhibit folates actions in microbial organisms such as bacteriaprotozoa and fungi The majority of antifolates work by inhibitingdihydrofolate reductase (DHFR) Many are primarily DHFR inhibitorsbut Raltitrexed is an inhibitor of thymidylate synthase andPemetrexed inhibits both and a third enzyme Antifolates act

specifically during DNA and RNA synthesis and thus are cytotoxic during the S-phase of the cell cycle Thus they havea greater toxic effect on rapidly dividing cells

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Purity 9517Clinical Data LaunchedSize 10 mg 50 mg

Purity 9524Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg 1 g 2 g

Purity 9973Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9973Clinical Data LaunchedSize 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Antifolate Inhibitors amp Modulators

Bioactivity Calcium N5-methyltetrahydrofolate(NSC173328) is the calciumsalt of levomefolic acid which has been proposed fortreatment of cardiovascular disease and advanced cancers suchas breast and colorectal cancers

Bioactivity Cycloguanil D6 is the deuterium labeled Cycloguanil which isa dihydrofolate reductase inhibitor

Bioactivity Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanilwhich is a dihydrofolate reductase inhibitor

Bioactivity Diaveridine (EGIS-5645) is a ( )dihydrofolate reductase DHFRinhibitor with a of 115 nM for the wild type DHFR and alsoKian antibacterial agent

Bioactivity EC0489 a conjugate of folic acid and desacetyl vinblastinehydrazide is a high-affinity ligand for the folate receptor(FR) Refractory or metastatic Tumor Small molecule-drug[1]

conjugate (SMDC) [2]

Bioactivity Folinic acid is an adjuvant used in cancer chemotherapyinvolving the drug methotrexate Target Antifolate Folinicacid is a 5-formyl derivative of tetrahydrofolic acid It isreadily converted to other reduced folic acid derivatives(eg tetrahydrofolate) and thus has vitamin activity thathellip

Bioactivity Leucovorin Calcium is a reduced folic acid IC50 Value 30 μMfor zcSHMT and70 μM for zmSHMT [2] Target Antifolate invitro Increasing concentrations of leucovorin (N5-CHO-THF)inhibit both zcSHMT and hcSHMT activities substantially yetto a lesser extent than zmSHMT The IC50 of leucovorin ishellip

Bioactivity Folinic Acid is a reduced folic acid which is used incombination with other chemotherapy drugs Target Folateanalog Approved 2008 Folinic acid (calcium salt pentahydrate)is the calcium salt form of folinic acid which is one of theforms of folate found naturally in foods Folate deficiency ishellip

Bioactivity Levoleucovorin calcium is the calcium salt of Levoleucovorinwhich is the enantiomerically active form of folinic acidIC50 value Target Levoleucovorin is used to treat or preventtoxic effects of methotrexate in people who have receivedmethotrexate to treat bone cancer Levoleucovorin is also usedhellip

Bioactivity Levomefolate is an artificial form of folate IC50 ValueTarget Antifolate The calcium salt ofL-5-methyltetrahydrofolic acid which belongs to the group offolate vitamins (Vitamin B9 Folacin) It is a coenzymatedform of folic acid and a more bioavailable alternative inhellip

Calcium N5-methyltetrahydrofolate (NSC173328) Cat No HY-17557

Cycloguanil D6 (Chlorguanide triazine D6) Cat No HY-12784S

Cycloguanil D6 Nitrate (Chlorguanide triazine D6 Nitrate) Cat No HY-12784S1

Diaveridine (EGIS-5645) Cat No HY-B1902

EC0489 Cat No HY-114306

Folinic acid (leucovorin) Cat No HY-17556

Folinic acid Calcium (Leucovorin Calcium Calcium Folinate) Cat No HY-13664

Folinic acid calcium salt pentahydrate (Leucovorin calcium salt pentahydrate) Cat No HY-B0080

Levoleucovorin Calcium (Calcium levofolinate CL307782) Cat No HY-13667

Levomefolate calcium Cat No HY-17383

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9923Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg

Purity 9977Clinical Data LaunchedSize 10mM x 1mL in Water

50 mg 100 mg 200 mg

Purity 9930Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity LY 254155 an antifolate inhibits and binds tohGARFT with s of 21plusmn02 and 17plusmn01 nM respectivelymFBP Ki

Bioactivity LY309887 is a potent inhibitor of glycinamide ribonucleotideformyltransferase ( ) with a of 65 nM and hasGARFT Kiantitumor activity

Bioactivity Methotrexate is a antagonist with median of 78 nMfolate IC50in assayin vitro

Bioactivity Pemetrexed is a novel the values of theantifolate Kipentaglutamate of LY231514 are 13 72 and 65 nM forinhibits thymidylate synthase ( ) dihydrofolate reductaseTS( ) and glycinamide ribonucleotide formyltransferase (DHFR

) respectivelyGARFT

Bioactivity Pemetrexed disodium is a novel that inhibits theantifolatefolatedependent enzymes thymidylate synthase dihydrofolate

and reductase glycinamide ribonucleotide with s of 13 72 and 65 nMformyltransferase Ki

respectively

Bioactivity Pemetrexed disodium hemipenta hydrate is a novel antifolatethe values of the pentaglutamate of LY231514 are 13 72Kiand 65 nM for inhibits thymidylate synthase ( )TSdihydrofolate reductase ( ) and glycinamideDHFRribonucleotide formyltransferase ( ) respectivelyGARFT

Bioactivity Pralatrexate(Folotyn) is an antifolate and structurally afolate analog Its IC50 is lt 300 nM in some cell linesIC50 Value lt 300 nM Target Antifolate Pralatrexate is anantifolate (a folate analogue metabolic inhibitor) designed toaccumulate preferentially in cancer cells Based onhellip

Bioactivity Pyrimethamine(RP4753) is a medication used for protozoalinfections interferes with tetrahydrofolic acid synthesisfrom folic acid by inhibiting the enzyme dihydrofolatereductase (DHFR) IC50 Value 154 nM (Plasmodium falciparum)[1] Target DHFR antifolate in vitro Three susceptibilityhellip

Bioactivity Trimethoprim is a bacteriostatic antibiotic used mainly in theprophylaxis and treatment of urinary tract infections

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LY 254155 Cat No HY-14523

LY309887 Cat No HY-10818

Methotrexate (Amethopterin CL14377 WR19039) Cat No HY-14519

Pemetrexed (LY231514) Cat No HY-10820

Pemetrexed disodium (LY231514 disodium) Cat No HY-10820A

Pemetrexed disodium hemipenta hydrate (LY231514 (disodium hemipenta hydrate)) Cat No HY-13781

Pralatrexate Cat No HY-10446

Pyrimethamine (Pirimecidan Pirimetamin RP 4753) Cat No HY-18062

Trimethoprim Cat No HY-B0510

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APCAnaphase promoting complex

APC (Anaphase-Promoting Complex) is an E3 ubiquitin ligase thatmarks target cell cycle proteins for degradation by the 26Sproteasome The APCC is a large complex of 11ndash13 subunit proteinsincluding a cullin (Apc2) and RING (Apc11) subunit much like SCF TheAPCCs main function is to trigger the transition from metaphase toanaphase by tagging specific proteins for degradation The twoproteins of most importance that get degraded in this process assubstrates of the APCC are securin and S and M cyclins Securinreleases separase a protease after being degraded which in turntriggers the cleavage of cohesin the protein complex that binds sisterchromatids together During metaphase sister chromatids are linked

by intact cohesin complexes When securin undergoes ubiquitination by the APCC and releases separase whichdegrades cohesin sister chromatids become free to move to opposite poles for anaphase The APCC also targets themitotic cyclins for degradation resulting in the inactivation of M-CdK (mitotic cyclin-dependent kinase) complexespromoting exit from mitosis and cytokinesis

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9911Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

APC Inhibitors amp Modulators

Bioactivity TAME is a inhibitor and can be also utilizedserine proteaseas a substrate for the serine proteases trypsin plasmin andthrombin TAME is an inhibitor of[1] [2] [3]

which binds to the hellipanaphase-promoting complex (APC)

Bioactivity TAME hydrochloride is a inhibitor and can beserine proteasealso utilized as a substrate for the serine proteases trypsinplasmin and thrombin TAME hydrochloride is an[1] [2] [3]

inhibitor of which bihellipanaphase-promoting complex (APC)

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TAME Cat No HY-13255

TAME hydrochloride Cat No HY-13255A

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ATMATRAtaxia telangiectasia mutatedATM and RAD3 related

ATMATR are members of the PI3 family of serine-threonine kinasesand function as essential links between the sensors and effectors ofthe DNA damage response The roles of ATM and ATR partiallyoverlap and are cooperative however they are also known to playdistinct roles in protecting the cell from DNA damage ATM is mostlyresponsible for sending signals from DSBs (double-strand breaks)induced by ionizing radiation while the closely related ATR respondsto UV damage or stalled replication forks ATM and ATR are known tophosphorylate common as well as specific substrates to activatecheckpoint signaling The G1 S and G2 cell cycle checkpoints areprimarily regulated by the ATM (ataxia telangiectasia mutated) and

ATR (ATM and Rad3-related) protein kinases

Purity 9976Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9904Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9960Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

ATMATR Inhibitors amp Modulators

Bioactivity ATM Inhibitor-1 is a highly potent selective and orallyactive inhibitor with an of 07 nM shows weakATM IC50activity against mTOR (IC 21 μM) DNAPK (IC 28 μM)50 50PI3Kα (IC 38 μM) PI3Kβ (IC 103 μM) PI3Kγ hellip50 50

Bioactivity ATR inhibitor 1 is a inhibitor extracted from patentATRWO2015187451A1 compound I-l has a value below 1 microΜ Ki

[1]

Bioactivity AZ20 is a potent and selective inhibitor of with an ATR IC50of 5 nM and has 8-fold selectivity against (IC =38mTOR 50nM)

Bioactivity AZ32 is an orally bioavailable and blood-brainbarrier-penetrating inhibitor with an of lt62ATM IC50nM for ATM enzyme and an of 031 μM for ATM in cellIC50

Bioactivity AZD0156 is an oral potent and selective inhibitor withATMan of 058 nMIC50

Bioactivity AZD1390 is an inhibitorATM

Bioactivity BAY-1895344 is a potent orally available and selective ATRinhibitor with of 7 nM Anti-tumor activity IC50

[1]Bioactivity BAY-1895344 hydrochloride is a potent orally available and

selective inhibitor with of 7 nM Anti-tumorATR IC50

activity [1]

Bioactivity Berzosertib (VE-822) is an inhibitor with a value ofATR Kiless than 02 nM It also inhibits with a of 34 nMATM Ki

Bioactivity Ceralasertib (AZD6738) is a potent inhibitor of kinaseATRwith an of 1 nMIC50

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ATM Inhibitor-1 Cat No HY-112614

ATR inhibitor 1 Cat No HY-111451

AZ20 Cat No HY-15557

AZ32 Cat No HY-112305

AZD0156 Cat No HY-100016

AZD1390 Cat No HY-109566

BAY-1895344 Cat No HY-101566

BAY-1895344 hydrochloride Cat No HY-101566A

Berzosertib (VE-822 VX-970) Cat No HY-13902

Ceralasertib (AZD6738) Cat No HY-19323

wwwMedChemExpresscom 11

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9947Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9988Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9840Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity CGK733 is a potent inhibitor used for the researchATMATRof cancer

Bioactivity CP-466722 is a rapidly reversible inhibitor of with anATM of 41 μM and has no effects on PI3K or closely relatedIC50

PI3K-like protein kinase (PIKK) family members

Bioactivity ETP-46464 is an effective and inhibitor withmTOR ATRs of 06 and 14 nM respectivelyIC50

Bioactivity KU 59403 is a potent inhibitor with an of 3 nMATM IC50

Bioactivity KU-55933 is a potent inhibitor with an and ofATM IC50 Ki129 and 22 nM respectively and is highly selective for ATMas compared to DNA-PK PI3KPI4K ATR and mTOR

Bioactivity KU-60019 is an improved kinase-specific inhibitor withATM of 63 nMIC50

Bioactivity VE-821 is a potent ATP-competitive inhibitor of with ATR Ki of 13 nM26 nMIC50

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

CGK733 Cat No HY-15520

CP-466722 Cat No HY-11002

ETP-46464 Cat No HY-15521

KU 59403 Cat No HY-18650

KU-55933 Cat No HY-12016

KU-60019 Cat No HY-12061

VE-821 Cat No HY-14731

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

Aurora Kinase

Aurora kinases are serinethreonine kinases that are essential for cellproliferation Aurora kinase helps the dividing cell dispense its geneticmaterials to its daughter cells More specifically Aurora kinases play acrucial role in cellular division by controlling chromatid segregationDefects in this segregation can cause genetic instability a conditionwhich is highly associated with tumorigenesis Three Aurora kinaseshave been identified in mammalian cells to date Aurora A Aurora BAurora C Besides being implicated as mitotic regulators these threekinases have generated significant interest in the cancer research fielddue to their elevated expression profiles in many human cancers Thehuman Aurora kinases present a similar domain organization with a

N-terminal domain of 39 to 129 residues in length a protein kinase domain and a short C-terminal domain containing15 to 20 residues The N-terminal domain of three proteins share low sequence conservation which determinesselectivity during protein-protein interactions

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Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9895Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9874Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Aurora Kinase Inhibitors amp Modulators

Bioactivity Alisertib (MLN 8237) is an oral active and selective Aurora A inhibitor with an of 12 nMkinase IC50

Bioactivity AMG 900 is a potent and highly selective kinasespan-Aurorainhibitor with of 5 nM 4 nM and 1 nM for IC50 Aurora A B

and respectivelyC

Bioactivity AT9283 is a multitargeted kinase inhibitor which potentlyinhibits ( =12 nM 11 nM)aurora kinase AB JAK23 IC50

Bioactivity Aurora A inhibitor I is a potent and highly selective Aurora inhibitor with with an of 34 nMA IC50

Bioactivity Aurora B inhibitor 1 is an (Aurora-1) inhibitorAurora Bextracted from patent WO2007059299A1 compound 1-3 has a Kivalue of lt0010 uM

Bioactivity Aurora inhibitor 1 is a potent inhibitor with an Aurora IC50of le 4 nM and le13 nM for and kinaseAurora A Aurora Brespectively [1]

Bioactivity AZD1152 is a pro-drug of Barasertib-hQPA which is a highlyselective inhibitor with of 037 nM in aAurora B IC50cell-free assay

Bioactivity AZD1152-HQPA is a highly selective Aurora inhibitor with an of 037 nM in aB IC50

cell-free assay and shows 3700-fold selectivity for Aurora Bover Aurora A

Bioactivity BI-847325 is an ATP competitive dual inhibitor of andMEKaurora kinases ( ) with values of 4 and 15 nM forAK IC50human MEK2 and AK-C respectively

Bioactivity CCT 137690 is a potent and orally available kinaseaurorainhibitor with s of 15 25 and 19 nM for aurora A B andIC50C respectively

Alisertib (MLN 8237) Cat No HY-10971

AMG 900 Cat No HY-13253

AT9283 Cat No HY-50514

Aurora A inhibitor I Cat No HY-70061

Aurora B inhibitor 1 Cat No HY-U00304

Aurora inhibitor 1 Cat No HY-111506

AZD1152 (Barasertib) Cat No HY-10127

Barasertib-HQPA (AZD2811 INH-34 AZD1152-HQPA) Cat No HY-10126

BI-847325 Cat No HY-18955

CCT 137690 Cat No HY-10804

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 1 mg 5 mg 10 mg 20 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9859Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9923Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9944Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data Phase 1Size 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 950Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity CCT129202 is an kinase inhibitor with s of 42aurora IC50198 and 227 nM for aurora A B and C respectively

Bioactivity CCT241736 is a potent and orally bioavailable dual andFLT3 inhibitor which inhibits Aurora kinasesAurora kinase

(Aurora-A 75 nM 38 nM Aurora-B 48 nM)Kd IC50 KdFLT3 kinase ( 62 nM) and FLT3 mutants includhellipKd

Bioactivity CYC-116 is a potent and inhibitor withaurora A aurora Bs of 8 and 9 nM respectivelyKi

Bioactivity Danusertib is a pyrrolo-pyrazole and inhibitoraurora kinasewith of 13 79 and 61 nM for Aurora A B and CIC50respectively

Bioactivity ENMD-2076 is a multi-targeted kinase inhibitor with s ofIC50186 14 582 159 927 708 564 nM for Aurora A Flt3

KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src PDGFRαrespectively

Bioactivity ENMD-2076 Tartrate is a multi-targeted kinase inhibitor withs of 186 14 582 159 927 708 564 nM for IC50 Aurora

A Flt3 KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src respectivelyPDGFRα

Bioactivity GSK-1070916 is a potent and selective ATP-competitiveinhibitor of and with s of 038 andaurora B aurora C Ki15 nM respectively and is gt250- fold selective overAurora A

Bioactivity Hesperadin is an ATP-competitive inhibitor of aurora Bkinase with an of 250 nMIC50

Bioactivity Ilorasertib (ABT-348) is an ATP-competitive multitargetedkinase inhibitor with s for inhibiting binding Aurora B (7IC50nM) C (1 nM) and A (120 nM) and also inhibits RET tyrosinekinase PDGFRβ and Flt1 with s of 7 nM 3 nM and 32 nMIC50

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

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CCT129202 Cat No HY-12049

CCT241736 Cat No HY-18161

CYC-116 Cat No HY-10558

Danusertib (PHA-739358) Cat No HY-10179

ENMD-2076 Cat No HY-10987A

ENMD-2076 Tartrate Cat No HY-10987

GSK-1070916 (GSK-1070916A) Cat No HY-70044

Hesperadin Cat No HY-12054

Ilorasertib (ABT-348) Cat No HY-16018

JNJ-7706621 Cat No HY-10329

wwwMedChemExpresscom 15

Purity 9820Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9928Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9911Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity KW-2449 is a multi-targeted kinase inhibitor of FLT3 ABL and with s of 66 14 4 and 48 nMABLT315I Aurora kinase IC50

respectively

Bioactivity LY3295668 is a potent orally active and highly specific inhibitor with values of 08 nM and 1038Aurora-A kinase Ki

nM for AurA and AurB respectively

Bioactivity MK-5108 is a highly potent and specific inhibitor of Aurora A with an value of 0064 nMkinase IC50

Bioactivity MK-8745 is an kinase inhibitor with an of 06aurora A IC50nM

Bioactivity MLN8054 is a potent selective and orally available aurora Akinase inhibitor with an of 4 nMIC50

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity PF-03814735 is a potent orally available and reversible and inhibitor with s of 08 and 05aurora A aurora B IC50

nM respectively

Bioactivity PHA-680632 is an kinase inhibitor with s of 27aurora IC50135 and 120 nM for aurora A B and C respectively

Bioactivity Reversine is a novel class of ATP-competitive Aurora kinaseinhibitor with s of 400 500 and 400 nM for IC50 Aurora A

and respectivelyAurora B Aurora C

Bioactivity SCH-1473759 is an inhibitor with s of 4 and 13 nMaurora IC50for aurora A and B respectively

KW-2449 Cat No HY-10339

LY3295668 (AK-01) Cat No HY-114258

MK-5108 (VX-689) Cat No HY-13252

MK-8745 Cat No HY-13819

MLN8054 Cat No HY-10180

NU6140 Cat No HY-107419

PF-03814735 Cat No HY-14574

PHA-680632 Cat No HY-10178

Reversine Cat No HY-14711

SCH-1473759 Cat No HY-10482

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg

Purity 9980Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity SCH-1473759 hydrochloride is an inhibitor with saurora IC50of 4 and 13 nM for aurora A and B respectively

Bioactivity SNS-314 is a potent and selective kinase inhibitoraurorawith s of 9 31 and 6 nM for aurora A B and CIC50respectively

Bioactivity TAK-632 is a potent inhibitor with of 14 24pan-RAF IC50

and 83 nM for respectivelyCRAF BRAFV600E BRAFWT

Bioactivity TAK-901 is a multi-targeted inhibitor with s of 21aurora IC50and 15 nM for aurora A and B respectively

Bioactivity Tozasertib (VX 680 MK-0457) is an inhibitor of Aurora ABC with s of 06 18 46 nM respectivelykinases Ki

Bioactivity XL228 is a multi-targeted tyrosine kinase inhibitor with sIC50of 5 31 16 61 2 nM for Bcr-Abl Aurora A IGF-1R Srcand respectivelyLyn

Bioactivity ZM-447439 is an kinase inhibitor with s of 110 andaurora IC50130 nM for aurora A and B respectively

16 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SCH-1473759 hydrochloride Cat No HY-10483

SNS-314 (SNS-314 Mesylate) Cat No HY-12003

TAK-632 Cat No HY-15767

TAK-901 Cat No HY-12201

Tozasertib (VX 680 MK-0457) Cat No HY-10161

XL228 Cat No HY-15749

ZM-447439 Cat No HY-10128

wwwMedChemExpresscom 17

Casein Kinase

Casein Kinases (CKs) are serinethreonine-selective enzymes thatfunction as regulators of signal transduction pathways in mosteukaryotic cell types

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9992Clinical Data Phase 2Size 1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Casein Kinase Inhibitors amp Modulators

Bioactivity Casein Kinase II Inhibitor IV is a small-molecule inducer ofepidermal keratinocyte differentiation

Bioactivity Casein Kinase II Inhibitor IV Hydrochloride is asmall-molecule inducer of epidermal keratinocytedifferentiation

Bioactivity CK1-IN-1 is a inhibitor extracted fromcasein kinase 1 (CK1)patent WO2015119579A1 compound 1c has s of 15 nM 16 nMIC50

73 nM for CK1δ and CK1ε p38σ MAPK respectively [1]

Bioactivity D4476 is a potent selective and cell-permeable inhibitor ofcasein kinase 1( ) with an value of 03 μM CK1 IC50 in vitro

Bioactivity DMAT is a potent and specific inhibitor with an CK2 IC50value of 130 nM

Bioactivity Ellagic acid is a natural antioxidant and acts as a potentand ATP-competitive inhibitor with an of 40 nM andCK2 IC50a of 20 nMKi

Bioactivity Emodin is a broad-spectrum anticancer agent Emodin inhibits II (CKII) activity with of 2 μMcasein kinase IC50

Bioactivity IC261 is a selective ATP-competitive inhibitor withCK1s of 1 μM 1 μM 16 μM for and Ckiα1IC50 Ckiδ Ckiε

respectively

Bioactivity LH846 is a selective inhibitor of with an of 290 nMCKIδ IC50and less potently inhibits CKIα and CKIε with s of 25 μMIC50and 13 μM respectively

Bioactivity Longdaysin is a and CK1α CK1δ extracellular inhibitor with s of  56signal-regulated kinase 2 (ERK2) IC50

microM 88 microM and 52 microM respectively [1] [2]

18 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Casein Kinase II Inhibitor IV Cat No HY-111378

Casein Kinase II Inhibitor IV Hydrochloride Cat No HY-111378A

CK1-IN-1 Cat No HY-111820

D4476 (Casein Kinase I Inhibitor) Cat No HY-10324

DMAT (Casein kinase II Inhibitor CK2 Inhibitor) Cat No HY-15535

Ellagic acid Cat No HY-B0183

Emodin (Frangula emodin) Cat No HY-14393

IC261 Cat No HY-12774

LH846 Cat No HY-15704

Longdaysin Cat No HY-18285

wwwMedChemExpresscom 19

Purity 9701Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9827Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Bioactivity NCC007 is a dual and inhibitorcasein kinase Iα (CKIα) δ (CKIδ)with s of 18 and 36 μM respectively and can be used inIC50

research of modulating mammalian circadian rhythms [1]

Bioactivity PF-4800567 is a potent and selective inhibitor of caseinkinase 1ϵ ( ) with an of 32 nM which is greaterCK1ϵ IC50than 20-fold selectivity over CK1δ ( 711 nM)IC50

Bioactivity PF-670462 is a potent and selective inhibitor of casein kinase with s of 77 nM and 14 nM( and )CK1ε CK1δ IC50

respectively

Bioactivity Silmitasertib (CX-4945) is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity Silmitasertib sodium salt is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity SR-3029 is a potent and ATP competitive and CK1δ CK1εinhibitor with s of 44 nM and 260 nM respectively andIC50

s of 97 nM for both kinasesKi

Bioactivity TA-01 is a potent and inhibitor with sCK1 p38 MAPK IC50of 64 nM 68 nM 67 nM for CK1ε CK1δ and p38 MAPKrespectively

Bioactivity TBB is a cell-permeable and ATP-competitive inhibitorCK2with an of 015 μM for rat liver CK2IC50

Bioactivity TTP 22 is a potent inhibitor with an of 100 nM andCK2 IC50a of 40 nMKi

NCC007 Cat No HY-128677

PF-4800567 Cat No HY-12470

PF-670462 Cat No HY-15490

Silmitasertib (CX-4945) Cat No HY-50855

Silmitasertib sodium salt (CX-4945 (sodium salt)) Cat No HY-50855B

SR-3029 Cat No HY-100011

TA-01 Cat No HY-100114

TBB (NSC 231634 Casein Kinase II Inhibitor I) Cat No HY-14394

TTP 22 Cat No HY-15479

CDKCyclin dependent kinase

CDKs (Cyclin-dependent kinases) are serine-threonine kinases firstdiscovered for their role in regulating the cell cycle They are alsoinvolved in regulating transcription mRNA processing and thedifferentiation of nerve cells CDKs are relatively small proteins withmolecular weights ranging from 34 to 40 kDa and contain little morethan the kinase domain In fact yeast cells can proliferate normallywhen their CDK gene has been replaced with the homologous humangene By definition a CDK binds a regulatory protein called a cyclinWithout cyclin CDK has little kinase activity only the cyclin-CDKcomplex is an active kinaseThere are around 20 Cyclin-dependent kinases (CDK1-20) known till

date CDK1 4 and 5 are involved in cell cycle and CDK 7 8 9 and 11 are associated with transcriptionCDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational Mostknowledge of CDK structure and function is based on CDKs of (Cdc2) (CDC28) and vertebratesS pombe S cerevisia(CDC2 and CDK2) The four major mechanisms of CDK regulation are cyclin binding CAK phosphorylation regulatoryinhibitory phosphorylation and binding of CDK inhibitory subunits (CKIs)

20 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 21

Purity 9815Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9969Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9973Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

CDK Inhibitors amp Modulators

Bioactivity (+)-BAY-1251152 is a inhibitor extracted from patent WOCDK92014076091 A1 example 1

Bioactivity (-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation(-) BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity (plusmn)-BAY-1251152 is a racemic mixture of BAY-1251152BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity 5-Iodo-indirubin-3-monoxime is a potent GSK-3β CDK5P25and inhibitor competing with ATP for binding toCDK1cyclin Bthe catalytic site of the kinase with s of 9 20 and 25IC50

nM respectively [1]

Bioactivity Abemaciclib (LY2835219) is a selective inhibitor withCDK46 values of 2 nM and 10 nM for CDK4 and CDK6 respectivelyIC50

Bioactivity Abemaciclib Metabolites M2 is a metabolite of abemaciclibacts as a potent and inhibitor with s in theCDK4 CDK6 IC50

range of 1-3 nM Anti-cancer activity [1]

Bioactivity Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is aselective inhibitor with s of 2 nM and 10 nM forCDK46 IC50CDK4 and CDK6 respectively

Bioactivity AMG 925 is a potent selective and orally available FLT3 dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMCDK4 IC50

respectively

Bioactivity AMG 925 HCl is a potent selective and orally available dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMFLT3 CDK4 IC50

respectively

Bioactivity AT7519 as a potent inhibitor of with s of 210 47CDKs IC50100 13 170 and lt10 nM for CDK1 CDK2 CDK4 to CDK6 andCDK9 respectively

(+)-BAY-1251152 Cat No HY-103019

(-)-BAY-1251152 Cat No HY-103019B

(plusmn)-BAY-1251152 Cat No HY-103019A

5-Iodo-indirubin-3-monoxime Cat No HY-111930

Abemaciclib (LY2835219) Cat No HY-16297A

Abemaciclib Metabolites M2 Cat No HY-128669

Abemaciclib methanesulfonate (LY2835219 (methanesulfonate)) Cat No HY-16297

AMG 925 Cat No HY-15889

AMG 925 HCl Cat No HY-15889A

AT7519 Cat No HY-50940

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 1Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9999Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9700Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9848Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9816Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity AT7519 Hydrochloride is a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity AT7519 trifluoroacetate as a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity Atuveciclib (BAY-1143572) is a potent and highly selectiveoral inhibitor Atuveciclib (BAY-1143572)PTEFb CDK9inhibits with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib Racemate (BAY-1143572 Racemate) is the racematemixture of Atuveciclib Atuveciclib is a potent and highlyselective oral inhibitor which supressesP-TEFb CDK9

with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is apotent and selective inhibitor which inhibits CDK9 CDK9

with an of 16 nMCycT1 IC50

Bioactivity AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 82nM AUZ 454 (K03861) inhibits CDK2 activity by competing withbinding of activating cyclins

Bioactivity AZD-5438 is a potent inhibitor of with of 16CDK129 IC50nM6 nM20 nM in cell-free assays AZD-5438 shows lessinhibition activity against GSK3β CDK5 and CDK6

Bioactivity AZD4573 is a inhibitor with an of lt3 nMCDK9 IC50extracted from patent US 20160376287 A1 example 14

Bioactivity BGG463 is a inhibitorCDK2 Bioactivity BI-1347 is a potent inhibitor extracted from patentCDK8WO2017202719A1 product I-003 has an of 11 nM IC50

[1]

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AT7519 Hydrochloride Cat No HY-50943

AT7519 trifluoroacetate Cat No HY-50940A

Atuveciclib (BAY-1143572) Cat No HY-12871B

Atuveciclib Racemate (BAY-1143572 Racemate) Cat No HY-12871

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) Cat No HY-12871C

AUZ 454 (K03861) Cat No HY-15004

AZD-5438 Cat No HY-10012

AZD4573 Cat No HY-112088

BGG463 Cat No HY-100600

BI-1347 Cat No HY-120350

wwwMedChemExpresscom 23

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9754Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9747Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity BMS-265246 is a potent and selective CDK12 inhibitor forCDK1cyclin B and CDK2cyclin E with IC50 of 6 nM and 9 nMrespectively

Bioactivity BS-181 is a highly selective inhibitor with an ofCDK7 IC5021 nM showing 40-fold selective over CDK1 2 4 5 6 or 9

Bioactivity BS-181 hydrochloride is a highly selective inhibitorCDK7with of 21 nM and gt 40-fold selective for CDK7 thanIC50CDK1 2 4 5 6 or 9

Bioactivity BSJ-03-123 is a potent and novel -selective small-moleculeCDK6degrader

Bioactivity Ca channel agonist 1 is an agonist of 2+ N-type Ca channel2+

and an inhibitor of with s of 1423 μM and 334Cdk2 EC50μM respectively and is used as a potential treatment formotor nerve terminal dysfunction

Bioactivity CC-671 is a dual ( )TTK protein kinase CDC2-like kinase CLK2inhibitor with s of 0005 and 0006 μM for TTK and CLK2IC50respectively

Bioactivity CCT-251921 is a potent selective and orally bioavailable inhibitor with an of 23 nMCDK8 IC50

Bioactivity CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 oflt8 nM extracted from reference 1 example 4 IC50 Valuelt8 nM [1] Target CDK9 In vitro In vivo

Bioactivity CDK46-IN-2 is a potent and inhibitor extractedCDK4 CDK6from patent US20180000819A1 Compound 1 has s of 27 andIC50

16 nM for CDK4 and CDK6 respectively [1]

Bioactivity CDK461 Inhibitor is a inhibitor with s of 3 andCDK46 IC501 nM respectively

BMS-265246 Cat No HY-15275

BS-181 Cat No HY-13266

BS-181 hydrochloride Cat No HY-13266A

BSJ-03-123 Cat No HY-111556

Ca2+ channel agonist 1 Cat No HY-41076

CC-671 Cat No HY-108709

CCT-251921 Cat No HY-19984

CDK-IN-2 (CDK inhibitor II) Cat No HY-13033

CDK46-IN-2 Cat No HY-114339

CDK461 Inhibitor Cat No HY-112280

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9548Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CDK8-IN-1 is a potent and selective inhibitor with anCDK8 of 3 nMIC50

Bioactivity CDK8-IN-3 is an inhibitor of extracted from patentCDK8WO2016041618A1 compound example 17

Bioactivity CDK8-IN-4 is an inhibitor of extracted from patentCDK8WO2014090692A1 compound example 16 with an of 02 nMIC50

Bioactivity CDK819-IN-1 is a potent selective and oral bioavailable dual inhibitor with s of 046 nM 099 nM andCDK819 IC50

270 nM for CDK8 CDK19 and CDK9 respectively

Bioactivity CDK9 Antagonist-1 (compounds 11c) is a potent and selective degrader based on PROTAC with an of 17 μM in MCF-7CDK9 IC50

cell lines Natural product Wogonin binds ubiquitin E3 ligasecereblon (CRBN) via a linker to form PROTAC [1]

Bioactivity CDK9-IN-1 is a novel selective inhibitor for theCDK9treatment of HIV infection with an of 39 nM forIC50CDK9CycT1 extracted from reference compound 87

Bioactivity CDK9-IN-2 is a special cyclin-dependent kinase 9 ( )CDK9inhibitor extracted from patent WO2012131594A1 compoundCDKI(8) has an of 5 nM and 7 nM in H929 multipleIC50myeloma(MM) cell line (72 hours) and A2058 skin cell line (72hours) respectively

Bioactivity CDK9-IN-8 is a highly effective and selective inhibitorCDK9with an of 12 nMIC50

Bioactivity CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM showsselective toxicity to CLL cells(LD50=80 nM) versus normal Bcell and normal CD34+ cell(LD50gt20 uM) IC50 value 4 nM80nM(KiLD50) [1] Target CDK9 inhibitor in vitro CDKI-73 wascytotoxic to all of the CLL samples tested (n = 38) with ahellip

Bioactivity CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 () inhibitor with an IC of 2 nMCLK1 50

24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CDK8-IN-1 Cat No HY-103492

CDK8-IN-3 Cat No HY-111463

CDK8-IN-4 Cat No HY-111465

CDK819-IN-1 Cat No HY-111427

CDK9 Antagonist-1 Cat No HY-112811

CDK9-IN-1 Cat No HY-13231

CDK9-IN-2 Cat No HY-16462

CDK9-IN-8 Cat No HY-102039

CDKI-73 Cat No HY-12445

CLK1-IN-1 Cat No HY-103082

wwwMedChemExpresscom 25

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9900Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9973Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9998Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CMPD 7 is a potent and selective inhibitor with an CDK12 IC50of 491 nM in enzymatic assay

Bioactivity CT7001 hydrochloride is a selective inhibitor withCDK7s of 41 nM and 578 nM for andIC50 CDK7CycHMAT1

respectivelyCDK2cycE1

Bioactivity Cucurbitacin E is a natural compound which from the climbingstem of Cucurbitacin E significantlyCucumic melo Lsuppresses the activity of the complexcyclin B1 CDC2

Bioactivity CVT-313 is a potent selective reversible andATP-competitive inhibitor of with of 05 μMCDK2 IC50

Bioactivity CYC065 is a second-generation orally availableATP-competitive inhibitor of kinasesCDK2 CDK 9

Bioactivity Dinaciclib is a potent inhibitor of with s of 1 1CDK IC503 and 4 nM for and respectivelyCDK2 CDK5 CDK1 CDK9

Bioactivity EHT 5372 is a strong inhibitor of family kinases withDYRKrsquos of 022 028 nM for DYRK1A and DYRK1B respectivelyIC s50

Bioactivity Flavopiridol is a broad spectrum and competitive inhibitor of inhibiting CDK1 CDK2 CDK4 with s of 30 170 100CDKs IC50

nM respectively

Bioactivity Flavopiridol Hydrochloride is a broad inhibitor of CDKcompeting with ATP to inhibit CDKs including CDK1 CDK2 CDK4with s of 30 170 100 nM respectivelyIC50

Bioactivity FMF-04-159-2 is a covalent inhibitor FMF-04-159-2CDK14inhibits CDK14 and CDK2 with s of 396 nM and 256 nM inIC50

NanoBRET assay respectively [1]

CMPD 7 Cat No HY-112261

CT7001 hydrochloride (ICEC0942 hydrochloride) Cat No HY-103712A

Cucurbitacin E (α-Elaterin α-Elaterine) Cat No HY-N0417

CVT-313 (Cdk2 Inhibitor III) Cat No HY-15339

CYC065 Cat No HY-101212

Dinaciclib (SCH 727965) Cat No HY-10492

EHT 5372 Cat No HY-111380

Flavopiridol (L868275 HMR-1275 Alvocidib) Cat No HY-10005

Flavopiridol Hydrochloride (HL 275 NSC 649890 MDL 107826A

FLAVOPIRIDOL HCL Alvocidib Hydrochloride) Cat No HY-10006

FMF-04-159-2 Cat No HY-127104

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9204Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 251 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9841Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity FN-1501 is a potent inhibitor of and with s ofFLT3 CDK IC50247 085 196 and 028 nM for CDK2cyclin A CDK4cyclinD1 CDK6cyclin D1 and FLT3 respectively FN-1501 hasanticancer activity

Bioactivity GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO) is apotent selective reversible and ATP-competitive inhibitor of

and complex with s of 5 nM320GSK-3αβ CDK1-cyclinB IC50nM80nM for (GSK-3αβ)CDK1CDK5 respectively

Bioactivity GSK3186899 is an inhibitor of cdc-2-related kinase 12 () with an of 14 μM for in anCRK12 EC50 L donovani

intra-macrophage assay

Bioactivity IIIM-290 is a potent and oral inhibitor with s of 90CDK IC50and 94 nM for CDK2A and CDK9T1

Bioactivity Indirubin-3-monoxime-5-sulphonic acid is a potent andselective inhibitor of and with s ofCDK1 CDK5 GSK-3β IC50

5 nM 7 nM and 80 nM respectively [1]

Bioactivity Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK)inhibitor with values of 55 nM 35 nM 150 nM 300 nMIC50and 65 nM for CDK1cyclin B CDK2cyclin A CDK2cyclin ECDK4cyclin D1 and CDK5p35 respectively [1]

Bioactivity JH-XI-10-02 is a potent and selective degrader of withCDK8an of 159 nM based on JH-XI-10-02 causesIC50 PROTAC

proteasomal degradation does not affect CDK8 mRNA levelsJH-XI-10-02 shows no effect on CDK19 [1]

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

Bioactivity JSH-150 is a highly selective and potent inhibitor withCDK9an IC of 1 nM50

Bioactivity Kenpaullone is a potent inhibitor of andCDK1cyclin B with s of 04 μM and 23 nM and also inhibitsGSK-3β IC50

CDK2cyclin A CDK2cyclin E and CDK5p25 with s of 068IC50μM 75 μM 085 μM respectively

26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

FN-1501 Cat No HY-111361

GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO MLS 2052) Cat No HY-10580

GSK3186899 (DDD-853651) Cat No HY-112622

IIIM-290 Cat No HY-111356

Indirubin-3-monoxime-5-sulphonic acid Cat No HY-111931

Indirubin-5-sulfonate Cat No HY-111932

JH-XI-10-02 Cat No HY-111518

JNJ-7706621 Cat No HY-10329

JSH-150 Cat No HY-X0150

Kenpaullone (9-Bromopaullone NSC-664704) Cat No HY-12302

wwwMedChemExpresscom 27

Purity 9861Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9847Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Bioactivity KH-CB19 is a potent and highly specific inhibitor of theCDC2-like kinase isoforms 1 and 4 (CLK1CLK4) IC50 value 20nM (CLK1) [1] Target CLK14 inhibitor in vitro KH-CB19showed potent inhibition of CLK1 with an IC50 of 20 nM andfor the pure isomer KH-CB19 almost 100-fold selectivityhellip

Bioactivity LDC000067 is a highly specific inhibitor with an CDK9 IC50value of 44plusmn10 nM in vitro

Bioactivity LDC4297 is a potent and selective inhibitor with an CDK7 IC50of 013 nM

Bioactivity Lerociclib (G1T38) is a potent and selective inhibitor of with of 1 nM 2 nM for CDK4CyclinD1 andCDK46 IC s50

CDK6CyclinD3 respectively

Bioactivity Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potentand selective inhibitor of with of 1 nMCDK4 CDK6 IC s50and 2 nM for and respectivelyCDK4 CyclinD1 CDK6 CyclinD3

Bioactivity LY2857785 is a type I reversible and competitive ATP kinaseinhibitor against ( 11 nM) and other transcriptionCDK9 IC50kinases ( 16 nM) and ( 246 nM)CDK8 IC50 CDK7 IC50

Bioactivity LY3177833 is an and inhibitor extracted fromCDC7 pMCM2patent US 20140275131and patent WO 2014143601 A1 compoundexample 4 has values of 33 nM and 290 nM respectivelyIC50

Bioactivity MBQ-167 is a dual inhibitor with of 103 nMRacCdc42 IC s50for Rac 123 and 78 nM for Cdc42 in MDA-MB-231 cellsrespectively

Bioactivity MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin inhibitor with an of 5 nM at least 22-fold moreT1 IC50

selective for CDK9 over other CDKs MC180295 also inhibitsGSK-3α and GSK-3β MC180295 ((rel)-MC180295) has pothellip

Bioactivity Milciclib (PHA-848125) is a potent dual inhibitor of andCDK with s of 45 150Tropomyosin receptor kinase (TRK) IC50

160 363 398 nM and 53 nM for cyclin ACDK2 cyclin HCDK7cyclin D1CDK4 cyclin ECDK2 cyclin BCDK1 and TRKArespectively

KH-CB19 Cat No HY-12828

LDC000067 (LDC067) Cat No HY-15878

LDC4297 Cat No HY-12653

Lerociclib (G1T38) Cat No HY-112272

Lerociclib dihydrochloride (G1T38 dihydrochloride) Cat No HY-112272A

LY2857785 Cat No HY-12293

LY3177833 Cat No HY-100023

MBQ-167 Cat No HY-112842

MC180295 ((rel)-MC180295) Cat No HY-119940

Milciclib (PHA-848125) Cat No HY-10424

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9703Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9851Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Bioactivity ML167 is a highly selective Cdc2-like kinase 4 ( )Clk4inhibitor with of 136 nM gt10-fold selectivity forIC50closely related kinases Clk1 Clk2 Clk3 and Dyrk1A1B

Bioactivity MSC2530818 is a potent selective and orally available CDK8inhibitor with an of 26 nM for CDK8IC50

Bioactivity NG 52 (Compound 52 ) is a potent cell-permeable reversibleselective and ATP-compatible inhibitor of the cellcycle-regulating kinase Cdc28p (IC50 = 7 μM) and the relatedPho85p kinase (IC50 = 2 μM)

Bioactivity Nimbolide is a triterpene derived from the leaves and flowersof neem ( L) Nimbolide induces apoptosisAzadirachta indicathrough inactivation of Nimbolide inhibits NF-κB CDK4

kinase activity Nimbolide suppresses the NF-κB WntCDK6PI3K-Akt MAPK and JAK-STAT signaling pathways [1]

Bioactivity NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and26 μM for CDK2 and CDK1 IC50 value 17μM (CDK2) 26μM (CDK1)Target CDK in vitro NU2058 is a competitive inhibitor ofCDK2 with respect to ATP (Ki value CDK2 12 3 μM) that bindsin the ATP binding pocket in a different orientation fromhellip

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity NU6300 is the first covalent ATP-competitive CDK2 inhibitorIC50 value Target CDK2 in vitro NU6300 is a covalent CDK2inhibitor that illustrates the potential of using vinylsulfones to mediate irreversible inhibition NU6300 blocks theinhibitor binding site The effect was time dependent andhellip

Bioactivity NVP-2 is a inhibitor with an of 05 nMCDK9 IC50

Bioactivity NVP-LCQ195 (AT9311 LCQ195) is a small molecule heterocyclicinhibitor of CDK1 CDK2 CDK3 and CDK5 with IC50 of 1-42 nM

Bioactivity ON-013100 an antineoplastic drug acts a mitotic inhibitorthat could inhibit expressionCyclin D1

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ML167 (CID44968231 NCGC00188654) Cat No HY-15951

MSC2530818 Cat No HY-101611

NG 52 (Compound 52) Cat No HY-15154

Nimbolide Cat No HY-116035

NU2058 (O6-(Cyclohexylmethyl)guanine) Cat No HY-19316

NU6140 Cat No HY-107419

NU6300 Cat No HY-18930

NVP-2 Cat No HY-12214A

NVP-LCQ195 (LCQ-195 AT9311) Cat No HY-15241

ON-013100 Cat No HY-112822

wwwMedChemExpresscom 29

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9996Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity ON123300 is a potent inhibitor of CDK4 with an IC50 of 38nM with little inhibitory activity against CDKs 125 and 8

Bioactivity Palbociclib (PD 0332991) is a selective and CDK4 CDK6inhibitor with s of 11 and 16 nM respectivelyIC50Palbociclib is a drug for the treatment of ER-positive andHER2-negative breast cancer

Bioactivity Palbociclib hydrochloride is a highly selective CDK46inhibitor with s of 11 nM and 16 nM respectivelyIC50

Bioactivity Palbociclib isethionate is a highly selective inhibitorof with s of 11 nM16 nMCDK46 IC50respectively

Bioactivity PF-06873600 is a selective and orally bioavailable inhibitorof cyclin-dependent kinase with values of 009 nM(CDK) Ki013 nM and 016 nM for CDK2 CDK4 and CDK6 respectivelyPF-06873600 has potential antineoplastic activity [1] [2]

Bioactivity PHA-767491 is a dual inhibitor with s of 10 nMCdc7Cdk9 IC50and 34 nM respectively

Bioactivity PHA-767491 hydrochloride is a dual inhibitor withCdc7Cdk9s of 10 nM and 34 nM respectivelyIC50

Bioactivity PHA-793887 is a potent ATP-competitive inhibitor canCDKinhibit Cdk2 Cdk1 Cdk4 and Cdk9 with s of 8 nM 60 nMIC5062 nM and 138 nM respectively and also inhibits glycogensynthase kinase 3β with an of 79 nMIC50

Bioactivity PROTAC CDK9 Degrader-1 is a selective degraderCDK9 Bioactivity Purvalanol A is a potent inhibitor which inhibitsCDKcdc2-cyclin B cdk2-cyclin A cdk2-cyclin E cdk4-cyclin D1and cdk5-p35 with s of 4 70 35 850 75 nMIC50resepctively

ON123300 Cat No HY-12624

Palbociclib (PD 0332991) Cat No HY-50767

Palbociclib hydrochloride (PD 0332991 hydrochloride) Cat No HY-50767A

Palbociclib isethionate (PD 0332991 isethionate) Cat No HY-A0065

PF-06873600 Cat No HY-114177

PHA-767491 (CAY10572) Cat No HY-13461

PHA-767491 hydrochloride (CAY-10572 hydrochloride) Cat No HY-13461A

PHA-793887 Cat No HY-11001

PROTAC CDK9 Degrader-1 Cat No HY-103628

Purvalanol A (NG-60) Cat No HY-18299A

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9900Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9983Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitorwith IC50 values of 6 6 9 gt 10000 and 6 nM forcdc2cyclin B cdk2cyclin A cdk2cyclin E cdk4cyclin D1and cdk5-p35 respectively

Bioactivity R547 is a potent ATP-competitive inhibitor of CDK124 with Kiof 2 nM3 nM1 nM

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity Ribociclib (LEE011) is a highly specific inhibitorCDK46with s of 10 nM and 39 nM respectivelyIC50

Bioactivity Ribociclib hydrochloride (LEE011 hydrochloride) is a highlyspecific inhibitor with values of 10 nM and 39CDK46 IC50nM respectively and is over 1000-fold less potent againstthe cyclin BCDK1 complex

Bioactivity Ribociclib succinate (LEE011 succinate) is a highly specific inhibitor with values of 10 nM and 39 nMCDK46 IC50

respectively and is over 1000-fold less potent against thecyclin BCDK1 complex

Bioactivity Ribociclib succinate hydrate (LEE011 succinate hydrate) is ahighly specific inhibitor with values of 10 nMCDK46 IC50and 39 nM respectively and is over 1000-fold less potentagainst the cyclin BCDK1 complex

Bioactivity Riviciclib (P276-00 free base) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib shows antituhellip[1] [2]

Bioactivity Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib hydrochlorhellip[1] [2]

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Purvalanol B (NG 95) Cat No HY-18299

R547 Cat No HY-10014

RGB-286638 Cat No HY-15504

RGB-286638 free base Cat No HY-15504A

Ribociclib (LEE011) Cat No HY-15777

Ribociclib hydrochloride (LEE011 (hydrochloride)) Cat No HY-15777A

Ribociclib succinate (LEE011 (succinate)) Cat No HY-15777B

Ribociclib succinate hydrate (LEE011 (succinate hydrate)) Cat No HY-15777C

Riviciclib (P276-00 (free base)) Cat No HY-16559A

Riviciclib hydrochloride (P276-00) Cat No HY-16559

wwwMedChemExpresscom 31

Purity 9850Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9907Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9677Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ro-3306 is a potent and selective inhibitor of with sCDK1 Kiof 20 nM 35 nM and 340 nM for CDK1 CDK1cyclin B1 andCDK2cyclin E respectively

Bioactivity Roniciclib is an orally bioavailable pan-cyclin dependentkinase inhibitor with of 5-25 nM for CDK1 CDK2(CDK) IC s50CDK3 CDK4 CDK7 and CDK9

Bioactivity SB1317 is a potent inhibitor of and forCDK2 JAK2 FLT3the treatment of cancer with of 13 73 and 56 nM forIC50CDK2 JAK2 and FLT3 respectively

Bioactivity SEL120-34A is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A HCl is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A monohydrochloride is an ATP-competitive andselective inhibitor inhibits kinase activities ofCDK8CDK8CycC and CDK19CycC complexes with s of 44 nM andIC50104 nM respectively with a of 3 nM for CDhellipKd

Bioactivity Seliciclib (Roscovitine) is a potent and selective CDKsinhibitor with s of 02 μM 065 μM and 07 μM for IC50 CDK5

and respectivelyCdc2 CDK2

Bioactivity Senexin A is a inhibitor with an of 280 nMCDK8 IC50

Bioactivity Simurosertib (TAK-931) is a selective cycle 7 kinase(CDC7)inhibitor with an lt03 nMIC50

Bioactivity SNS-032 (BMS-387032) is a selective inhibitor of CDK2 and with s of 38 nM 62 nM and 4CDK7 CDK9 IC50

nM respectively

Ro-3306 Cat No HY-12529

Roniciclib (BAY 1000394) Cat No HY-13914

SB1317 (TG02) Cat No HY-15166

SEL120-34A Cat No HY-111388

SEL120-34A HCl Cat No HY-111388B

SEL120-34A monohydrochloride Cat No HY-111388A

Seliciclib (Roscovitine CYC202 R-roscovitine) Cat No HY-30237

Senexin A Cat No HY-15681

Simurosertib (TAK-931) Cat No HY-100888

SNS-032 (BMS-387032) Cat No HY-10008

Purity 9846Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9796Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9882Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity SU9516 is a potent inhibitor with an of 22 nM andCDK2 IC50also shows inhibitory effects on CDK1 and CDK4 with s ofIC5040 200 nM respectively

Bioactivity SY-1365 is a highly selective covalent inhibitor of CDK7SY-1365 possesses therapeutic potential in both hematologicaland solid tumors [1]

Bioactivity T025 is an orally available and highly potent Cdc2-like kinase inhibitor with s of 48 0096 65 and 061 nM(CLK) Kd

for CLK1 CLK2 CLK3 and CLK4 respectively

Bioactivity THAL-SNS-032 is a selective degrader PROTAC consistingCDK9of a CDK-binding SNS-032 ligand linked to a thalidomidederivative that binds the E3 ubiquitin ligase Cereblon (CRBN)

[1]

Bioactivity THZ1 is a selective and potent covalent inhibitor withCDK7an of 32 nMIC50

Bioactivity THZ1 Hydrochloride is a selective and potent inhibitorCDK7with an of 32 nMIC50

Bioactivity THZ1-R is a non-cysteine reactive analog of THZ1 whichdisplays diminished activity for inhibition THZ1-RCDK7binds to with a of 142 nMCDK7 Kd

Bioactivity THZ2 is a potent and selective inhibitor with an ofCDK7 IC50139 nM

Bioactivity THZ531 is a covalent inhibitor of both and withCDK12 CDK13s of 158 nM and 69 nM respectivelyIC50

Bioactivity Trilaciclib is a inhibitor with s of 1 nM and 4 nMCDK46 IC50for CDK4 and CDK6 respectively

32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SU9516 Cat No HY-18629

SY-1365 Cat No HY-128587

T025 Cat No HY-112296

THAL-SNS-032 Cat No HY-123937

THZ1 Cat No HY-80013

THZ1 Hydrochloride Cat No HY-80013A

THZ1-R Cat No HY-19988

THZ2 Cat No HY-12280

THZ531 Cat No HY-103618

Trilaciclib (G1T28) Cat No HY-101467

wwwMedChemExpresscom 33

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Trilaciclib hydrochloride is a inhibitor with s ofCDK46 IC501 nM and 4 nM for CDK4 and CDK6 respectively

Bioactivity Voruciclib hydrochloride is a clinical stage oral CDK9inhibitor Voruciclib hydrochloride represses expression ofMCL-1 in multiple models of diffuse large B-cell lymphoma(DLBCL) [1]

Bioactivity Wogonin is a naturally occurring mono-flavonoid can inhibitthe activity of and and exhibitsCDK8 Wntanti-inflammatory and anti-tumor effects

Bioactivity XL413 is a potent selective and ATP competitive inhibitor of with an of 34 nM and also shows potent effectCdc7 IC50

with s of 215 42 nM on CK2 PIM1 respectively and anIC50 of 118 nM on pMCMEC50

Bioactivity XL413 hydrochloride is a potent selective and ATP competitiveinhibitor of with an of 34 nM and also showsCdc7 IC50potent effect with s of 215 42 nM on CK2 PIM1IC50respectively and an of 118 nM on pMCMEC50

Trilaciclib hydrochloride (G1T28 hydrochloride) Cat No HY-101467A

Voruciclib hydrochloride Cat No HY-12422A

Wogonin Cat No HY-N0400

XL413 Cat No HY-15260

XL413 hydrochloride Cat No HY-15260A

Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) are protein kinases that are involved in cellcycle control Two checkpoint kinase subtypes have been identifiedChk1 and Chk2 Chk1 is a central component of genome surveillancepathways and is a key regulator of the cell cycle and cell survivalChk1 is required for the initiation of DNA damage checkpoints andhas recently been shown to play a role in the normal (unperturbed)cell cycle Chk1 impacts various stages of the cell cycle including the Sphase G2M transition and M phase In addition to mediating cellcycle checkpoints Chk1 also contributes to DNA repair processesgene transcription embryo development cellular responses to HIVinfection and somatic cell viability Chk2 is a protein kinase that is

activated in response to DNA damage and is involved in cell cycle arrest In response to DNA damage and replicationblocks cell cycle progression is halted through the control of cell cycle regulators The protein encoded by this gene isa cell cycle checkpoint regulator and putative tumor suppressor

34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 35

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9877Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9990Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Checkpoint Kinase (Chk) Inhibitors amp Modulators

Bioactivity AZD-7762 is a potent ATP-competitive checkpoint kinase ( )Chkinhibitor in with an of 5 nM for Chk1IC50

Bioactivity BML-277 is a selective checkpoint kinase 2 ( ) inhibitorChk2with an of 15 nMIC50

Bioactivity CCT241533 is a potent and selective ATP competitive inhibitorof with an of 3 nM and of 116 nMCHK2 IC50 Ki

Bioactivity CCT241533 hydrochloride is a potent and selective CHK2inhibitor with an of 3 nM and a of 116 nMIC50 Ki

Bioactivity CCT244747 is a potent orally bioavailable and highlyselective inhibitor with an of 77 nM CCT244747CHK1 IC50also abrogates G2 checkpoint with an of 29 nMIC50

Bioactivity CCT245737 is a orally active and seletive inhibitorChk1with an of 13 nMIC50

Bioactivity CHIR-124 is a potent and selective inhibitor with Chk1 IC50of 03 nM and also potently targets and withPDGFR FLT3

s of 66 nM and 58 nMIC50

Bioactivity CHK-IN-1 is an inhibitor of and withCHK1 CHK2anti-proliferative activities

Bioactivity CHK1 inhibitor is an inhibitor of CHK1 Bioactivity CHK1-IN-2 is a checkpoint kinase 1 inhibitor with an(CHK1) of 6 nMIC50

AZD-7762 Cat No HY-10992

BML-277 (Chk2 Inhibitor II) Cat No HY-13946

CCT241533 Cat No HY-14715

CCT241533 hydrochloride Cat No HY-14715B

CCT244747 Cat No HY-18175

CCT245737 Cat No HY-18958

CHIR-124 Cat No HY-13263

CHK-IN-1 Cat No HY-U00345

CHK1 inhibitor Cat No HY-104022

CHK1-IN-2 Cat No HY-111369

Purity 9965Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9791Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity CHK1-IN-3 is a inhibitor with anCheckpoint Kinase 1 (CHK1) of 04 nM IC50

[1]Bioactivity GDC-0575 (ARRY-575 RG7741) is a highly-selective oral

small-molecule inhibitor with an of 12nMChk1 IC50

Bioactivity GDC-0575 dihydrochloride is an orally bioavailable CHK1inhibitor with an of 12 nM and has antitumor activityIC50

Bioactivity PF 477736 is a potent selective ATP-competitive inhibitor of with a of 049 nM 100-fold selectivity versus Chk1 Ki Chk2

( 47 nM)Ki

Bioactivity Prexasertib (LY2606368) is a potent selective andATP-competitive inhibitor with ancheckpoint kinase 1 (Chk1)

and a of lt1 nM and 09 nM respectivelyIC50 Ki

Bioactivity Prexasertib dihydrochloride (LY2606368 dihydrochloride) is apotent and selective ATP competitive inhibitor of the Chk1protein kinase with s of lt1 nM and 8 nM for CHK1 andIC50CHK2 respectively and a of 09 nM against purified CHK1Ki

Bioactivity Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is apotent selective ATP competitive and inhibitorCHK1 CHK2with a of 09 nM for CHK1 and s of lt1 nM 8 nM forKi IC50CHK1 and CHK2 respectively Prexasertib Mesylate Hydrateinhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2hellip

Bioactivity Rabusertib (LY2603618) is a potent and selective inhibitor of with an of 7 nMChk1 IC50

Bioactivity SCH900776 is a potent selective and oral inhibitor ofcheckpoint kinase1 ( ) with an of 3 nM It shows 50-Chk1 IC50and 500-fold selectivity over CDK2 andChk2 respectively

36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CHK1-IN-3 Cat No HY-128601

GDC-0575 (ARRY-575 RG7741) Cat No HY-112167

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride RG7741 dihydrochloride) Cat No HY-112167A

PF 477736 (PF 00477736) Cat No HY-10032

Prexasertib (LY2606368) Cat No HY-18174

Prexasertib dihydrochloride (LY2606368 (dihydrochloride)) Cat No HY-18174A

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate LY2940930) Cat No HY-18174B

Rabusertib (LY2603618 IC-83) Cat No HY-14720

SCH900776 (MK-8776) Cat No HY-15532

wwwMedChemExpresscom 37

CRISPRCas9

CRISPRCas9 (Clustered Regularly-Interspaced Short PalindromicRepeatsCas9) is a bacterial immune system that has been adaptedfor genome editing in mammalian cells Cas9 is a programmablenuclease that generates double-stranded breaks (DSB) in DNAdictated by binding of a ~20 nucleotide recombinant ldquoguide RNArdquo(gRNA) to the target site DSBrsquos produced by Cas9 are most oftenrepaired through the cellrsquos error-prone non-homologous end joining(NHEJ) pathway resulting in small insertions or deletions (indels) Thevast majority of indels shift the reading frame introducing apremature stop codon or resulting in nonsense mediated decay ofthe mRNA-effectively ldquoknocking outrdquo a gene

The CRISPRCas9 system has substantially advanced efforts in specific gene editing and has been successfully appliedto modify the episomal genomes of human and other organisms The CRISPRCas9 system utilizes a prokaryoticRNA-guided programmable nuclease that can make a double-strand DNA break (DSB) at a specific site under theguidance of a leading RNA This DSB process depends on the co-expression of two basic components a guide RNA(gRNA) and Cas9 nuclease Making a specific DSB can trigger DNA repair via either error-prone non-homologous endjoining (NHEJ) or homology-directed repair (HDR) In the presence of the CRISPRCas9 system the NHEJ inhibitorSCR7 is proven to increase the efficiency of Cas9-mediated HDR by at least by 7-fold in mammalian cells Genomeediting via CRISPRCas9 has become an efficient and reliable way to make precise targeted changes to the genome ofliving cells

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

CRISPRCas9 Inhibitors amp Modulators

Bioactivity Brefeldin A is a specific inhibitor of whichprotein traffickingblocks the protein transport from the endoplasmic reticulum tothe Golgi complex

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity L755507 is a potent selective agonist of with an β -AR3 IC50of 35 nM

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity Zidovudine is a nucleoside reverse transcriptase inhibitor () widely used to treat HIV infection Zidovudine increasesNRTI

CRISPRCas9-mediated editing frequency

38 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Brefeldin A (BFA Cyanein Decumbin) Cat No HY-16592

KU-57788 (NU7441) Cat No HY-11006

L755507 Cat No HY-19334

Nocodazole (Oncodazole R17934) Cat No HY-13520

RS-1 Cat No HY-19793

SCR7 Cat No HY-12742

Zidovudine (Azidothymidine AZT ZDV) Cat No HY-17413

wwwMedChemExpresscom 39

DeubiquitinaseDUBs

Deubiquitinases (DUBs) are a large group of proteases that cleaveubiquitin from proteins and other molecules Ubiquitin is attached toproteins in order to regulate the degradation of proteins via theproteasome and lysosome coordinate thecellular localisation ofproteins activate and inactivate proteins and modulateprotein-protein interactions DUBs can reverse these effects bycleaving the peptide or isopeptide bond between ubiquitin and itssubstrate protein In humans there are nearly 100 DUB genes whichcan be classified into two main classes cysteine proteases andmetalloproteases The cysteine proteases comprise ubiquitin-specificproteases (USPs) ubiquitin C-terminal hydrolases (UCHs)

Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU) The metalloprotease groupcontains only the Jab1Mov34Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases DUBs play several roles inthe ubiquitin pathway One of the best characterised functions of DUBs is the removal of monoubiqutin andpolyubiquitin chainsfrom proteins

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9940Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9892Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9893Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Deubiquitinase Inhibitors amp Modulators

Bioactivity 6-Thioguanine (Thioguanine) is an anti-leukemia andimmunosuppressant agent acts as an inhibitor of SARS and MERScoronavirus papain-like proteases ( ) and also potentlyPLprosinhibits activity with s of 25 μM and 40 μM forUSP2 IC50Plpros and recombinant human USP2 respectively

Bioactivity b-AP15 is a specific inhibitor of the enzymesdeubiquitinating and UCHL5 Usp14

Bioactivity BAY 11-7082 is a inhibitor which decreases NF-κB byNF-κBinhibiting TNF-α-induced phosphorylation of IκB-α BAY 11-7082inhibits ubiquitin-specific protease and withUSP7 USP21

s of 019 μM and 096 μM respectivelyIC50

Bioactivity C527 is a is a pan inhibitor with a highDUB enzymepotency for the complex ( =088 μM)USP1UAF1 IC50

Bioactivity Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB)inhibitor directly inhibiting DUB activity of USP9x USP5USP14 and UCH37 Degrasyn has been shown to downregulate theantiapoptotic proteins and Bcr-Abl JAK2

Bioactivity DUBs-IN-1 is an active inhibitor of ubiquitin-specific with an of 024 μM for USP8proteases (USPs) IC50

Bioactivity DUBs-IN-2 is a potent inhibitor with an ofdeubiquitinase IC50028 μM for USP8

Bioactivity DUBs-IN-3 is a potent enzyme inhibitordeubiquitinase (USP)extracted from reference compound 22c with an of 056 μMIC50for USP8

Bioactivity EOAI3402143 is a ( ) inhibitor whichdeubiquitinase DUBinhibits dose-dependently inhibits and Usp9x Usp24 Usp5

Bioactivity FT671 is a potent non-covalent and selective inhibitorUSP7with an of 52 nM and binds to the USP7 catalytic domainIC50with a of 65 nMKd

40 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

6-Thioguanine (Thioguanine2-Amino-6-purinethiol) Cat No HY-13765

b-AP15 (NSC 687852) Cat No HY-13989

BAY 11-7082 (BAY 11-7821) Cat No HY-13453

C527 Cat No HY-12988

Degrasyn (WP1130) Cat No HY-13264

DUBs-IN-1 Cat No HY-50736

DUBs-IN-2 Cat No HY-50737A

DUBs-IN-3 Cat No HY-50737

EOAI3402143 Cat No HY-111408

FT671 Cat No HY-107985

wwwMedChemExpresscom 41

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9773Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9684Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity FT827 is a selective and covalent ubiquitin-specific protease7 ( ) inhibitor with an of 52 nMUSP7 IC50

Bioactivity GNE-6640 is a selective and non-covalent inhibitor ofubiquitin epecific peptidase 7 with values of(USP7) IC50075 μM 043 μM 203 μM and 023 μM for full length USP7USP7 catalytic domain full length USP43 and Ub-MDM2respectively

Bioactivity GNE-6776 is a selective inhibitorUSP7 Bioactivity HBX 19818 is a specific inhibitor of ubiquitin-specific with an of 281 μMprotease 7 (USP7) IC50

Bioactivity IU1 is a special inhibitor with of 4-5 μMUsp14 IC50 Bioactivity IU1-47 is a potent inhibitor with an of 06 μMUSP14 IC50

IU1-47 induces tau elimination in cultured neurons [1]

Bioactivity LDN-57444 is a reversible competitive and site-directedinhibitor of withubiquitin C-terminal hydrolase L1 (UCH-L1)an of 088 μM and a of 040 μM LDN-57444 alsoIC50 Kisuppresses UCH-L3 activity with an of 25 μMIC50

Bioactivity MF-094 is a potent and selective inhibitor with an USP30 IC50of 120 nM

Bioactivity ML-323 is a reversible potent inhibitor with USP1-UAF1 IC50of 76 nM in a Ub-Rho assay The measured inhibition constantsof ML-323 for the free enzyme ( ) is 68 nMKi

Bioactivity ML364 is an inhibitor of ubiquitin specific peptidase 2 and can be used for the research of breast cancer(USP2)

extracted from patent WO 2016134026 A1 compound Figure 10G

FT827 Cat No HY-111350

GNE-6640 Cat No HY-112937

GNE-6776 Cat No HY-107986

HBX 19818 Cat No HY-17540

IU1 Cat No HY-13817

IU1-47 Cat No HY-122243

LDN-57444 Cat No HY-18637

MF-094 Cat No HY-112438

ML-323 Cat No HY-17543

ML364 Cat No HY-100900

Purity 9800Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9737Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9843Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NSC632839 is a nonselective isopeptidase inhibitor whichinhibits and with s of 45plusmn4 μMUSP2 USP7 SENP2 EC5037plusmn1 μM and 98plusmn18 μM respectively

Bioactivity P 22077 is a cell-permeable ubiquitin-specific protease 7 inhibitor with an of 801 μM It also inhibits(USP7) EC50

USP47 with an of 874 μMEC50

Bioactivity P005091 is a selective and potent inhibitor of with anubiquitin-specific protease 7 (USP7)

of 42 μMEC50

Bioactivity PR-619 is a broad-range inhibitor with of 393DUB EC5049 686 72 and 861 μM for USP4 USP8 USP7 USP2and respectivelyUSP5

Bioactivity SJB2-043 is an inhibitor of the native complex withUSP1UAF1 of 544 nMIC50

Bioactivity SJB3-019A is a potent and novel inhibitor 5 times moreUSP1potent than SJB2-043 in promoting ID1 degradation andcytoxicity in K562 cells with of 00781 μMIC50

Bioactivity USP7-IN-1 is a selective and reversible inhibitor of with an of 77 μMubiquitin-specific protease 7 (USP7) IC50

and can be used for the research of cancer

Bioactivity USP7-IN-3 (Compound 5) is a potent and selective allostericubiquitin-specific protease 7 ( ) inhibitor USP7 [1]

Bioactivity USP7USP47 inhibitor is a selective ubiquitin-specific protease inhibitor with s of 042 μM and 10747 (USP7USP47) EC50

μM respectively

Bioactivity VLX1570 is a competitive inhibitor of proteasomedeubiquitinases ( ) with an of approximate 10 μMDUBs IC50

42 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NSC632839 Cat No HY-100708

P 22077 Cat No HY-13865

P005091 (P5091) Cat No HY-15667

PR-619 Cat No HY-13814

SJB2-043 Cat No HY-15757

SJB3-019A Cat No HY-80012

USP7-IN-1 Cat No HY-16709

USP7-IN-3 Cat No HY-112128

USP7USP47 inhibitor Cat No HY-13487

VLX1570 Cat No HY-12471

wwwMedChemExpresscom 43

DNA AlkylatorCrosslinker

DNA alkylatorcrosslinker is a molecule that alkylates DNA or cancross link with DNA DNA alkylatorcrosslinker can have mutagenicpharmaceutical or other effects Alkylation is the transfer of an alkylgroup from one molecule to another The alkyl group may betransferred as an alkyl carbocation a free radical a carbanion or acarbene Alkylating agents are widely used in chemistry because thealkyl group is probably the most common group encountered inorganic molecules Selective alkylation or adding parts to the chainwith the desired functional groups is used especially if there is nocommonly available biological precursor Alkylation with only onecarbon is termed methylation In medicine alkylation of DNA is used

in chemotherapy to damage the DNA of cancer cells Alkylation is accomplished with the class of drugs calledalkylating antineoplastic agents Crosslinking of DNA occurs when various exogenous or endogenous agents reactwith two different positions in the DNA This can either occur in the same strand (intrastrand crosslink) or in theopposite strands of the DNA (interstrand crosslink) Crosslinks also occur between DNA and protein DNA replicationis blocked by crosslinks which causes replication arrest and cell death if the crosslink is not repaired The RAD51family plays a role in repair

Purity 990Clinical Data LaunchedSize 100 mg 500 mg

Purity 9879Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9844Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9961Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

DNA AlkylatorCrosslinker Inhibitors amp Modulators

Bioactivity Altretamine is an antineoplastic agentalkylating Bioactivity Altretamine hydrochloride is an antineoplasticalkylatingagent

Bioactivity Bendamustine D4 is the deuterium labeled BendamustineBendamustine is a agent that causes DNADNA cross-linkingbreaks with alkylating and antimetabolite properties

Bioactivity Bendamustine hydrochloride is a agent thatDNA cross-linkingcauses DNA breaks with alkylating and antimetaboliteproperties

Bioactivity Busulfan is a potent with selective immunosuppressivealkylatoreffect on bone marrow

Bioactivity Calicheamicin is a cytotoxic agent that causes double-strandDNA breaks

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity Carmustine is an antitumor chemotherapeutic agent which worksby akylating DNA and RNA

Bioactivity Chlorambucil is an agent with antitumor activityalkylating Bioactivity Cisplatin is a antineoplastic chemotherapy drug which works bycross-linking with and causing DNA damage in cancerDNAcells

44 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Altretamine (ENT-50852 RB-1515 WR-95704) Cat No HY-B0181

Altretamine hydrochloride (ENT-50852 hydrochloride RB-1515

hydrochloride WR-95704 hydrochloride) Cat No HY-B0181A

Bendamustine D4 (SDX-105 D4) Cat No HY-13567S

Bendamustine hydrochloride (SDX-105 EP-3101) Cat No HY-B0077

Busulfan Cat No HY-B0245

Calicheamicin (Calicheamicin γ1) Cat No HY-19609

Carboplatin (NSC 241240) Cat No HY-17393

Carmustine Cat No HY-13585

Chlorambucil (CB-1348 WR-139013) Cat No HY-13593

Cisplatin (CDDP cis-Diaminodichloroplatinum) Cat No HY-17394

wwwMedChemExpresscom 45

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 980Clinical Data LaunchedSize 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Bioactivity Cyclophosphamide is a synthetic agent chemicallyalkylatingrelated to the nitrogen mustards with antineoplastic andimmunosuppressive activities

Bioactivity Cyclophosphamide hydrate is a synthetic agentalkylatingchemically related to the nitrogen mustards withantineoplastic and immunosuppressive activities

Bioactivity Fotemustine is a agent with antitumor activityDNA-alkylating Bioactivity Ifosfamide is an chemotherapeutic agent withalkylatingactivity against a wide range of tumors

Bioactivity Lomustine (CCNU) is a agent with antitumorDNA alkylatingactivity

Bioactivity Melphalan is an effective agent with potentDNA alkylatingantitumor activity

Bioactivity Methylnitronitrosoguanidine (MNNG) is an agent withalkylatingtoxic and mutagenic effects [1]

Bioactivity Miriplatin is a chemotherapy agent which belongs to the classof agentsalkylating

Bioactivity Miriplatin hydrate is a chemotherapy agent which belongs tothe class of agentsalkylating

Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Cyclophosphamide Cat No HY-17420

Cyclophosphamide hydrate (Cyclophosphamide monohydrate) Cat No HY-17420A

Fotemustine (S10036) Cat No HY-B0733

Ifosfamide Cat No HY-17419

Lomustine (CCNU NSC 79037) Cat No HY-13669

Melphalan (L-PAM) Cat No HY-17575

Methylnitronitrosoguanidine (MNNG) Cat No HY-128612

Miriplatin (SM-11355) Cat No HY-16325A

Miriplatin hydrate (SM-11355 (hydrate)) Cat No HY-16325

Mitomycin C (Ametycine) Cat No HY-13316

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9926Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9986Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Oxaliplatin is a inhibitor It causes DNADNA synthesiscrosslinking damage prevents DNA replication andtranscription and causes cell death

Bioactivity Palifosfamide is a novel DNA alkylator and the activemetabolite of ifosfamide with antitumor activity

Bioactivity Procarbazine Hydrochloride is an agent withalkylatinganticancer activity

Bioactivity RITA is an inhibitor of binds top53-HDM-2 interactionp53dN with a of 15 nM and also induces Kd DNA-DNA

cross-links

Bioactivity Satraplatin is an agent with potent antitumoralkylatingeffect

Bioactivity SJG-136 is a agent with an of 45 nMDNA cross-linking XL50for pBR322 DNA SJG-136 has potent antitumor activity

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity Temozolomide (NSC 362856 CCRG 81045) is an oral DNA agent used to treat some brain cancersalkylating

Bioactivity Thio-TEPA is a agent with antitumor activityDNA alkylating Bioactivity Treosulfan (NSC 39069Treosulphan) is an agent withalkylatingactivity in ovarian cancer and other solid tumor types

46 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Oxaliplatin Cat No HY-17371

Palifosfamide (Isophosphoramide mustard IPM ZIO-201) Cat No HY-14798

Procarbazine Hydrochloride Cat No HY-13733

RITA (NSC 652287) Cat No HY-13424

Satraplatin (BMS182751 BMY45594 JM216) Cat No HY-17576

SJG-136 (NSC-694501) Cat No HY-14573

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

Temozolomide (NSC 362856 CCRG 81045 TMZ) Cat No HY-17364

Thio-TEPA Cat No HY-17574

Treosulfan (NSC 39069 Treosulphan) Cat No HY-16503

wwwMedChemExpresscom 47

Purity 980Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Uramustine is an oral agent effective in thealkylatingtreatment of lymphosarcoma chronic lymphatic leukaemia andthrombocythemia

Bioactivity VAL-083 is an agent that creates N7 methylation onalkylatingDNA with antitumor activity

Uramustine (Uracil mustard) Cat No HY-13544

VAL-083 (Dianhydrodulcitol Dianhydrogalactitol) Cat No HY-16513

DNA-PKDNA-dependent protein kinase

DNA-PKcs (DNA-dependent protein kinase catalytic subunit) is anenzyme that in humans is encoded by the PRKDC gene DNA-PKcsbelongs to the phosphatidylinositol 3-kinase-related kinase proteinfamily DNA-PKcs is the catalytic subunit of a nuclear DNA-dependentserinethreonine protein kinase called DNA-PK The secondcomponent is the autoimmune antigen Ku On its own DNA-PKcs isinactive and relies on Ku to direct it to DNA ends and trigger itskinase activity DNA-PKcs is required for the non-homologous endjoining (NHEJ) pathway of DNA repair Many proteins have beenidentified as substrates for the kinase activity of DNA-PKAutophosphorylation of DNA-PKcs appears to play a key role in NHEJ

and is thought to induce a conformational change that allows end processing enzymes to access the ends of thedouble-strand break DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNAdamage checkpoint

48 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 49

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9943Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9722Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9664Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9239Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

DNA-PK Inhibitors amp Modulators

Bioactivity (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer ofNedisertib with an in the range of 7-30 nM for IC50 DNA-PK

[1]

Bioactivity AZD-7648 is a potent and selective inhibitorDNA-PKAnti-tumor activity [1]

Bioactivity CC-115 is a potent and dual and kinaseDNA-PK mTORinhibitor with s of 13 nM and 21 nM respectively CC-115IC50blocks both and signalingmTORC1 mTORC2

Bioactivity CC-115 hydrochloride is a potent and dual and DNA-PK mTORkinase inhibitor with s of 13 nM and 21 nM respectivelyIC50CC-115 blocks both and signalingmTORC1 mTORC2

Bioactivity Compound 401 is a synthetic inhibitor of ( = 028DNA-PK IC50μM) that also targets mTOR but not PI3K in vitro

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity LTURM34 is a specific inhibitor with an of 0034DNA-PK IC50μM

Bioactivity LY3023414 potently and selectively inhibits class I PI3Kisoforms and with s of 607 nM 776DNA-PK mTORC12 IC50nM 38 nM 238 nM 424 nM and 165 nM for PI3Kα PI3KβPI3Kδ PI3Kγ DNA-PK and mTOR respectively LY3023414potently inhibits at low nanomolarhellipmTORC1 2

Bioactivity Nedisertib (M3814) is a potent and selective inhibitor of ( ) with an of lt3DNA-dependent Protein Kinase DNA-PK IC50

nM

Bioactivity NU 7026 is a novel specific inhibitor with ofDNA-PK IC50023plusmn001 μM also inhibits with of 13plusmn3 μMPI3K IC50

(R)-Nedisertib ((R)-M3814) Cat No HY-101570A

AZD-7648 Cat No HY-111783

CC-115 Cat No HY-16962

CC-115 hydrochloride Cat No HY-16962A

Compound 401 Cat No HY-19341

KU-57788 (NU7441) Cat No HY-11006

LTURM34 Cat No HY-101667

LY3023414 Cat No HY-12513

Nedisertib (M3814) Cat No HY-101570

NU 7026 (DNA-PK Inhibitor II LY293646) Cat No HY-15719

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9937Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9145Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity PI-103 is a potent and inhibitor with s of 8PI3K mTOR IC50nM 88 nM 48 nM 150 nM 20 nM and 83 nM for p110α p110β

and PI-103 also inhibitsp110δ p110γ mTORC1 mTORC2 with an of 2 nMDNA-PK IC50

Bioactivity PI-103 Hydrochloride is a dual and inhibitor withPI3K mTORs of 8 nM 88 nM 48 nM 150 nM 20 nM and 83 nM forIC50

and p110α p110β p110δ p110γ mTORC1 mTORC2PI-103 also inhibits with an of 2 nMDNA-PK IC50

Bioactivity PIK-75 is a and inhibitor which inhibits DNA-PKDNA-PK PI3K and p110γ with s of 2 58 and 76 nM respectivelyp110α IC50

PIK-75 inhibits p110α gt200-fold more potently than p110β(IC =13 μM)50

Bioactivity PIK-90 is a and inhibitor which inhibits DNA-PK PI3K p110α and with s of 11 18 and 13 nMp110γ DNA-PK IC50

respectively

Bioactivity Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib apotent inhibitor with an of lt3 nM DNA-PK IC50

[1]Bioactivity SF2523 is a highly selective and potent inhibitor of withPI3K

s of 34 nM 158 nM 9 nM 241 nM and 280 nM for IC50 PI3Kα

BRD4 and mTOR respectivelyPI3Kγ DNA-PK

Bioactivity STL127705 (Compound L) is a Ku 7080 heterodimer proteininhibitor inhibits Ku7080-DNA interaction with an ofIC5035 μM STL127705 also inhibits Ku-dependent activation ofDNA-PKCS kinase ( 25 μM) IC50

[1]

Bioactivity Torin 2 is an inhibitor with of 025 nM formTOR EC50inhibiting cellular mTOR activity and exhibits 800-foldselectivity over PI3K (EC 200 nM) Torin 2 also inhibits50

with an of 05 nM in the cell free assay TorihellipDNA-PK IC50

Bioactivity VX-984 is a potent inhibitorDNA-PK Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

50 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

PI-103 Cat No HY-10115

PI-103 Hydrochloride Cat No HY-10115A

PIK-75 (PIK-75 Hydrochloride) Cat No HY-13281

PIK-90 Cat No HY-12030

Rac-Nedisertib (Rac-M3814) Cat No HY-101570B

SF2523 Cat No HY-101146

STL127705 Cat No HY-122727

Torin 2 Cat No HY-13002

VX-984 (M9831) Cat No HY-19939S

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

wwwMedChemExpresscom 51

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity YU238259 is an inhibitor of homology-dependent DNA repair () used for cancer researchHDR

YU238259 Cat No HY-19977

DNARNA Synthesis

RNA synthesis which is also called DNA transcription is a highlyselective process Transcription by RNA polymerase II extends beyondRNA synthesis towards a more active role in mRNA maturationsurveillance and export to the cytoplasmSingle-strand breaks are repaired by DNA ligase using thecomplementary strand of the double helix as a template with DNAligase creating the final phosphodiester bond to fully repair theDNADNA ligases discriminate against substrates containing RNAstrands or mismatched base pairs at positions near the ends of thenickedDNA Bleomycin (BLM) exerts its genotoxicity by generatingfree radicals whichattack C-4prime in the deoxyribose backbone of DNA

leading to opening of the ribose ring and strand breakage it is an S-independentradiomimetic agent that causesdouble-strand breaks in DNAFirst strand cDNA is synthesized using random hexamer primers and M-MuLV Reverse Transcriptase (RNase H)Second strand cDNA synthesis is subsequently performed using DNA Polymerase I and RNase H The remainingoverhangs are converted into blunt ends using exonucleasepolymerase activity After adenylation of the 3prime ends ofDNA fragments NEBNext Adaptor with hairpin loop structure is ligated to prepare the samples for hybridization Cellcycle and DNA replication are the top two pathways regulated by BET bromodomain inhibition Cycloheximide blocksthe translation of mRNA to protein

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wwwMedChemExpresscom 53

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 1 mg 2 mg 5 mg

Purity 9876Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9989Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 9968Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

25 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

DNARNA Synthesis Inhibitors amp Modulators

Bioactivity 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is amodified nucleoside 2-(Methylamino)-1H-purin-6(7H)-one is anendogenous methylated nucleoside found in human fluids

Bioactivity 374-Trihydroxyflavone isolated from Rhus javanica var is a flavonoid with DNA strand-scission activityroxburghiana

[1]

Bioactivity 5-Methoxyflavone belonged to Flavonoid family is a DNApolymerase-beta inhibitor and neuroprotective agent againstbeta-amyloid toxicity possess central nervous system (CNS)depressant effect mediated through the ionotropic GABA Areceptors

Bioactivity 6-Thio-2-Deoxyguanosine is a nucleoside analogue that can beincorporated into de novo-synthesized telomeres by telomerase

Bioactivity Acelarin (NUC-1031) is a ProTide transformation andenhancement of the widely-used nucleoside analoguegemcitabine

Bioactivity Actinomycin D inhibits with an of 042 μMDNA repair IC50

Bioactivity Adenine is a purine derivative and a nucleobase with a varietyof roles in biochemistry Target Nucleosideantimetaboliteanalog Adenine is a nucleobase with a varietyof roles in biochemistry including cellular respiration inthe form of both the energy-rich adenosine triphosphate (ATP)hellip

Bioactivity alpha-Amanitin is the principal toxin of several deadlypoisonous mushrooms exerting its toxic function by inhibiting

RNA-polymerase II

Bioactivity Anisomycin is a potent inhibitor whichprotein synthesisinterferes with protein and by inhibitingDNA synthesispeptidyl transferase or the 80S ribosome system Anisomycin isa JNK activator which increases phospho-JNK

Bioactivity Beaucage reagent is found to be potent in causing DNAcleavage

2-(Methylamino)-1H-purin-6(7H)-one (N2-methylguanine) Cat No HY-101412

374-Trihydroxyflavone (5-Deoxykampferol) Cat No HY-111806

5-Methoxyflavone Cat No HY-107790

6-Thio-2-Deoxyguanosine (6-thio-dG β-TGdR) Cat No HY-18762

Acelarin (NUC-1031) Cat No HY-100885

Actinomycin D (Dactinomycin Actinomycin IV) Cat No HY-17559

Adenine (6-Aminopurine Vitamin B4) Cat No HY-B0152

alpha-Amanitin (α-Amanitin α-Amatoxin) Cat No HY-19610

Anisomycin (Flagecidin Wuningmeisu C) Cat No HY-18982

Beaucage reagent Cat No HY-100951

Purity 9847Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity 9804Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9896Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Bioactivity Bleomycin sulfate is a inhibitor with potentDNA synthesisantitumor activity

Bioactivity BMH-21 is a small molecule DNA intercalator that bindsribosomal DNA and inhibits RNA polymerase I (Pol I)transcription does not cause phosphorylation of H2AX

Bioactivity Branaplam (LMI070) is a highly potent selective and orallyactive small molecule modulatorSMN2 splicing

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity CeMMEC1 is an inhibitor of and also has high affinityBRD4for with an of 09 μM for TAF1 and a of 18TAF1 IC50 KdμM for TAF1 (2)

Bioactivity CeMMEC13 is a potent inhibitor of bromodomain withTAF1 (2)an of 21 μMIC50

Bioactivity Chebulinic acid is a potent natural inhibitor of Mtuberculosis DNA gyrase also can inhibit SMAD-3phosphorylation inhibit H+ K+-ATPase activity

Bioactivity COH29 is a potent ribonucleotide reductase ( ) inhibitorRNRwith anticancer activity COH29 inhibits α and β subunit ofRNR with s of 16 μMIC50

Bioactivity CX-5461 is a potent and oral inhibitor ItrRNA synthesisinhibits RNA polymerase I-driven transcription of rRNA with

s of 142 113 and 54 nM in HCT-116 A375 and MIA PaCa-2IC50cells respectively

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Bleomycin sulfate Cat No HY-17565

BMH-21 Cat No HY-12484

Branaplam (LMI070 NVS-SM1) Cat No HY-19620

Capecitabine Cat No HY-B0016

Carboplatin (NSC 241240) Cat No HY-17393

CeMMEC1 Cat No HY-111445

CeMMEC13 Cat No HY-101088

Chebulinic acid Cat No HY-N2033

COH29 (RNR Inhibitor COH29) Cat No HY-19931

CX-5461 Cat No HY-13323

wwwMedChemExpresscom 55

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9872Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9963Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9945Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg

Bioactivity CX-5461 dihydrochloride is a potent and orally bioavailableinhibitor of Pol I-mediated with s of 142rRNA synthesis IC50nM in HCT-116 113 nM in A375 and 54 nM in MIA PaCa-2 cellsand shows little or no effect on Pol II ( ge25 μM)IC50

Bioactivity Cycloheximide (Naramycin A) is an eukaryote protein synthesisinhibitor with s of 5325 nM and 2880 nM for proteinIC50synthesis and RNA synthesis respectivelyin vivo

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Datelliptium chloride is a DNA-intercalating agent derivedfrom ellipticine with anti-tumor activities

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Didox (NSC-324360) is a synthetic (ribonucleotide reductase) inhibitorRR

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

CX-5461 dihydrochloride Cat No HY-13323A

Cycloheximide (Naramycin A Actidione CHX) Cat No HY-12320

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Datelliptium chloride Cat No HY-U00337

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Didox (NSC-324360) Cat No HY-19387

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Bioactivity Folic acid(Vitamin M Vitamin B9) is a B vitamin is necessaryfor the production and maintenance of new cells for DNAsynthesis and RNA synthesis

Bioactivity GC7 Sulfate is a ( ) inhibitordeoxyhypusine synthase DHPS

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity GNE-371 is a potent and selective chemical probe for thesecond bromodomains of human transcription-initiation-factor

subunit 1 and transcription-initiation-factor TFIID TFIIDsubunit 1-like with an of 10 nM for TAF1(2)IC50

Bioactivity Guanine is one of the fundamental components of nucleic acids( and ) Guanine is a purine derivative consistingDNA RNAof a fused pyrimidine-imidazole ring system with conjugateddouble bonds

Bioactivity Halofuginone (RU-19110) is a less-toxic form of Febrifuginewhich is isolated from the plant Dichroa febrifuga [1]

Halofuginone inhibits in anprolyl-tRNA synthetaseATP-dependent manner with a of 183 nM HalofuginhellipKi

[2]

Bioactivity Halofuginone hydrobromide (RU-19110 hydrobromide) is aless-toxic form of Febrifugine which is isolated from theplant Halofuginone inhibits Dichroa febrifuga [1] prolyl-tRNA

in an ATP-dependent manner with a of 183hellipsynthetase Ki

Bioactivity Hydroxyurea is a cell apoptosis inducer that inhibit DNAsynthesis through inhibition of ribonucleotide reductase

Bioactivity L189 is a novel human DNA ligase inhibitor inhibitshLigIIIIIV with IC50 of 595 μM

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Folic acid (Vitamin B9 Vitamin M) Cat No HY-16637

GC7 Sulfate Cat No HY-108314A

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

GNE-371 Cat No HY-112803

Guanine Cat No HY-Y1055

Halofuginone (RU-19110) Cat No HY-N1584

Halofuginone hydrobromide (RU-19110 (hydrobromide)) Cat No HY-N1584A

Hydroxyurea (Hydroxycarbamide) Cat No HY-B0313

L189 Cat No HY-15588

wwwMedChemExpresscom 57

Purity 990Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9839Clinical Data No Development ReportedSize 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9977Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9988Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity L67 is a novel competitive human DNA ligase inhibitorinhibits DNA ligases I and III with IC50 of 10 μM and 10 μM

Bioactivity Madrasin is a potent and cell penetrant splicing inhibitorthat interferes with the early stages of spliceosome assemblyMadrasin is cytotoxic at higher concentrations although atlower concentrations it induces cell cycle arrest promotes aspecific reorganization of subnuclear protein localizationhellip

Bioactivity MB-7133 is a inhibitorDNA synthesis Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Bioactivity ML216(CID-49852229) is a potent inhibitor of the DNA unwindingactivity of BLM helicase showing similar IC50s of 30 and097 μM for full length BLM and BLM636ndash1298 respectively IC50value 30097 uM(Full length636ndash1298 BLM) Target BLMhelicase inhibitor ML216 shows cell-based activity and canhellip

Bioactivity Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNAdamage agent

Bioactivity NITD008 is a potent and selective inhibitor whichflavivirusecan inhibit with an ofDengue Virus Type 2 (DENV-2) EC50064 μM

Bioactivity Oxolinic acid is a potent inhibitor of DNA gyrase and DNAsynthesis lead to DNA cleavage when extracted chromosomes areincubated with sodium dodecyl sulfate

Bioactivity Phen-DC3 is a (G4) specific ligand which canG-quadruplexinhibit and helicases with s of 65plusmn6 and 50plusmn10FANCJ DinG IC50nM respectively

Bioactivity Plicamycin is a selective specificity protein 1 ( )Sp1inhibitor Plicamycin inhibits the growth of various cancersby decreasing Sp1 protein

L67 (DNA Ligase Inhibitor) Cat No HY-15586

Madrasin (DDD00107587) Cat No HY-100236

MB-7133 Cat No HY-16311

Mitomycin C (Ametycine) Cat No HY-13316

ML216 (CID-49852229) Cat No HY-12342

Nedaplatin (NSC 375101D) Cat No HY-13700

NITD008 (7-Deaza-2-C-acetylene-adenosine) Cat No HY-12957

Oxolinic acid Cat No HY-B1002

Phen-DC3 Cat No HY-15594

Plicamycin (Mithramycin A) Cat No HY-A0122

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9762Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9931Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Quarfloxin (CX 3543) a fluoroquinolone derivative withantineoplastic activity targets and inhibits RNA pol Iactivity with IC values in the nanomolar range in50neuroblastoma cells Quarfloxin disrupts the interactionbetween the nucleolin protein and a G-quadruplex DNA structurehellip

Bioactivity RG7800 a small molecule splicing modifier to enterSMN2human clinical trials to treat spinal muscular atrophy

Bioactivity RG7800 hydrochloride is an orally active splicingSMN2modulator with s of 23 nM and 87 nM for EC15x SMN2

splicing and RG7800 hydrochloride has theSMN proteinpotential to treat spinal muscular atrophy

Bioactivity Risdiplam (RG7916 RO7034067) is an orally administeredcentrally and peripherally distributed pre-mRNASMN2splicing modifier that increases survival motor neuron (SMN)protein levels

Bioactivity Saccharin 1-methylimidazole is an activator for DNARNASynthesis

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity SMN-C3 is an orally active splicing modulator and hasSMN2the potential to treat spinal muscular atrophy (SMA)

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 valueof 08 nM less potent for MTH2 NUDT5 NUDT12 NUDT14 andNUDT16

Bioactivity TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) withan IC50 value of 08 nM less potent for MTH2 NUDT5 NUDT12NUDT14 and NUDT16

58 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Quarfloxin (CX 3543) Cat No HY-14776

RG7800 (RO6885247) Cat No HY-101792

RG7800 hydrochloride (RO6885247 hydrochloride) Cat No HY-101792A

Risdiplam (RG7916 RO7034067) Cat No HY-109101

Saccharin 1-methylimidazole Cat No HY-112060

SCR7 Cat No HY-12742

SMN-C3 Cat No HY-112633

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

TH287 Cat No HY-16965

TH287 hydrochloride Cat No HY-16965A

wwwMedChemExpresscom 59

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9920Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 25 mg 50 mg 100 mg

Bioactivity TH588 is first-in-class nudix hydrolase family inhibitor thatpotently and selectively engage and inhibit the (MTH1

= 5 nM)IC50

Bioactivity TH588 hydrochloride is first-in-class nudix hydrolase familyinhibitor that potently and selectively engage and inhibit the

( = 5 nM)MTH1 IC50

Bioactivity Thiarabine (OSI-7836) shows potent anti-tumor activity andinhibition of synthesisDNA

Bioactivity Triapine is a novel inhibitor of the M2 subunit of ( ) and is a potentribonucleotide reductase RR

radiosensitizer

Bioactivity Triciribine is a inhibitor also inhibits DNA synthesis Aktand with of 130 nM and 002-046 μMHIV-12 IC50respectively

Bioactivity YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding tothe oncogenic transciption factor EWS-FLI1 YK-4-279 inhibitsEwings sarcoma family tumor (ESFT) cell growth YK-4-279induces apoptosis

Bioactivity Zoliflodacin (ETX0914AZD0914) is a novelspiropyrimidinetrione bacterial DNA gyrasetopoisomeraseinhibitor Zoliflodacin has potent antibacterialin vitroactivity against Gram-positive and Gram-negative organismsincluding with the of 025 μgmLS aureus MIC90

TH588 Cat No HY-12814

TH588 hydrochloride Cat No HY-12814A

Thiarabine (OSI-7836) Cat No HY-16496

Triapine (3-AP PAN-811 OCX191 NSC663249) Cat No HY-10082

Triciribine (API-2 NSC 154020 TCN) Cat No HY-15457

YK-4-279 Cat No HY-14507

Zoliflodacin (ETX0914 AZD0914) Cat No HY-17647

Eukaryotic Initiation Factor (eIF)

Eukaryotic initiation factors (eIFs) are proteins involved in theinitiation phase of eukaryotic translation These proteins help stabilizethe formation of the functional ribosome around the start codon andalso provide regulatory mechanisms in translation initiationEukaryotic initiation factor 2B (eIF2B) is a guaninenucleotide-exchange factor which mediates the exchange of GDP(bound to initiation factor eIF2) for GTP thus regenerating the active[eIF2GTP] complex that is required for peptide-chain initiation Theactivity of eIF2B is a key control point for eukaryotic protein synthesisand is altered in response to viral infection hormones nutrientsgrowth factors and certain stresses

Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis oncapped mRNAs in the cytoplasm Eukaryotic initiation factor (elF) 4A functions as a subunit of the initiation factorcomplex elF4F which mediates the binding of mRNA to the ribosome

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wwwMedChemExpresscom 61

Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 2 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Eukaryotic Initiation Factor (eIF) Inhibitors amp Modulators

Bioactivity 4E1RCat is an inhibitor of cap-dependent translation andinhibits interaction with an an of 4 μMeIF4EeIF4GI IC50

Bioactivity 4E2RCat is an inhibitor of interaction with an eIF4E-eIF4G IC50of 135 μM

Bioactivity 4EGI-1 is an inhibitor of interaction with a eIF4EeIF4G Kdof 25 μM against eIF4E binding

Bioactivity Briciclib is a water soluble derivative of ON 013100 and hasthe potential in targeting for solid cancerseIF4E

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic inhibitor with an of 110initiation factor 4A-3 (eIF4A3) IC50

nM

Bioactivity Episilvestrol is a derivative of silvestrol isolated from thefruits and twigs of and is a specificAglaia silvestris

-targeting translation inhibitor with antitumor activityeIF4A

Bioactivity GCN2iB is an ATP-competitive inhibitor of aserinethreonine-protein kinase general control

with an of 24 nMnonderepressible 2 (GCN2) IC50

Bioactivity SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1and disrupts the eIF4F complex

Bioactivity Silvestrol is a eukaryotic translation initiation factor 4A () inhibitor isolated from the fruits and twigs of eIF4A Aglaia

foveolata

4E1RCat Cat No HY-14427

4E2RCat Cat No HY-100733

4EGI-1 Cat No HY-19831

Briciclib (ON 014185) Cat No HY-16366

CCT020312 Cat No HY-119240

eIF4A3-IN-2 Cat No HY-101785

Episilvestrol Cat No HY-15359

GCN2iB Cat No HY-112654

SBI-0640756 (SBI-756) Cat No HY-19560

Silvestrol ((-)-Silvestrol) Cat No HY-13251

G-quadruplex

G-quadruplexes (G-tetrads or G4-DNA) are nucleic acid sequencesthat are rich in guanine and are capable of forming a four-strandedstructure Four guanine bases can associate through Hoogsteenhydrogen bonding to form a square planar structure called a guaninetetrad and two or more guanine tetrads can stack on top of eachother to form a G-quadruplex The quadruplex structure is furtherstabilized by the presence of a cation especially potassium which sitsin a central channel between each pair of tetradsThey can be formedof DNA RNA LNA and PNA and may be intramolecular bimolecularor tetramolecular Depending on the direction of the strands or partsof a strand that form the tetrads structures may be described as

parallel or antiparallel

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Purity 980Clinical Data No Development ReportedSize 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity 9680Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

G-quadruplex Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity APTO-253 is an inducer of andKruppel-like factor 4 (KLF4)also stabilizes with anti-proliferative activityGquadruplex

Bioactivity Phen-DC3 Trifluoromethanesulfonate is a (G4)G-quadruplexspecific ligand which can inhibit and helicasesFANCJ DinGwith s of 65plusmn6 and 50plusmn10 nM respectivelyIC50

Bioactivity Pyridostatin is a stabilizer with a of 490G-quadruplexe KdnM

Bioactivity Pyridostatin hydrochloride is a stabilizer withG-quadruplexea of 490 nMKd

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

APTO-253 (LOR-253 LT-253) Cat No HY-16291

Phen-DC3 Trifluoromethanesulfonate (Phen-DC3 Triflate) Cat No HY-15594A

Pyridostatin (RR82) Cat No HY-15176

Pyridostatin hydrochloride (RR-82 hydrochloride) Cat No HY-15176A

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

Haspin Kinase

Haspin is a protein kinase that regulates chromosome and spindlefunction during mitosis and meiosis Haspin expression is detected infetal liver skin kidney small intestine and in all proliferating cellsHaspin phosphorylates H3 thr3 (H3T3ph) in human cell lines anddepletion of Haspin by RNA interference reveals that Haspin isrequired for H3 thr3 phosphorylation in mitotic cells Phosphorylationof H3T3ph by Haspin is necessary for chromosomal passengercomplex (CPC) accumulation at centromeres H3T3ph then positionsthe CPC at centromeres to regulate selected targets of Aurora Bduring mitosis

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Purity 9956Clinical Data No Development ReportedSize 5 mg

Purity 9812Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Haspin Kinase Inhibitors amp Modulators

Bioactivity CHR-6494 is a potent inhibitor of inhibiting histonehaspinH3T3 phosphorylation with an of 2 nMIC50

Bioactivity LDN-192960 is a potent ( Haspin Haploid Germ Cell-Specific) inhibitor with an of 0010 microMNuclear Protein Kinase IC50

CHR-6494 Cat No HY-15217

LDN-192960 Cat No HY-13455

HDACHistone deacetylases

HDAC (Histone deacetylases) are a class of enzymes that removeacetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid onahistone allowing the histones to wrap the DNA more tightly This isimportant because DNA is wrapped around histones and DNAexpression is regulated by acetylation and de-acetylation Its action isopposite to that of histone acetyltransferase HDAC proteins are nowalso called lysine deacetylases (KDAC) to describe their functionrather than their target which also includes non-histone proteinsTogether with the acetylpolyamine amidohydrolases and the acetoinutilization proteins the histone deacetylases form an ancient proteinsuperfamily known as the histone deacetylase superfamily

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Purity 9600Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9971 Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9896Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

HDAC Inhibitors amp Modulators

Bioactivity Abexinostat (CRA 024781) is a novel pan- inhibitorHDACmostly targeting HDAC1 with of 7 nMKi

Bioactivity ACY-1083 is a selective and brain-penetrating inhibitorHDAC6with an of 3 nM and is 260-fold more selective for HDAC6IC50than all other classes of HDAC isoforms ACY-1083 effectivelyreverses chemotherapy-induced peripheral neuropathy [1]

Bioactivity ACY-738 is a potent selective and orally-bioavailable HDAC6inhibitor with an of 17 nM ACY-738 also inhibitsIC50HDAC1 HDAC2 and HDAC3 with s of 94 128 and 218 nMIC50

Bioactivity ACY-775 is a potent and selective inhibitor of the of histonedeacetylase 6 ( ) with an of 75nMHDAC6 IC50

Bioactivity ACY-957 is a selective inhibitor of and withHDAC1 HDAC2s of 7 nM 18 nM and 1300 nM against HDAC123IC50

respectively and shows no inhibition on HDAC456789

Bioactivity AES-135 is a potent inhibitor inhibits HDAC HDAC3 HDAC6 with s of 654 190 and 636 nM respectivelyHDAC11 IC50

Anti-tumor activity [1]

Bioactivity Belinostat is a potent inhibitor with an of 27 nMHDAC IC50in HeLa cell extracts

Bioactivity Benzenebutyric acid is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity BG45 is an HDAC class I inhibitor with selectivity for HDAC3(IC50 = 289 nM) It inhibits HDAC1 HDAC2 and HDAC6 withgreatly reduced potency (IC50s = 2 22 and gt20 μMrespectively) IC50 value 289 nM (HDAC3) 2 μM (HDAC1) 22μM (HDAC2) gt20 μM (HDAC6) Target HDAC At concentrationshellip

Bioactivity BML-210 is a novel HDAC inhibitor and its mechanism of actionhas not been characterized IC50 value 5 μM[1] Target HDAC4In vitro Cell cycle analysis indicated that HeLa celltreatment with 20 and 30 μM concentration of BML-210 increasedthe proportion of cells in G0G1 phase and causedhellip

Abexinostat (CRA 024781 PCI-24781) Cat No HY-10990

ACY-1083 Cat No HY-111791

ACY-738 Cat No HY-19327

ACY-775 Cat No HY-19328

ACY-957 Cat No HY-104008

AES-135 Cat No HY-114483

Belinostat (PXD101 PX105684) Cat No HY-10225

Benzenebutyric acid (4-Phenylbutyric acid) Cat No HY-A0281

BG45 Cat No HY-18712

BML-210 Cat No HY-19350

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9875Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9906Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BRD 4354 is a moderately potent inhibitor of andHDAC5 with of 085 and 188 μM respectivelyHDAC9 IC s50

Bioactivity BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitorof and with of 085 and 188 μMHDAC5 HDAC9 IC s50

respectively [1]

Bioactivity BRD73954 ia a potent and selective HDAC inhibitor with IC50 of36 nM and 120 nM for HDAC6 and HDAC8 respectively

Bioactivity Bufexamac is a class IIB histone deacetylases (HDAC6 andHDAC10) inhibitor used as an anti-inflammatory agent

Bioactivity CAY10603 (BML-281) is a potent and selective inhibitorHDAC6with an of 2 pM CAY10603 (BML-281) also inhibits HDAC1IC50HDAC2 HDAC3 HDAC8 HDAC10 with s of 271 252 042IC506851 907 nM

Bioactivity CHDI-390576 a potent cell permeable and CNS penetrant class inhibitor with s of 54 nMIIa histonedeacetylase (HDAC) IC50

60 nM 31 nM 50 nM for class IIa HDAC4 HDAC5 HDAC7 HDAC9respectively shows gt500-fold selectivity over class IHDACs (1 2 3) and ~150-fold selectivity over HDAC8 and thehellip

Bioactivity Citarinostat is a HDAC6 specific inhibitor with IC50 of 4 nMand 76 nM for HDAC6 and HDAC3 respectively IC50 value 4 nM(HDAC6) 76 nM (HDAC3) Target HDAC The detailed informationplease refer to WO2015061684A1 and 2015054197A1

Bioactivity CM-675 is a dual and phosphodiesterase 5 (PDE5) class I histone-selective inhibitor with values of 114 nMdeacetylases IC50

and 673 nM for PDE5 and HDAC1 respectively CM-675 haspotential to treat Alzheimerrsquos disease [1]

Bioactivity Corin is a dual inhibitor of histone lysine specificdemethylase and histone deacetylase with a(LSD1) (HDAC)

of 110 nM for LSD1 and an IC of 147 nM forK (inact)i 50HDAC1

Bioactivity CRA-026440 is a potent broad-spectrum inhibitor The HDAC Kivalues against recombinant HDAC isoenzymes HDAC1 HDAC2

and are 4 14 11 15 7 andHDAC3 HDAC6 HDAC8 HDAC1020 nM respectively

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BRD 4354 Cat No HY-112719

BRD 4354 ditrifluoroacetate Cat No HY-112719B

BRD73954 Cat No HY-18700

Bufexamac (Bufexamic acid) Cat No HY-B0494

CAY10603 (BML-281) Cat No HY-18613

CHDI-390576 Cat No HY-119939

Citarinostat (ACY241) Cat No HY-15994

CM-675 Cat No HY-114303

Corin Cat No HY-111048

CRA-026440 Cat No HY-19754

wwwMedChemExpresscom 69

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in Ethanol

2 mg 5 mg 10 mg 50 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9809Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9959Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity CUDC-101 is a potent inhibitor of and withHDAC EGFR HER2s of 44 24 and 157 nM respectivelyIC50

Bioactivity Dacinostat is a potent inhibitor with an of 32 nMHDAC IC50Dacinostat also inhibits with an of 9 nM and usedHDAC1 IC50in cancer research

Bioactivity Domatinostat (4SC-202 free base) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Domatinostat tosylate (4SC-202) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Droxinostat(NS41080) is a selective inhibitor of HDAC3 HDAC6and HDAC8 with IC50 of 169 247 and 146 μM respectivelygt 8-fold selective against HDAC3 and no inhibition toHDAC1 2 4 5 7 9 and 10 IC50 Value 169 μM(HDAC3) 247μM(HDAC6) 146 μM(HDAC8) Target HDAC368 in vitrohellip

Bioactivity EDO-S101 is a pan inhibitor inhibits HDAC1 HDAC2 andHDACHDAC3 with values of 9 9 and 25 nM respectivelyIC50

Bioactivity Entinostat is an oral and selective class I inhibitorHDACwith s of 243 nM 453 nM and 248 nM for IC50 HDAC1 HDAC2

and respectivelyHDAC3

Bioactivity Fimepinostat (CUDC-907) potently inhibits class I s as wellPI3Kas classes I and II enzymes with an of 195439 nMHDAC IC50and 17501828 nM for PI3KαPI3KβPI3Kδ andHDAC1HDAC2HDAC3HDAC10 respectively

Bioactivity FT895 is a potent and selective inhibitor with an HDAC11 IC50

of 3 nM [1]

Bioactivity Givinostat (ITF-2357) is a inhibitor with an of 198HDAC IC50and 157 nM for and respectivelyHDAC1 HDAC3

CUDC-101 Cat No HY-10223

Dacinostat (NVP-LAQ824 LAQ824) Cat No HY-13606

Domatinostat (4SC-202 (free base)) Cat No HY-16012A

Domatinostat tosylate (4SC-202) Cat No HY-16012

Droxinostat (NS 41080) Cat No HY-13267

EDO-S101 (Tinostamustine) Cat No HY-101780

Entinostat (MS-275 SNDX-275) Cat No HY-12163

Fimepinostat (CUDC-907) Cat No HY-13522

FT895 Cat No HY-112285

Givinostat (ITF-2357) Cat No HY-14842

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9849Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9609Clinical Data LaunchedSize 2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Bioactivity Givinostat hydrochloride (ITF-2357 hydrochloride) is a HDACinhibitor with an of 198 and 157 nM for andIC50 HDAC1

respectivelyHDAC3

Bioactivity Givinostat hydrochloride monohydrate (ITF-2357 hydrochloridemonohydrate) is a inhibitor with an of 198 and 157HDAC IC50nM for and respectivelyHDAC1 HDAC3

Bioactivity HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2008040934 A1

Bioactivity HDAC-IN-4 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2007045844 A1 20070426

Bioactivity HDAC-IN-5 is a histone deacetylase inhibitor(HDAC) Bioactivity HDAC-IN-7 (Chidamide impurity) is an impurity of ChidamideChidamide is a potent and orally bioavailable HDAC enzymesclass I (HDAC123) and class IIb (HDAC10) inhibitor

Bioactivity HDAC6-IN-1 is a potent and selective inhibitor for withHDAC6an of 17 nM and shows 25-fold and 200-fold selectivityIC50relative to ( =422 nM) and ( =3398 nM)HDAC1 IC50 HDAC8 IC50respectively

Bioactivity HDAC8-IN-1 is a inhibitor with an of 272 nMHDAC8 IC50

Bioactivity HDACsmTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs)and targetmammalian target of Rapamycin (mTOR)inhibitor for treating hematologic malignancies with ofIC s50019 nM 18 nM 12 nM and gt500 nM for HDAC1 HDAC6 mTORand PI3Kα respectively HDACsmTOR Inhibitor 1 stimulateshellip

Bioactivity HPOB is a highly potent and selective inhibitor of histonedeacetylase 6 (HDAC6) with IC50 of 56 nM gt30 fold lesspotent against other HDACs target HDAC6 [1] IC 50 56nM [1]In vitro HPOB causes growth inhibition of normal andtransformed cells but does not induce cell death HPOBhellip

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Givinostat hydrochloride (ITF-2357 hydrochloride) Cat No HY-14842A

Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) Cat No HY-14842B

HDAC-IN-3 Cat No HY-19772

HDAC-IN-4 (CXD101) Cat No HY-100748

HDAC-IN-5 Cat No HY-18362

HDAC-IN-7 (Chidamide impurity) Cat No HY-13592

HDAC6-IN-1 Cat No HY-18947

HDAC8-IN-1 Cat No HY-111342

HDACsmTOR Inhibitor 1 Cat No HY-114414

HPOB Cat No HY-19747

wwwMedChemExpresscom 71

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg 100 mg

Bioactivity IDO1 and HDAC1 Inhibitor (Compound 10) is a dual andIDO1 inhibitor with s of 690 nM and 665 nMHDAC1 IC50

respectively [1]

Bioactivity ITSA-1 is membrane permeable and specifically suppresses TSAinhibition of HDAC (histone deacetylase) but not other HDACinhibitors

Bioactivity J22352 is a PROTAC (proteolysis-targeting chimeras)-like andhighly selective inhibitor with an value of 47HDAC6 IC50nM J22352 promotes HDAC6 degradation and induces anticancereffects by inhibiting autophagy and eliciting the antitumorimmune response in glioblastoma cancers and leading to thehellip

Bioactivity JAKHDAC-IN-1 is a potent dual inhibitor exhibitsJAK2HDACantiproliferative and proapoptotic activities in severalhematological cell lines JAKHDAC-IN-1 shows s of 4 and 2IC50

nM for JAK2 and HDAC respectively [1]

Bioactivity LMK-235 is a potent and selective inhibitor inhibitsHDAC45HDAC5 HDAC4 HDAC6 HDAC1 HDAC2 HDAC11 and HDAC8 with

s of 422 nM 119 nM 557 nM 320 nM 881 nM 852 nM andIC501278 nM respectively and is used in cancer research

Bioactivity M344 (D 237) is an inhibitor of ( =100histone deacetylase IC50nM) and an inducer of terminal cell fifferentiation

Bioactivity MC1568 is a selective class II (IIa) histone deacetylas () inhibitor used for cancer researchHDAC II

Bioactivity Mocetinostat (MGCD0103) is a potent orally active andisotype-selective inhibitor with s ofHDAC (Class IIV) IC50015 029 166 and 059 μM for andHDAC1 HDAC2 HDAC3

respectively Mocetinostat shows no inhibition onHDAC11HDAC4 HDAC5 HDAC6 HDAC7 or HDAC8

Bioactivity Nanatinostat (CHR-3996) is a potent class I selective andorally active inhibitor with anhistone deacetylase (HDAC)

of 8 nM IC50[1]

Bioactivity Nexturastat A is a potent and selective HDAC6 inhibitor withIC50 of 5 nM no inhibition on other HDAC forms

IDO1 and HDAC1 Inhibitor Cat No HY-112147

ITSA-1 Cat No HY-100508

J22352 Cat No HY-126147

JAKHDAC-IN-1 Cat No HY-126141

LMK-235 Cat No HY-18998

M344 (D 237 MS 344) Cat No HY-13506

MC1568 Cat No HY-16914

Mocetinostat (MGCD0103) Cat No HY-12164

Nanatinostat (CHR-3996) Cat No HY-13432

Nexturastat A Cat No HY-16699

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9907Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9867Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9797Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NKL 22 is a HDAC inhibitor The value of IC 50 is 78 uM NKL 22increase frataxin protein concentrations NKL 22 inhibitorsincrease FXN mRNA in FRDA lymphocytes HDAC inhibitors actdirectly on FXN [1]

Bioactivity Oxamflatin (Metacept-3) is a potent inhibitor with anHDAC of 157 nMIC50

Bioactivity Panobinostat is a non-selective histone deacetylase ( )HDACinhibitor

Bioactivity PCI-34051 is a potent and selective inhibitor with HDAC8 IC50of 10 nM with gt200-fold selectivity over the other HDACisoforms

Bioactivity PI3KHDAC-IN-1 is a potent dual inhibitor of PI3KHDACpotently inhibits PI3Kδ and HDAC1 with s of 81 nM and 14IC50

nM respectively [1]

Bioactivity Pimelic diphenylamide 106 is a slow tight-binding inhibitorof class I HDAC (HDAC 1 2 and 3 with IC50 values of 150 nM 760nM and 370 nM respectively) demonstrating no activityagainst class II HDACs

Bioactivity Pracinostat is a potent inhibitorhistone deacetylase (HDAC)with s of 40-140 nM used for cancer researchIC50

Bioactivity PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDACPTACH exerts potent growth inhibition against various humancancer cells with EC50 values ranging from 1 to 10 μM

Bioactivity Quisinostat (JNJ-26481585) is an orally available potent inhibitor with an of 011 nM for HDAC1HDAC IC50

Bioactivity Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of which is under developmenthistone deacetylase enzymes (HDAC)

for the treatment of cutaneous T-cell lymphoma [1]

72 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NKL 22 Cat No HY-100384

Oxamflatin (Metacept-3) Cat No HY-102033

Panobinostat (LBH589 NVP-LBH589) Cat No HY-10224

PCI-34051 Cat No HY-15224

PI3KHDAC-IN-1 Cat No HY-128582

Pimelic Diphenylamide 106 (RGFA-8 TC-H 106 Histone Deacetylase Inhibitor VII) Cat No HY-19348

Pracinostat (SB939) Cat No HY-13322

PTACH (NCH-51) Cat No HY-12954

Quisinostat (JNJ-26481585) Cat No HY-15433

Remetinostat (SHP-141) Cat No HY-100365

wwwMedChemExpresscom 73

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9970Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Bioactivity Resminostat is a potent inhibitor of andHDAC1 HDAC3 with mean values of 425 501 718 nMHDAC6 IC50

respectively and shows less potent activities against HDAC8with an of 877 nMIC50

Bioactivity Resminostat hydrochloride is a potent inhibitor of HDAC1 and with mean values of 425 501 718HDAC3 HDAC6 IC50

nM respectively and shows less potent activities againstHDAC8 with an of 877 nMIC50

Bioactivity RG2833 is a brain-penetrant inhibitor with of 60 nMHDAC IC50and 50 nM for HDAC1 and HDAC3 respectively

Bioactivity RGFP966 is a highly selective inhibitor with an ofHDAC3 IC5080 nM and shows no inhibition to other HDACs at concentrationsup to 15 μM

Bioactivity Ricolinostat (ACY-1215) is a potent and selective HDAC6inhibitor with an of 5 nM ACY-1215 also inhibitsIC50

and with s of 58 48 and 51 nMHDAC1 HDAC2 HDAC3 IC50respectively

Bioactivity Romidepsin is a potent and inhibitor with sHDAC1 HDAC2 IC50of 36 and 47 nM respectively

Bioactivity RTS-V5 is a dual inhibitor with s ofHDACproteasome IC5069 18 15 027 053 μM for HDAC1 HDAC2 HDAC3 HDAC6HDAC8 respectively

Bioactivity Santacruzamate A (CAY-10683) is a potent and selective HDAC2inhibitor with an of 119 pM IC50

[1]

Bioactivity Scriptaid is a potent inhibitorhistone deacetylase (HDAC)used in cancer research

Bioactivity Sinapinic acid (Sinapic acid) is a phenolic compound isolatedfrom Jack Rhizome acts as anHydnophytum formicaruminhibitor of with an of 227 mM and alsoHDAC IC50

[1]

inhibits activity Sinapinic acid posssess pothellipACE-I [2]

Resminostat (RAS2410 4SC-201) Cat No HY-14718

Resminostat hydrochloride (RAS2410 hydrochloride 4SC-201 hydrochloride) Cat No HY-14718A

RG2833 (RGFP109) Cat No HY-16425

RGFP966 Cat No HY-13909

Ricolinostat (ACY-1215 Rocilinostat) Cat No HY-16026

Romidepsin (FK 228 FR 901228 NSC 630176) Cat No HY-15149

RTS-V5 Cat No HY-112908

Santacruzamate A (CAY-10683) Cat No HY-N0931

Scriptaid (Scriptide GCK1026) Cat No HY-15489

Sinapinic acid (Sinapic acid) Cat No HY-W009732

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg

Purity 9800Clinical Data Phase 3Size 10mM x 1mL in Water

1 g 5 g 500 g

Bioactivity Butyric acid is a inhibitor withhistone deacetylase (HDAC)anti-tumor effects in several cancers

Bioactivity Sodium phenylbutyrate is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity SR-4370 is an inhibitor of with s of 013 μM 058HDAC IC50μM 0006 μM 23 μM and 34 μM for HDAC1 HDAC2 HDAC3HDAC8 and HDAC6 respectively

Bioactivity ST8154AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity ST8155AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity Sulforaphane is an isothiocyanate present naturally in widelyconsumed vegetables has shown anticancer and cardioprotectiveactivities

Bioactivity SW-100 a selective inhibitorhistone deacetylase 6 (HDAC6)with an of 23 nM shows at least 1000-fold selectivityIC50for HDAC6 relative to all other HDAC isozymes SW-100 displaysa significantly improved ability to cross hellip

Bioactivity Tacedinaline (N-acetyldinaline) is an inhibitor of the histonedeacetylase ( ) with s of 09 09 12 μM forHDAC IC50recombinant HDAC 1 2 and 3 respectively

Bioactivity Tasquinimod is an oral antiangiogenic agent in clinical trialsfor the treatment of castration-resistant prostate cancerTasquinimod binds to the regulatory Zn binding domain of2+

with of 10-30 nMHDAC4 Kd

Bioactivity TH34 an inhibitor with s of 46 μM 19HDAC6 8 10 IC50μM and 77 μM respectively shows high selectivity overHDAC123 [1]

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Sodium Butyrate (Butanoic acid sodium salt) Cat No HY-B0350A

Sodium phenylbutyrate (Sodium 4-phenylbutyrate TriButyrate) Cat No HY-15654

SR-4370 Cat No HY-111400

ST8154AA1 Cat No HY-112805

ST8155AA1 Cat No HY-112806

Sulforaphane Cat No HY-13755

SW-100 Cat No HY-115475

Tacedinaline (N-acetyldinaline CI-994 Goe-5549) Cat No HY-50934

Tasquinimod (ABR-215050) Cat No HY-10528

TH34 Cat No HY-111818

wwwMedChemExpresscom 75

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g 25 g

Purity 9867Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g 25 g

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9887Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TMP195 is a selective class IIa histone deacetylase ( )HDACinhibitor with s of 59 60 26 15 nM for HDAC4 HDAC5KiHDAC7 and HDAC9 respectively

Bioactivity TMP269 is a novel and selective class IIa histone deacetylase inhibitor with s of 157 nM 97 nM 43 nM and 23 nM(HDAC) IC50

for HDAC4 HDAC5 HDAC7 and HDAC9 respectively

Bioactivity Trichostatin A is a potent and specific inhibitor of HDAC with an value of 18 nM for HDACclass III IC50

Bioactivity Tubacin is a potent and selective inhibitor of with anHDAC6 value of 4 nM and approximately 350-fold selectivity overIC50

HDAC1

Bioactivity Tubastatin A (Hydrochloride) is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tubastatin-A is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tucidinostat is a potent and orally bioavailable enzymesHDACclass I ( ) and class IIb ( ) inhibitor withHDAC123 HDAC10

s of 95 160 67 and 78 nM less active on HDAC8 andIC50HDAC11 ( s 733 nM 432 nM respectively) and showshellipIC50

Bioactivity UF010 is a potent and selective HDAC inhibitor with IC50 ~006μM 01 μM 05 μM and 15 μM for HDACs 3 2 1 and 8respectively It has gt 6-fold selectivity over other HDACsIC50 value 006 μM (HDAC3) 01 μM (HDAC2) 05 μM (HDAC1)15 μM(HDAC 8) Target HDAC in vitro UF010 is a competitivehellip

Bioactivity Valproic acid is an inhibitor with in the range ofHDAC IC5005 and 2 mM also inhibits ( 400 μM) andHDAC1 IC50induces proteasomal degradation of Valproic acidHDAC2sodium salt is used in the treatment of epilepsy bipohellip

Bioactivity Valproic acid sodium salt is an anticonvulsants used to treatepilepsy bipolar disorder and migraines Valproic acidinhibits with an of 04 mMhistone deacetylase 1 (HDAC1) IC50

TMP195 Cat No HY-18361

TMP269 Cat No HY-18360

Trichostatin A (TSA) Cat No HY-15144

Tubacin Cat No HY-13428

Tubastatin A Hydrochloride (Tubastatin A HCl TSA HCl) Cat No HY-13271

Tubastatin-A Cat No HY-13271A

Tucidinostat (Chidamide HBI-8000 CS 055) Cat No HY-109015

UF010 Cat No HY-18976

Valproic acid (VPA 2-Propylpentanoic Acid) Cat No HY-10585

Valproic acid sodium salt (Sodium Valproate) Cat No HY-10585A

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

250 mg 500 mg 1 g 5 g

Bioactivity Vorinostat is a potent and orally available inhibitor of and andHDAC1 HDAC2 HDAC3 (Class I) HDAC7 (Class II)

with values of 10 nM and 20 nM forHDAC11 (Class IV ) ID50HDAC1 and HDAC3 respectively

Bioactivity WT-161 is a potent and selective inhibitor with an HDAC6 IC50of 040 nM

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Vorinostat (SAHA) Cat No HY-10221

WT-161 Cat No HY-100871

wwwMedChemExpresscom 77

HSPHeat shock proteins

HSP (Heat shock proteins) are a group of proteins induced by heatshock the most prominent members of this group are a class offunctionally related proteins involved in the folding and unfolding ofother proteins HSP expression is increased when cells are exposed toelevated temperatures or other stress This increase in expression istranscriptionally regulated The dramatic upregulation of the heatshock proteins is a key part of the heat shock response and is inducedprimarily by heat shock factor (HSF) HSPs are found in virtually allliving organisms from bacteria to humans Heat shock proteinsappear to serve a significant cardiovascular role Hsp90 Hsp84Hsp70 Hsp27 Hsp20 and alpha B crystallin all have been reported as

having roles in the cardiovasculature

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 g

Purity 9997Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9932Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 1 mg

HSP Inhibitors amp Modulators

Bioactivity Alvespimycin is a potent inhibitor of binding to Hsp90Hsp90with an of 62 plusmn 29 nMEC50

Bioactivity Alvespimycin hydrochloride is a potent inhibitor of Hsp90binding to Hsp90 with of 62plusmn29 nMEC50

Bioactivity Apoptozole is an inhibitor of the ATPase domain of andHsc70 with s of 021 and 014 μM respectively and canHsp70 Kd

induce apoptosis

Bioactivity Arimoclomol maleate (BRX-220) is a co-inducer of heat shockproteins ( )HSP

Bioactivity BIIB021 is an orally available fully synthetic inhibitor of with and of 17 nM and 38 nM respectivelyHSP90 Ki EC50

Bioactivity Bimoclomol is a coinducer used forheat shock protein (HSP)treatment of cardiovascular diseases

Bioactivity CCT251236 is an orally available pirin ligand from a heatshock transcription factor 1 (hsf1) phenotypic screen with an

of 19 nM for inhibition of HSF1-mediated IC50 HSP72

induction

Bioactivity Col003 is a potent inhibitor of competitively binds toHsp47the collagen binding site on Hsp47 ( 18 μM) andIC50inhibits collagen secretion by destabilizing the collagentriple helix [1]

Bioactivity Debio 0932 is an orally active inhibitor with s ofHSP90 IC50100 and 103 nM for HSP90α and HSP90β respectively

Bioactivity Ethoxyquin is an antioxidant which has been used in animalfeed for many years and also an inhibitor of heat shock

( )protein 90 Hsp90

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Alvespimycin (17-DMAG NSC 707545) Cat No HY-10389

Alvespimycin hydrochloride (17-DMAG hydrochloride KOS-1022 BMS 826476) Cat No HY-12024

Apoptozole (Apoptosis Activator VII) Cat No HY-15098

Arimoclomol maleate (BRX-220) Cat No HY-106443A

BIIB021 (CNF2024) Cat No HY-10212

Bimoclomol Cat No HY-U00398

CCT251236 Cat No HY-101026

Col003 Cat No HY-124817

Debio 0932 (CUDC-305) Cat No HY-13469

Ethoxyquin Cat No HY-B1425

wwwMedChemExpresscom 79

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9994Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Bioactivity Feretoside a phenolic compound extracted from the barks of E is a which act as cytoprotectiveulmoides HSP inducer

agent

Bioactivity Ganetespib is a heat shock protein 90 ( ) inhibitorHSP90which exhibits potent cytotoxicity in a wide variety ofhematological and solid tumor cell lines

Bioactivity Geldanamycin is a inhibitor with antimicrobial activityHsp90against many Gram-positive and some Gram-negative bacteria

Bioactivity Grp94 Inhibitor-1 is a potent selective inhibitor withGrp94an value of 2 nM and over 1000-fold selectivity to Grp94IC50

against Hsp90α [1]

Bioactivity HA15 a molecule that targets specifically BiP GRP78 HSPA5inhibits the ATPase activity of BiP HA15 strongly increasesBiP protein expression in A375 melanoma cells [1]

Bioactivity HSF1A is a cell-permeable activator of heat shocktranscription factor 1 ( )HSF1

Bioactivity HSP70-IN-1 is a heat shock protein ( ) inhibitor inhibitsHSPthe growth of Kasumi-1 cells with an of 23 μMIC50

Bioactivity JG-98 is an allosteric heat shock protein 70 (Hsp70)inhibitor with anti-cancer activities which disrupts Hsp70

and affects signalinginteraction with a co-chaperone Bag3pathways important for cancer development [1] [2] [3]

Bioactivity KNK437 is a inhibitor and inhibits the induction ofHSPHSP105 HSP70 and HSP40

Bioactivity KRIBB11 is an inhibitor of withHeat shock factor 1 (HSF1) of 12 μMIC50

Feretoside Cat No HY-N6249

Ganetespib (STA-9090) Cat No HY-15205

Geldanamycin Cat No HY-15230

Grp94 Inhibitor-1 Cat No HY-112910

HA15 Cat No HY-100437

HSF1A Cat No HY-103000

HSP70-IN-1 Cat No HY-12622

JG-98 Cat No HY-117282

KNK437 (Heat Shock Protein Inhibitor I) Cat No HY-100110

KRIBB11 Cat No HY-100872

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 100 mg

Purity 9569Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9914Clinical Data Phase 2Size 5 mg 10 mg 25 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity KU-32 is a novel novobiocin-based inhibitor that canHsp90protect against neuronal cell death

Bioactivity KW-2478 is an inhibitor of with an of 38 nMHsp90α IC50and has antitumor activity against various human hematologicaltumor cells

Bioactivity Luminespib (NVP-AUY922) is a potent inhibitor withHSP90s of 78 and 21 nM for HSP90α and HSP90β respectivelyIC50

Bioactivity MKT-077 is a rhodacyanine dye and also a heat shock protein 70( ) inhibitor which exhibits significant antitumorHsp70activity

Bioactivity NVP-HSP990 is a potent and selective inhibitor withHsp90 values of 06 08 and 85 nM for Hsp90α Hsp90β andIC50

Grp94 respectively

Bioactivity Onalespib (AT13387) is a potent inhibitor of with aHsp90 of 071 nMKd

Bioactivity p5 Ligand for Dnak and DnaJ is a nonapeptide whichcorresponds to the main binding site for the 23-residue partof the presequence of mitochondrial aspartateaminotransferase p5 Ligand for Dnak and DnaJ is ahigh-affinity ligand for DnaK and DnaJ [1]

Bioactivity Pifithrin-μ is an inhibitor of and with antitumorp53 HSP70and neuroprotective activity

Bioactivity PU-WS13 is a selective inhibitor with an ofGrp94 EC50022 μM

Bioactivity Retaspimycin is a potent and water-soluble inhibitor of with s of 119 nM for both Hsp90 and Grp9Hsp90 EC50

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KU-32 Cat No HY-108248

KW-2478 Cat No HY-13468

Luminespib (NVP-AUY922 AUY922 VER-52296) Cat No HY-10215

MKT-077 (FJ-776) Cat No HY-15096

NVP-HSP990 (HSP-990) Cat No HY-15190

Onalespib (AT13387) Cat No HY-14463

p5 Ligand for Dnak and DnaJ Cat No HY-P1887

Pifithrin-μ (PFTμ 2-Phenylethynesulfonamide) Cat No HY-10940

PU-WS13 Cat No HY-18680

Retaspimycin Cat No HY-15263

wwwMedChemExpresscom 81

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9740Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9982Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9903Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Retaspimycin Hydrochloride is a potent and water-solubleinhibitor of with s of 119 nM for both Hsp90 andHsp90 EC50Grp9

Bioactivity Shepherdin (79-87) is amino acids 79 to 87 fragment ofShepherdin Shepherdin is a peptidomimetic antagonist of thecomplex between Hsp90 and Survivin Anticancer activity [1]

Bioactivity SNX-5422 Mesylate (PF-04929113 Mesylate) a prodrug ofSNX-2112 is an orally active inhibitor with a ofHsp90 Kd41 nM and also induces Her-2 degradation with an ofIC5037nM

Bioactivity Tanespimycin (17-AAG) is a potent inhibitor with anHSP90 of 5 nM having a 100-fold higher binding affinity forIC50

tumour cell derived HSP90 than normal cell derived HSP90

Bioactivity TAS-116 is an oral bioavailable ATP-competitive highlyspecific inhibitor ( s of 347 nM and 213HSP90αHSP90β KinM respectively) without inhibiting other HSP90 familyproteins such as GRP94 TAS-116 demonstrates less ocuhellip[1]

Bioactivity Teprenone is a anti-ulcer drug and works as an inducer ofheat shock proteins ( )HSPs

Bioactivity TRC051384 is a heat shock protein 70 ( ) inducerHSP70 Bioactivity VER-155008 is an inhibitor of with s of 05 μMHsp70 IC5026 μM and 26 μM for Hsc70 and Grp7 respectivelyHsp70and with a of 03 μM for Kd Hsp70

Bioactivity VER-49009 is a inhibitor with an of 25 nM and aHsp90 IC50 of 78 nMKd

Bioactivity VER-50589 is a inhibitor with an of 21 nM and aHsp90 IC50 of 45 nMKd

Retaspimycin Hydrochloride (IPI-504) Cat No HY-10210

Shepherdin 79-87 Cat No HY-P1750

SNX-5422 Mesylate (PF-04929113 (Mesylate)) Cat No HY-10213A

Tanespimycin (17-AAG NSC 330507 CP 127374) Cat No HY-10211

TAS-116 Cat No HY-15785

Teprenone (Geranylgeranylacetone) Cat No HY-B0779

TRC051384 Cat No HY-101712

VER-155008 Cat No HY-10941

VER-49009 (CCT 129397) Cat No HY-15986

VER-50589 Cat No HY-15984

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9924Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity VER-82576 (NVP-BEP800) is a potent orally available andselective inhibitor with an of 58 nM for Hsp90βHsp90 IC50VER-82576 also slightly blocks Grp94 and Trap-1 with s ofIC5041 and 55 μM respectively

Bioactivity XL888 is a heat shock protein-90 ( ) inhibitor with anHSP90 of 24 nMIC50

Bioactivity YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathwayagainst glioblastoma directly binding to heat shock protein

with an of 820 nM on NFAT nuclear90 (HSP90) IC50translocation YZ129-induced GBM cell-cycle arrest at the G2Mphase promotes apoptosis and inhibited tumor cellhellip

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VER-82576 (NVP-BEP800) Cat No HY-10942

XL888 Cat No HY-13313

YZ129 Cat No HY-114413

wwwMedChemExpresscom 83

IRE1Inositol requiring enzyme 1

The serinethreonine-protein kinaseendoribonucleaseinositol-requiring enzyme 1 (IRE1) is an enzyme that in humans isencoded by the gene IRE1 is an endoplasmic reticulum (ER)ERN1transmembrane sensor that activates UPR to maintain ER and cellularfunction While mammalian IRE1 promotes cell survive it can initiateapoptosis via decay of anti-apoptotic microRNAsIRE1 activation is initiated by homotypic interactions of thestress-sensing lumenal domain favoring transautophosphorylation ofthe kinase-extension nuclease (KEN) domain on the cytoplasmic sideof the ER membraneIRE1XBP-1 has been shown to regulate a variety of genes in various

cell types in response to ER stress mostly related to ER function and the secretory pathway although the target genesvary depending on the cell type and nature of the stress stimuli

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9875Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg

IRE1 Inhibitors amp Modulators

Bioactivity 36-DMAD hydrochloride is a inhibitor of the pathwayIRE1α-XBP1of the unfolded protein response

Bioactivity 4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor ofIRE1α

Bioactivity 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1αinhibitor with an of 008 μM extracted from patent WOIC502008154484 A1 IRE-lα inhibitor compound 3-5

Bioactivity APY29 is an allosteric modulator of which inhibits IRE1αIRE1αautophosphorylation with of 280 nM and activates IRE1αIC50RNase activity

Bioactivity B I09 is an RNase inhibitor with an of 1230 nMIRE-1 IC50 Bioactivity GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1alpha ( ) which can inhibit and IRE1α IRE1α kinase activity RNase

with s of 20 and 200 nM respectivelyactivity IC50

Bioactivity GSK2850163 hydrochloride is a novel inhibitor ofinositol-requiring enzyme-1 alpha ( ) which can inhibitIRE1α

and with s of 20 andIRE1α kinase activity RNase activity IC50200 nM respectively

Bioactivity KIRA6 allosterically inhibits activity withIRE1α RNase kinasean of 06 microMIC50

Bioactivity Kira8 is a mono-selective inhibitor that allostericallyIRE1αattenuates with an of 59 nM IRE1α RNase activity IC50

[1]Bioactivity MKC3946 is a potent and soluble inhibitor used forIRE1α

cancer research

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36-DMAD hydrochloride Cat No HY-U00460

4μ8C (IRE1 Inhibitor III) Cat No HY-19707

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) Cat No HY-107371

APY29 Cat No HY-17537

B I09 Cat No HY-107400

GSK2850163 Cat No HY-U00459

GSK2850163 hydrochloride Cat No HY-U00459B

KIRA6 Cat No HY-19708

Kira8 Cat No HY-114368

MKC3946 Cat No HY-19710

wwwMedChemExpresscom 85

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity MKC8866 is an inhibitor with an of less thanIRE1 RNase IC5001 μM for IRE1α RNase

Bioactivity MKC9989 is a ( ) inhibitor and alsoHydroxy aryl aldehydes HAAinhibits with an of 023 to 44 μMIRE1α IC50

Bioactivity STF-083010 is an inhibitor STF-083010 inhibits Ire1Ire1endonuclease activity without affecting its kinase activityafter endoplasmic reticulum stress

MKC8866 Cat No HY-104040

MKC9989 Cat No HY-12399

STF-083010 Cat No HY-15845

Kinesin

Kinesin is a protein belonging to a class of motor proteins found ineukaryotic cells Kinesins move along microtubule filaments and arepowered by the hydrolysis of ATP (thus kinesins are ATPases) Theactive movement of kinesins supports several cellular functionsincluding mitosis meiosis and transport of cellular cargo Mostkinesins walk towards the plus end of a microtubule entailstransporting cargo from the centre of the cell towards the peripheryKinesins were discovered as microtubule (MT)-based anterogradeintracellular transport motors The founding member of thissuperfamily the genomes of mammals encode more than 40 kinesinproteins organized into at least 14 families named kinesin-1 through

kinesin-14

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wwwMedChemExpresscom 87

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9871Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9973Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Kinesin Inhibitors amp Modulators

Bioactivity (R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of ARRY-520(R)-Filanesib ((R)-ARRY-520) is a synthetic kinesin spindle

inhibitor with of 6 nMprotein (KSP) IC50

Bioactivity AZ82 is a selective kinesin-like protein KIFC1 (HSETKIFC1)inhibitor with a of 43 nM and an of 300 nM for KIFC1Ki IC50

Bioactivity CW-069 is an allosteric inhibitor of microtubule motor with an of 75 μMprotein HSET IC50

Bioactivity Dimethylenastron is a potent inhibitor with ankinesin Eg5 of 200 nMIC50

Bioactivity Eg5 Inhibitor V trans-24 is a potent and specific kinesin Eg5inhibitor with an of 065 μM and can be used in theIC50research of cancer

Bioactivity EMD534085 is a potent and selective inhibitor of the mitotic with an of 8 nMkinesin-5 IC50

Bioactivity Filanesib (ARRY-520) is a synthetic kinesin spindle protein inhibitor with of 6 nM(KSP) IC50

Bioactivity Ispinesib is a specific inhibitor of kinesin spindle protein with a of 17 nM(KSP) Ki app

Bioactivity K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5with an of 13 μMIC50

Bioactivity Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member and is used for the research of cellular15 (Kif15)

proliferative diseases

(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A

AZ82 Cat No HY-12241

CW-069 Cat No HY-15857

Dimethylenastron Cat No HY-19944

Eg5 Inhibitor V trans-24 Cat No HY-112915

EMD534085 Cat No HY-15000

Filanesib (ARRY-520) Cat No HY-15187

Ispinesib (SB-715992) Cat No HY-50759

K858 Racemic Cat No HY-19966

Kif15-IN-1 Cat No HY-15948

Purity 9731Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9705Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg

Purity 9959Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9651Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Kif15-IN-2 is an inhibitor of the mitotic and iskinesin Kif15used for the research of cellular proliferative diseases

Bioactivity Litronesib is a selective mitosis-specific kinesin Eg5inhibitor with antitumor activity

Bioactivity Litronesib (Racemate) is the racemate of litronesibLitronesib is a selective allosteric inhibitor of kinesin

Eg5

Bioactivity Monastrol is a potent and cell-permeable inhibitor of themitotic with an value of 14 μMkinesin Eg5 IC50

Bioactivity Paprotrain is a cell-permeable inhibitor of the kinesin inhibits the ATPase activity of MKLP-2 with an MKLP-2 IC50

of 135 μM and a of 336 μM and shows a moderate inhibitionKiactivity on with an of 55 μMDYRK1A IC50

Bioactivity PF-2771 is a potent and selective centromere protein E inhibitor inhibiting CENP-E motor activity with an(CENP-E)

of 161 nM PF-2771 is used as an anticancer agentIC50

Bioactivity SB-743921 is a potent inhibitor of the mitotic kinesin KSP with a of 01 nM(Eg5) Ki

88 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Kif15-IN-2 Cat No HY-15949

Litronesib (LY-2523355 KF-89617) Cat No HY-14846

Litronesib Racemate (LY-2523355 Racemate KF-89617 Racemate) Cat No HY-14846A

Monastrol ((plusmn)-Monastrol) Cat No HY-101071A

Paprotrain Cat No HY-101298

PF-2771 Cat No HY-19530

SB-743921 Cat No HY-12069

wwwMedChemExpresscom 89

LIM Kinase (LIMK)LIMKs

LIM kinases (LIMKs) are important cell cytoskeleton regulators thatplay a prominent role in cancer manifestation and neuronal diseasesThe LIMK family consists of two homologues LIMK1 and LIMK2which differ from one another in expression profile intercellularlocalization and function The main substrate of LIMK is cofilin amember of the actin-depolymerizing factor (ADF) protein familyWhen phosphorylated by LIMK cofilin is inactive LIMKs play acontributory role in several neurodevelopmental disorders and incancer growth and metastasisLIM domain kinases (LIMK1 and 2) are substrate for Cdc42Rac-PAKand modulate actin dynamics by phosphorylating cofilin at serine-3

This modification inactivates cofilinrsquos actin severing and depolymerizing activity LIMKs also translocate into thenucleus and regulate cell cycle progression LIMKs are potential therapeutic targets for NF2 and other merlin-deficienttumors

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

LIM Kinase (LIMK) Inhibitors amp Modulators

Bioactivity BMS-3 is a potent inhibitor with s of 5 nM and 6LIMK IC50nM for and respectivelyLIMK1 LIMK2

Bioactivity BMS-5 (LIMKi 3) is a potent inhibitor with s of 7LIMK IC50nM and 8 nM for and respectivelyLIMK1 LIMK2

Bioactivity R-10015 a broad-spectrum antiviral compound for HIVinfection acts as a potent and selective inhibitor of LIM

and binds to the ATP-binding pocketdomain kinase (LIMK)with an of 38 nM for human LIMK1 IC50

[1]

Bioactivity T56-LIMKi is a selective inhibitor of inhibits theLIMK2growth of Panc-1 cells with an of 352 μMIC50

90 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

BMS-3 Cat No HY-18304

BMS-5 (LIMKi 3) Cat No HY-18305

R-10015 Cat No HY-120097

T56-LIMKi (T5601640) Cat No HY-19352

wwwMedChemExpresscom 91

MicrotubuleTubulin

Microtubules are a component of the cytoskeleton found throughoutthe cytoplasm These tubular polymers of tubulin can grow as long as50 micrometres with an average length of 25 microm and are highlydynamic The outer diameter of a microtubule is about 24 nm whilethe inner diameter is about 12 nm Microtubules are found ineukaryotic cells and are formed by the polymerization of a dimer oftwo globular proteins alpha and beta tubulin Tubulin is one ofseveral members of a small family of globular proteins The tubulinsuperfamily includes five distinct families the alpha- beta- gamma-delta- and epsilon-tubulins and a sixth family which is present only inkinetoplastid protozoa The most common members of the tubulin

family are α-tubulin and β-tubulin the proteins that make up microtubules Microtubules are very important in anumber of cellular processes They are involved in maintaining the structure of the cell

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9987Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9920Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9982Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

MicrotubuleTubulin Inhibitors amp Modulators

Bioactivity 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivativewith improved pharmacological features and higher watersolubility IC50 value Target Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cyclearrest and apoptosis as measured by flow cytometry DNAhellip

Bioactivity 10-Oxo Docetaxel (Docetaxel Impurity) is a novel taxoid havingremarkable anti-tumor properties and a Docetaxel intermediate

Bioactivity 2-Methoxyestradiol is an inhibitor and angiogenesis apoptosisinducer with potent antineoplastic activity2-Methoxyestradiol also destablize microtubules

Bioactivity 4-Demethylepipodophyllotoxin(4-DMEP) is a key intermediatecompound for the preparation of podophyllotoxin-typeanti-cancer drugs a potent inhibitor of microtubule assembly

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity ofdocetaxel detected by high performance liquid chromatography(HPLC)

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity C 7-Epitaxotere)is a impurity of docetaxel

Bioactivity 7-epi-Taxol is an active metabolite of taxol with activitycomparable to that of taxol against cell replicationpromoting bundle formation and againstmicrotubulemicrotubule depolymerization

Bioactivity 7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel)derivative Paclitaxel binds to tubulin and inhibits thedisassembly of microtubules

Bioactivity ABT-751(E 7010) is a novel bioavailable tubulin-binding andantimitotic sulfonamide agent with IC50 of about 15 and 34μM in neuroblastoma and non-neuroblastoma cell linesrespectively IC50 Value 15 μM(neuroblastoma) 34μM(non-neuroblastoma) Target MicrotubuleTubulin in vitrohellip

Bioactivity Amphethinile is an agent The affinity constantanti-tubulinfor the association ( ) of Amphethinile with tubulin isKa13 μM

92 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol

10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584

10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674

2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033

4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435

7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675

7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676

7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227

7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574

ABT-751 (E7010) Cat No HY-13270

Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190

wwwMedChemExpresscom 93

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9903Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9949Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9751Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ansamitocin P-3 is a inhibitor Ansamitocin P-3microtubuleis a macrocyclic antitumor antibiotic

Bioactivity Auristatin E is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAE analog and cytotoxin inAntibody-drug conjugates

Bioactivity Auristatin F is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAF analog and cytotoxin inAntibody-drug conjugates

Bioactivity BNC105 is a tubulin polymerization inhibitor with potentantiproliferative and tumor vascular disrupting properties

Bioactivity BTB-1 is a potent selective and reversible mitotic motorprotein inhibitor with an of 169 μMKif18A IC50

Bioactivity Cabazitaxel is a semi-synthetic derivative of the naturaltaxoid 10-deacetylbaccatin III with potential antineoplasticactivity

Bioactivity CCB02 is a selective inhibitor bindingCPAP-tubulin interactionto tubulin and competing for the CPAP binding site ofβ-tubulin with an of 689 nM and shows potent anti-tumorIC50activity CCB02 shows no inhibition on the cell cycle- andcentrosome-related kinases or the phosphorylation status ofhellip

Bioactivity Cephalomannine is a taxol derivative with antitumorantiproliferative properties

Bioactivity Cevipabulin (TTI-237) is an oral microtubule-active antitumorcompound and inhibits the binding of [ H] vinblastine to3

tubulin with an of 18-40 nM for cytotoxicity in humanIC50

tumor cell line [1] [2]

Bioactivity Cevipabulin fumarate (TTI-237 fumarate) is an oralmicrotubule-active antitumor compound and inhibits thebinding of [ H] vinblastine to tubulin with an of3 IC50

18-40 nM for cytotoxicity in human tumor cell line [1] [2]

Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739

Auristatin E Cat No HY-15582

Auristatin F Cat No HY-15583

BNC105 Cat No HY-16114

BTB-1 Cat No HY-101770

Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459

CCB02 Cat No HY-114302

Cephalomannine Cat No HY-77554

Cevipabulin (TTI-237) Cat No HY-14949

Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C

Purity 9828Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9956Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9831Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Bioactivity Colchicine is a inhibitor and a tubulin microtubuledisrupting agent Colchicine inhibits microtubulepolymerization with an of 3 nMIC50

Bioactivity Combretastatin A4 is a -targeting agent thatmicrotubulebinds with of 04 μMβ-tubulin Kd

Bioactivity Crolibulin is a small molecule tubulin polymerizationinhibitor

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate IC50 Value NATarget tubulin ADCs For comparison purposes the ADC A1-mc-MMAD andor A1 -vc-MMAD were used The linker payloadmc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) washellip

Bioactivity D-64131 is a novel inhibitor of Tubulin polymerization thatcompetitively binds with [(3)H]colchicine to αβ-Tubulin

Bioactivity D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule

Bioactivity D8-MMAE is a deuterated labeled MMAE a potent mitoticinhibitor

Bioactivity D8-MMAF is a deuterated form of MMAF which is a disrupting agentmicrotubule

Bioactivity D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a disrupting agentmicrotubule

Bioactivity DM4 is is an agent that inhibit cell division DM4antitubulincan be used in the preparation of antibody drug conjugate

94 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Colchicine Cat No HY-16569

Combretastatin A4 (CRC 87-09) Cat No HY-N2146

Crolibulin (EPC2407) Cat No HY-13603

Cys-mcMMAD Cat No HY-15750

D-64131 Cat No HY-15482

D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8

Monomethyl Dolastatin 10 D8) Cat No HY-15581S

D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A

D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S

D8-MMAF hydrochloride Cat No HY-15579AS

DM4 Cat No HY-12454

wwwMedChemExpresscom 95

Purity 9897Clinical Data LaunchedSize 500u g 1 mg

Purity gt98Clinical Data LaunchedSize 1 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Purity 9988Clinical Data Phase 3Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9555Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9983Clinical Data Phase 2Size 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg

Bioactivity Docetaxel is an antineoplastic drug by inhibiting depolymerization and attenuating of themicrotubule

effects of and gene expressionbcl-2 bcl-xL

Bioactivity Docetaxel Trihydrate is a semi-synthetic taxane analogue actsas a stabilizermicrotubule

Bioactivity Angiotensin II human is a vasoconstrictor that acts on the and the receptorAT1 AT2

Bioactivity ELR510444 is a novel microtubule disruptor inhibitsMDA-MB-231 cell proliferation with IC50 of 309 nM not asubstrate for the P-glycoprotein drug transporter and retainsactivity in βIII-tubulin-overexpressing cell lines

Bioactivity Entasobulin is a polymerization inhibitor withβ-tubulinpotential anticancer activity

Bioactivity Epothilone A is a competitive inhibitor of the binding of [H] paclitaxel to polymers with a of 06-14 μM3 tubulin Ki

Bioactivity Epothilone B is a stabilizer with a ofmicrotubule Ki071μM It acts by binding to the αβ-tubulin heterodimersubunit which causes decreasing of αβ-tubulin dissociation

Bioactivity Epothilone D (KOS 862) is a potent stabilizermicrotubule

Bioactivity Eribulin (E7389) is a targeting agent that ismicrotubuleused in the treatment of metastatic breast cancer Eribulin(E7389) inhibits the proliferation of cancer cells by bindingmicrotubule proteins and microtubules

Bioactivity Eribulin mesylate (E7389 mesylate) is a microtubuletargeting agent that is used in the treatment of metastaticbreast cancer Eribulin mesylate (E7389 mesylate) inhibits theproliferation of cancer cells by binding microtubule proteinsand microtubules

Docetaxel (RP-56976) Cat No HY-B0011

Docetaxel Trihydrate (RP-56976 (Trihydrate)) Cat No HY-B0011A

Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580

ELR510444 Cat No HY-16191

Entasobulin Cat No HY-16777

Epothilone A (Epo A) Cat No HY-13503

Epothilone B (EPO 906 Patupilone) Cat No HY-17029

Epothilone D (KOS 862) Cat No HY-15278

Eribulin (B1939 E7389 ER-086526) Cat No HY-13442

Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A

Purity 9874Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9723Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9947Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9801Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Bioactivity Estramustine phosphate sodium is an antimicrotubulechemotherapy agent arrests prostate cancer cells in the G2Mphase of the cell cycle

Bioactivity Fosbretabulin disodium(CA 4DP CA 4P) is a microtubuledestabilizing drug a type of vascular-targeting agent a drugdesigned to damage the vasculature (blood vessels) of cancertumors causing central necrosis IC50 Value 4 nM [1] Targetmicrotubule in vitro Cytotoxic IC(50) values of CA-4 in humanhellip

Bioactivity Ixabepilone is an orally bioavailable inhibitor which binds to tubulin andmicrotubule

promotes tubulin polymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of the cell cycle andinduces tumor cell apoptosis

Bioactivity Lexibulin(CYT-997) is a potent tubulin polymerisationinhibitor with IC50 of 10-100 nM in cancer cell lines withpotent cytotoxic and vascular disrupting activity in vitro andin vivo

Bioactivity Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM in cancer celllines with potent cytotoxic and vascular disrupting activityin vitro and in vivo

Bioactivity Maytansinol inhibits microtubule assembly and inducesmicrotubule disassembly in vitro Target MicrotubuleTubulinin vitro Maytansinol disrupts the mitotic spindle andprevents mitotic exit in Drosophila Maytansinol reduces thegrowth andor survival of HCT116 cells in a dose-dependenthellip

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate Mc-MMAD is aprotective group (maleimidocaproyl) -conjugated MMAD IC50Value Target tubulin ADCs For comparison purposes the ADCA1 -mc-MMAD andor A1 -vc-MMAD were used The linkerpayloadhellip

Bioactivity Mc-MMAE is a protective group (maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE) which is a potent tubulininhibitor is a toxin payload in antibody drug conjugate (

)ADC

Bioactivity Mc-MMAF is a protective group-conjugated MMAF MMAF is a morepotent drug than Monomethyl auristatin E (MMAE) but ischarged and relatively membrane-impermeable is a potenttubulin inhibitor is a toxin payload in antibody drugconjugate Target MMAF is a new auristatin derivative with ahellip

Bioactivity Mertansine (DM1) is a inhibitor and is anmicrotubulinantibody-conjugatable maytansinoid that is developed toovercome systemic toxicity associated with maytansine and toenhance tumor-specific delivery Mertansine can be attached toa monoclonal antibody with a linker to create an antibody-drughellip

96 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Estramustine phosphate sodium Cat No HY-13627

Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449

Ixabepilone (Azaepothilone B BMS 247550 BMS 247550-1) Cat No HY-10222

Lexibulin (CYT-997) Cat No HY-10498

Lexibulin dihydrochloride (CYT-997 dihydrochloride) Cat No HY-10498A

Maytansinol (Ansamitocin P-0) Cat No HY-19474

Mc-MMAD Cat No HY-15740

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741

McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578

Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792

wwwMedChemExpresscom 97

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9957Clinical Data Phase 3Size 10mM x 1mL in Water

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 4Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity Microtubule inhibitor 1 is an antitumor agent with inhibitory activity with anmicrotubule polymerization

value of 9-16 nM in cancer cells IC50[1]

Bioactivity MMAD is a potent inhibitor is a toxin payload intubulinantibody drug conjugates ( )ADCs

Bioactivity MMAF (Monomethylauristatin F) is an antitubulin agent thatinhibit cell division inhibits H3397 cell growth with an IC50of 105 nM

Bioactivity MMAF hydrochloride is an antitubulin agent that inhibit celldivision inhibits H3397 cell growth with an of 105 nMIC50

Bioactivity Monomethyl auristatin E (MMAE SGD-1010) is a syntheticderivative of dolastatin 10 and functions as a potent

inhibitor by inhibiting tubulin polymerizationmitoticMMAE is widely used as a cytotoxic component of antibody-drug

to treat several different cancer typesconjugates (ADCs)

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity Ombrabulin (AVE8062) is a derivative of CA-4 phosphate whichis known to exhibit antivascular effects through selectivedisruption of the cytoskeleton of endothelial cellstubulin

Bioactivity Ombrabulin hydrochloride is a derivative of CA-4 phosphatewhich is known to exhibit antivascular effects throughselective disruption of the cytoskeleton of endothelialtubulincells

Bioactivity OSIP-486823 is a novel -interfering agent withmicrotubuledistinct biological effects on both protein kinase G (PKG) andmicrotubules

Bioactivity Paclitaxel (Taxol) a naturally occurring antineoplasticagent stabilizes resulting intubulin polymerizationarrest at the G2M phase of the cell cycle and apoptotic celldeath [1] [2]

Microtubule inhibitor 1 Cat No HY-114313

MMAD (Demethyldolastatin 10 Monomethylauristatin D

Monomethyl Dolastatin 10) Cat No HY-15581

MMAF (Monomethylauristatin F) Cat No HY-15579

MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat No HY-15579A

Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162

Nocodazole (Oncodazole R17934) Cat No HY-13520

Ombrabulin (AVE8062 AC7700) Cat No HY-14797

Ombrabulin hydrochloride (AVE8062 (hydrochloride) AC7700 (hydrochloride)) Cat No HY-18256

OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004

Paclitaxel (Taxol) Cat No HY-B0015

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9979Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9344Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9968Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Bioactivity Parbendazole is a potent inhibitor of assemblymicrotubuledestabilizes tubulin with an of 879nM and exhibitsEC50a broad-spectrum anthelmintic activity

Bioactivity PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX) compound acts asa -depolymerizing agent and an apoptotic agentmicrotubule

Bioactivity PE859 is a potent inhibitor of both and aggregationtau Aβwith values of 066 and 12 μM respectivelyIC50

Bioactivity PF-06380101 is a novel cytotoxic Dolastatin 10 analogue withexcellent potencies in tumor cell proliferation assays anddifferential ADME properties when compared to other syntheticauristatin analogues that are used in the preparation of ADCsIC50 value ~02 nM(GI50 in BT474 MDA-MB-361-DYT2 and N87hellip

Bioactivity Plinabulin (NPI-2358) is a vascular disrupting agents (VDA)against tubulin-depolymerizing with IC50 of 98~18 nM in tumorcells IC50 Value 98~18 nM Target MicrotubuleTubulin invitro NPI-2358 binds to the colchicine-binding site oftubulin and has potent inhibitory to human tumor cell lineshellip

Bioactivity Podofilox (Podophyllotoxin) is a potent inhibitor ofmicrotubule assembly and DNA topoisomerase II

Bioactivity Rosabulin is a potent inhibitor withmicrotubuleanti-cancer activities

Bioactivity Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10derivative and inhibitor of polymerizationtubulin

Bioactivity SSE15206 is a polymerization inhibitor (GI microtubule 50= 197 nM in HCT116 cells) that overcomes multidrug resistanceCauses aberrant mitosis resulting in G2M arrest due toincomplete spindle formation in cancer cells [1]

Bioactivity Taltobulin (HTI-286 SPA-110) is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibitedproliferation of all three hepatic tumor cell lines (mean IC50= 2 nmolL +- 1 nmolL) in vitro Interestingly no decreasehellip

98 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Parbendazole (SKF 29044) Cat No HY-115364

PBOX 6 Cat No HY-U00446

PE859 Cat No HY-12662

PF-06380101 Cat No HY-12522

Plinabulin (NPI-2358) Cat No HY-14444

Podofilox (Podophyllotoxin) Cat No HY-15552

Rosabulin (STA 5312) Cat No HY-14934

Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672

SSE15206 Cat No HY-111425

Taltobulin (HTI-286 SPA-110) Cat No HY-15584

wwwMedChemExpresscom 99

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9624Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9996Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Taltobulin hydrochloride is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibits proliferationof all three hepatic tumor cell lines (mean IC50 = 2 nmolL+- 1 nmolL) Interestingly no decrease in viable primaryhellip

Bioactivity Taltobulin trifluoroacetate (HTI-286 SPA-110) is an analogueof Hemiasterlin potent tubulin inhibitor ADCs cytotoxinIC50 value Target tubulin in vitro HTI-286 significantlyinhibited proliferation of all three hepatic tumor cell lines(mean IC50 = 2 nmolL +- 1 nmolL) in vitro Interestinglyhellip

Bioactivity Tasidotin hydrochloride is a peptide analog of the antimitoticdepsipeptide dolastatin 15 as an inhibitor of microtubuleassembly and microtubule dynamics

Bioactivity Tirbanibulin (KX2-391) is an inhibitor of that targetsSrcthe peptide substrate site of Src with of 9-60 nM inGI50cancer cell lines

Bioactivity Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) isan inhibitor of that targets the peptide substrate siteSrcof Src with of 9-60 nM in cancer cell linesGI50

Bioactivity Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitorof that targets the peptide substrate site of Src withSrc

of 9-60 nM in cancer cell linesGI50

Bioactivity Triclabendazole(CGA89317) is a benzimidazole it binds totubulin impairing intracellular transport mechanisms andinterferes with protein synthesis Target MicrotubuleTubulinTriclabendazole treatment produces percentage decreases of thefluke egg output by 153 43 and 366 respectively inhellip

Bioactivity Tubulin inhibitor 1 is a inhibitor occupying thetubulincolchicine binding site inhibits tubulin polymerizationTubulin inhibitor 1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase and inducescellular apoptosis [1]

Bioactivity Tubulysin A(TubA) is a myxobacterial product that can functionas an antiangiogenic agent in many in vitro assaysanti-microtubule anti-mitotic an apoptosis induceranticancer anti-angiogenic and antiproliferative IC50value Target microtubule Tubulysin A is a novel antibiotichellip

Bioactivity Valecobulin (CKD516) a valine prodrug of (S516) and avascular disrupting agent (VDA) is a potent beta-tubulin

inhibitor with marked antitumor activitypolymerizationagainst murine and human solid tumors [1] [2]

Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A

Tasidotin hydrochloride (ILX651) Cat No HY-13760

Tirbanibulin (KX2-391 KX-01) Cat No HY-10340

Tirbanibulin dihydrochloride (KX2-391 (dihydrochloride) KX-01 (dihydrochloride)) Cat No HY-10340A

Tirbanibulin Mesylate (KX2-391 (Mesylate) KX01 (Mesylate)) Cat No HY-10340B

Triclabendazole (CGA89317) Cat No HY-B0621

Tubulin inhibitor 1 Cat No HY-112607

Tubulysin A (TubA) Cat No HY-15995

Valecobulin (CKD-516) Cat No HY-13598

Purity 9958Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9914Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data LaunchedSize 10 mg 50 mg 100 mg 200 mg

Purity 9987Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9989Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Bioactivity Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulininhibitor (MMAD) Vc-MMAD is an antibody drug conjugate IC50Valu NA Target tubulin ADCs Monomethyl auristatin D(MMAD) a potent tubulin inhibitor is a toxin payload andantibody drug conjugate For comparison purposes the ADC A1hellip

Bioactivity VcMMAE is a with potentdrug-linker conjugate for ADCantitumor activity by using the anti-mitotic agent monomethylauristatin E (MMAE) linked via the lysosomally cleavabledipeptide valine-citrulline (vc)

Bioactivity Vinblastine sulfate is a cytotoxic alkaloid used againstvarious cancer types Vinblastine sulfate inhibits theformation of microtubule and suppresses nAChR with an ofIC5089 μM

Bioactivity Vincristine sulfate is an antitumor vinca alkaloid whichinhibits formation in mitotic spindlemicrotubuleresulting in an arrest of dividing cells at the metaphasestage It binds to with a of 85 nMmicrotubule Ki

Bioactivity Vinflunine is a new vinca alkaloid uniquely fluorinated withthe properties of mitotic-arresting and tubulin-interactingactivity

Bioactivity Vinflunine Tartrat is a new vinca alkaloid uniquelyfluorinated with the properties of mitotic-arresting andtubulin-interacting activity Target MicrotubuleTubulin Themajor effects of Vinflunine on dynamic instability are aslowing of the microtubule growth rate an increase in growthhellip

Bioactivity Vinorelbine is an anti-mitotic agent which inhibits theproliferation of Hela cells with IC of 125 nM50

Bioactivity Vinorelbine (ditartrate) is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC of 12550nM

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Vc-MMAD Cat No HY-15742

VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575

Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780

Vincristine sulfate (Leurocristine sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488

Vinflunine Cat No HY-B0628

Vinflunine Tartrate Cat No HY-B0628A

Vinorelbine (KW-2307 base) Cat No HY-12053

Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A

wwwMedChemExpresscom 101

Mps1Monopolar spindle 1

Monopolar spindle 1 (Mps1) also known as TTK is a serine threoninekinase which ensures proper biorientation of sister chromatids on themitotic spindle by the activation of the spindle assembly checkpoint(SAC) Mps1 has been shown to function as the key kinase thatactivates the spindle assembly checkpoint (SAC) to secure properdistribution of chromosomes to daughter cellsMps1 is a dual specificity protein kinase that is essential for thebipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomesare properly attached Mps1 is expressed at high levels during mitosisand is abundantly expressed in cancer cells Disruption of Mps1

function induces aneuploidy and cell death

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Mps1 Inhibitors amp Modulators

Bioactivity AZ3146 is a reasonably potent and selective inhibitorMps1with of 35 nM for Mps1 IC50

CatBioactivity BAY 1217389 is a potent and selective inhibitor of the

monopolar spindle 1 ( ) kinase with an value lessMPS1 IC50than 10 nM

Bioactivity BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1)checkpoint with an of 2 nMIC50

Bioactivity CCT251455 is a potent and selective mitotic kinase monopolarspindle 1 ( ) inhibitor with an of 3 nMMPS1 IC50

Bioactivity CFI-402257 is a highly selective and orally bioavailable inhibitor with an of 17 nM for TTK in vitroTTKMps1 IC50

CFI-402257 has anti-cancer activity [1]

Bioactivity CFI-402257 hydrochloride is a highly selective and orallybioavailable inhibitor with an of 17 nM forTTKMps1 IC50TTK in vitro CFI-402257 hydrochloride has anti-canceractivity [1]

Bioactivity Empesertib (BAY 1161909) is a potent inhibitor withMps1an of lt 1 nMIC50

Bioactivity MPI-0479605 is a potent and selective ATP-competitiveinhibitor of with an of 18 nMMps1 IC50

Bioactivity Mps1-IN-1 is a potent selective and ATP-competitive Mps1kinase inhibitor with an and a of 367 nM and 27 nMIC50 Kd

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

102 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

AZ3146 Cat No HY-14710

BAY1217389 Cat No HY-12859

BOS-172722 Cat No HY-112162

CCT251455 Cat No HY-12603

CFI-402257 Cat No HY-101340

CFI-402257 hydrochloride Cat No HY-101340A

Empesertib (BAY 1161909) Cat No HY-12858

MPI-0479605 Cat No HY-12660

Mps1-IN-1 Cat No HY-13298

Mps1-IN-2 Cat No HY-13994

wwwMedChemExpresscom 103

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-3 is a potent and selective kinase inhibitorMPS1with an of 50 nMIC50

Bioactivity NMS-P715 is a selective ATP-competitive inhibitor of MPS1with an of 182 nMIC50

Bioactivity NMS-P715 analog is an inhibitor of with an of 84MPS1 IC50nM

Mps1-IN-3 Cat No HY-12401

NMS-P715 Cat No HY-12382

NMS-P715 analog Cat No HY-14712

Nucleoside AntimetaboliteAnalog

Nucleoside analogues are molecules that act like nucleosides in DNAsynthesis They include a range of antiviral products used to preventviral replication in infected cells Nucleoside analogues can be usedagainst hepatitis B virus hepatitis C virus herpes simplex and HIVOnce they are phosphorylated they work as antimetabolites by beingsimilar enough to nucleotidesto be incorporated into growing DNAstrands Less selective nucleoside analogues are used aschemotherapy agents to treat cancer eg gemcitabine and 5-FUAntimetabolite is a chemical that inhibits the use of a metabolitewhich is another chemical that is part of normal metabolism Suchsubstances are often similar in structure to the metabolite that they

interfere with such as the antifolates that interfere with the use of folic acid The presence of antimetabolites can havetoxic effects on cells such as halting cell growth and cell division so these compounds are used as chemotherapy forcancer

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wwwMedChemExpresscom 105

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Nucleoside AntimetaboliteAnalog Inhibitors amp Modulators

Bioactivity 1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is abicyclic nucleoside

Bioactivity 1-Methylcytosine is a methylated form of the DNA base cytosineand used as a nucleobase of hachimoji DNA in which it pairswith Isoguanine [1] [2]

Bioactivity 1-Methylinosine is a modified nucleotide found at position 37in tRNA 3 to the anticodon of eukaryotic tRNA [1]

Bioactivity 2-Deoxypseudoisocytidine is a nucleoside analogue

Bioactivity 2rsquo-O4rsquo-C-Methyleneuridine (Compound 15a) is a bicyclicnucleoside

Bioactivity 3-Azido-3-deoxy-5-fluorocytidine (Compound 12) is a cytidinederivative

Bioactivity 3-Azido-3-deoxy-beta-L-uridine (Compound 25) is a nucleosidederivative

Bioactivity 3-Methylcytidine a urinary nucleoside can be used as abiomarker of four different types of cancer lung cancergastric cancer colon cancer and breast cancer [1]

Bioactivity 5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methyluridine is a derivative of LNA-type nucleoside

Bioactivity 5-Aza-7-deazaguanine is a substrate for wild-type (WT) E coli and its Ser90Ala mutant in thepurine nucleoside phosphorylase

synthesis of base-modified nucleosides [1]

1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine Cat No HY-111638

1-Methylcytosine Cat No HY-W006395

1-Methylinosine (N1-Methylinosine) Cat No HY-113139

2-Deoxypseudoisocytidine Cat No HY-101968

2rsquo-O4rsquo-C-Methyleneuridine Cat No HY-111639

3-Azido-3-deoxy-5-fluorocytidine Cat No HY-111641

3-Azido-3-deoxy-beta-L-uridine Cat No HY-111642

3-Methylcytidine Cat No HY-111645

5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methylurid

ine

Cat No HY-111807

5-Aza-7-deazaguanine Cat No HY-111627

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9874Clinical Data Phase 4Size 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 960Clinical Data LaunchedSize 50 mg 100 mg 500 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in Water

50 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Bioactivity 5-Azacytidine is a nucleoside analogue of cytidine thatspecifically inhibits DNA methylation by trapping DNA

methyltransferases

Bioactivity 5-BrdU is a nucleoside analog that competes with thymidine forincorporation into DNA 5-BrdU is commonly used in thedetection of proliferating cells

Bioactivity 5-Fluorouracil is a potent antitumor agent that affectspyrimidine synthesis by inhibiting thymidylate synthetasethus depleting intracellular dTTP pools

Bioactivity 6-Amino-5-nitropyridin-2-one is a pyridine base and used as anucleobase of hachimoji DNA in which it pairs with5-aza-7-deazaguanine [1]

Bioactivity 6-Mercaptopurine is a purine analogue which acts as anantagonist of the and has been widely usedendogenous purinesas antileukemic agent and immunosuppressive drug

Bioactivity 6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MPhydrate) is a purine analogue which acts as an antagonist ofthe and has been widely used asendogenous purinesantileukemic agent and immunosuppressive drug

Bioactivity 6-O-Methyl Guanosine is a modified nucleoside 6-O-Methyl[1]

Guanosine (6-methylguanosine) inhibit colony-forming abilityin a malignant xeroderma pigmentosum cell line [2]

Bioactivity 7-Methylguanosine is a novel cNIIIB nucleotidase inhibitorwith IC value of 878 plusmn 75 microM50

Bioactivity 8-Azaguanine is a purine analogue which shows antineoplasticactivity

Bioactivity Adenosine is a nucleoside composed of a molecule of adenineattached to a ribose sugar molecule (ribofuranose) moiety viaa β-N9-glycosidic bond Target Nucleosideantimetaboliteanalog Adenosine plays an important role inbiochemical processes such as energy transfer mdash as adenosinehellip

106 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

5-Azacytidine (Ladakamycin 5-AzaC Azacitidine) Cat No HY-10586

5-BrdU (BUdR BRDU) Cat No HY-15910

5-Fluorouracil (5-FU) Cat No HY-90006

6-Amino-5-nitropyridin-2-one Cat No HY-50071

6-Mercaptopurine (Mercaptopurine 6-MP) Cat No HY-13677

6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MP hydrate) Cat No HY-13677A

6-O-Methyl Guanosine Cat No HY-111648

7-Methylguanosine Cat No HY-122524

8-Azaguanine Cat No HY-B1468

Adenosine (Adenine riboside D-Adenosine) Cat No HY-B0228

wwwMedChemExpresscom 107

Purity 9818Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 1 g

Purity 9897Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carmofur is a derivative of fluorouracil an antimetaboliteused as an antineoplastic agent

Bioactivity Clofarabine(Clolar Clofarex) inhibits the enzymaticactivities of ribonucleotide reductase (IC50 = 65 nM) and DNApolymerase IC50 Value 65 nM Target in vitro Clofarabine isa second generation purine nucleoside analog withantineoplastic activity It is phosphorylated intracellularlyhellip

Bioactivity CNDAC is a major metabolite of oral drug sapacitabine and anucleoside analog

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Cytidine is a nucleoside molecule that is formed when cytosineis attached to a ribose ring cytidine is a component of RNATarget Nucleoside antimetaboliteanalog Cytidine is anucleoside molecule that is formed when cytosine is attachedto a ribose ring (also known as a ribofuranose) via ahellip

Bioactivity Dacarbazine(DTIC-Dome DTIC) is an antineoplastic agent Ithas significant activity against melanomas Target Nucleosideantimetaboliteanalog Approved May 1975 Dacarbazine (DTIC) isthe only single-agent approved by the Food and DrugAdministration for treating metastatic melanoma With DTIC ashellip

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Deoxypseudouridine is a nucleotide analog

Capecitabine Cat No HY-B0016

Carmofur (HCFU) Cat No HY-B0182

Clofarabine Cat No HY-A0005

CNDAC Cat No HY-16445A

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Cytidine (Cytosine β-D-riboside Cytosine-1-β-D-ribofuranoside) Cat No HY-B0158

Dacarbazine (Imidazole Carboxamide) Cat No HY-B0078

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Deoxypseudouridine Cat No HY-101970

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in Water

1000u g 2500u g 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 2500u g 5 mg 10 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 50 mg

Bioactivity DMTr-LNA-5MeU-3-CED-phosphoramidite is a nucleoside derivative[1]

Bioactivity Doxifluridine is a thymidine phosphorylase activator forPC9-DPE2 cells with IC50 of 062 μM

Bioactivity Ethynylcytidine is a new nucleoside antimetabolite Bioactivity Floxuridine (5-fluorodeoxyuridine) is an oncology drug thatbelongs to the class known as antimetabolites with an GI50 of51 μM for the inhibition of PEPT1 IC50 value TargetNucleoside antimetaboliteanalog Floxuridine (Fludara) is aprodrug of floxuridine and an oncology agent with an GI50 ofhellip

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

Bioactivity Fludarabine (phosphate) is an analogue of adenosine anddeoxyadenosine which is able to compete with dATP forincorporation into DNA and inhibit DNA synthesis

Bioactivity Forodesine(BCX-1777 freebase Immucillin-H) is an orallybioavailable PNP inhibitor with picomolar potency inducesapoptosis mainly in T cells

Bioactivity Forodesine hydrochloride is a potent and oral purine nucleoside inhibitor with s ranging from 048 tophosphorylase (PNP) IC50

157 nM

Bioactivity Fosteabine is an oral and prodrug analogue of cytarabine whichis resistant to deoxycytidine deaminase

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

108 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

DMTr-LNA-5MeU-3-CED-phosphoramidite Cat No HY-111531

Doxifluridine (Ro 21-9738 5-Fluoro-5-deoxyuridine 5-DFUR) Cat No HY-B0021

Ethynylcytidine (ECyD TAS-106 3-C-Ethynylcytidine) Cat No HY-16200

Floxuridine (5-Fluorouracil 2-deoxyriboside) Cat No HY-B0097

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Fludarabine phosphate (NSC 118218 (phosphate)) Cat No HY-B0028

Forodesine (BCX-1777 freebase Immucillin-H) Cat No HY-16210

Forodesine hydrochloride (BCX-1777 Immucillin-H hydrochloride) Cat No HY-16209

Fosteabine (Cytarabine ocfosfate YNK 01) Cat No HY-106349

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

wwwMedChemExpresscom 109

Purity 9575Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 9971Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9829Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Gemcitabine elaidate(CP-4126 CO-101) is a lipophilicunsaturated fatty acid ester derivative of gemcitabine (dFdC)an antimetabolite deoxynucleoside analogue with potentialantineoplastic activity IC50 value Target Gemcitabineanalog Upon hydrolysis intracellularly by esterases thehellip

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity Isocytosine is a non-natural nucleobase and an isomer ofcytosine It is used in combination with Isoguanine in studiesof unnatural nucleic acid analogues of the normal base pairsin DNA and used as a nucleobase of hachimoji RNA [1] [2]

Bioactivity Isoguanine is a purine base that is an isomer of guanine Abuilding block in organic synthesis

Bioactivity LY2334737 is an orally available prodrug of gemcitabine whichis a nucleoside analog used as chemotherapy

Bioactivity N2-methylguanosine is a modified nucleoside that occurs atseveral specific locations in many tRNAs

Bioactivity N6N6-Dimethyladenosine is a modified ribonucleosidepreviously found in rRNA and also exhibits in mycobacteriumbovis Bacille Calmette-Gueacuterin tRNA [1]

Bioactivity N6-Etheno 2-deoxyadenosine is a reactive oxygen species(ROS)reactive nitrogen species (RNS)-induced DNA oxidationproduct used as a biomarker to evaluate chronic inflammationand lipid peroxidation in animal or human tissues [1]

Bioactivity Nelarabine (Arranon 506U78) is a purine nucleoside analog andDNA synthesis inhibitor with IC50 from 0067-215 μM in tumorcells Nelarabine is a chemotherapy drug used in T-cell acutelymphoblastic leukemia

Bioactivity Orotic acid (OA) is an intermediate in pyrimidine metabolismIC50 Value Target Nucleoside antimetaboliteanalog in vitroOA increases cell proliferation and decreases apoptosis inserum-starved SK-Hep1 hepatocellular carcinoma cells whichmay ascribe to the inhibition of AMP-activated protein kinasehellip

Gemcitabine elaidate (CP-4126 CO-101 Gemcitabine 5-elaidate) Cat No HY-13538

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

Isocytosine Cat No HY-W002272

Isoguanine Cat No HY-124143

LY2334737 Cat No HY-13672

N2-Methylguanosine Cat No HY-111647

N6N6-Dimethyladenosine Cat No HY-101984

N6-Etheno 2-deoxyadenosine Cat No HY-111646

Nelarabine (506U78 GW 506U78 Nelzarabine) Cat No HY-13701

Orotic acid (6-Carboxyuracil Vitamin B13) Cat No HY-N0157

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9972Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9783Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9887Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9745Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity Pseudothymidine is a C-nucleoside analog of thymidine Bioactivity Raltitrexed is an antimetabolite drug used in chemotherapyacting by inhibiting thymidylate synthase

Bioactivity RX-3117(TV-1360 Fluorocyclopentenylcytosine) is novel acytidine analog shows anticancer activity in several cancercell lines including gemcitabine-resistant variants

Bioactivity Sapacitabine is an orally available prodrugnucleoside analogthat is structurally related to cytarabine

Bioactivity Tegafur (FT 207 NSC 148958) is a chemotherapeutic 5-FUprodrug used in the treatment of cancers is a component oftegafur-uracil

Bioactivity Tipiracil is a thymidine phosphorylase ( ) inhibitorTPase

Bioactivity Tipiracil (hydrochloride) is a thymidine phosphorylaseinhibitor (TPI) used for cancer research

Bioactivity Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT)is an irreversible inhibitor andthymidylate synthasethereby suppresses Trifluridine is an antiviralDNA synthesisdrug for infectionherpes simplex virus (HSV)

Bioactivity Trifluridine-tipiracil hydrochloride mixture (TAS-102) is anovel oral combination drug that consists of an antineoplasticthymidine-based nucleoside analog trifluorothymidine and apotent inhibitor tipiracil in athymidine phosphorylase105 molar ratio

Bioactivity Vidarabine (Ara-A) an antiviral drug which is active againstherpes simplex and varicella zoster viruses

110 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Pseudothymidine (5-Methyl-2-Deoxypseudouridin) Cat No HY-101969

Raltitrexed (ZD1694 D1694 ICI-D1694) Cat No HY-10821

RX-3117 (TV-1360 fluorocyclopentenylcytosine) Cat No HY-15228

Sapacitabine (CS682 CYC682) Cat No HY-16445

Tegafur (FT 207NSC 148958) Cat No HY-17400

Tipiracil Cat No HY-A0063A

Tipiracil hydrochloride Cat No HY-A0063

Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT) Cat No HY-A0061

Trifluridinetipiracil hydrochloride mixture (TAS-102) Cat No HY-16478

Vidarabine (Ara-A Adenine Arabinoside

9-β-D-Arabinofuranosyladenine) Cat No HY-B0277

wwwMedChemExpresscom 111

p97VCPCdc48

p97 an abundant hexameric ATPase of the AAA family is involved inhomotypic membrane fusion It is thought to disassemble SNAREcomplexes formed during the process of membrane fusion Twostructures have been reported a crystal structure of the N-terminaland D1 ATPase domains of murine p97 at 29 A resolution and acryoelectron microscopy structure of full-length rat p97 at 18 Aresolution Together these structures show that the D1 and D2hexamers pack in a tail-to-tail arrangement and that the N domain isflexible A comparison with NSF D2 (ATP complex) reveals possibleconformational changes induced by ATP hydrolysis

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9765Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

p97 Inhibitors amp Modulators

Bioactivity CB-5083 is a potent selective and orally bioavailable p97inhibitor with an value of 11 nMIC50

Bioactivity DBeQ is a selective potent reversible and ATP-competitive inhibitor with an value of 15 μM and 16 μM forp97 IC50

p97(wt) and p97(C522A) respectively DBeQ also inhibits Vps4with an of 115 μMIC50

Bioactivity ML240 is a potent inhibitor inhibiting p97 ATPase withp97 value of 100 nMIC50

Bioactivity ML241 hydrochloride is a potent inhibitor inhibiting p97p97ATPase with value of 100 nMIC50

Bioactivity NMS-859 is a potent covalent inhibitor withVCP (p97)s of 037 and 036 μM for wild-type VCP in the presence ofIC50

60 μM and 1 mM ATP in cells respectively

Bioactivity NMS-873 is a potent selective allosteric inhibitorVCPp97with value of 30 nMIC50

112 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CB-5083 Cat No HY-12861

DBeQ (JRF 12) Cat No HY-15945

ML240 Cat No HY-19795

ML241 hydrochloride Cat No HY-19797A

NMS-859 Cat No HY-15714

NMS-873 Cat No HY-15713

wwwMedChemExpresscom 113

PAKp21 activated kinases

PAKs (p21-activated kinases) are key regulators of actin dynamics cellproliferation and cell survival PAKs are SerThr kinases that areclassified into two groups on the basis of their structural andfunctional features group I (PAK1ndash3) and group II (PAK4ndash6) Group IPAKs have an auto-inhibitory domain (also called an inhibitory switchdomain) and a kinase domain (catalytic domain CD) and are activatedby the binding of the active (that is GTP-bound) forms of RhoGTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPasesBecause the deregulation of PAKs is closely associated with varioushuman diseasessmall-molecule inhibitors of these kinases have great

potential as therapeutic agents In addition these compounds can also be used as powerful tools in studies aimed atunderstanding the PAK signaling pathwayPAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actinremodelling and their ability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role intumor cell invasion and metastasis The current evidence suggests the involvement of PAKs in motility cell survivalanchorage-independent growth angiogenesis invasion migration and regulation of cell cycle and mitosisConsequently PAKs have also been implicated in a number of pathological conditions including cancer

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9902Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 1 g 5 g

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

PAK Inhibitors amp Modulators

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Fingolimod is a ( ) antagonistsphingosine 1-phosphate S1Pwith of 0033 nM in K562 and NK cells Fingolimod also isIC50a activatorpak1

Bioactivity Fingolimod hydrochloride is a ( )sphingosine 1-phosphate S1Pantagonist with an of 0033 nM in K562 and NK cellsIC50Fingolimod hydrochloride also is a activatorpak1

Bioactivity FRAX1036 is a inhibitor with s of 233 nM 724 nM andPAK Ki24 μM for PAK1 PAK2 and PAK4 respectively

Bioactivity FRAX486 is a p21-activated kinase ( ) inhibitor with sPAK IC50of 14 33 and 39 nM for PAK1 PAK2 and PAK3 respectively

Bioactivity FRAX597 is a potent group I p21-activated Kinases ( s)PAKinhibitor with of 8 13 and 19 nM for and IC50 PAK1 2 3

Bioactivity G-5555 is a potent p21-activated kinase 1 ( ) inhibitorPAK1with s of 37 nM and 11 nM for PAK1 and PAK2 respectivelyKi

Bioactivity G-5555 hydrochloride is a potent and selective p21-activatedkinase 1 ( ) inhibitor with a of 37 nMPAK1 Ki

Bioactivity IPA-3 is a selective non-ATP competitive inhibitor withPAK1 of 25 μM and shows no inhibition to group II PAKs (PAKsIC50

4-6)

Bioactivity NVS-PAK1-1 is a potent and selective allosteric PAK1inhibitor with an of 5 nMIC50

114 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Fingolimod (FTY720 free base) Cat No HY-11063

Fingolimod hydrochloride (FTY720) Cat No HY-12005

FRAX1036 Cat No HY-19538

FRAX486 Cat No HY-15542B

FRAX597 Cat No HY-15542A

G-5555 Cat No HY-19635

G-5555 hydrochloride Cat No HY-19635A

IPA-3 Cat No HY-15663

NVS-PAK1-1 Cat No HY-100519

wwwMedChemExpresscom 115

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity PAK-IN-1 is a inhibitor that displays group IIPAKselectivity PAK-IN-1 inhibits PAK4 PAK5 and PAK6 with sIC50of 75 36 126 nM respectively

Bioactivity PF-3758309 is an inhbitor of with of 13 nM forPAK IC50PAK4

PAK-IN-1 Cat No HY-12632

PF-3758309 Cat No HY-13007

PARPpoly ADP ribose polymerase

PARP is a family of proteins involved in a number of cellular processesinvolving mainly DNA repair and programmed cell death The PARPfamily comprises 17 members They have all very different structuresand functions in the cell PARP1 PARP2 VPARP (PARP4) Tankyrase-1and -2 (PARP-5a or TNKS and PARP-5b or TNKS2) have a confirmedPARP activity Others include PARP3 PARP6 TIPARP (or PARP7)PARP8 PARP9 PARP10 PARP11 PARP12 PARP14 PARP15 andPARP16 PARP is found in the cellrsquos nucleus The main role is to detectand signal single-strand DNA breaks (SSB) to the enzymaticmachinery involved in the SSB repair

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wwwMedChemExpresscom 117

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9839Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in Water

200 mg 500 mg

PARP Inhibitors amp Modulators

Bioactivity 3-Aminobenzamide is a potent inhibitor of with of appr 50 nM in CHO cellsPARP IC50

and acts as a mediator of oxidant-induced myocyte dysfunctionduring reperfusion

Bioactivity A-966492 is a novel and potent inhibitor of and with of 1 nM andPARP1 PARP2 Ki

15 nM respectively

Bioactivity AG14361 is a potent inhibitor with a of lt 5 nMPARP-1 Kiand in permeabilized SW620 and intact SW620 cells the sIC50are 29 nM and 14 nM respectively

Bioactivity AZ6102 is a potent dual and inhibitor withTNKS1 TNKS2s of 3 nM and 1 nM respectively and alao has 100-foldIC50

selectivity against other PARP family enzymes with s ofIC5020 μM 05 μM and gt3 μM for PARP1 PARP2 and PARhellip

Bioactivity AZD-2461 is a potent inhibitor with s of 5 nM 2 nMPARP IC50and 200 nM for PARP1 PARP2 and PARP3 respectively

Bioactivity BGP-15 is a inhibitor with an and a of 120 andPARP IC50 Ki57 μM respectively

Bioactivity BRCA1-IN-1 is a novel small-molecule-like inhibitorBRCA1with and of 053 μM and 071 μM respecrivelyIC50 Ki

Bioactivity Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolatedfrom traditional Chinese herb WT WangCorydalis yanhusuoDehydrocorydaline regulates protein expression of Bax Bcl-2activates and inactivates caspase-7 caspase-8 PARP

Bioactivity E7449 is a potent and inhibitor and alsoPARP1 PARP2inhibits and with s of 20 10 50 andTNKS1 TNKS2 IC5050 nM for PARP1 PARP2 TNKS1 and TNKS2 respectively using

P-NAD as substrate32 +

Bioactivity G007-LK is a potent and selective inhibitor of andTNKS1 with s of 46 nM and 25 nM respectivelyTNKS2 IC50

3-Aminobenzamide (PARP-IN-1) Cat No HY-12022

A-966492 Cat No HY-10614

AG14361 Cat No HY-12032

AZ6102 Cat No HY-12975

AZD-2461 Cat No HY-13536

BGP-15 Cat No HY-100828

BRCA1-IN-1 Cat No HY-100863

Dehydrocorydaline (13-Methylpalmatine) Cat No HY-N0674

E7449 Cat No HY-12418

G007-LK Cat No HY-12438

Purity 9952Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Bioactivity GeA-69 is a selective highly cell permeable allostericinhibitor of poly-adenosine-diphosphate-ribose polymerase 14

targeting macrodomain 2 with a of 21 microM (PARP14) Kd[1]

Bioactivity Iniparib (BSI-201) is an irreversible inhibitor of PARP1used in the research of triple negative breast cancer

Bioactivity JW 55 is a potent and selective signaling pathwayβ-catenininhibitor which functions via inhibition of the PARP domainof tankyrase 1 and tankyrase 2 (TNKS12) JW 55 decreasesauto-PARsylation of TNKS12 in vitro with s of 19 μM andIC50830 nM respectively

Bioactivity K-756 is a direct and selective ( ) inhibitortankyrase TNKSwhich inhibits the ADP-ribosylation activity of andTNKS1

with s of 31 and 36 nM respectivelyTNKS2 IC50

Bioactivity ME0328 is a potent and selective inhibitor withARTD3 PARP3an of 089plusmn028 μMIC50

Bioactivity MN-64 is a potent inhibitor with s of 6 nMtankyrase 1 IC5072 nM 191 μM and 394 μM for TNKS2 ARTD1 andTNKS1ARTD2 respectively

Bioactivity Niraparib (MK-4827) is a highly potent and PARP1 PARP2inhibitor with s of 38 and 21 nM respectivelyIC50

Bioactivity Niraparib hydrochloride (MK-4827 hydrochloride) is anexcellent and inhibitor with of 38 and 21PARP1 PARP2 IC50nM respectively

Bioactivity Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent inhibitor with of 24 nMPARP1 IC50

Bioactivity Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1and inhibitor with an of 38 and 21 nMPARP2 IC50respectively

118 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

GeA-69 Cat No HY-108708

Iniparib (BSI-201 NSC-746045 IND-71677) Cat No HY-12015

JW 55 Cat No HY-13968

K-756 Cat No HY-U00422

ME0328 Cat No HY-100225

MN-64 Cat No HY-19351

Niraparib (MK-4827) Cat No HY-10619

Niraparib hydrochloride (MK-4827 (hydrochloride)) Cat No HY-10619A

Niraparib R-enantiomer (MK 4827 (R-enantiomer)) Cat No HY-10619D

Niraparib tosylate (MK-4827 (tosylate)) Cat No HY-10619B

wwwMedChemExpresscom 119

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg

Purity 9768Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2 g

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NMS-P118 is a potent orally available and highly selective Inhibitor for cancer therapyPARP-1

Bioactivity NMS-P515 is a potent and stereospecific inhibitorPARP-1with an of 27 nM in hela cells Anti-tumor activity IC50

[1]

Bioactivity NVP-TNKS656 is a highly potent selective and orally active inhibitor with of 6 nM and is gt 300 foldTNKS2 IC50

selectivity against and PARP1 PARP2

Bioactivity Olaparib (AZD2281KU0059436) is a potent and oral PARPinhibitor with s of 5 and 1 nM for and IC50 PARP1 PARP2

respectively

Bioactivity Pamiparib is a inhibitor which can be used for thePARPtreatment of various cancers including the solid tumorextracted from patent WO 2013097225 A1

Bioactivity PARP-2-IN-1 is a potent and selective inhibitor withPARP-2an of 115 nMIC50

Bioactivity PJ34 is a potent specific inhibitor of with ofPARPl 2 IC50110 nM and 86 nM respectively

Bioactivity PJ34 hydrochloride is an inhibitor of with of 110PARPl12 IC50nM and 86 nM respectively

Bioactivity PROTAC PARP1 degrader is a degrader based on thePARP1 technology It induces significant PARP1 cleavage andPROTAC

programmed cell death PROTAC PARP1 degrader at 10 μM at 24 hinhibits MDA-MB-231 cell line with an of 612 μMIC50

Bioactivity RK-287107 is a potent and specific inhibitor withtankyrases of 143 and 106 nM for and IC50 tankyrase-1 tankyrase-2

respectively RK-287107 blocks colorectal cancer cell growth[1]

NMS-P118 Cat No HY-18954

NMS-P515 Cat No HY-128599

NVP-TNKS656 (TNKS656) Cat No HY-13990

Olaparib (AZD2281 KU0059436) Cat No HY-10162

Pamiparib (BGB-290) Cat No HY-104044

PARP-2-IN-1 Cat No HY-102035

PJ34 Cat No HY-13688A

PJ34 hydrochloride Cat No HY-13688

PROTAC PARP1 degrader Cat No HY-114324

RK-287107 Cat No HY-123892

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9962Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9888Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9508Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9983Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9989Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9981Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity Rucaparib (AG014699) is an inhibitor of with of 14 nM for PARP1 in aPARP Ki

cell-free assay and also shows binding affinity to eightother PARP domains

Bioactivity Rucaparib Camsylate is an inhibitor of with a of 14PARP KinM for PARP1 and also shows binding affinity to eight otherPARP domains

Bioactivity Rucaparib phosphate (AG-014699 phosphate) is a potent and oral inhibitor with a of 14 nM for PARP1 in cell-freePARP Ki

assay also showing binding affinity to eight other PARPdomains

Bioactivity Talazoparib (BMN-673) is a highly potent inhibitorPARP12with s of 12 nM and 087 nM respectivelyKi

Bioactivity Talazoparib 8R9S (BMN-673 8R9S) is an enantiomer ofTalazoparib less active than Talazoparib on the inhibition of

with an of 144 nMPARP1 IC50

Bioactivity Talazoparib tosylate (BMN 673ts) is a novel potent and orallyavailable inhibitor with an of 057 nM forPARP12 IC50PARP1

Bioactivity UPF 1069 is a inhibitor with s of 8 and 03 μM forPARP IC50PARP-1 and PARP-2 respectively

Bioactivity Veliparib is a potent inhibitor inhibiting andPARP PARP1 with s of 52 and 29 nM respectivelyPARP2 Ki

Bioactivity Veliparib (dihydrochloride) is a potent inhibitor of and with s of 52PARP1 PARP2 Ki

nM and 29 nM in cell-free assays respectively

Bioactivity WD2000-012547 is a selective poly(ADP-ribose)-polymerase(PARP-1) inhibitor with a pK of 8221i

120 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Rucaparib (AG014699 PF-01367338) Cat No HY-10617A

Rucaparib Camsylate Cat No HY-102003

Rucaparib phosphate (AG-014699 phosphate PF-01367338 phosphate) Cat No HY-10617

Talazoparib (BMN-673 LT-673) Cat No HY-16106

Talazoparib 8R9S (BMN-673 (8R9S) (8R9S)-LT-673) Cat No HY-16106A

Talazoparib tosylate (BMN 673ts) Cat No HY-108413

UPF 1069 Cat No HY-14478

Veliparib (ABT-888) Cat No HY-10129

Veliparib dihydrochloride (ABT-888 dihydrochloride) Cat No HY-10130

WD2000-012547 Cat No HY-U00223

wwwMedChemExpresscom 121

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity XAV-939 is a inhibitor and an indirecttankyrase (TNKS)inhibitor of with s of 5 and 2Wntβ-catenin signaling IC50nM for TNKS1 and TNKS2 respectively

XAV-939 Cat No HY-15147

PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinase

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) isactivated in response to a variety of endoplasmic reticulum stressesimplicated in numerous disease states PERK is implicated intumorigenesis and cancer cell survival GSK2606414 is an orallyavailable potent and selective PERK inhibitor GSK2606414 inhibitsPERK activation in cells and inhibits the growth of a human tumorxenograft in mice PERK activation is independent of the largeincrease in unfolded nascent proteins within the ER followingtransient global brain ischemia

122 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 123

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

PERK Inhibitors amp Modulators

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity GSK2606414 is a cell-permeable and orally available proteinkinase R-like endoplasmic reticulum (ER) kinase (PERK)inhibitor with an of 04 nMIC50

Bioactivity GSK2656157 is a selective and ATP-competitive inhibitor ofprotein kinase R (PKR)-like endoplasmic reticulum kinase (

) with an of 09 nMPERK IC50

Bioactivity ISRIB (trans-isomer) is a potent inhibitor of with anPERK of 5 nMIC50

CCT020312 Cat No HY-119240

GSK2606414 Cat No HY-18072

GSK2656157 Cat No HY-13820

ISRIB trans-isomer Cat No HY-12495

Polo-like Kinase (PLK)

Polo-like Kinases (PLKs) are important regulators of the cell cycle Plksare involved in the formation of and the changes in the mitoticspindle and in the activation of CDKcyclin complexes duringM-phase of the cell cyclePolo-like kinases (Plks) are a family ofconserved serinethreonine kinases involved in the regulation of cellcycle progression through G2 and mitosis Mammalian polo-likekinases include Plk1 (Xenopus Plx1) Plk2Snk (Xenopus Plx2)Plk3PrkFnK (Xenopus Plx3) Plk4Sak and Plk5 Plk1 is involved in theregulation of key steps during cell division DNA damage repairpathways apoptosis and the progression of the cell cycle Plk3 is amultifunctional stress response protein that responses to signals

induced by DNA damage andor mitotic spindle disruption

124 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 125

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9982Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9897Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9857Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Polo-like Kinase (PLK) Inhibitors amp Modulators

Bioactivity BI 2536 is a dual and inhibitor with s of 083PLK1 BRD4 IC50

and 25 nM respectively BI-2536 suppresses IFNB[1]

(encoding IFN-β) gene transcription [4]

Bioactivity Centrinone (LCR-263) is a selective and reversible inhibitorof polo-like kinase 4 ( ) with a of 016 nMPlK4 Ki

Bioactivity Centrinone-B (LCR-323) is a potent and highly selective PLK4inhibitor with a of 059 nMKi

Bioactivity CFI-400945 free base is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity CFI-400945 fumarate is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity GSK461364 is a selective reversible and ATP-competitive inhibitor with a value of 22 nMPolo-like kinase 1 (PLK1) Ki

Bioactivity GW843682X is a selective ATP-competitive inhibitor of PLK1and with s of 22 nM and 91 nM respectively andPLK3 IC50is also gt100-fold selective against 30 other kinases

Bioactivity HMN-214 an orally bioavailable prodrug of HMN-176 is aninhibitor of polo-like kinase-1 ( ) with antitumorplk1activity

Bioactivity LFM-A13 is a potent inhibitor inhibitsBTK JAK2 PLKrecombinant BTK Plx1 and PLK3 with s of 25 μM 10 μM andIC5061 μM LFM-A13 shows no effects on JAK1 and JAK3 Src familykinase HCK EGFR and IRK

Bioactivity MLN0905 is a potent inhibitor with an of 2 nMPLK1 IC50

BI 2536 Cat No HY-50698

Centrinone (LCR-263) Cat No HY-18682

Centrinone-B (LCR-323) Cat No HY-18683

CFI-400945 free base Cat No HY-12300

CFI-400945 fumarate Cat No HY-12300B

GSK461364 (GSK461364A) Cat No HY-50877

GW843682X (GW843682) Cat No HY-11003

HMN-214 (IVX-214) Cat No HY-12045

LFM-A13 Cat No HY-18009

MLN0905 (PLK1 Inhibitor) Cat No HY-15155

Purity 9759Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9949Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9809Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9626Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9970Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

Bioactivity NMS-1286937 is a potent selective and orally available PLK1inhibitor with an of 2 nMIC50

Bioactivity Poloxime a hydrolysis product of poloxin is anon-ATP-competitive inhibitor with moderate Plk1Plk1inhibitory activity

Bioactivity Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1)inhibitor that targets the polo-box domain with an ofIC50appr 48 μM

Bioactivity Rigosertib (ON-01910) is a multi-kinase inhibitor and aselective anti-cancer agent which induces apoptosis byinhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib is a selective andhellip[1] [2]

Bioactivity Rigosertib sodium (ON-01910 sodium) is a multi-kinaseinhibitor and a selective anti-cancer agent which inducesapoptosis by inhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib sodium is a selective andhellip[1] [2]

Bioactivity Ro3280 is a potent highly selective inhibitor of withPLK1an and a of 3 nM and 009 nM respectively andIC50 Kdnearly has no effect on PLK2 and PLK3

Bioactivity SBE13 is a potent and selective inhibitor with an ofPlk1 IC50200 pM SBE13 poorly inhibits Plk2 (IC gt66 μM) or Plk350(IC =875 nM)50

Bioactivity SBE13 Hydrochloride is a potent and selective inhibitorPlk1with an of 200 pM SBE13 Hydrochloride poorly inhibitsIC50Plk2 (IC gt66 μM) or Plk3 (IC =875 nM)50 50

Bioactivity TAK-960 is an orally available selective inhibitor of with an of 08 nM at 10 μMpolo-like kinase 1 (PLK1) IC50

ATP TAK-960 also shows inhibitory activities against PLK2and with s of 169 and 502 nM respectivelyPLK3 IC50

126 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Mps1-IN-2 Cat No HY-13994

NMS-1286937 (NMS-P937) Cat No HY-15828

Poloxime Cat No HY-77195

Poloxin Cat No HY-12134

Rigosertib (ON-01910) Cat No HY-12037A

Rigosertib sodium (ON-01910 sodium) Cat No HY-12037

Ro3280 Cat No HY-15161

SBE13 Cat No HY-15158A

SBE13 Hydrochloride Cat No HY-15158

TAK-960 Cat No HY-15160

wwwMedChemExpresscom 127

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9955Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TAK-960 dihydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 dihydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TAK-960 hydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 hydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TC-S 7005 is a inhibitor with s ofPolo-like kinases (Plks) IC504 nM 24 nM and 214 nM for Plk2 Plk3 and Plk1 respectively

[1]

Bioactivity Volasertib is a highly potent Polo-like kinase 1 (PLK1)inhibitor with an of 087 nM as well as the two closelyIC50related kinases and with s of 5 and 56 nMPLK2 PLK3 IC50respectively

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

TAK-960 dihydrochloride Cat No HY-15160B

TAK-960 hydrochloride Cat No HY-15160A

TC-S 7005 Cat No HY-108597

Volasertib (BI 6727) Cat No HY-12137

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

PPARPeroxisome proliferator-activated receptors

PPARs (Peroxisome proliferator-activated receptors) areligand-activated transcription factors of nuclear hormone receptorsuperfamily comprising of the following three subtypes PPARαPPARγ and PPARβδ PPARs play essential roles in the regulation ofcellular differentiation development and metabolism (carbohydratelipid protein) and tumorigenesis of higher organisms All PPARsheterodimerize with the retinoid X receptor (RXR) and bind to specificregions on the DNA of target genes Activation of PPAR-α reducestriglyceride level and is involved in regulation of energy homeostasisActivation of PPAR-γ enhances glucose metabolism whereasactivation of PPAR-βδ enhances fatty acids metabolism

128 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 129

Purity 9905Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9921Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 980Clinical Data Phase 4Size 50 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg

Purity gt98Clinical Data Phase 2Size 1 mg

Purity 9900Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

PPAR Inhibitors amp Modulators

Bioactivity 4-O-Methyl honokiol is a natural neolignan isolated from acts as a agonist and inhibtisMagnolia officinalis PPARγ

activity used for cancer and inflammation researchNF-κB

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Adelmidrol exerts important anti-inflammatory effects that arepartly dependent on Adelmidrol reduces PPARγ NF-κBtranslocation and expressionCOX-2

Bioactivity Aleglitazar(R1439 RO-0728804) is a new dual PPAR-αγ agonistwith IC50 of 28 nM46 nM

Bioactivity Arhalofenate (MBX 102) is a selective partial agonist ofperoxisome proliferator-activated receptor used for(PPAR)-γthe treatment of type 2 diabetes

Bioactivity Astaxanthin a red dietary carotenoid isolated from is an inhibitor of and aHaematococcus pluvialis PPARγ

potent antioxidant with antiproliferative neuroprotective andanti-inflammatory activity Astaxanthin has potential in[1]

the treatment of various diseases such as cancers andhellip

Bioactivity Astragalus polysaccharide are active components of thepolysaccharides extract of Astragulus attenuatesTNF-α-induced insulin resistance by suppressing miR-721 andactivating and in 3T3-L1 adipocytesPPAR-γ PI3KAkt

Bioactivity AVE-8134 is a potent agonist with values of 100PPARα EC50and 3000 nM for human and rodent PPARα receptor respectively

Bioactivity Balaglitazone is a selective partial agonist with anPPARγ of 1351 μM for human EC50 PPARγ

Bioactivity Bezafibrate is an agonist of with s of 50 μM 60PPAR EC50μM 20 μM for and and 90 μMhuman PPARα PPARγ PPARδ55 μM 110 μM for and murine PPARα PPARγ PPARδrespectively Bezafibrate is used as an hypolipidemic agent

4-O-Methyl honokiol Cat No HY-U00450

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Adelmidrol Cat No HY-B1026

Aleglitazar (R1439 RO0728804) Cat No HY-14728

Arhalofenate (MBX 102 JNJ 39659100) Cat No HY-14831

Astaxanthin Cat No HY-B2163

Astragalus polysaccharide (Astragalus Polysacharin) Cat No HY-N0937

AVE-8134 Cat No HY-U00014

Balaglitazone (DRF 2593 NN 2344) Cat No HY-16086

Bezafibrate (BM15075) Cat No HY-B0637

Purity 9877Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data Phase 4Size 10mM x 1mL in DMSO

500 mg 1 g 5 g 10 g

Purity 9959Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9981Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BMS-687453 is a potent and selective agonist with anPPARα and of 10 nM and 260 nM for human and 4100EC50 IC50 PPARα

nM and gt15000 nM for PPARγ in PPAR-GAL4 transactivationassays

Bioactivity CDDO-Im (CDDO-imidazolide) is an activator of and Nrf2 PPARwith s of 232 and 344 nM for PPARα and PPARγKi

Bioactivity Chiglitazar is a dual agonist with of 12PPARαγ EC s50008 17 μM for PPARα PPARγ and PPARδ respectively

Bioactivity Choline Fenofibrate (ABT-335) is the choline salt offenofibric acid under clinical development as a combinationtherapy with rosuvastatin for the management of dyslipidemia

Bioactivity Ciprofibrate is a peroxisome proliferator-activated receptoragonist

Bioactivity Ciprofibrate D6 is deuterium labeled Ciprofibrate which is aperoxisome proliferator-activated receptor agonist

Bioactivity Clofibrate is an agonist of with s of 50 μM 500PPAR EC50μM for murine PPARα and PPARγ and 55 μM 500 μM for humanPPARα and PPARγ respectively

Bioactivity Daidzein is a soy isoflavone which acts as a activatorPPAR

Bioactivity DG172 dihydrochloride is a selective antagonist withPPARβδan of 27 nMIC50

Bioactivity Elafibranor is a agonist with s of 45 and 175PPARαδ EC50nM respectively

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BMS-687453 Cat No HY-10678

CDDO-Im (RTA-403 TP-235 CDDO-Imidazolide) Cat No HY-15725

Chiglitazar Cat No HY-106266

Choline Fenofibrate (ABT-335) Cat No HY-14739

Ciprofibrate (Win35833) Cat No HY-B0664

Ciprofibrate D6 Cat No HY-B0664S

Clofibrate Cat No HY-B0287

Daidzein Cat No HY-N0019

DG172 dihydrochloride Cat No HY-19737A

Elafibranor (GFT505) Cat No HY-16737

wwwMedChemExpresscom 131

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Ertiprotafib is an inhibitor of PTP1B IkB kinase β (IKK-β)and a dual agonist with an of 16 μMPPARα and PPARβ IC50for PTP1B 400 nM for IKK-β an of ~1 μM forEC50PPARαPPARβ

Bioactivity Eupatilin a lipophilic flavonoid isolated from Artemisiaspecies is a agonist and possesses anti-apoptoticPPARαanti-oxidative and anti-inflammatory activities

Bioactivity Fenofibrate is a agonist with an of 30 μMPPARα EC50 Bioactivity Fenofibric acid an active metabolite of fenofibrate is a activitor with s of 224 microM 147 microM and 106 microMPPAR EC50

for PPARα PPARγ and PPARδ respectively Fenofibric acid alsoinhibits enzyme activity with an of 48 nMCOX-2 IC50

Bioactivity FH535 is an inhibitor of and withWntβ-catenin PPARanti-tumor activities

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Fonadelpar is a agonist used in the research ofPPARδneuroparalytic keratopathy

Bioactivity Gemfibrozil is an activator of used as aPPAR-αlipid-lowering drug Gemfibrozil is also a nonselectiveinhibitor of several isoforms with values forP450 KiCYP2C9 2C19 2C8 and 1A2 of 58 24 69 and 82 μMrespectively

Bioactivity Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2Sanchinoside Rh1) is isolated from the root of Panax GinsengGinsenoside Rh1 inhibits the expression of PPAR-γ TNF-α

and IL-6 IL-1β

Bioactivity Glabridin is a natural isoflavan from bindsGlycyrrhiza glabrato and activates with an of 6115 nM GlabridinPPARγ EC50exhibits antioxidant anti-bacterial anti-nephriticanti-diabetic anti-fungal antitumor anti-inflammatoryantiosteoporotic cardiovascular protective neuroprotectivehellip

Ertiprotafib (PTP 112) Cat No HY-19383

Eupatilin Cat No HY-N0783

Fenofibrate Cat No HY-17356

Fenofibric acid (FNF acid) Cat No HY-B0760

FH535 Cat No HY-15721

Fisetin Cat No HY-N0182

Fonadelpar (NPS-005 SJP-0035) Cat No HY-17633

Gemfibrozil (CI-719) Cat No HY-B0258

Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2 Sanchinoside Rh1) Cat No HY-N0604

Glabridin Cat No HY-N0393

Purity 9875Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9727Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9667Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity GSK0660 is a potent antagonist of and withPPARβ PPARδs of 155 nM for both isoformsIC50

Bioactivity GSK376501A is a selective peroxisome proliferator-activatedreceptor gamma ( ) modulator for the treatment of type 2PPARγdiabetes mellitus

Bioactivity GSK3787 is a selective and irreversible peroxisomeproliferator-activated receptor δ ( ) antagonist withPPARδ

of 66pIC50

Bioactivity GW 501516 is a agonist with an of 11 nMPPARδ EC50

Bioactivity GW 6471 is a potent antagonistPPARα Bioactivity GW0742 is a potent and agonist with an ofPPARβ PPARδ IC501 nM for human in binding assay and s of 1 nMPPARδ EC5011 μM and 2 μM for human PPARα and PPARγPPARδrespectively

Bioactivity GW1929 is a potent agonist with a of 884 forPPAR-γ pKihuman and s of 856 and 827 for human PPAR-γ pEC50 PPAR-γ

and murine respectivelyPPAR-γ

Bioactivity GW7647 is a potent agonist with s of 6 nM 11PPARα EC50μM and 62 μM for human PPARα PPARγ and PPARδ respectively

Bioactivity GW9662 is a potent and selective antagonist with anPPARγ of 33 nM showing 10 and 1000-fold selectivity overIC50

PPARα and PPARδ respectively

Bioactivity Icariin is a flavonol glycoside Icariin inhibits andPDE5 activities with s of 432 nM and 7350 μMPDE4 IC50

respectively Icariin also is a activatorPPARα

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GSK0660 Cat No HY-12377

GSK376501A Cat No HY-101746

GSK3787 Cat No HY-15577

GW 501516 (GW 1516 GSK-516) Cat No HY-10838

GW 6471 Cat No HY-15372

GW0742 (GW610742) Cat No HY-13928

GW1929 Cat No HY-15655

GW7647 Cat No HY-13861

GW9662 Cat No HY-16578

Icariin (Ieariline) Cat No HY-N0014

wwwMedChemExpresscom 133

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9889Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9921Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 2Size 5 mg

Purity 9942Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Bioactivity Imiglitazar (TAK559) is a potent and dual human andPPARα agonist with values of 67 and 31 nMPPARγ1 EC50

Bioactivity Indeglitazar is an orally available peroxisomeproliferator-activated receptor ( ) pan-agonist for allPPARthree PPAR subtypes alpha (α) delta (δ) and gamma (γ)

Bioactivity Inolitazone a novel high-affinity agonist that isPPARγdependent upon PPARγ for its biological activity with ofIC5008 nM for growth inhibition

Bioactivity Inolitazone dihydrochloride is a novel high-affinity PPARγagonist that is dependent upon PPARγ for its biologicalactivity with of 08 nM for growth inhibitionIC50

Bioactivity KD3010 is a potent orally active and selective PPARδagonist

Bioactivity L-165041 is a cell permeable agonist with s of 6 nMPPARδ Kiand appr 730 nM for PPARδ and PPARγ respectively and inducesadipocyte differentiation in NIH-PPARδ cells

Bioactivity Lanifibranor is a pan peroxisome proliferator-activated ( ) agonist with s of 15 087 and 021receptor PPAR EC50

μM for human and respectivelyPPARα PPARσ PPARγ

Bioactivity LJ570 is a dual agonist with s of 105PPARα PPARγ EC50

and 012 μM respectively [1]

Bioactivity MA-0204 is a potent highly selective and orally availableperoxisome proliferator activated receptor δ ( )PPARδmodulator with s of 04 nM 79 nM and 10 nM for humanEC50mouse and rat PPARδ respectively Potential treatment hellip

Bioactivity Magnolol a natural lignan isolated from the stem bark of is a dual agonist of both andMagnolia officinalis RXRα

with values of 104 microM and 177 microMPPARγ EC50respectively

Imiglitazar (TAK-559) Cat No HY-101649

Indeglitazar (PPM 204) Cat No HY-14817

Inolitazone (Efatutazone CS-7017 RS5444) Cat No HY-14792

Inolitazone dihydrochloride (Efatutazone (dihydrochloride)

CS-7017 (dihydrochloride) RS5444 (dihydrochloride)) Cat No HY-14792B

KD-3010 Cat No HY-111068

L-165041 Cat No HY-20019

Lanifibranor (IVA337) Cat No HY-104049

LJ570 Cat No HY-111775

MA-0204 Cat No HY-114739

Magnolol Cat No HY-N0163

Purity 9639Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9918Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in Ethanol

10 mg

Purity gt98Clinical DataSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9872Clinical Data Phase 1Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Bioactivity Naringenin is the predominant flavanone in grapefruitdisplays strong anti-inflammatory and antioxidant activities

Bioactivity Naveglitazar racemate is the racemate of NaveglitazarNaveglitazar is a nonthiozolidinedione peroxisomeproliferator-activated receptor ( ) α-γ dual γ-dominantPPARagonist that has shown glucose-lowering potential in animalmodels and in the clinic

Bioactivity NXT629 is a potent selective and competitive PPAR-αantagonist with an of 77 nM for human PPARα shows highIC50selectivity over other nuclear hormone receptor such asPPARδ PPARγ ERβ GR and TRβ s are 60 15 152 3hellipIC50

Bioactivity Oleoylethanolamide is a high affinity endogenous PPAR-αagonist which plays an important role in the treatment ofobesity and arteriosclerosis

Bioactivity Palmitelaidic acid is the trans isomer of palmitoleic acidPalmitoleic acid is one of the most abundant fatty acids inserum and tissue

Bioactivity Peliglitazar racemate is the racemate of PeliglitazarPeliglitazar is a novel dual αγ PPAR activator

Bioactivity Pemafibrate is a highly selective agonist with anPPARα of 1 nMEC50

Bioactivity Pemafibrate racemate is the racemate of pemafibrate andactivates activity with s of 1 nM gt10 μM andPPARα EC5017 μM for h-PPARα h-PPARγ and h-PPARδ respectively

Bioactivity Pioglitazone is a potent and selective agonist withPPARγhigh affinity binding to the PPARγ ligand-binding domain with

of 093 and 099 μM for human and mouse PPARγEC50respectively

Bioactivity Pioglitazone hydrochloride is a potent and selective PPARγagonist with s of 093 and 099 μM for human and mouseEC50PPARγ respectively

134 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Naringenin Cat No HY-N0100

Naveglitazar racemate Cat No HY-U00036

NXT629 Cat No HY-114263

Oleoylethanolamide (N-(2-Hydroxyethyl)oleamide

N-Oleoyl-2-aminoethanol N-Oleoylethanolamide hellip) Cat No HY-107542

Palmitelaidic Acid (9-trans-Hexadecenoic acid trans-Palmitoleic acid) Cat No HY-N2341

Peliglitazar racemate (BMS 426707-01 racemate) Cat No HY-101738A

Pemafibrate ((R)-K-13675) Cat No HY-17618

Pemafibrate racemate (K13675 (racemate)) Cat No HY-17618A

Pioglitazone (U 72107) Cat No HY-13956

Pioglitazone hydrochloride (U 72107A AD 4833) Cat No HY-14601

wwwMedChemExpresscom 135

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9836Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 250 mg

Bioactivity Pirinixic acid (Wy-14643) is a potent agonist of withPPARαs of 063 μM 32 μM for murine and PPARγ and 50EC50 PPARα

μM 60 μM 35 μM for human PPARγ and PPARδPPARαrespectively

Bioactivity PPAR agonist 1 is an agonist of and usedPPAR α PPAR γfor reducing blood glucose lipid levels lowering cholesteroland reducing body weight

Bioactivity PPARα-MO-1 is a potent modulator extracted from patentPPARαWO2004110982A1 formula I

Bioactivity PPARδ agonist is a agonist extracted from patentPPARδUS20180071304 compound example 10

Bioactivity Pparδ agonist 1 is a agonist with an of 506PPAR-δ EC50nM used in the research of PPAR-delta related diseases suchas mitochondrial diseases muscular diseases vasculardiseases demyelinating diseases and metabolic diseases

Bioactivity Pparδ agonist 2 is a agonist extracted from patent WOPPARδ2016057656 A1

Bioactivity Raspberry ketone is a major aromatic compound of redraspberry widely used as a fragrance in cosmetics and as aflavoring agent in foodstuff also shows agonisticPPAR-αactivity

Bioactivity Retinoic acid is a metabolite of vitamin A that playsimportant roles in cell growth differentiation andorganogenesis Retinoic acid is a natural agonist of RARnuclear receptors with s of 14 nM for RARαβγ RetinhellipIC50

Bioactivity RG-12525 is a a specific competitive and orally effectiveantagonist of the and peptidoleukotrienes LTC4 LTD4 LTE4inhibiting LTC4- LTD4- and LTE4-inducd guinea pig parenchymalstrips contractions with s of 26 nM 25 nM and 7 nMIC50respectively RG-12525 is also a peroxisomehellip

Bioactivity Rosiglitazone (BRL49653) is a selective agonist withPPARγs of 30 nM 100 nM and 60 nM for andEC50 PPARγ1 PPARγ2

respectivelyPPARγ

Pirinixic acid (Wy-14643) Cat No HY-16995

PPAR agonist 1 Cat No HY-U00340

PPARα-MO-1 Cat No HY-U00068

Pparδ agonist Cat No HY-112597

Pparδ agonist 1 Cat No HY-107901

Pparδ agonist 2 Cat No HY-100120

Raspberry ketone (Frambione 4-(4-Hydroxyphenyl)-2-butanone) Cat No HY-N1426

Retinoic acid (ATRA Tretinoin Vitamin A acid all-trans-Retinoic acid) Cat No HY-14649

RG-12525 (NID 525) Cat No HY-101676

Rosiglitazone (BRL49653) Cat No HY-17386

Purity 9953Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9852Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9885Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9803Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9925Clinical Data LaunchedSize 100 mg 500 mg

Bioactivity Rosiglitazone maleate is a potent and selective activator of with s of 30 nM 100 nM and 60 nM for PPARγ EC50 PPARγ1

and respectively and a of appr 40 nMPPARγ2 PPARγ Kdfor Rosiglitazone maleate is also an modulator of PPARγ hellip

Bioactivity Saroglitazar is a novel peroxisome proliferator-activatedreceptor ( ) agonist with predominant PPARα and moderatePPARPPARγ activity with values of 065 pM and 3 nM in HepG2EC50cells respectively

Bioactivity Saroglitazar magnesium is a novel peroxisomeproliferator-activated receptor ( ) agonist withPPARpredominant PPARα and moderate PPARγ activity with EC50values of 065 pM and 3 nM in HepG2 cells respectively

Bioactivity Seladelpar is an orally active potent (50 effectconcentration 2 nM) and specific agonistEC50 PPAR-δ

Bioactivity Seladelpar sodium salt (MBX-8025) is an orally active potentand specific agonist with an of 2 nM showingPPARδ EC50more than 750-fold and 2500-fold selectivity over the PPARαand PPARγ receptors respectively

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

Bioactivity Troglitazone is a agonist with s of 550 nM andPPARγ EC50780 nM for human and murinePPARγ receptor respectively

136 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Rosiglitazone maleate (BRL 49653C) Cat No HY-14600

Saroglitazar Cat No HY-19937

Saroglitazar Magnesium Cat No HY-19937A

Seladelpar (MBX-8025) Cat No HY-19522

Seladelpar sodium salt (MBX-8025 sodium salt RWJ-800025 sodium salt) Cat No HY-19522A

T0070907 Cat No HY-13202

Troglitazone (CS-045) Cat No HY-50935

wwwMedChemExpresscom 137

RAD51

RAD51 protein family assist in repair of DNA double strand breaksRAD51 family members are homologous to the bacterial RecA andyeast Rad51 In humans RAD51 is a 339-amino acid protein that playsa major role in homologous recombination of DNA during doublestrand break repair RAD51 is involved in the search for homologyand strand pairing stages of the process RAD51 can interact with thessDNA-binding protein RPA BRCA2 PALB2 and RAD52 Recentstudies using fluorescent labeled Rad5 has indicated that Rad51fragments elongate via multiple nucleation events followed bygrowth with the total fragment terminating when it reaches about 2μm in length

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

500 mg

RAD51 Inhibitors amp Modulators

Bioactivity Harmine is a natural dual-specificity tyrosinephosphorylation-regulated kinase ( ) inhibitor with(DYRK)anticancer and anti-inflammatory activities

Bioactivity IBR2 is a specific inhibitorRAD51

Bioactivity RAD51 Inhibitor B02 (B02) is an inhibitor of human withRAD51an of 274 μMIC50

Bioactivity RAD51-IN-2 (compound example 67A) is a inhibitorRAD51extracted from patent WO2019051465A1 [1]

Bioactivity RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM Bioactivity RI-2 is a reversible inhibitor with an of 4417RAD51 IC50μM and specifically inhibits homologous recombination repairin human cells

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

138 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Harmine (Telepathine) Cat No HY-N0737A

IBR2 Cat No HY-103710

RAD51 Inhibitor B02 (B02) Cat No HY-101462

RAD51-IN-2 Cat No HY-111887

RI-1 Cat No HY-15317

RI-2 Cat No HY-16904

RS-1 Cat No HY-19793

T0070907 Cat No HY-13202

wwwMedChemExpresscom 139

ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROK

ROCK (Rho-associated protein kinase) is a kinase belonging to theAGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopusinvertebrates and chicken Human ROCK1 has a molecular mass of158 kDa and is a major downstream effector of the small GTPaseRhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces thekinase activity of ROCKs by an autoinhibitory intramolecular fold ifRhoA-GTP is not present ROCK plays a role in a wide range ofdifferent cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators

of the cytoskeleton

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9954Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

ROCK Inhibitors amp Modulators

Bioactivity AT13148 is an orally active and ATP-competitive multi- AGC inhibitor with s of 38 nM402 nM50 nM 8 nM 3 nMkinase IC50

and 6 nM4 nM for Akt123 p70S6K PKA and ROCKIIIrespectively

Bioactivity Azaindole 1 is an orally active and ATP-competitive ROCKinhibitor with s of 06 and 11nM for human andIC50 ROCK-1

respectivelyROCK-2

Bioactivity BDP5290 is a potent inhibitor of both and withROCK MRCKs of 5 nM 50 nM 10 nM and 100 nM for IC50 ROCK1 ROCK2

and respectivelyMRCKα MRCKβ

Bioactivity Chroman 1 is a highly potent inhibitor with an ofROCK2 IC501 nM

Bioactivity Fasudil (HA-1077 AT877) a potent inhibitor of with aROCK of 033 μM for ROCK1 which is also a potent Ki Ca channel2+

antagonist and vasodilator

Bioactivity Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877Hydrochloride) a potent inhibitor of with a of 033ROCK Ki

μM for ROCK1 which is also a potent antagonistCa channel2+

and vasodilator

Bioactivity GSK180736A is a G protein-coupled receptor kinase 2 ( )GRK2inhibitor with an of 077 μMIC50

Bioactivity GSK269962A is a potent inhibitor with s of 16 and 4ROCK IC50nM for recombinant human and respectivelyROCK1 ROCK2

Bioactivity GSK429286A is a selective inhibitor of with an ROCK1 IC50value of 14 nM

Bioactivity H-1152 is a membrane-permeable and selective inhibitorROCKwith a value of 16 nM and an value of 12 nM forKi IC50

ROCK2

140 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

AT13148 Cat No HY-16071

Azaindole 1 (TC-S 7001) Cat No HY-10319

BDP5290 Cat No HY-12437

Chroman 1 Cat No HY-15392

Fasudil (HA-1077 AT877) Cat No HY-10341A

Fasudil Hydrochloride (HA-1077 (Hydrochloride) AT-877 (Hydrochloride)) Cat No HY-10341

GSK180736A Cat No HY-18990

GSK269962A (GSK 269962) Cat No HY-15556

GSK429286A Cat No HY-11000

H-1152 Cat No HY-15720

wwwMedChemExpresscom 141

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9726Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical DataSize 10 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9929Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9940Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9813Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity H-1152 dihydrochloride is a membrane-permeable and selective inhibitor with a value of 16 nM and an valueROCK Ki IC50

of 12 nM for ROCK2

Bioactivity Hydroxyfasudil is a inhibitor with s of 073 andROCK IC50072 μM for and respectivelyROCK1 ROCK2

Bioactivity Hydroxyfasudil hydrochloride is a inhibitor with sROCK IC50of 073 and 072 μM for and respectivelyROCK1 ROCK2

Bioactivity LX7101 is a potent inhibitor of and with LIMK ROCK2 IC50values of 24 16 and 10 nM for LIMK1 LIMK2 and ROCK2respectively also inhibits with an less than 1 nMPKA IC50

Bioactivity Narciclasine is a plant growth modulator Narciclasinemodulates the RhoRho kinaseLIM kinasecofilin signalingpathway greatly increasing GTPase RhoA activity as well asinducing actin stress fiber formation in a RhoA-dependentmanner

Bioactivity Pentanoic acid a short-chain fatty acid is a product ofbacterial metabolism and are associated with allergic skindisorders Pentanoic acid activates signaling pathwayROCK

Bioactivity Ripasudil (K-115) is a specific inhibitor of with sROCK IC50of 19 and 51 nM for and respectivelyROCK2 ROCK1

Bioactivity Ripasudil free base (K-115 free base) is a specific inhibitorof with s of 19 and 51 nM for and ROCK IC50 ROCK2 ROCK1

respectively

Bioactivity RKI-1447 is a potent small molecule inhibitor of andROCK1 with values of 145 nM and 62 nM respectivelyROCK2 IC50

Bioactivity ROCK inhibitor-2 is a selective dual and ROCK1 ROCK2inhibitor with s of 17 nM and 2 nM respectively IC50

[1]

H-1152 dihydrochloride Cat No HY-15720A

Hydroxyfasudil (HA-1100) Cat No HY-13911

Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100

hydrochloride HA1100 hydrochloride) Cat No HY-13911A

LX7101 Cat No HY-12659

Narciclasine (Lycoricidinol) Cat No HY-16563

Pentanoic acid Cat No HY-N6056

Ripasudil (K-115) Cat No HY-15685

Ripasudil free base (K-115 (free base)) Cat No HY-15685A

RKI-1447 Cat No HY-15755

ROCK inhibitor-2 Cat No HY-119937

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2g

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9843Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Bioactivity ROCK-IN-1 is a potent inhibitor of with an of 12ROCK IC50nM for ROCK2

Bioactivity ROCK2-IN-2 is a selective inhibitor extracted fromROCK2patent US20180093978A1 Compound A-30 has an of lt1IC50μM

Bioactivity SAR407899 is a selective potent and ATP-competitive ROCKinhibitor with an of 135 nM for and s of 36IC50 ROCK-2 KinM and 41 nM for human and rat respectivelyROCK-2

Bioactivity SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an of 135 nM forROCK IC50

and s of 36 nM and 41 nM for human and rat ROCK-2 Ki ROCK-2

respectively

Bioactivity SB-772077B dihydrochloride is an aminofurazan-based Rho inhibitor with s of 56 nM and 6 nM towardkinase( ROCK) IC50

ROCK1 and ROCK2 respevtively [1]

Bioactivity SLx-2119 (KD-025) is a selective inhibitor of with anROCK2 of 105 nMIC50

Bioactivity SR-3677 is a potent and selective inhibitor with anROCK-II of ~3 nMIC50

Bioactivity Thiazovivin is a potent inhibitor which can protectROCKhuman embryonic stem cells

Bioactivity Y-27632 is an ATP-competitive inhibitor of and ROCK-I ROCK-IIwith of 220 nM and 300 nM for and Ki ROCK-I ROCK-II

respectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

Bioactivity Y-27632 dihydrochloride is a cell-permeable ATP-competitiveinhibitor of and with s of 220 and 300 nMROCK-I ROCK-II Kirespectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

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ROCK-IN-1 Cat No HY-U00351

ROCK2-IN-2 Cat No HY-103620

SAR407899 Cat No HY-15687A

SAR407899 hydrochloride Cat No HY-15687

SB-772077B dihydrochloride Cat No HY-108518

SLx-2119 (KD-025) Cat No HY-15307

SR-3677 Cat No HY-13300

Thiazovivin Cat No HY-13257

Y-27632 Cat No HY-10071

Y-27632 dihydrochloride Cat No HY-10583

wwwMedChemExpresscom 143

Purity 9923Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity Y-33075 is a selective inhibitor derived from Y-27632ROCKand is more potent than Y-27632 with an of 36 nMIC50

Bioactivity Y-33075 dihydrochloride is a selective inhibitor with anROCK of 36 nMIC50

Bioactivity ZINC00881524 is a inhibitorROCK

Y-33075 (Y 39983) Cat No HY-10067

Y-33075 dihydrochloride Cat No HY-10069

ZINC00881524 Cat No HY-101244

Sirtuin

Sirtuin (Sir2 proteins) are a class of proteins that possess eithermono-ADP-ribosyltransferase or deacylase activity includingdeacetylase desuccinylase demalonylase demyristoylase anddepalmitoylase activity Sirtuins regulate important biologicalpathways in bacteria archaeaand eukaryotes Sirtuins have beenimplicated in influencing a wide range of cellular processes like agingtranscription apoptosis inflammation and stress resistance as well asenergy efficiency and alertness during low-calorie situations Sirtuinscan also control circadian clocks and mitochondrial biogenesis

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wwwMedChemExpresscom 145

Purity 9891Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9909Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Sirtuin Inhibitors amp Modulators

Bioactivity 3-TYP is a selective inhibitor with an of 16 nMSIRT3 IC50more potent over SIRT1 ( =88 nM) SIRT2 ( =92 nM)IC50 IC50

Bioactivity AGK2 is a selective inhibitor with of 35 μM AGK2SIRT2 IC50can also inhibit and with of 30 and 91 μMSIRT1 SIRT3 IC50respectively

Bioactivity AK-1 is a potent specific and cell-permeable inhibitorSIRT2with an of 125 μMIC50

Bioactivity AK-7 is a selective cell- and brain-permeable inhibitorSIRT2with an of 155 μMIC50

Bioactivity Cambinol is a and inhibitor with values of 56SIRT1 SIRT2 IC50and 59 μM respectively

Bioactivity CAY10602 is a activatorSIRT1

Bioactivity Dihydrocoumarin is a compound found in Melilotus Dihydrocoumarin is a inhibitorofficinalis yeast Sir2p

Dihydrocoumarin also inhibits and withhuman SIRT1 SIRT2s of 208 μM and 295 μM respectively IC50

[1]

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Ginkgolide C is a flavone isolated from leavesGinkgo bilobapossessing multiple biological functions such as decreasingplatelet aggregation and ameliorating Alzheimer disease

Bioactivity Inauhzin is a dual inhibitor and acts as anSirT1IMPDH2activator used in the research of cancerp53

3-TYP Cat No HY-108331

AGK2 Cat No HY-100578

AK-1 Cat No HY-101465

AK-7 Cat No HY-16691

Cambinol Cat No HY-100732

CAY10602 Cat No HY-104073

Dihydrocoumarin (Hydrocoumarin Chroman-2-one) Cat No HY-N1926

Fisetin Cat No HY-N0182

Ginkgolide C (BN-52022 Ginkgolide-C) Cat No HY-N0785

Inauhzin (INZ) Cat No HY-15869

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9876Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity MC3482 is a specific sirtuin5 ( ) inhibitorSIRT5 Bioactivity Nicotinamide is a form of vitamin B3 that plays essentialroles in cell physiology through facilitating NAD+ redoxhomeostasis and providing NAD+ as a substrate to a class ofenzymes that catalyze non-redox reactions Nicotinamide is aninhibitor of SIRT1

Bioactivity OSS_128167 is a selective inhibitor with s of 89SIRT6 IC501578 and 751 μM for and respectivelySIRT6 SIRT1 SIRT2

Bioactivity PROTAC Sirt2 Degrader-1 is a SirReal-based acts as aPROTAC degrader composed of a highly potent andSirt2

isotype-selective inhibitor a linker and a bona fideSirt2cereblon ligand for E3 ubiquitin ligase PROTAC Sirt2Degrader-1 shows an of 025 μM for Sirt2 with no effecthellipIC50

Bioactivity Salermide is an inhibitor of and can cause strongSirt1 Sirt2cancer-specific apoptotic cell death

Bioactivity Selisistat (EX-527) is a potent and selective inhibitorSIRT1with of 98 nMIC50

Bioactivity Selisistat S-enantiomer (EX-527 S-enantiomer) is theS-enantiomer of Selisistat with an of 123 nM for SIRT1IC50Selisistat S-enantiomer is much more potent than SelisistatR-enantiomer

Bioactivity SIRT-IN-1 is a potent inhibitor of with of 15SIRT123 IC s5010 33 μM respectively

Bioactivity SIRT-IN-2 is a potent inhibitor of with of 4SIRT123 IC s504 7 μM respectively

Bioactivity Sirt2-IN-1 (Compound 9) is a ( ) inhibitor withsirtuin 2 Sirt2an of 163 nM IC50

[1]

146 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

MC3482 Cat No HY-112587

Nicotinamide (Niacinamide Nicotinic acid amide Vitamin B3) Cat No HY-B0150

OSS_128167 Cat No HY-107454

PROTAC Sirt2 Degrader-1 Cat No HY-103636

Salermide Cat No HY-101073

Selisistat (EX-527) Cat No HY-15452

Selisistat S-enantiomer (EX-527 (S-enantiomer)) Cat No HY-15452A

SIRT-IN-1 Cat No HY-16615

SIRT-IN-2 Cat No HY-16616

Sirt2-IN-1 Cat No HY-112427

wwwMedChemExpresscom 147

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9939Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9887Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9944Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity SIRT5 inhibitor 1 is a potent Human deacylaseSirtuin 5inhibitor with an of 011 μMIC50

Bioactivity Sirtinol is a inhibitor with s of 48 μM 577 μMsirtuin IC50and 131 μM for ySir2 hSIRT2 and hSIRT2 respectively

Bioactivity Sirtuin modulator 1 is a modulator of a homolog of SIRTl SIRT3with EC of lt 1 μM extracted from patent WO 201007185315A1 Compound No4

Bioactivity SRT 1460 a potent activator with an Sirtuin-1 (SIRT1) EC15value of 29 μM shows good selectivity for activation ofSIRT1 versus SIRT2 and SIRT3 (EC15 gt 300 μM) and is morepotent than Resveratrol and the closest sirtuin homologhellip

Bioactivity SRT 1720 is a selective activator of human with anSIRT1 of 016 μM and shows less potent activities agaiinstEC15

SIRT2 and SIRT3 with EC s of 37 μM and gt 300 μM15respectively

Bioactivity SRT 1720 Hydrochloride is a selective activator of withSIRT1an of 016 μM and shows less potent activities onEC15SIRT2 and SIRT3 with EC s of 37 μM and 300 μM15respectively

Bioactivity SRT 2104 is a first-in-class highly selective andbrain-permeable activator of the NAD dependent deacetylase+

increases Sirt1 protein but shows no effect on Sirt1Sirt1mRNA Used in the research of diabetes mellitus hellip

Bioactivity SRT 2183 is a selective activator with anSirtuin-1 (SIRT1) value of 036 μM SRT 2183 induces growth arrestEC15

[1]

and apoptosis concomitant with deacetylation of STAT3 andNF-κB and reduction of c-Myc protein levels [2]

Bioactivity Tenovin-1 is an inhibitor of and ansirtuin 1 sirtuin 2activator of and may have potential in the management ofp53cancer

Bioactivity Tenovin-6 is an inhibitor of and slightly inhibitsSIRT1 SIRT2 and is also a potent activator of with s ofHDAC8 p53 IC50

21 μM 10 μM and 67 μM for SirT1 SirT2 and SirT3respectively

SIRT5 inhibitor 1 Cat No HY-112634

Sirtinol Cat No HY-13515

Sirtuin modulator 1 Cat No HY-19758A

SRT 1460 Cat No HY-124037

SRT 1720 Cat No HY-10532

SRT 1720 Hydrochloride Cat No HY-15145

SRT 2104 Cat No HY-15262

SRT 2183 Cat No HY-19759

Tenovin-1 Cat No HY-13423

Tenovin-6 Cat No HY-15510

Purity 9855Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Tenovin-6 Hydrochloride is an inhibitor of and SIRT1 SIRT2slightly inhibits and is also a potent activator ofHDAC8

with s of 21 μM 10 μM and 67 μM for SirT1 SirT2p53 IC50and SirT3 respectively

Bioactivity Thiomyristoyl is a potent and specific inhibitor with anSIRT2 of 28 nMIC50

Bioactivity UBCS039 is the first synthetic specific Sirtuin 6 (SIRT6)activator inducing autophagy in human tumor cells with an

of 38 μM EC50[1]

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Tenovin-6 Hydrochloride Cat No HY-15510B

Thiomyristoyl Cat No HY-101278

UBCS039 Cat No HY-115453

wwwMedChemExpresscom 149

SRPKSerine-arginine protein kinases

SRPKs is a critical enzyme family that regulates splicing activity in thecell The first serine-arginine (SR) protein kinase identified is SRPK1which is isolated from mitotic cells and it is described tophosphorylate SR proteins and to promote their release from nuclearspeckles during the G2M phase of the cell cycle SRPK1 is theprototype of the SRPK family which also includes the twohomologous SRPK2 and SRPK3 proteins SRPKs are characterized by abipartite catalytic domain separated by a unique spacer sequence andare mainly localized in the cytoplasm of mammalian cellsSRPKs can translocate into the nucleus of cells under severalconditions such as during the G2M phase of the cell cycle or after

osmotic stress or as a consequence of activation of the epidermal growth factor (EGF) signal transduction pathway

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9917Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

SRPK Inhibitors amp Modulators

Bioactivity SPHINX31 is a potent and selective inhibitor of with an ofserinearginine-rich protein kinase 1 (SRPK1) IC50

59 nM SPHINX31 inhibits phosphorylation ofserinearginine-rich splicing factor 1 (SRSF1) SPHINX31 is apotential topical therapeutic for neovascular eye diseasehellip

Bioactivity SRPIN340 is an ATP-competitive serine-arginine-rich proteinkinase ( ) inhibitor with a of 089 μM for SRPK1SRPK Ki

Bioactivity SRPKIN-1 is a covalent and irreversible inhibitorSRPK12with s of 356 and 98 nM respectively Anti-angiogenesisIC50

effect [1]

150 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SPHINX31 Cat No HY-117661

SRPIN340 (SRPK inhibitor) Cat No HY-13949

SRPKIN-1 Cat No HY-116856

wwwMedChemExpresscom 151

Telomerase

Telomerase is a ribonucleoprotein that is an enzyme that adds DNAsequence repeats (TTAGGG in all vertebrates) to the 3 end of DNAstrands in the telomere regions which are found at the ends ofeukaryotic chromosomes This region of repeated nucleotide calledtelomeres contains noncoding DNA and hinders the loss of importantDNA from chromosome ends As a result every time the chromosomeis copied only 100ndash200 nucleotides are lost which causes no damageto the organisms DNA Telomerase is a reverse transcriptase thatcarries its own RNA molecule which is used as a template when itelongates telomeres which are shortened after each replication cycleTelomerase a eukaryotic ribonucleoprotein (RNP) complex contains

both an essential RNA and a protein reverse transcriptase subunit By reverse transcription the telomerase RNPmaintains telomere length stability in almost all cancer cells

Purity 980Clinical Data No Development ReportedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Telomerase Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity BIBR 1532 is a potent selective and non-competitive inhibitor with of 100 nM intelomerase IC50

a cell-free assay

Bioactivity Telomerase-IN-1 is a inhibitor with an ofTelomerase IC50019 μM

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

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360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

BIBR 1532 Cat No HY-17353

Telomerase-IN-1 Cat No HY-U00268

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

wwwMedChemExpresscom 153

TOPKT-LAK cell-originated protein kinase

TOPK (T-lymphokine-activated killer cellndashoriginated protein kinasealso known as PBK or PDZ-binding kinase) is a SerThr protein kinasethat is highly expressed in many types of human cancer includingbreast and lung cancers TOPK is included in the ldquoconsensus stemnessranking signaturerdquo gene list that is up-regulated in cancer stemcell-enriched tumors and is associated with poor prognosis inmultiple types of cancerTOPKPBK is an oncogenic kinase upregulated in most humancancers TOPK is important for mitotic cell division and thatphosphorylation by Cdk1 is needed for its activationTOPK a member of the MEK36-related MAPKK family is expressed in

a wide range of proliferating cells and tissues including cancer cells and testis TOPK negatively regulates the activityof p38α by phosphorylating the p38α-specific phosphatase MKP1 and enhancing the stability of MKP1 The MAPKphosphatase MKP1 an archetypal member of the MKP family plays a pivotal role in the deactivation of p38 through adephosphorylation reaction

Purity 9563Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

TOPK Inhibitors amp Modulators

Bioactivity HI-TOPK-032 is a potent and specific inhibitorTOPK Bioactivity OTS-964 is a potent T-lymphokine-activated killer inhibitor ( =28cell-originated protein kinase (TOPK) IC50

nM) which inhibits TOPK kinase activity with high affinityand selectivity

Bioactivity OTS514 is a highly potent inhibitor which inhibits TOPKTOPKkinase activity with a median inhibitory concentration ( )IC50value of 26 nM

154 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

HI-TOPK-032 Cat No HY-101550

OTS-964 Cat No HY-12467

OTS514 Cat No HY-18621

wwwMedChemExpresscom 155

Topoisomerase

Topoisomerases are enzymes that regulate the overwinding orunderwinding of DNA The winding problem of DNA arises due to theintertwined nature of its double-helical structure Topoisomerases areisomerase enzymes that act on the topology of DNA Type Itopoisomerase cuts one strand of a DNA double helix relaxationoccurs and then the cut strand is reannealed Type I topoisomerasesare subdivided into two subclasses type IA topoisomerases whichshare many structural and mechanistic features with the type IItopoisomerases and type IB topoisomerases which utilize acontrolled rotary mechanism Type II topoisomerase cuts both strandsof one DNA double helix pass another unbroken DNA helix through

it and then reanneal the cut strands This class is also split into two subclasses type IIA and type IIB topoisomeraseswhich possess similar structure and mechanisms

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 1 mg 5 mg

Purity 980Clinical Data LaunchedSize 1 mg 5 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9243Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 9808Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9889Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Topoisomerase Inhibitors amp Modulators

Bioactivity 9-Aminocamptothecin is a inhibitor withtopoisomerase Ipotent anticancer activity

Bioactivity Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) afluorescent molecule and the first described non-peptidicinhibitor showing discrete specificity for the CTRL(chymotrypsin-like) activity of the 20S proteasome [1]

Aclacinomycin A hydrochloride is also a dual inhibitor ofhellip

Bioactivity Aldoxorubicin (INNO-206) is an albumin-binding prodrug ofdoxorubicin which is released from albumin under acidicconditions Aldoxorubicin (INNO-206) has potent antitumoractivities in various cancer cell lines and in murine tumormodels

Bioactivity Amonafide is a inhibitor and DNAtopoisomerase IIintercalator that induces apoptotic signaling by blocking thebinding of Topo II to DNA

Bioactivity Amrubicin (SM-5887) is a DNA inhibitortopoisomerase IIused for the research of cancer

Bioactivity Amrubicin (hydrochloride) (SM-5887 (hydrochloride)) is a DNA inhibitor used for the research of cancertopoisomerase II

Bioactivity Amsacrine (m-AMSA) is an inhibitor of andtopoisomerase IIacts as an antineoplastic agent which can intercalates intothe DNA of tumor cells

Bioactivity Amsacrine hydrochloride (mAMSA hydrochloride) is an inhibitorof and acts as an antineoplastic agenttopoisomerase IIwhich can intercalates into the DNA of tumor cells

Bioactivity Banoxantrone D12 (AQ4N D12) is the deuterium labeledbanoxantrone Banoxantrone is a novel bioreductive agent thatcan be reduced to a stable DNA-affinic compound AQ4 which isa potent inhibitortopoisomerase II

Bioactivity Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) isthe deuterium labeled banoxantrone dihydrochlorideBanoxantrone is a novel bioreductive agent that can be reducedto a stable DNA-affinic compound AQ4 which is a potent

inhibitortopoisomerase II

156 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

9-amino-CPT (9-amino-20(S)-camptothecin) Cat No HY-100309

Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) Cat No HY-N2306A

Aldoxorubicin (INNO-206 DOXO-EMCH) Cat No HY-16261

Amonafide (AS1413) Cat No HY-10982

Amrubicin (SM-5887 AMR) Cat No HY-B0067

Amrubicin hydrochloride (SM-5887 (hydrochloride) AMR (hydrochloride)) Cat No HY-B0067A

Amsacrine (m-AMSA acridinyl anisidide) Cat No HY-13551

Amsacrine hydrochloride (m-AMSA hydrochloride acridinyl anisidide hydrochloride) Cat No HY-13551A

Banoxantrone D12 (AQ4N D12) Cat No HY-13562S

Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) Cat No HY-13562AS

wwwMedChemExpresscom 157

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity 9826Clinical Data Phase 4Size 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9635Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg

Purity 9818Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9880Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg

Bioactivity Banoxantrone dihydrochloride is a novel bioreductive agentthat can be reduced to a stable DNA-affinic compound AQ4which is a potent inhibitortopoisomerase II

Bioactivity Belotecan hydrochloride (CKD-602 hydrochloride) a inhibitor is a synthetic and water-solubleTopoisomerase I

camptothecin derivative

Bioactivity Berberine chloride is an alkaloid isolated from the Chineseherbal medicine Huanglian as an Berberine chlorideantibioticinduces reactive oxygen species ( ) generation andROSinhibits Antineoplastic propertiesDNA topoisomerase

[1]

Bioactivity Berberine chloride hydrate is an alkaloid isolated from theChinese herbal medicine Huanglian as an Berberineantibioticchloride hydrate induces reactive oxygen species ( )ROSgeneration and inhibits AntineoplasticDNA topoisomeraseproperties [1]

Bioactivity Betulinic acid is a natural pentacyclic triterpenoid acts asa eukaryotic inhibitor with an of 5topoisomerase I IC50μM and possesses anti-HIV anti-malarial anti-inflammatoryand anti-tumor properties

Bioactivity Bisantrene is a highly effective antitumor drug targetseukaryotic type II topoisomerases

Bioactivity Campathecin is a potent DNA enzyme topoisomerase Iinhibitor with an of 679 nMIC50

Bioactivity Daun02 is a prodrug of the inhibitortopoisomeraseDaunorubicin

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Banoxantrone dihydrochloride (AQ4N dihydrochloride) Cat No HY-13562A

Belotecan hydrochloride (CKD-602) Cat No HY-13566A

Berberine chloride (Natural Yellow 18 (chloride)) Cat No HY-18258

Berberine chloride hydrate (Natural Yellow 18 (chloride hydrate)) Cat No HY-17577

Betulinic acid (Lupatic acid Betulic acid) Cat No HY-10529

Bisantrene (CL216942) Cat No HY-100875

Campathecin (Camptothecin (S)-(+)-Camptothecin CPT) Cat No HY-16560

Daun02 Cat No HY-13061

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9965Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9888Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9839Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9947Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Doxorubicin is a cytotoxic anthracycline antibiotic for thetreatment of multiple cancers The possible mechanisms bywhich doxorubicin acts in the cancer cell are intercalationinto DNA and disruption of -mediated DNAtopoisomerase-IIrepair

Bioactivity Doxorubicin hydrochloride is a cytotoxic anthracyclineantibiotic for the treatment of multiple cancers The possiblemechanisms by which doxorubicin acts in the cancer cell areintercalation into DNA and disruption of

-mediated DNA repairtopoisomerase-II

Bioactivity Dxd is a potent inhibitor with an ofDNA topoisomerase I IC50031 μM used as a conjugated drug of HER2-targeting ADC(DS-8201a)

Bioactivity Edotecarin is a potent inhibitor of that cantopoisomerase Iinduces single-strand DNA cleavage with of 50 nMIC50

Bioactivity Ellipticine (NSC 71795) is a potent antineoplastic agentinhibits activitiesDNA topoisomerase II

Bioactivity Ellipticine (NSC 71795) hydrochloride is a potentantineoplastic agent inhibits DNA topoisomerase IIactivities

Bioactivity Epirubicin is a semisynthetic L-arabino derivative ofdoxorubicin and an antineoplastic agent by inhibiting

Topoisomerase

Bioactivity Epirubicin (hydrochloride) is a semisynthetic L-arabinoderivative of doxorubicin and an antineoplastic agent byinhibiting Topoisomerase

Bioactivity Etoposide (VP-16 VP-16-213) a chemotherapy medication usedfor the treatments of a number of types of cancer inhibits

by forming a complex with topoisomerase II andDNA synthesisDNA Etoposide arrests cell cycle in G2 and induces apoptoshellip

Bioactivity Exatecan is a water soluble inhibitor withtopoisomerase Ian of 22 μM (0975 μgmL) and can be used in cancerIC50research

158 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Doxorubicin (Hydroxydaunorubicin) Cat No HY-15142A

Doxorubicin hydrochloride (Hydroxydaunorubicin (hydrochloride)) Cat No HY-15142

Dxd (Exatecan derivative for ADC) Cat No HY-13631D

Edotecarin (J 107088 PF 804950) Cat No HY-13618

Ellipticine (NSC 71795) Cat No HY-15753

Ellipticine hydrochloride (NSC 71795 (hydrochloride)) Cat No HY-15753A

Epirubicin Cat No HY-13624

Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride) Cat No HY-13624A

Etoposide (VP-16 VP-16-213) Cat No HY-13629

Exatecan (DX-8951) Cat No HY-13631

wwwMedChemExpresscom 159

Purity 9830Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9803Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9912Clinical Data Phase 3Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg 500 mg

Bioactivity Exatecan Mesylate is a water soluble topoisomerase Iinhibitor with an of 22 μM (0975 μgmL) and can beIC50used in cancer research

Bioactivity Flumequine (R-802) is a quinolone antibiotic and acts as a inhibitor with an of 15 μM (392topoisomerase II IC50

μgmL)

Bioactivity Genz-644282 is a non-camptothecin inhibitortopoisomerase Iused for cancer research

Bioactivity Idarubicin hydrochloride is an anthracycline antileukemicdrug It inhibits the interfering with thetopoisomerase IIreplication of DNA and RNA transcription

Bioactivity Indotecan (LMP-400) is a potent topoisomerase 1(Top1)inhibitor with values of 300 1200 560 nM for P388IC50HCT116 MCF-7 cell lines respectively

Bioactivity Intoplicine is a and inhibitorDNA topoisomerase I II

Bioactivity Irinotecan is a water soluble inhibitortopoisomerase Ipreventing religation of the DNA strand by binding totopoisomerase I-DNA complex

Bioactivity Irinotecan hydrochloride is a water soluble topoisomerase Iinhibitor mainly used to treat colon cancer and rectal cancer

Bioactivity Irinotecan hydrochloride trihydrate is a water soluble inhibitor with antitumor activitytopoisomerase I

Bioactivity Karenitecin (Cositecan) is a inhibitor withtopoisomerase Ipotent anti-cancer activity

Exatecan Mesylate (DX8951f) Cat No HY-13631A

Flumequine (R-802) Cat No HY-B0526

Genz-644282 Cat No HY-16228

Idarubicin hydrochloride (4-Demethoxydaunorubicin hydrochloride) Cat No HY-17381

Indotecan (LMP-400 NSC-724998) Cat No HY-18351

Intoplicine Cat No HY-101647

Irinotecan ((+)-Irinotecan CPT-11) Cat No HY-16562

Irinotecan hydrochloride (CPT-11 hydrochloride Camptothecin 11 hydrochloride) Cat No HY-16562A

Irinotecan hydrochloride trihydrate Cat No HY-16568

Karenitecin (Cositecan BNP 1350) Cat No HY-14812

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9690Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9902Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9702Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg

Bioactivity LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I inhibitor with antitumor activity (Top1) [1]

Bioactivity LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNAintercalator and inhibitor withTopoisomerase I (Top1)antitumor activity [1]

Bioactivity MC-DOXHZN is an albumin-binding prodrug of Doxorubicin withacid-sensitive properties [1]

Bioactivity MC-DOXHZN hydrochloride is an albumin-binding prodrug ofDoxorubicin with acid-sensitive properties [1]

Bioactivity Mitoxantrone is a inhibitor also inhibitstopoisomerase IIprotein kinase C ( ) activity with an of 85 μMPKC IC50

Bioactivity Mitoxantrone dihydrochloride is a topoisomerase IIinhibitor also inhibits protein kinase C ( ) activityPKCwith an of 85 μMIC50

Bioactivity Namitecan is a potent inhibitor withtopoisomerase Iantitumor property

Bioactivity Pirarubicin is an anthracycline antibiotics acts as a inhibitor and is a widely used fortopoisomerase II

treatment of various cancers in particular solid tumors

Bioactivity Pirarubicin Hydrochloride is an anthracycline antibioticsacts as a inhibitor and is a widely usedtopoisomerase IIfor treatment of various cancers in particular solid tumors

Bioactivity Pixantrone is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

160 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

LMP744 (MJ-III65 NSC706744) Cat No HY-U00248

LMP744 hydrochloride (MJ-III65 hydrochloride NSC706744 hydrochloride) Cat No HY-U00248A

MC-DOXHZN (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat No HY-16261A

MC-DOXHZN hydrochloride (Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat No HY-16261B

Mitoxantrone (mitozantrone) Cat No HY-13502

Mitoxantrone dihydrochloride (mitozantrone dihydrochloride) Cat No HY-13502A

Namitecan (ST-1968) Cat No HY-14821

Pirarubicin (THP) Cat No HY-13725

Pirarubicin Hydrochloride (THP Hydrochloride) Cat No HY-13725A

Pixantrone (BBR 2778) Cat No HY-13727

wwwMedChemExpresscom 161

Purity 9920Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 100 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 50 mg 100 mg 200 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9960Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Pixantrone dimaleate is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

Bioactivity Podocarpusflavone A is a DNA topoisomerase I inhibitor havemoderated anti-proliferative activity induce cell apoptosis inMCF-7 is developing anti-tumor drugs target DNAtopoisomerase I In vitro podocarpusflavone-A show significantinhibitions against DLD KB MCF-7 HEp-2 tumor cell lineshellip

Bioactivity SN-38 (NK012) is an active metabolite of the Topoisomerase Iinhibitor Irinotecan SN-38 (NK012) inhibits and DNA RNA

with s of 0077 and 13 μM respectivelysynthesis IC50

Bioactivity SW044248 is a non-canonical inhibitor andtopoisomerase Iselectively toxic for certain non-small cell lung cancer(NSCLC) cell lines

Bioactivity TAS-103 is a dual inhibitor of DNA usedtopoisomerase IIIfor cancer research

Bioactivity TAS-103 dihydrochloride is a dual inhibitor of DNA used for cancer researchtopoisomerase III

Bioactivity Teniposide is a podophyllotoxin derivative acts as a inhibitor and used as a chemotherapeutictopoisomerase II

agent

Bioactivity Top1 inhibitor 1 (compound 28) is a potent human inhibitor with an value of 29topoisomerase I (Top1) IC50

nM [1]

Bioactivity Topotecan (SKF 104864A NSC 609669) is a Topoisomerase Iinhibitor The values of Topotecan at 24 h are 273plusmn025IC50μM of U251 cells 295plusmn023 μM of U87 cells 546plusmn041 μM ofGSCs-U251 and 595plusmn024 μM of GSCs-U87

Bioactivity Topotecan Hydrochloride (SKF 104864A Hydrochloride NSC 609669Hydrochloride) is a inhibitor with potentTopoisomerase Iantineoplastic activities

Pixantrone dimaleate (BBR 2778 dimaleate) Cat No HY-13727A

Podocarpusflavone A Cat No HY-N2198

SN-38 (NK012) Cat No HY-13704

SW044248 Cat No HY-19637

TAS-103 (BMS-247615) Cat No HY-13758

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) Cat No HY-13758A

Teniposide (VM26) Cat No HY-13761

Top1 inhibitor 1 Cat No HY-126142

Topotecan (SKF 104864A NSC 609669) Cat No HY-13768

Topotecan Hydrochloride (SKF 104864A (Hydrochloride) NSC 609669 (Hydrochloride)) Cat No HY-13768A

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Bioactivity Voreloxin is a first-in-class inhibitortopoisomerase IIthat intercalates DNA and induces site-selective DNA DSB G2arrest and apoptosis

Bioactivity Voreloxin Hydrochloride is a first-in-class topoisomerase IIinhibitor that intercalates DNA and induces site-selective DNADSB G2 arrest and apoptosis

Bioactivity β-Lapachone is a naturally occurring O-naphthoquinone acts asa inhibitor and induces apoptosis bytopoisomerase Iinhibiting cell cycle progression

162 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Voreloxin (SNS-595 Vosaroxin AG 7352) Cat No HY-10534

Voreloxin Hydrochloride (SNS-595 Hydrochloride Vosaroxin

Hydrochloride AG 7352 Hydrochloride) Cat No HY-16518

β-Lapachone (ARQ-501 NSC-26326) Cat No HY-13555

wwwMedChemExpresscom 163

Wee1

Wee1 is a nuclear kinase belonging to the SerThr family of proteinkinases in the fission yeast ( )Schizosaccharomyces pombe S pombeWee1 has amolecular mass of 96 kDa and it is a key regulator of cellcycle progression Wee1 influences cell size by inhibiting the entryinto mitosis through inhibiting Cdk1 Wee1 has homologues in manyother organisms including mammals Wee1 inhibits Cdk1 byphosphorylating it on two different sites Tyr15 and Thr14 Cdk1 iscrucial for the cyclin-dependent passage of the various cell cyclecheckpoints At least three checkpoints exist for which the inhibitionof Cdk1 by Wee1 is important G M checkpoint Cell size checkpoint2DNA damage checkpoint Wee1 is shown to phosphorylate histone

H2B at tyrosine 37 residue which regulates global expression of histones

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Wee1 Inhibitors amp Modulators

Bioactivity Adavosertib (AZD-1775 MK-1775) is a potent inhibitorWee1with an of 52 nMIC50

Bioactivity PD0166285 is a inhibitor and a weak inhibitorWEE1 Myt1with s of 24 and 72 nM respectivelyIC50

164 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Adavosertib (AZD1775 MK-1775) Cat No HY-10993

PD0166285 Cat No HY-13925

Page 2: Cell Cycle/DNA Damage - MedchemExpress.com · 2019. 7. 2. · G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition,

2 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 3

bull Nucleoside AntimetaboliteAnalog 104

bull p97 111

bull PAK 113

bull PARP 116

bull PERK 122

bull Polo-like Kinase (PLK) 124

bull PPAR 128

bull RAD51 137

bull ROCK 139

bull Sirtuin 144

bull SRPK 149

bull Telomerase 151

bull TOPK 153

bull Topoisomerase 155

bull Wee1 163

bull Antifolate 3

bull APC 7

bull ATMATR 9

bull Aurora Kinase 12

bull Casein Kinase 17

bull CDK 20

bull Checkpoint Kinase (Chk) 34

bull CRISPRCas9 37

bull Deubiquitinase 39

bull DNA AlkylatorCrosslinker 43

bull DNA-PK 48

bull DNARNA Synthesis 52

bull Eukaryotic Initiation Factor (eIF) 60

bull G-quadruplex 62

bull Haspin Kinase 64

bull HDAC 66

bull HSP 77

bull IRE1 83

bull Kinesin 86

bull LIM Kinase (LIMK) 89

bull MicrotubuleTubulin 91

bull Mps1 101

Inhibitors Agonists Screening LibrarieswwwMedChemExpresscom

Target List in Cell CycleDNA Damage

Antifolate

Antifolates are compounds that antagonise the actions of folic acid(vitamin B9) Folic acids primary function in the body is as a cofactorto various methyltransferases involved in serine methioninethymidine and purine biosynthesis Consequently antifolates inhibitcell division DNARNA synthesis and repair and protein synthesisSome such as Proguanil Pyrimethamine and Trimethoprim selectivelyinhibit folates actions in microbial organisms such as bacteriaprotozoa and fungi The majority of antifolates work by inhibitingdihydrofolate reductase (DHFR) Many are primarily DHFR inhibitorsbut Raltitrexed is an inhibitor of thymidylate synthase andPemetrexed inhibits both and a third enzyme Antifolates act

specifically during DNA and RNA synthesis and thus are cytotoxic during the S-phase of the cell cycle Thus they havea greater toxic effect on rapidly dividing cells

4 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 5

Purity 9517Clinical Data LaunchedSize 10 mg 50 mg

Purity 9524Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg 1 g 2 g

Purity 9973Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9973Clinical Data LaunchedSize 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Antifolate Inhibitors amp Modulators

Bioactivity Calcium N5-methyltetrahydrofolate(NSC173328) is the calciumsalt of levomefolic acid which has been proposed fortreatment of cardiovascular disease and advanced cancers suchas breast and colorectal cancers

Bioactivity Cycloguanil D6 is the deuterium labeled Cycloguanil which isa dihydrofolate reductase inhibitor

Bioactivity Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanilwhich is a dihydrofolate reductase inhibitor

Bioactivity Diaveridine (EGIS-5645) is a ( )dihydrofolate reductase DHFRinhibitor with a of 115 nM for the wild type DHFR and alsoKian antibacterial agent

Bioactivity EC0489 a conjugate of folic acid and desacetyl vinblastinehydrazide is a high-affinity ligand for the folate receptor(FR) Refractory or metastatic Tumor Small molecule-drug[1]

conjugate (SMDC) [2]

Bioactivity Folinic acid is an adjuvant used in cancer chemotherapyinvolving the drug methotrexate Target Antifolate Folinicacid is a 5-formyl derivative of tetrahydrofolic acid It isreadily converted to other reduced folic acid derivatives(eg tetrahydrofolate) and thus has vitamin activity thathellip

Bioactivity Leucovorin Calcium is a reduced folic acid IC50 Value 30 μMfor zcSHMT and70 μM for zmSHMT [2] Target Antifolate invitro Increasing concentrations of leucovorin (N5-CHO-THF)inhibit both zcSHMT and hcSHMT activities substantially yetto a lesser extent than zmSHMT The IC50 of leucovorin ishellip

Bioactivity Folinic Acid is a reduced folic acid which is used incombination with other chemotherapy drugs Target Folateanalog Approved 2008 Folinic acid (calcium salt pentahydrate)is the calcium salt form of folinic acid which is one of theforms of folate found naturally in foods Folate deficiency ishellip

Bioactivity Levoleucovorin calcium is the calcium salt of Levoleucovorinwhich is the enantiomerically active form of folinic acidIC50 value Target Levoleucovorin is used to treat or preventtoxic effects of methotrexate in people who have receivedmethotrexate to treat bone cancer Levoleucovorin is also usedhellip

Bioactivity Levomefolate is an artificial form of folate IC50 ValueTarget Antifolate The calcium salt ofL-5-methyltetrahydrofolic acid which belongs to the group offolate vitamins (Vitamin B9 Folacin) It is a coenzymatedform of folic acid and a more bioavailable alternative inhellip

Calcium N5-methyltetrahydrofolate (NSC173328) Cat No HY-17557

Cycloguanil D6 (Chlorguanide triazine D6) Cat No HY-12784S

Cycloguanil D6 Nitrate (Chlorguanide triazine D6 Nitrate) Cat No HY-12784S1

Diaveridine (EGIS-5645) Cat No HY-B1902

EC0489 Cat No HY-114306

Folinic acid (leucovorin) Cat No HY-17556

Folinic acid Calcium (Leucovorin Calcium Calcium Folinate) Cat No HY-13664

Folinic acid calcium salt pentahydrate (Leucovorin calcium salt pentahydrate) Cat No HY-B0080

Levoleucovorin Calcium (Calcium levofolinate CL307782) Cat No HY-13667

Levomefolate calcium Cat No HY-17383

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9923Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg

Purity 9977Clinical Data LaunchedSize 10mM x 1mL in Water

50 mg 100 mg 200 mg

Purity 9930Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity LY 254155 an antifolate inhibits and binds tohGARFT with s of 21plusmn02 and 17plusmn01 nM respectivelymFBP Ki

Bioactivity LY309887 is a potent inhibitor of glycinamide ribonucleotideformyltransferase ( ) with a of 65 nM and hasGARFT Kiantitumor activity

Bioactivity Methotrexate is a antagonist with median of 78 nMfolate IC50in assayin vitro

Bioactivity Pemetrexed is a novel the values of theantifolate Kipentaglutamate of LY231514 are 13 72 and 65 nM forinhibits thymidylate synthase ( ) dihydrofolate reductaseTS( ) and glycinamide ribonucleotide formyltransferase (DHFR

) respectivelyGARFT

Bioactivity Pemetrexed disodium is a novel that inhibits theantifolatefolatedependent enzymes thymidylate synthase dihydrofolate

and reductase glycinamide ribonucleotide with s of 13 72 and 65 nMformyltransferase Ki

respectively

Bioactivity Pemetrexed disodium hemipenta hydrate is a novel antifolatethe values of the pentaglutamate of LY231514 are 13 72Kiand 65 nM for inhibits thymidylate synthase ( )TSdihydrofolate reductase ( ) and glycinamideDHFRribonucleotide formyltransferase ( ) respectivelyGARFT

Bioactivity Pralatrexate(Folotyn) is an antifolate and structurally afolate analog Its IC50 is lt 300 nM in some cell linesIC50 Value lt 300 nM Target Antifolate Pralatrexate is anantifolate (a folate analogue metabolic inhibitor) designed toaccumulate preferentially in cancer cells Based onhellip

Bioactivity Pyrimethamine(RP4753) is a medication used for protozoalinfections interferes with tetrahydrofolic acid synthesisfrom folic acid by inhibiting the enzyme dihydrofolatereductase (DHFR) IC50 Value 154 nM (Plasmodium falciparum)[1] Target DHFR antifolate in vitro Three susceptibilityhellip

Bioactivity Trimethoprim is a bacteriostatic antibiotic used mainly in theprophylaxis and treatment of urinary tract infections

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LY 254155 Cat No HY-14523

LY309887 Cat No HY-10818

Methotrexate (Amethopterin CL14377 WR19039) Cat No HY-14519

Pemetrexed (LY231514) Cat No HY-10820

Pemetrexed disodium (LY231514 disodium) Cat No HY-10820A

Pemetrexed disodium hemipenta hydrate (LY231514 (disodium hemipenta hydrate)) Cat No HY-13781

Pralatrexate Cat No HY-10446

Pyrimethamine (Pirimecidan Pirimetamin RP 4753) Cat No HY-18062

Trimethoprim Cat No HY-B0510

wwwMedChemExpresscom 7

APCAnaphase promoting complex

APC (Anaphase-Promoting Complex) is an E3 ubiquitin ligase thatmarks target cell cycle proteins for degradation by the 26Sproteasome The APCC is a large complex of 11ndash13 subunit proteinsincluding a cullin (Apc2) and RING (Apc11) subunit much like SCF TheAPCCs main function is to trigger the transition from metaphase toanaphase by tagging specific proteins for degradation The twoproteins of most importance that get degraded in this process assubstrates of the APCC are securin and S and M cyclins Securinreleases separase a protease after being degraded which in turntriggers the cleavage of cohesin the protein complex that binds sisterchromatids together During metaphase sister chromatids are linked

by intact cohesin complexes When securin undergoes ubiquitination by the APCC and releases separase whichdegrades cohesin sister chromatids become free to move to opposite poles for anaphase The APCC also targets themitotic cyclins for degradation resulting in the inactivation of M-CdK (mitotic cyclin-dependent kinase) complexespromoting exit from mitosis and cytokinesis

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9911Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

APC Inhibitors amp Modulators

Bioactivity TAME is a inhibitor and can be also utilizedserine proteaseas a substrate for the serine proteases trypsin plasmin andthrombin TAME is an inhibitor of[1] [2] [3]

which binds to the hellipanaphase-promoting complex (APC)

Bioactivity TAME hydrochloride is a inhibitor and can beserine proteasealso utilized as a substrate for the serine proteases trypsinplasmin and thrombin TAME hydrochloride is an[1] [2] [3]

inhibitor of which bihellipanaphase-promoting complex (APC)

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TAME Cat No HY-13255

TAME hydrochloride Cat No HY-13255A

wwwMedChemExpresscom 9

ATMATRAtaxia telangiectasia mutatedATM and RAD3 related

ATMATR are members of the PI3 family of serine-threonine kinasesand function as essential links between the sensors and effectors ofthe DNA damage response The roles of ATM and ATR partiallyoverlap and are cooperative however they are also known to playdistinct roles in protecting the cell from DNA damage ATM is mostlyresponsible for sending signals from DSBs (double-strand breaks)induced by ionizing radiation while the closely related ATR respondsto UV damage or stalled replication forks ATM and ATR are known tophosphorylate common as well as specific substrates to activatecheckpoint signaling The G1 S and G2 cell cycle checkpoints areprimarily regulated by the ATM (ataxia telangiectasia mutated) and

ATR (ATM and Rad3-related) protein kinases

Purity 9976Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9904Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9960Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

ATMATR Inhibitors amp Modulators

Bioactivity ATM Inhibitor-1 is a highly potent selective and orallyactive inhibitor with an of 07 nM shows weakATM IC50activity against mTOR (IC 21 μM) DNAPK (IC 28 μM)50 50PI3Kα (IC 38 μM) PI3Kβ (IC 103 μM) PI3Kγ hellip50 50

Bioactivity ATR inhibitor 1 is a inhibitor extracted from patentATRWO2015187451A1 compound I-l has a value below 1 microΜ Ki

[1]

Bioactivity AZ20 is a potent and selective inhibitor of with an ATR IC50of 5 nM and has 8-fold selectivity against (IC =38mTOR 50nM)

Bioactivity AZ32 is an orally bioavailable and blood-brainbarrier-penetrating inhibitor with an of lt62ATM IC50nM for ATM enzyme and an of 031 μM for ATM in cellIC50

Bioactivity AZD0156 is an oral potent and selective inhibitor withATMan of 058 nMIC50

Bioactivity AZD1390 is an inhibitorATM

Bioactivity BAY-1895344 is a potent orally available and selective ATRinhibitor with of 7 nM Anti-tumor activity IC50

[1]Bioactivity BAY-1895344 hydrochloride is a potent orally available and

selective inhibitor with of 7 nM Anti-tumorATR IC50

activity [1]

Bioactivity Berzosertib (VE-822) is an inhibitor with a value ofATR Kiless than 02 nM It also inhibits with a of 34 nMATM Ki

Bioactivity Ceralasertib (AZD6738) is a potent inhibitor of kinaseATRwith an of 1 nMIC50

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ATM Inhibitor-1 Cat No HY-112614

ATR inhibitor 1 Cat No HY-111451

AZ20 Cat No HY-15557

AZ32 Cat No HY-112305

AZD0156 Cat No HY-100016

AZD1390 Cat No HY-109566

BAY-1895344 Cat No HY-101566

BAY-1895344 hydrochloride Cat No HY-101566A

Berzosertib (VE-822 VX-970) Cat No HY-13902

Ceralasertib (AZD6738) Cat No HY-19323

wwwMedChemExpresscom 11

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9947Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9988Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9840Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity CGK733 is a potent inhibitor used for the researchATMATRof cancer

Bioactivity CP-466722 is a rapidly reversible inhibitor of with anATM of 41 μM and has no effects on PI3K or closely relatedIC50

PI3K-like protein kinase (PIKK) family members

Bioactivity ETP-46464 is an effective and inhibitor withmTOR ATRs of 06 and 14 nM respectivelyIC50

Bioactivity KU 59403 is a potent inhibitor with an of 3 nMATM IC50

Bioactivity KU-55933 is a potent inhibitor with an and ofATM IC50 Ki129 and 22 nM respectively and is highly selective for ATMas compared to DNA-PK PI3KPI4K ATR and mTOR

Bioactivity KU-60019 is an improved kinase-specific inhibitor withATM of 63 nMIC50

Bioactivity VE-821 is a potent ATP-competitive inhibitor of with ATR Ki of 13 nM26 nMIC50

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

CGK733 Cat No HY-15520

CP-466722 Cat No HY-11002

ETP-46464 Cat No HY-15521

KU 59403 Cat No HY-18650

KU-55933 Cat No HY-12016

KU-60019 Cat No HY-12061

VE-821 Cat No HY-14731

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

Aurora Kinase

Aurora kinases are serinethreonine kinases that are essential for cellproliferation Aurora kinase helps the dividing cell dispense its geneticmaterials to its daughter cells More specifically Aurora kinases play acrucial role in cellular division by controlling chromatid segregationDefects in this segregation can cause genetic instability a conditionwhich is highly associated with tumorigenesis Three Aurora kinaseshave been identified in mammalian cells to date Aurora A Aurora BAurora C Besides being implicated as mitotic regulators these threekinases have generated significant interest in the cancer research fielddue to their elevated expression profiles in many human cancers Thehuman Aurora kinases present a similar domain organization with a

N-terminal domain of 39 to 129 residues in length a protein kinase domain and a short C-terminal domain containing15 to 20 residues The N-terminal domain of three proteins share low sequence conservation which determinesselectivity during protein-protein interactions

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wwwMedChemExpresscom 13

Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9895Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9874Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Aurora Kinase Inhibitors amp Modulators

Bioactivity Alisertib (MLN 8237) is an oral active and selective Aurora A inhibitor with an of 12 nMkinase IC50

Bioactivity AMG 900 is a potent and highly selective kinasespan-Aurorainhibitor with of 5 nM 4 nM and 1 nM for IC50 Aurora A B

and respectivelyC

Bioactivity AT9283 is a multitargeted kinase inhibitor which potentlyinhibits ( =12 nM 11 nM)aurora kinase AB JAK23 IC50

Bioactivity Aurora A inhibitor I is a potent and highly selective Aurora inhibitor with with an of 34 nMA IC50

Bioactivity Aurora B inhibitor 1 is an (Aurora-1) inhibitorAurora Bextracted from patent WO2007059299A1 compound 1-3 has a Kivalue of lt0010 uM

Bioactivity Aurora inhibitor 1 is a potent inhibitor with an Aurora IC50of le 4 nM and le13 nM for and kinaseAurora A Aurora Brespectively [1]

Bioactivity AZD1152 is a pro-drug of Barasertib-hQPA which is a highlyselective inhibitor with of 037 nM in aAurora B IC50cell-free assay

Bioactivity AZD1152-HQPA is a highly selective Aurora inhibitor with an of 037 nM in aB IC50

cell-free assay and shows 3700-fold selectivity for Aurora Bover Aurora A

Bioactivity BI-847325 is an ATP competitive dual inhibitor of andMEKaurora kinases ( ) with values of 4 and 15 nM forAK IC50human MEK2 and AK-C respectively

Bioactivity CCT 137690 is a potent and orally available kinaseaurorainhibitor with s of 15 25 and 19 nM for aurora A B andIC50C respectively

Alisertib (MLN 8237) Cat No HY-10971

AMG 900 Cat No HY-13253

AT9283 Cat No HY-50514

Aurora A inhibitor I Cat No HY-70061

Aurora B inhibitor 1 Cat No HY-U00304

Aurora inhibitor 1 Cat No HY-111506

AZD1152 (Barasertib) Cat No HY-10127

Barasertib-HQPA (AZD2811 INH-34 AZD1152-HQPA) Cat No HY-10126

BI-847325 Cat No HY-18955

CCT 137690 Cat No HY-10804

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 1 mg 5 mg 10 mg 20 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9859Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9923Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9944Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data Phase 1Size 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 950Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity CCT129202 is an kinase inhibitor with s of 42aurora IC50198 and 227 nM for aurora A B and C respectively

Bioactivity CCT241736 is a potent and orally bioavailable dual andFLT3 inhibitor which inhibits Aurora kinasesAurora kinase

(Aurora-A 75 nM 38 nM Aurora-B 48 nM)Kd IC50 KdFLT3 kinase ( 62 nM) and FLT3 mutants includhellipKd

Bioactivity CYC-116 is a potent and inhibitor withaurora A aurora Bs of 8 and 9 nM respectivelyKi

Bioactivity Danusertib is a pyrrolo-pyrazole and inhibitoraurora kinasewith of 13 79 and 61 nM for Aurora A B and CIC50respectively

Bioactivity ENMD-2076 is a multi-targeted kinase inhibitor with s ofIC50186 14 582 159 927 708 564 nM for Aurora A Flt3

KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src PDGFRαrespectively

Bioactivity ENMD-2076 Tartrate is a multi-targeted kinase inhibitor withs of 186 14 582 159 927 708 564 nM for IC50 Aurora

A Flt3 KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src respectivelyPDGFRα

Bioactivity GSK-1070916 is a potent and selective ATP-competitiveinhibitor of and with s of 038 andaurora B aurora C Ki15 nM respectively and is gt250- fold selective overAurora A

Bioactivity Hesperadin is an ATP-competitive inhibitor of aurora Bkinase with an of 250 nMIC50

Bioactivity Ilorasertib (ABT-348) is an ATP-competitive multitargetedkinase inhibitor with s for inhibiting binding Aurora B (7IC50nM) C (1 nM) and A (120 nM) and also inhibits RET tyrosinekinase PDGFRβ and Flt1 with s of 7 nM 3 nM and 32 nMIC50

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

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CCT129202 Cat No HY-12049

CCT241736 Cat No HY-18161

CYC-116 Cat No HY-10558

Danusertib (PHA-739358) Cat No HY-10179

ENMD-2076 Cat No HY-10987A

ENMD-2076 Tartrate Cat No HY-10987

GSK-1070916 (GSK-1070916A) Cat No HY-70044

Hesperadin Cat No HY-12054

Ilorasertib (ABT-348) Cat No HY-16018

JNJ-7706621 Cat No HY-10329

wwwMedChemExpresscom 15

Purity 9820Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9928Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9911Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity KW-2449 is a multi-targeted kinase inhibitor of FLT3 ABL and with s of 66 14 4 and 48 nMABLT315I Aurora kinase IC50

respectively

Bioactivity LY3295668 is a potent orally active and highly specific inhibitor with values of 08 nM and 1038Aurora-A kinase Ki

nM for AurA and AurB respectively

Bioactivity MK-5108 is a highly potent and specific inhibitor of Aurora A with an value of 0064 nMkinase IC50

Bioactivity MK-8745 is an kinase inhibitor with an of 06aurora A IC50nM

Bioactivity MLN8054 is a potent selective and orally available aurora Akinase inhibitor with an of 4 nMIC50

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity PF-03814735 is a potent orally available and reversible and inhibitor with s of 08 and 05aurora A aurora B IC50

nM respectively

Bioactivity PHA-680632 is an kinase inhibitor with s of 27aurora IC50135 and 120 nM for aurora A B and C respectively

Bioactivity Reversine is a novel class of ATP-competitive Aurora kinaseinhibitor with s of 400 500 and 400 nM for IC50 Aurora A

and respectivelyAurora B Aurora C

Bioactivity SCH-1473759 is an inhibitor with s of 4 and 13 nMaurora IC50for aurora A and B respectively

KW-2449 Cat No HY-10339

LY3295668 (AK-01) Cat No HY-114258

MK-5108 (VX-689) Cat No HY-13252

MK-8745 Cat No HY-13819

MLN8054 Cat No HY-10180

NU6140 Cat No HY-107419

PF-03814735 Cat No HY-14574

PHA-680632 Cat No HY-10178

Reversine Cat No HY-14711

SCH-1473759 Cat No HY-10482

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg

Purity 9980Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity SCH-1473759 hydrochloride is an inhibitor with saurora IC50of 4 and 13 nM for aurora A and B respectively

Bioactivity SNS-314 is a potent and selective kinase inhibitoraurorawith s of 9 31 and 6 nM for aurora A B and CIC50respectively

Bioactivity TAK-632 is a potent inhibitor with of 14 24pan-RAF IC50

and 83 nM for respectivelyCRAF BRAFV600E BRAFWT

Bioactivity TAK-901 is a multi-targeted inhibitor with s of 21aurora IC50and 15 nM for aurora A and B respectively

Bioactivity Tozasertib (VX 680 MK-0457) is an inhibitor of Aurora ABC with s of 06 18 46 nM respectivelykinases Ki

Bioactivity XL228 is a multi-targeted tyrosine kinase inhibitor with sIC50of 5 31 16 61 2 nM for Bcr-Abl Aurora A IGF-1R Srcand respectivelyLyn

Bioactivity ZM-447439 is an kinase inhibitor with s of 110 andaurora IC50130 nM for aurora A and B respectively

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SCH-1473759 hydrochloride Cat No HY-10483

SNS-314 (SNS-314 Mesylate) Cat No HY-12003

TAK-632 Cat No HY-15767

TAK-901 Cat No HY-12201

Tozasertib (VX 680 MK-0457) Cat No HY-10161

XL228 Cat No HY-15749

ZM-447439 Cat No HY-10128

wwwMedChemExpresscom 17

Casein Kinase

Casein Kinases (CKs) are serinethreonine-selective enzymes thatfunction as regulators of signal transduction pathways in mosteukaryotic cell types

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9992Clinical Data Phase 2Size 1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Casein Kinase Inhibitors amp Modulators

Bioactivity Casein Kinase II Inhibitor IV is a small-molecule inducer ofepidermal keratinocyte differentiation

Bioactivity Casein Kinase II Inhibitor IV Hydrochloride is asmall-molecule inducer of epidermal keratinocytedifferentiation

Bioactivity CK1-IN-1 is a inhibitor extracted fromcasein kinase 1 (CK1)patent WO2015119579A1 compound 1c has s of 15 nM 16 nMIC50

73 nM for CK1δ and CK1ε p38σ MAPK respectively [1]

Bioactivity D4476 is a potent selective and cell-permeable inhibitor ofcasein kinase 1( ) with an value of 03 μM CK1 IC50 in vitro

Bioactivity DMAT is a potent and specific inhibitor with an CK2 IC50value of 130 nM

Bioactivity Ellagic acid is a natural antioxidant and acts as a potentand ATP-competitive inhibitor with an of 40 nM andCK2 IC50a of 20 nMKi

Bioactivity Emodin is a broad-spectrum anticancer agent Emodin inhibits II (CKII) activity with of 2 μMcasein kinase IC50

Bioactivity IC261 is a selective ATP-competitive inhibitor withCK1s of 1 μM 1 μM 16 μM for and Ckiα1IC50 Ckiδ Ckiε

respectively

Bioactivity LH846 is a selective inhibitor of with an of 290 nMCKIδ IC50and less potently inhibits CKIα and CKIε with s of 25 μMIC50and 13 μM respectively

Bioactivity Longdaysin is a and CK1α CK1δ extracellular inhibitor with s of  56signal-regulated kinase 2 (ERK2) IC50

microM 88 microM and 52 microM respectively [1] [2]

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Casein Kinase II Inhibitor IV Cat No HY-111378

Casein Kinase II Inhibitor IV Hydrochloride Cat No HY-111378A

CK1-IN-1 Cat No HY-111820

D4476 (Casein Kinase I Inhibitor) Cat No HY-10324

DMAT (Casein kinase II Inhibitor CK2 Inhibitor) Cat No HY-15535

Ellagic acid Cat No HY-B0183

Emodin (Frangula emodin) Cat No HY-14393

IC261 Cat No HY-12774

LH846 Cat No HY-15704

Longdaysin Cat No HY-18285

wwwMedChemExpresscom 19

Purity 9701Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9827Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Bioactivity NCC007 is a dual and inhibitorcasein kinase Iα (CKIα) δ (CKIδ)with s of 18 and 36 μM respectively and can be used inIC50

research of modulating mammalian circadian rhythms [1]

Bioactivity PF-4800567 is a potent and selective inhibitor of caseinkinase 1ϵ ( ) with an of 32 nM which is greaterCK1ϵ IC50than 20-fold selectivity over CK1δ ( 711 nM)IC50

Bioactivity PF-670462 is a potent and selective inhibitor of casein kinase with s of 77 nM and 14 nM( and )CK1ε CK1δ IC50

respectively

Bioactivity Silmitasertib (CX-4945) is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity Silmitasertib sodium salt is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity SR-3029 is a potent and ATP competitive and CK1δ CK1εinhibitor with s of 44 nM and 260 nM respectively andIC50

s of 97 nM for both kinasesKi

Bioactivity TA-01 is a potent and inhibitor with sCK1 p38 MAPK IC50of 64 nM 68 nM 67 nM for CK1ε CK1δ and p38 MAPKrespectively

Bioactivity TBB is a cell-permeable and ATP-competitive inhibitorCK2with an of 015 μM for rat liver CK2IC50

Bioactivity TTP 22 is a potent inhibitor with an of 100 nM andCK2 IC50a of 40 nMKi

NCC007 Cat No HY-128677

PF-4800567 Cat No HY-12470

PF-670462 Cat No HY-15490

Silmitasertib (CX-4945) Cat No HY-50855

Silmitasertib sodium salt (CX-4945 (sodium salt)) Cat No HY-50855B

SR-3029 Cat No HY-100011

TA-01 Cat No HY-100114

TBB (NSC 231634 Casein Kinase II Inhibitor I) Cat No HY-14394

TTP 22 Cat No HY-15479

CDKCyclin dependent kinase

CDKs (Cyclin-dependent kinases) are serine-threonine kinases firstdiscovered for their role in regulating the cell cycle They are alsoinvolved in regulating transcription mRNA processing and thedifferentiation of nerve cells CDKs are relatively small proteins withmolecular weights ranging from 34 to 40 kDa and contain little morethan the kinase domain In fact yeast cells can proliferate normallywhen their CDK gene has been replaced with the homologous humangene By definition a CDK binds a regulatory protein called a cyclinWithout cyclin CDK has little kinase activity only the cyclin-CDKcomplex is an active kinaseThere are around 20 Cyclin-dependent kinases (CDK1-20) known till

date CDK1 4 and 5 are involved in cell cycle and CDK 7 8 9 and 11 are associated with transcriptionCDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational Mostknowledge of CDK structure and function is based on CDKs of (Cdc2) (CDC28) and vertebratesS pombe S cerevisia(CDC2 and CDK2) The four major mechanisms of CDK regulation are cyclin binding CAK phosphorylation regulatoryinhibitory phosphorylation and binding of CDK inhibitory subunits (CKIs)

20 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 21

Purity 9815Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9969Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9973Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

CDK Inhibitors amp Modulators

Bioactivity (+)-BAY-1251152 is a inhibitor extracted from patent WOCDK92014076091 A1 example 1

Bioactivity (-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation(-) BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity (plusmn)-BAY-1251152 is a racemic mixture of BAY-1251152BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity 5-Iodo-indirubin-3-monoxime is a potent GSK-3β CDK5P25and inhibitor competing with ATP for binding toCDK1cyclin Bthe catalytic site of the kinase with s of 9 20 and 25IC50

nM respectively [1]

Bioactivity Abemaciclib (LY2835219) is a selective inhibitor withCDK46 values of 2 nM and 10 nM for CDK4 and CDK6 respectivelyIC50

Bioactivity Abemaciclib Metabolites M2 is a metabolite of abemaciclibacts as a potent and inhibitor with s in theCDK4 CDK6 IC50

range of 1-3 nM Anti-cancer activity [1]

Bioactivity Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is aselective inhibitor with s of 2 nM and 10 nM forCDK46 IC50CDK4 and CDK6 respectively

Bioactivity AMG 925 is a potent selective and orally available FLT3 dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMCDK4 IC50

respectively

Bioactivity AMG 925 HCl is a potent selective and orally available dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMFLT3 CDK4 IC50

respectively

Bioactivity AT7519 as a potent inhibitor of with s of 210 47CDKs IC50100 13 170 and lt10 nM for CDK1 CDK2 CDK4 to CDK6 andCDK9 respectively

(+)-BAY-1251152 Cat No HY-103019

(-)-BAY-1251152 Cat No HY-103019B

(plusmn)-BAY-1251152 Cat No HY-103019A

5-Iodo-indirubin-3-monoxime Cat No HY-111930

Abemaciclib (LY2835219) Cat No HY-16297A

Abemaciclib Metabolites M2 Cat No HY-128669

Abemaciclib methanesulfonate (LY2835219 (methanesulfonate)) Cat No HY-16297

AMG 925 Cat No HY-15889

AMG 925 HCl Cat No HY-15889A

AT7519 Cat No HY-50940

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 1Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9999Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9700Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9848Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9816Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity AT7519 Hydrochloride is a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity AT7519 trifluoroacetate as a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity Atuveciclib (BAY-1143572) is a potent and highly selectiveoral inhibitor Atuveciclib (BAY-1143572)PTEFb CDK9inhibits with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib Racemate (BAY-1143572 Racemate) is the racematemixture of Atuveciclib Atuveciclib is a potent and highlyselective oral inhibitor which supressesP-TEFb CDK9

with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is apotent and selective inhibitor which inhibits CDK9 CDK9

with an of 16 nMCycT1 IC50

Bioactivity AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 82nM AUZ 454 (K03861) inhibits CDK2 activity by competing withbinding of activating cyclins

Bioactivity AZD-5438 is a potent inhibitor of with of 16CDK129 IC50nM6 nM20 nM in cell-free assays AZD-5438 shows lessinhibition activity against GSK3β CDK5 and CDK6

Bioactivity AZD4573 is a inhibitor with an of lt3 nMCDK9 IC50extracted from patent US 20160376287 A1 example 14

Bioactivity BGG463 is a inhibitorCDK2 Bioactivity BI-1347 is a potent inhibitor extracted from patentCDK8WO2017202719A1 product I-003 has an of 11 nM IC50

[1]

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AT7519 Hydrochloride Cat No HY-50943

AT7519 trifluoroacetate Cat No HY-50940A

Atuveciclib (BAY-1143572) Cat No HY-12871B

Atuveciclib Racemate (BAY-1143572 Racemate) Cat No HY-12871

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) Cat No HY-12871C

AUZ 454 (K03861) Cat No HY-15004

AZD-5438 Cat No HY-10012

AZD4573 Cat No HY-112088

BGG463 Cat No HY-100600

BI-1347 Cat No HY-120350

wwwMedChemExpresscom 23

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9754Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9747Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity BMS-265246 is a potent and selective CDK12 inhibitor forCDK1cyclin B and CDK2cyclin E with IC50 of 6 nM and 9 nMrespectively

Bioactivity BS-181 is a highly selective inhibitor with an ofCDK7 IC5021 nM showing 40-fold selective over CDK1 2 4 5 6 or 9

Bioactivity BS-181 hydrochloride is a highly selective inhibitorCDK7with of 21 nM and gt 40-fold selective for CDK7 thanIC50CDK1 2 4 5 6 or 9

Bioactivity BSJ-03-123 is a potent and novel -selective small-moleculeCDK6degrader

Bioactivity Ca channel agonist 1 is an agonist of 2+ N-type Ca channel2+

and an inhibitor of with s of 1423 μM and 334Cdk2 EC50μM respectively and is used as a potential treatment formotor nerve terminal dysfunction

Bioactivity CC-671 is a dual ( )TTK protein kinase CDC2-like kinase CLK2inhibitor with s of 0005 and 0006 μM for TTK and CLK2IC50respectively

Bioactivity CCT-251921 is a potent selective and orally bioavailable inhibitor with an of 23 nMCDK8 IC50

Bioactivity CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 oflt8 nM extracted from reference 1 example 4 IC50 Valuelt8 nM [1] Target CDK9 In vitro In vivo

Bioactivity CDK46-IN-2 is a potent and inhibitor extractedCDK4 CDK6from patent US20180000819A1 Compound 1 has s of 27 andIC50

16 nM for CDK4 and CDK6 respectively [1]

Bioactivity CDK461 Inhibitor is a inhibitor with s of 3 andCDK46 IC501 nM respectively

BMS-265246 Cat No HY-15275

BS-181 Cat No HY-13266

BS-181 hydrochloride Cat No HY-13266A

BSJ-03-123 Cat No HY-111556

Ca2+ channel agonist 1 Cat No HY-41076

CC-671 Cat No HY-108709

CCT-251921 Cat No HY-19984

CDK-IN-2 (CDK inhibitor II) Cat No HY-13033

CDK46-IN-2 Cat No HY-114339

CDK461 Inhibitor Cat No HY-112280

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9548Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CDK8-IN-1 is a potent and selective inhibitor with anCDK8 of 3 nMIC50

Bioactivity CDK8-IN-3 is an inhibitor of extracted from patentCDK8WO2016041618A1 compound example 17

Bioactivity CDK8-IN-4 is an inhibitor of extracted from patentCDK8WO2014090692A1 compound example 16 with an of 02 nMIC50

Bioactivity CDK819-IN-1 is a potent selective and oral bioavailable dual inhibitor with s of 046 nM 099 nM andCDK819 IC50

270 nM for CDK8 CDK19 and CDK9 respectively

Bioactivity CDK9 Antagonist-1 (compounds 11c) is a potent and selective degrader based on PROTAC with an of 17 μM in MCF-7CDK9 IC50

cell lines Natural product Wogonin binds ubiquitin E3 ligasecereblon (CRBN) via a linker to form PROTAC [1]

Bioactivity CDK9-IN-1 is a novel selective inhibitor for theCDK9treatment of HIV infection with an of 39 nM forIC50CDK9CycT1 extracted from reference compound 87

Bioactivity CDK9-IN-2 is a special cyclin-dependent kinase 9 ( )CDK9inhibitor extracted from patent WO2012131594A1 compoundCDKI(8) has an of 5 nM and 7 nM in H929 multipleIC50myeloma(MM) cell line (72 hours) and A2058 skin cell line (72hours) respectively

Bioactivity CDK9-IN-8 is a highly effective and selective inhibitorCDK9with an of 12 nMIC50

Bioactivity CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM showsselective toxicity to CLL cells(LD50=80 nM) versus normal Bcell and normal CD34+ cell(LD50gt20 uM) IC50 value 4 nM80nM(KiLD50) [1] Target CDK9 inhibitor in vitro CDKI-73 wascytotoxic to all of the CLL samples tested (n = 38) with ahellip

Bioactivity CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 () inhibitor with an IC of 2 nMCLK1 50

24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CDK8-IN-1 Cat No HY-103492

CDK8-IN-3 Cat No HY-111463

CDK8-IN-4 Cat No HY-111465

CDK819-IN-1 Cat No HY-111427

CDK9 Antagonist-1 Cat No HY-112811

CDK9-IN-1 Cat No HY-13231

CDK9-IN-2 Cat No HY-16462

CDK9-IN-8 Cat No HY-102039

CDKI-73 Cat No HY-12445

CLK1-IN-1 Cat No HY-103082

wwwMedChemExpresscom 25

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9900Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9973Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9998Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CMPD 7 is a potent and selective inhibitor with an CDK12 IC50of 491 nM in enzymatic assay

Bioactivity CT7001 hydrochloride is a selective inhibitor withCDK7s of 41 nM and 578 nM for andIC50 CDK7CycHMAT1

respectivelyCDK2cycE1

Bioactivity Cucurbitacin E is a natural compound which from the climbingstem of Cucurbitacin E significantlyCucumic melo Lsuppresses the activity of the complexcyclin B1 CDC2

Bioactivity CVT-313 is a potent selective reversible andATP-competitive inhibitor of with of 05 μMCDK2 IC50

Bioactivity CYC065 is a second-generation orally availableATP-competitive inhibitor of kinasesCDK2 CDK 9

Bioactivity Dinaciclib is a potent inhibitor of with s of 1 1CDK IC503 and 4 nM for and respectivelyCDK2 CDK5 CDK1 CDK9

Bioactivity EHT 5372 is a strong inhibitor of family kinases withDYRKrsquos of 022 028 nM for DYRK1A and DYRK1B respectivelyIC s50

Bioactivity Flavopiridol is a broad spectrum and competitive inhibitor of inhibiting CDK1 CDK2 CDK4 with s of 30 170 100CDKs IC50

nM respectively

Bioactivity Flavopiridol Hydrochloride is a broad inhibitor of CDKcompeting with ATP to inhibit CDKs including CDK1 CDK2 CDK4with s of 30 170 100 nM respectivelyIC50

Bioactivity FMF-04-159-2 is a covalent inhibitor FMF-04-159-2CDK14inhibits CDK14 and CDK2 with s of 396 nM and 256 nM inIC50

NanoBRET assay respectively [1]

CMPD 7 Cat No HY-112261

CT7001 hydrochloride (ICEC0942 hydrochloride) Cat No HY-103712A

Cucurbitacin E (α-Elaterin α-Elaterine) Cat No HY-N0417

CVT-313 (Cdk2 Inhibitor III) Cat No HY-15339

CYC065 Cat No HY-101212

Dinaciclib (SCH 727965) Cat No HY-10492

EHT 5372 Cat No HY-111380

Flavopiridol (L868275 HMR-1275 Alvocidib) Cat No HY-10005

Flavopiridol Hydrochloride (HL 275 NSC 649890 MDL 107826A

FLAVOPIRIDOL HCL Alvocidib Hydrochloride) Cat No HY-10006

FMF-04-159-2 Cat No HY-127104

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9204Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 251 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9841Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity FN-1501 is a potent inhibitor of and with s ofFLT3 CDK IC50247 085 196 and 028 nM for CDK2cyclin A CDK4cyclinD1 CDK6cyclin D1 and FLT3 respectively FN-1501 hasanticancer activity

Bioactivity GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO) is apotent selective reversible and ATP-competitive inhibitor of

and complex with s of 5 nM320GSK-3αβ CDK1-cyclinB IC50nM80nM for (GSK-3αβ)CDK1CDK5 respectively

Bioactivity GSK3186899 is an inhibitor of cdc-2-related kinase 12 () with an of 14 μM for in anCRK12 EC50 L donovani

intra-macrophage assay

Bioactivity IIIM-290 is a potent and oral inhibitor with s of 90CDK IC50and 94 nM for CDK2A and CDK9T1

Bioactivity Indirubin-3-monoxime-5-sulphonic acid is a potent andselective inhibitor of and with s ofCDK1 CDK5 GSK-3β IC50

5 nM 7 nM and 80 nM respectively [1]

Bioactivity Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK)inhibitor with values of 55 nM 35 nM 150 nM 300 nMIC50and 65 nM for CDK1cyclin B CDK2cyclin A CDK2cyclin ECDK4cyclin D1 and CDK5p35 respectively [1]

Bioactivity JH-XI-10-02 is a potent and selective degrader of withCDK8an of 159 nM based on JH-XI-10-02 causesIC50 PROTAC

proteasomal degradation does not affect CDK8 mRNA levelsJH-XI-10-02 shows no effect on CDK19 [1]

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

Bioactivity JSH-150 is a highly selective and potent inhibitor withCDK9an IC of 1 nM50

Bioactivity Kenpaullone is a potent inhibitor of andCDK1cyclin B with s of 04 μM and 23 nM and also inhibitsGSK-3β IC50

CDK2cyclin A CDK2cyclin E and CDK5p25 with s of 068IC50μM 75 μM 085 μM respectively

26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

FN-1501 Cat No HY-111361

GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO MLS 2052) Cat No HY-10580

GSK3186899 (DDD-853651) Cat No HY-112622

IIIM-290 Cat No HY-111356

Indirubin-3-monoxime-5-sulphonic acid Cat No HY-111931

Indirubin-5-sulfonate Cat No HY-111932

JH-XI-10-02 Cat No HY-111518

JNJ-7706621 Cat No HY-10329

JSH-150 Cat No HY-X0150

Kenpaullone (9-Bromopaullone NSC-664704) Cat No HY-12302

wwwMedChemExpresscom 27

Purity 9861Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9847Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Bioactivity KH-CB19 is a potent and highly specific inhibitor of theCDC2-like kinase isoforms 1 and 4 (CLK1CLK4) IC50 value 20nM (CLK1) [1] Target CLK14 inhibitor in vitro KH-CB19showed potent inhibition of CLK1 with an IC50 of 20 nM andfor the pure isomer KH-CB19 almost 100-fold selectivityhellip

Bioactivity LDC000067 is a highly specific inhibitor with an CDK9 IC50value of 44plusmn10 nM in vitro

Bioactivity LDC4297 is a potent and selective inhibitor with an CDK7 IC50of 013 nM

Bioactivity Lerociclib (G1T38) is a potent and selective inhibitor of with of 1 nM 2 nM for CDK4CyclinD1 andCDK46 IC s50

CDK6CyclinD3 respectively

Bioactivity Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potentand selective inhibitor of with of 1 nMCDK4 CDK6 IC s50and 2 nM for and respectivelyCDK4 CyclinD1 CDK6 CyclinD3

Bioactivity LY2857785 is a type I reversible and competitive ATP kinaseinhibitor against ( 11 nM) and other transcriptionCDK9 IC50kinases ( 16 nM) and ( 246 nM)CDK8 IC50 CDK7 IC50

Bioactivity LY3177833 is an and inhibitor extracted fromCDC7 pMCM2patent US 20140275131and patent WO 2014143601 A1 compoundexample 4 has values of 33 nM and 290 nM respectivelyIC50

Bioactivity MBQ-167 is a dual inhibitor with of 103 nMRacCdc42 IC s50for Rac 123 and 78 nM for Cdc42 in MDA-MB-231 cellsrespectively

Bioactivity MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin inhibitor with an of 5 nM at least 22-fold moreT1 IC50

selective for CDK9 over other CDKs MC180295 also inhibitsGSK-3α and GSK-3β MC180295 ((rel)-MC180295) has pothellip

Bioactivity Milciclib (PHA-848125) is a potent dual inhibitor of andCDK with s of 45 150Tropomyosin receptor kinase (TRK) IC50

160 363 398 nM and 53 nM for cyclin ACDK2 cyclin HCDK7cyclin D1CDK4 cyclin ECDK2 cyclin BCDK1 and TRKArespectively

KH-CB19 Cat No HY-12828

LDC000067 (LDC067) Cat No HY-15878

LDC4297 Cat No HY-12653

Lerociclib (G1T38) Cat No HY-112272

Lerociclib dihydrochloride (G1T38 dihydrochloride) Cat No HY-112272A

LY2857785 Cat No HY-12293

LY3177833 Cat No HY-100023

MBQ-167 Cat No HY-112842

MC180295 ((rel)-MC180295) Cat No HY-119940

Milciclib (PHA-848125) Cat No HY-10424

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9703Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9851Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Bioactivity ML167 is a highly selective Cdc2-like kinase 4 ( )Clk4inhibitor with of 136 nM gt10-fold selectivity forIC50closely related kinases Clk1 Clk2 Clk3 and Dyrk1A1B

Bioactivity MSC2530818 is a potent selective and orally available CDK8inhibitor with an of 26 nM for CDK8IC50

Bioactivity NG 52 (Compound 52 ) is a potent cell-permeable reversibleselective and ATP-compatible inhibitor of the cellcycle-regulating kinase Cdc28p (IC50 = 7 μM) and the relatedPho85p kinase (IC50 = 2 μM)

Bioactivity Nimbolide is a triterpene derived from the leaves and flowersof neem ( L) Nimbolide induces apoptosisAzadirachta indicathrough inactivation of Nimbolide inhibits NF-κB CDK4

kinase activity Nimbolide suppresses the NF-κB WntCDK6PI3K-Akt MAPK and JAK-STAT signaling pathways [1]

Bioactivity NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and26 μM for CDK2 and CDK1 IC50 value 17μM (CDK2) 26μM (CDK1)Target CDK in vitro NU2058 is a competitive inhibitor ofCDK2 with respect to ATP (Ki value CDK2 12 3 μM) that bindsin the ATP binding pocket in a different orientation fromhellip

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity NU6300 is the first covalent ATP-competitive CDK2 inhibitorIC50 value Target CDK2 in vitro NU6300 is a covalent CDK2inhibitor that illustrates the potential of using vinylsulfones to mediate irreversible inhibition NU6300 blocks theinhibitor binding site The effect was time dependent andhellip

Bioactivity NVP-2 is a inhibitor with an of 05 nMCDK9 IC50

Bioactivity NVP-LCQ195 (AT9311 LCQ195) is a small molecule heterocyclicinhibitor of CDK1 CDK2 CDK3 and CDK5 with IC50 of 1-42 nM

Bioactivity ON-013100 an antineoplastic drug acts a mitotic inhibitorthat could inhibit expressionCyclin D1

28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

ML167 (CID44968231 NCGC00188654) Cat No HY-15951

MSC2530818 Cat No HY-101611

NG 52 (Compound 52) Cat No HY-15154

Nimbolide Cat No HY-116035

NU2058 (O6-(Cyclohexylmethyl)guanine) Cat No HY-19316

NU6140 Cat No HY-107419

NU6300 Cat No HY-18930

NVP-2 Cat No HY-12214A

NVP-LCQ195 (LCQ-195 AT9311) Cat No HY-15241

ON-013100 Cat No HY-112822

wwwMedChemExpresscom 29

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9996Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity ON123300 is a potent inhibitor of CDK4 with an IC50 of 38nM with little inhibitory activity against CDKs 125 and 8

Bioactivity Palbociclib (PD 0332991) is a selective and CDK4 CDK6inhibitor with s of 11 and 16 nM respectivelyIC50Palbociclib is a drug for the treatment of ER-positive andHER2-negative breast cancer

Bioactivity Palbociclib hydrochloride is a highly selective CDK46inhibitor with s of 11 nM and 16 nM respectivelyIC50

Bioactivity Palbociclib isethionate is a highly selective inhibitorof with s of 11 nM16 nMCDK46 IC50respectively

Bioactivity PF-06873600 is a selective and orally bioavailable inhibitorof cyclin-dependent kinase with values of 009 nM(CDK) Ki013 nM and 016 nM for CDK2 CDK4 and CDK6 respectivelyPF-06873600 has potential antineoplastic activity [1] [2]

Bioactivity PHA-767491 is a dual inhibitor with s of 10 nMCdc7Cdk9 IC50and 34 nM respectively

Bioactivity PHA-767491 hydrochloride is a dual inhibitor withCdc7Cdk9s of 10 nM and 34 nM respectivelyIC50

Bioactivity PHA-793887 is a potent ATP-competitive inhibitor canCDKinhibit Cdk2 Cdk1 Cdk4 and Cdk9 with s of 8 nM 60 nMIC5062 nM and 138 nM respectively and also inhibits glycogensynthase kinase 3β with an of 79 nMIC50

Bioactivity PROTAC CDK9 Degrader-1 is a selective degraderCDK9 Bioactivity Purvalanol A is a potent inhibitor which inhibitsCDKcdc2-cyclin B cdk2-cyclin A cdk2-cyclin E cdk4-cyclin D1and cdk5-p35 with s of 4 70 35 850 75 nMIC50resepctively

ON123300 Cat No HY-12624

Palbociclib (PD 0332991) Cat No HY-50767

Palbociclib hydrochloride (PD 0332991 hydrochloride) Cat No HY-50767A

Palbociclib isethionate (PD 0332991 isethionate) Cat No HY-A0065

PF-06873600 Cat No HY-114177

PHA-767491 (CAY10572) Cat No HY-13461

PHA-767491 hydrochloride (CAY-10572 hydrochloride) Cat No HY-13461A

PHA-793887 Cat No HY-11001

PROTAC CDK9 Degrader-1 Cat No HY-103628

Purvalanol A (NG-60) Cat No HY-18299A

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9900Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9983Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitorwith IC50 values of 6 6 9 gt 10000 and 6 nM forcdc2cyclin B cdk2cyclin A cdk2cyclin E cdk4cyclin D1and cdk5-p35 respectively

Bioactivity R547 is a potent ATP-competitive inhibitor of CDK124 with Kiof 2 nM3 nM1 nM

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity Ribociclib (LEE011) is a highly specific inhibitorCDK46with s of 10 nM and 39 nM respectivelyIC50

Bioactivity Ribociclib hydrochloride (LEE011 hydrochloride) is a highlyspecific inhibitor with values of 10 nM and 39CDK46 IC50nM respectively and is over 1000-fold less potent againstthe cyclin BCDK1 complex

Bioactivity Ribociclib succinate (LEE011 succinate) is a highly specific inhibitor with values of 10 nM and 39 nMCDK46 IC50

respectively and is over 1000-fold less potent against thecyclin BCDK1 complex

Bioactivity Ribociclib succinate hydrate (LEE011 succinate hydrate) is ahighly specific inhibitor with values of 10 nMCDK46 IC50and 39 nM respectively and is over 1000-fold less potentagainst the cyclin BCDK1 complex

Bioactivity Riviciclib (P276-00 free base) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib shows antituhellip[1] [2]

Bioactivity Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib hydrochlorhellip[1] [2]

30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Purvalanol B (NG 95) Cat No HY-18299

R547 Cat No HY-10014

RGB-286638 Cat No HY-15504

RGB-286638 free base Cat No HY-15504A

Ribociclib (LEE011) Cat No HY-15777

Ribociclib hydrochloride (LEE011 (hydrochloride)) Cat No HY-15777A

Ribociclib succinate (LEE011 (succinate)) Cat No HY-15777B

Ribociclib succinate hydrate (LEE011 (succinate hydrate)) Cat No HY-15777C

Riviciclib (P276-00 (free base)) Cat No HY-16559A

Riviciclib hydrochloride (P276-00) Cat No HY-16559

wwwMedChemExpresscom 31

Purity 9850Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9907Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9677Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ro-3306 is a potent and selective inhibitor of with sCDK1 Kiof 20 nM 35 nM and 340 nM for CDK1 CDK1cyclin B1 andCDK2cyclin E respectively

Bioactivity Roniciclib is an orally bioavailable pan-cyclin dependentkinase inhibitor with of 5-25 nM for CDK1 CDK2(CDK) IC s50CDK3 CDK4 CDK7 and CDK9

Bioactivity SB1317 is a potent inhibitor of and forCDK2 JAK2 FLT3the treatment of cancer with of 13 73 and 56 nM forIC50CDK2 JAK2 and FLT3 respectively

Bioactivity SEL120-34A is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A HCl is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A monohydrochloride is an ATP-competitive andselective inhibitor inhibits kinase activities ofCDK8CDK8CycC and CDK19CycC complexes with s of 44 nM andIC50104 nM respectively with a of 3 nM for CDhellipKd

Bioactivity Seliciclib (Roscovitine) is a potent and selective CDKsinhibitor with s of 02 μM 065 μM and 07 μM for IC50 CDK5

and respectivelyCdc2 CDK2

Bioactivity Senexin A is a inhibitor with an of 280 nMCDK8 IC50

Bioactivity Simurosertib (TAK-931) is a selective cycle 7 kinase(CDC7)inhibitor with an lt03 nMIC50

Bioactivity SNS-032 (BMS-387032) is a selective inhibitor of CDK2 and with s of 38 nM 62 nM and 4CDK7 CDK9 IC50

nM respectively

Ro-3306 Cat No HY-12529

Roniciclib (BAY 1000394) Cat No HY-13914

SB1317 (TG02) Cat No HY-15166

SEL120-34A Cat No HY-111388

SEL120-34A HCl Cat No HY-111388B

SEL120-34A monohydrochloride Cat No HY-111388A

Seliciclib (Roscovitine CYC202 R-roscovitine) Cat No HY-30237

Senexin A Cat No HY-15681

Simurosertib (TAK-931) Cat No HY-100888

SNS-032 (BMS-387032) Cat No HY-10008

Purity 9846Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9796Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9882Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity SU9516 is a potent inhibitor with an of 22 nM andCDK2 IC50also shows inhibitory effects on CDK1 and CDK4 with s ofIC5040 200 nM respectively

Bioactivity SY-1365 is a highly selective covalent inhibitor of CDK7SY-1365 possesses therapeutic potential in both hematologicaland solid tumors [1]

Bioactivity T025 is an orally available and highly potent Cdc2-like kinase inhibitor with s of 48 0096 65 and 061 nM(CLK) Kd

for CLK1 CLK2 CLK3 and CLK4 respectively

Bioactivity THAL-SNS-032 is a selective degrader PROTAC consistingCDK9of a CDK-binding SNS-032 ligand linked to a thalidomidederivative that binds the E3 ubiquitin ligase Cereblon (CRBN)

[1]

Bioactivity THZ1 is a selective and potent covalent inhibitor withCDK7an of 32 nMIC50

Bioactivity THZ1 Hydrochloride is a selective and potent inhibitorCDK7with an of 32 nMIC50

Bioactivity THZ1-R is a non-cysteine reactive analog of THZ1 whichdisplays diminished activity for inhibition THZ1-RCDK7binds to with a of 142 nMCDK7 Kd

Bioactivity THZ2 is a potent and selective inhibitor with an ofCDK7 IC50139 nM

Bioactivity THZ531 is a covalent inhibitor of both and withCDK12 CDK13s of 158 nM and 69 nM respectivelyIC50

Bioactivity Trilaciclib is a inhibitor with s of 1 nM and 4 nMCDK46 IC50for CDK4 and CDK6 respectively

32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SU9516 Cat No HY-18629

SY-1365 Cat No HY-128587

T025 Cat No HY-112296

THAL-SNS-032 Cat No HY-123937

THZ1 Cat No HY-80013

THZ1 Hydrochloride Cat No HY-80013A

THZ1-R Cat No HY-19988

THZ2 Cat No HY-12280

THZ531 Cat No HY-103618

Trilaciclib (G1T28) Cat No HY-101467

wwwMedChemExpresscom 33

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Trilaciclib hydrochloride is a inhibitor with s ofCDK46 IC501 nM and 4 nM for CDK4 and CDK6 respectively

Bioactivity Voruciclib hydrochloride is a clinical stage oral CDK9inhibitor Voruciclib hydrochloride represses expression ofMCL-1 in multiple models of diffuse large B-cell lymphoma(DLBCL) [1]

Bioactivity Wogonin is a naturally occurring mono-flavonoid can inhibitthe activity of and and exhibitsCDK8 Wntanti-inflammatory and anti-tumor effects

Bioactivity XL413 is a potent selective and ATP competitive inhibitor of with an of 34 nM and also shows potent effectCdc7 IC50

with s of 215 42 nM on CK2 PIM1 respectively and anIC50 of 118 nM on pMCMEC50

Bioactivity XL413 hydrochloride is a potent selective and ATP competitiveinhibitor of with an of 34 nM and also showsCdc7 IC50potent effect with s of 215 42 nM on CK2 PIM1IC50respectively and an of 118 nM on pMCMEC50

Trilaciclib hydrochloride (G1T28 hydrochloride) Cat No HY-101467A

Voruciclib hydrochloride Cat No HY-12422A

Wogonin Cat No HY-N0400

XL413 Cat No HY-15260

XL413 hydrochloride Cat No HY-15260A

Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) are protein kinases that are involved in cellcycle control Two checkpoint kinase subtypes have been identifiedChk1 and Chk2 Chk1 is a central component of genome surveillancepathways and is a key regulator of the cell cycle and cell survivalChk1 is required for the initiation of DNA damage checkpoints andhas recently been shown to play a role in the normal (unperturbed)cell cycle Chk1 impacts various stages of the cell cycle including the Sphase G2M transition and M phase In addition to mediating cellcycle checkpoints Chk1 also contributes to DNA repair processesgene transcription embryo development cellular responses to HIVinfection and somatic cell viability Chk2 is a protein kinase that is

activated in response to DNA damage and is involved in cell cycle arrest In response to DNA damage and replicationblocks cell cycle progression is halted through the control of cell cycle regulators The protein encoded by this gene isa cell cycle checkpoint regulator and putative tumor suppressor

34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 35

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9877Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9990Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Checkpoint Kinase (Chk) Inhibitors amp Modulators

Bioactivity AZD-7762 is a potent ATP-competitive checkpoint kinase ( )Chkinhibitor in with an of 5 nM for Chk1IC50

Bioactivity BML-277 is a selective checkpoint kinase 2 ( ) inhibitorChk2with an of 15 nMIC50

Bioactivity CCT241533 is a potent and selective ATP competitive inhibitorof with an of 3 nM and of 116 nMCHK2 IC50 Ki

Bioactivity CCT241533 hydrochloride is a potent and selective CHK2inhibitor with an of 3 nM and a of 116 nMIC50 Ki

Bioactivity CCT244747 is a potent orally bioavailable and highlyselective inhibitor with an of 77 nM CCT244747CHK1 IC50also abrogates G2 checkpoint with an of 29 nMIC50

Bioactivity CCT245737 is a orally active and seletive inhibitorChk1with an of 13 nMIC50

Bioactivity CHIR-124 is a potent and selective inhibitor with Chk1 IC50of 03 nM and also potently targets and withPDGFR FLT3

s of 66 nM and 58 nMIC50

Bioactivity CHK-IN-1 is an inhibitor of and withCHK1 CHK2anti-proliferative activities

Bioactivity CHK1 inhibitor is an inhibitor of CHK1 Bioactivity CHK1-IN-2 is a checkpoint kinase 1 inhibitor with an(CHK1) of 6 nMIC50

AZD-7762 Cat No HY-10992

BML-277 (Chk2 Inhibitor II) Cat No HY-13946

CCT241533 Cat No HY-14715

CCT241533 hydrochloride Cat No HY-14715B

CCT244747 Cat No HY-18175

CCT245737 Cat No HY-18958

CHIR-124 Cat No HY-13263

CHK-IN-1 Cat No HY-U00345

CHK1 inhibitor Cat No HY-104022

CHK1-IN-2 Cat No HY-111369

Purity 9965Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9791Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity CHK1-IN-3 is a inhibitor with anCheckpoint Kinase 1 (CHK1) of 04 nM IC50

[1]Bioactivity GDC-0575 (ARRY-575 RG7741) is a highly-selective oral

small-molecule inhibitor with an of 12nMChk1 IC50

Bioactivity GDC-0575 dihydrochloride is an orally bioavailable CHK1inhibitor with an of 12 nM and has antitumor activityIC50

Bioactivity PF 477736 is a potent selective ATP-competitive inhibitor of with a of 049 nM 100-fold selectivity versus Chk1 Ki Chk2

( 47 nM)Ki

Bioactivity Prexasertib (LY2606368) is a potent selective andATP-competitive inhibitor with ancheckpoint kinase 1 (Chk1)

and a of lt1 nM and 09 nM respectivelyIC50 Ki

Bioactivity Prexasertib dihydrochloride (LY2606368 dihydrochloride) is apotent and selective ATP competitive inhibitor of the Chk1protein kinase with s of lt1 nM and 8 nM for CHK1 andIC50CHK2 respectively and a of 09 nM against purified CHK1Ki

Bioactivity Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is apotent selective ATP competitive and inhibitorCHK1 CHK2with a of 09 nM for CHK1 and s of lt1 nM 8 nM forKi IC50CHK1 and CHK2 respectively Prexasertib Mesylate Hydrateinhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2hellip

Bioactivity Rabusertib (LY2603618) is a potent and selective inhibitor of with an of 7 nMChk1 IC50

Bioactivity SCH900776 is a potent selective and oral inhibitor ofcheckpoint kinase1 ( ) with an of 3 nM It shows 50-Chk1 IC50and 500-fold selectivity over CDK2 andChk2 respectively

36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CHK1-IN-3 Cat No HY-128601

GDC-0575 (ARRY-575 RG7741) Cat No HY-112167

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride RG7741 dihydrochloride) Cat No HY-112167A

PF 477736 (PF 00477736) Cat No HY-10032

Prexasertib (LY2606368) Cat No HY-18174

Prexasertib dihydrochloride (LY2606368 (dihydrochloride)) Cat No HY-18174A

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate LY2940930) Cat No HY-18174B

Rabusertib (LY2603618 IC-83) Cat No HY-14720

SCH900776 (MK-8776) Cat No HY-15532

wwwMedChemExpresscom 37

CRISPRCas9

CRISPRCas9 (Clustered Regularly-Interspaced Short PalindromicRepeatsCas9) is a bacterial immune system that has been adaptedfor genome editing in mammalian cells Cas9 is a programmablenuclease that generates double-stranded breaks (DSB) in DNAdictated by binding of a ~20 nucleotide recombinant ldquoguide RNArdquo(gRNA) to the target site DSBrsquos produced by Cas9 are most oftenrepaired through the cellrsquos error-prone non-homologous end joining(NHEJ) pathway resulting in small insertions or deletions (indels) Thevast majority of indels shift the reading frame introducing apremature stop codon or resulting in nonsense mediated decay ofthe mRNA-effectively ldquoknocking outrdquo a gene

The CRISPRCas9 system has substantially advanced efforts in specific gene editing and has been successfully appliedto modify the episomal genomes of human and other organisms The CRISPRCas9 system utilizes a prokaryoticRNA-guided programmable nuclease that can make a double-strand DNA break (DSB) at a specific site under theguidance of a leading RNA This DSB process depends on the co-expression of two basic components a guide RNA(gRNA) and Cas9 nuclease Making a specific DSB can trigger DNA repair via either error-prone non-homologous endjoining (NHEJ) or homology-directed repair (HDR) In the presence of the CRISPRCas9 system the NHEJ inhibitorSCR7 is proven to increase the efficiency of Cas9-mediated HDR by at least by 7-fold in mammalian cells Genomeediting via CRISPRCas9 has become an efficient and reliable way to make precise targeted changes to the genome ofliving cells

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

CRISPRCas9 Inhibitors amp Modulators

Bioactivity Brefeldin A is a specific inhibitor of whichprotein traffickingblocks the protein transport from the endoplasmic reticulum tothe Golgi complex

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity L755507 is a potent selective agonist of with an β -AR3 IC50of 35 nM

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity Zidovudine is a nucleoside reverse transcriptase inhibitor () widely used to treat HIV infection Zidovudine increasesNRTI

CRISPRCas9-mediated editing frequency

38 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Brefeldin A (BFA Cyanein Decumbin) Cat No HY-16592

KU-57788 (NU7441) Cat No HY-11006

L755507 Cat No HY-19334

Nocodazole (Oncodazole R17934) Cat No HY-13520

RS-1 Cat No HY-19793

SCR7 Cat No HY-12742

Zidovudine (Azidothymidine AZT ZDV) Cat No HY-17413

wwwMedChemExpresscom 39

DeubiquitinaseDUBs

Deubiquitinases (DUBs) are a large group of proteases that cleaveubiquitin from proteins and other molecules Ubiquitin is attached toproteins in order to regulate the degradation of proteins via theproteasome and lysosome coordinate thecellular localisation ofproteins activate and inactivate proteins and modulateprotein-protein interactions DUBs can reverse these effects bycleaving the peptide or isopeptide bond between ubiquitin and itssubstrate protein In humans there are nearly 100 DUB genes whichcan be classified into two main classes cysteine proteases andmetalloproteases The cysteine proteases comprise ubiquitin-specificproteases (USPs) ubiquitin C-terminal hydrolases (UCHs)

Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU) The metalloprotease groupcontains only the Jab1Mov34Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases DUBs play several roles inthe ubiquitin pathway One of the best characterised functions of DUBs is the removal of monoubiqutin andpolyubiquitin chainsfrom proteins

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9940Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9892Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9893Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Deubiquitinase Inhibitors amp Modulators

Bioactivity 6-Thioguanine (Thioguanine) is an anti-leukemia andimmunosuppressant agent acts as an inhibitor of SARS and MERScoronavirus papain-like proteases ( ) and also potentlyPLprosinhibits activity with s of 25 μM and 40 μM forUSP2 IC50Plpros and recombinant human USP2 respectively

Bioactivity b-AP15 is a specific inhibitor of the enzymesdeubiquitinating and UCHL5 Usp14

Bioactivity BAY 11-7082 is a inhibitor which decreases NF-κB byNF-κBinhibiting TNF-α-induced phosphorylation of IκB-α BAY 11-7082inhibits ubiquitin-specific protease and withUSP7 USP21

s of 019 μM and 096 μM respectivelyIC50

Bioactivity C527 is a is a pan inhibitor with a highDUB enzymepotency for the complex ( =088 μM)USP1UAF1 IC50

Bioactivity Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB)inhibitor directly inhibiting DUB activity of USP9x USP5USP14 and UCH37 Degrasyn has been shown to downregulate theantiapoptotic proteins and Bcr-Abl JAK2

Bioactivity DUBs-IN-1 is an active inhibitor of ubiquitin-specific with an of 024 μM for USP8proteases (USPs) IC50

Bioactivity DUBs-IN-2 is a potent inhibitor with an ofdeubiquitinase IC50028 μM for USP8

Bioactivity DUBs-IN-3 is a potent enzyme inhibitordeubiquitinase (USP)extracted from reference compound 22c with an of 056 μMIC50for USP8

Bioactivity EOAI3402143 is a ( ) inhibitor whichdeubiquitinase DUBinhibits dose-dependently inhibits and Usp9x Usp24 Usp5

Bioactivity FT671 is a potent non-covalent and selective inhibitorUSP7with an of 52 nM and binds to the USP7 catalytic domainIC50with a of 65 nMKd

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6-Thioguanine (Thioguanine2-Amino-6-purinethiol) Cat No HY-13765

b-AP15 (NSC 687852) Cat No HY-13989

BAY 11-7082 (BAY 11-7821) Cat No HY-13453

C527 Cat No HY-12988

Degrasyn (WP1130) Cat No HY-13264

DUBs-IN-1 Cat No HY-50736

DUBs-IN-2 Cat No HY-50737A

DUBs-IN-3 Cat No HY-50737

EOAI3402143 Cat No HY-111408

FT671 Cat No HY-107985

wwwMedChemExpresscom 41

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9773Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9684Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity FT827 is a selective and covalent ubiquitin-specific protease7 ( ) inhibitor with an of 52 nMUSP7 IC50

Bioactivity GNE-6640 is a selective and non-covalent inhibitor ofubiquitin epecific peptidase 7 with values of(USP7) IC50075 μM 043 μM 203 μM and 023 μM for full length USP7USP7 catalytic domain full length USP43 and Ub-MDM2respectively

Bioactivity GNE-6776 is a selective inhibitorUSP7 Bioactivity HBX 19818 is a specific inhibitor of ubiquitin-specific with an of 281 μMprotease 7 (USP7) IC50

Bioactivity IU1 is a special inhibitor with of 4-5 μMUsp14 IC50 Bioactivity IU1-47 is a potent inhibitor with an of 06 μMUSP14 IC50

IU1-47 induces tau elimination in cultured neurons [1]

Bioactivity LDN-57444 is a reversible competitive and site-directedinhibitor of withubiquitin C-terminal hydrolase L1 (UCH-L1)an of 088 μM and a of 040 μM LDN-57444 alsoIC50 Kisuppresses UCH-L3 activity with an of 25 μMIC50

Bioactivity MF-094 is a potent and selective inhibitor with an USP30 IC50of 120 nM

Bioactivity ML-323 is a reversible potent inhibitor with USP1-UAF1 IC50of 76 nM in a Ub-Rho assay The measured inhibition constantsof ML-323 for the free enzyme ( ) is 68 nMKi

Bioactivity ML364 is an inhibitor of ubiquitin specific peptidase 2 and can be used for the research of breast cancer(USP2)

extracted from patent WO 2016134026 A1 compound Figure 10G

FT827 Cat No HY-111350

GNE-6640 Cat No HY-112937

GNE-6776 Cat No HY-107986

HBX 19818 Cat No HY-17540

IU1 Cat No HY-13817

IU1-47 Cat No HY-122243

LDN-57444 Cat No HY-18637

MF-094 Cat No HY-112438

ML-323 Cat No HY-17543

ML364 Cat No HY-100900

Purity 9800Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9737Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9843Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NSC632839 is a nonselective isopeptidase inhibitor whichinhibits and with s of 45plusmn4 μMUSP2 USP7 SENP2 EC5037plusmn1 μM and 98plusmn18 μM respectively

Bioactivity P 22077 is a cell-permeable ubiquitin-specific protease 7 inhibitor with an of 801 μM It also inhibits(USP7) EC50

USP47 with an of 874 μMEC50

Bioactivity P005091 is a selective and potent inhibitor of with anubiquitin-specific protease 7 (USP7)

of 42 μMEC50

Bioactivity PR-619 is a broad-range inhibitor with of 393DUB EC5049 686 72 and 861 μM for USP4 USP8 USP7 USP2and respectivelyUSP5

Bioactivity SJB2-043 is an inhibitor of the native complex withUSP1UAF1 of 544 nMIC50

Bioactivity SJB3-019A is a potent and novel inhibitor 5 times moreUSP1potent than SJB2-043 in promoting ID1 degradation andcytoxicity in K562 cells with of 00781 μMIC50

Bioactivity USP7-IN-1 is a selective and reversible inhibitor of with an of 77 μMubiquitin-specific protease 7 (USP7) IC50

and can be used for the research of cancer

Bioactivity USP7-IN-3 (Compound 5) is a potent and selective allostericubiquitin-specific protease 7 ( ) inhibitor USP7 [1]

Bioactivity USP7USP47 inhibitor is a selective ubiquitin-specific protease inhibitor with s of 042 μM and 10747 (USP7USP47) EC50

μM respectively

Bioactivity VLX1570 is a competitive inhibitor of proteasomedeubiquitinases ( ) with an of approximate 10 μMDUBs IC50

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NSC632839 Cat No HY-100708

P 22077 Cat No HY-13865

P005091 (P5091) Cat No HY-15667

PR-619 Cat No HY-13814

SJB2-043 Cat No HY-15757

SJB3-019A Cat No HY-80012

USP7-IN-1 Cat No HY-16709

USP7-IN-3 Cat No HY-112128

USP7USP47 inhibitor Cat No HY-13487

VLX1570 Cat No HY-12471

wwwMedChemExpresscom 43

DNA AlkylatorCrosslinker

DNA alkylatorcrosslinker is a molecule that alkylates DNA or cancross link with DNA DNA alkylatorcrosslinker can have mutagenicpharmaceutical or other effects Alkylation is the transfer of an alkylgroup from one molecule to another The alkyl group may betransferred as an alkyl carbocation a free radical a carbanion or acarbene Alkylating agents are widely used in chemistry because thealkyl group is probably the most common group encountered inorganic molecules Selective alkylation or adding parts to the chainwith the desired functional groups is used especially if there is nocommonly available biological precursor Alkylation with only onecarbon is termed methylation In medicine alkylation of DNA is used

in chemotherapy to damage the DNA of cancer cells Alkylation is accomplished with the class of drugs calledalkylating antineoplastic agents Crosslinking of DNA occurs when various exogenous or endogenous agents reactwith two different positions in the DNA This can either occur in the same strand (intrastrand crosslink) or in theopposite strands of the DNA (interstrand crosslink) Crosslinks also occur between DNA and protein DNA replicationis blocked by crosslinks which causes replication arrest and cell death if the crosslink is not repaired The RAD51family plays a role in repair

Purity 990Clinical Data LaunchedSize 100 mg 500 mg

Purity 9879Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9844Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9961Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

DNA AlkylatorCrosslinker Inhibitors amp Modulators

Bioactivity Altretamine is an antineoplastic agentalkylating Bioactivity Altretamine hydrochloride is an antineoplasticalkylatingagent

Bioactivity Bendamustine D4 is the deuterium labeled BendamustineBendamustine is a agent that causes DNADNA cross-linkingbreaks with alkylating and antimetabolite properties

Bioactivity Bendamustine hydrochloride is a agent thatDNA cross-linkingcauses DNA breaks with alkylating and antimetaboliteproperties

Bioactivity Busulfan is a potent with selective immunosuppressivealkylatoreffect on bone marrow

Bioactivity Calicheamicin is a cytotoxic agent that causes double-strandDNA breaks

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity Carmustine is an antitumor chemotherapeutic agent which worksby akylating DNA and RNA

Bioactivity Chlorambucil is an agent with antitumor activityalkylating Bioactivity Cisplatin is a antineoplastic chemotherapy drug which works bycross-linking with and causing DNA damage in cancerDNAcells

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Altretamine (ENT-50852 RB-1515 WR-95704) Cat No HY-B0181

Altretamine hydrochloride (ENT-50852 hydrochloride RB-1515

hydrochloride WR-95704 hydrochloride) Cat No HY-B0181A

Bendamustine D4 (SDX-105 D4) Cat No HY-13567S

Bendamustine hydrochloride (SDX-105 EP-3101) Cat No HY-B0077

Busulfan Cat No HY-B0245

Calicheamicin (Calicheamicin γ1) Cat No HY-19609

Carboplatin (NSC 241240) Cat No HY-17393

Carmustine Cat No HY-13585

Chlorambucil (CB-1348 WR-139013) Cat No HY-13593

Cisplatin (CDDP cis-Diaminodichloroplatinum) Cat No HY-17394

wwwMedChemExpresscom 45

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 980Clinical Data LaunchedSize 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Bioactivity Cyclophosphamide is a synthetic agent chemicallyalkylatingrelated to the nitrogen mustards with antineoplastic andimmunosuppressive activities

Bioactivity Cyclophosphamide hydrate is a synthetic agentalkylatingchemically related to the nitrogen mustards withantineoplastic and immunosuppressive activities

Bioactivity Fotemustine is a agent with antitumor activityDNA-alkylating Bioactivity Ifosfamide is an chemotherapeutic agent withalkylatingactivity against a wide range of tumors

Bioactivity Lomustine (CCNU) is a agent with antitumorDNA alkylatingactivity

Bioactivity Melphalan is an effective agent with potentDNA alkylatingantitumor activity

Bioactivity Methylnitronitrosoguanidine (MNNG) is an agent withalkylatingtoxic and mutagenic effects [1]

Bioactivity Miriplatin is a chemotherapy agent which belongs to the classof agentsalkylating

Bioactivity Miriplatin hydrate is a chemotherapy agent which belongs tothe class of agentsalkylating

Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Cyclophosphamide Cat No HY-17420

Cyclophosphamide hydrate (Cyclophosphamide monohydrate) Cat No HY-17420A

Fotemustine (S10036) Cat No HY-B0733

Ifosfamide Cat No HY-17419

Lomustine (CCNU NSC 79037) Cat No HY-13669

Melphalan (L-PAM) Cat No HY-17575

Methylnitronitrosoguanidine (MNNG) Cat No HY-128612

Miriplatin (SM-11355) Cat No HY-16325A

Miriplatin hydrate (SM-11355 (hydrate)) Cat No HY-16325

Mitomycin C (Ametycine) Cat No HY-13316

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9926Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9986Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Oxaliplatin is a inhibitor It causes DNADNA synthesiscrosslinking damage prevents DNA replication andtranscription and causes cell death

Bioactivity Palifosfamide is a novel DNA alkylator and the activemetabolite of ifosfamide with antitumor activity

Bioactivity Procarbazine Hydrochloride is an agent withalkylatinganticancer activity

Bioactivity RITA is an inhibitor of binds top53-HDM-2 interactionp53dN with a of 15 nM and also induces Kd DNA-DNA

cross-links

Bioactivity Satraplatin is an agent with potent antitumoralkylatingeffect

Bioactivity SJG-136 is a agent with an of 45 nMDNA cross-linking XL50for pBR322 DNA SJG-136 has potent antitumor activity

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity Temozolomide (NSC 362856 CCRG 81045) is an oral DNA agent used to treat some brain cancersalkylating

Bioactivity Thio-TEPA is a agent with antitumor activityDNA alkylating Bioactivity Treosulfan (NSC 39069Treosulphan) is an agent withalkylatingactivity in ovarian cancer and other solid tumor types

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Oxaliplatin Cat No HY-17371

Palifosfamide (Isophosphoramide mustard IPM ZIO-201) Cat No HY-14798

Procarbazine Hydrochloride Cat No HY-13733

RITA (NSC 652287) Cat No HY-13424

Satraplatin (BMS182751 BMY45594 JM216) Cat No HY-17576

SJG-136 (NSC-694501) Cat No HY-14573

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

Temozolomide (NSC 362856 CCRG 81045 TMZ) Cat No HY-17364

Thio-TEPA Cat No HY-17574

Treosulfan (NSC 39069 Treosulphan) Cat No HY-16503

wwwMedChemExpresscom 47

Purity 980Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Uramustine is an oral agent effective in thealkylatingtreatment of lymphosarcoma chronic lymphatic leukaemia andthrombocythemia

Bioactivity VAL-083 is an agent that creates N7 methylation onalkylatingDNA with antitumor activity

Uramustine (Uracil mustard) Cat No HY-13544

VAL-083 (Dianhydrodulcitol Dianhydrogalactitol) Cat No HY-16513

DNA-PKDNA-dependent protein kinase

DNA-PKcs (DNA-dependent protein kinase catalytic subunit) is anenzyme that in humans is encoded by the PRKDC gene DNA-PKcsbelongs to the phosphatidylinositol 3-kinase-related kinase proteinfamily DNA-PKcs is the catalytic subunit of a nuclear DNA-dependentserinethreonine protein kinase called DNA-PK The secondcomponent is the autoimmune antigen Ku On its own DNA-PKcs isinactive and relies on Ku to direct it to DNA ends and trigger itskinase activity DNA-PKcs is required for the non-homologous endjoining (NHEJ) pathway of DNA repair Many proteins have beenidentified as substrates for the kinase activity of DNA-PKAutophosphorylation of DNA-PKcs appears to play a key role in NHEJ

and is thought to induce a conformational change that allows end processing enzymes to access the ends of thedouble-strand break DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNAdamage checkpoint

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wwwMedChemExpresscom 49

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9943Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9722Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9664Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9239Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

DNA-PK Inhibitors amp Modulators

Bioactivity (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer ofNedisertib with an in the range of 7-30 nM for IC50 DNA-PK

[1]

Bioactivity AZD-7648 is a potent and selective inhibitorDNA-PKAnti-tumor activity [1]

Bioactivity CC-115 is a potent and dual and kinaseDNA-PK mTORinhibitor with s of 13 nM and 21 nM respectively CC-115IC50blocks both and signalingmTORC1 mTORC2

Bioactivity CC-115 hydrochloride is a potent and dual and DNA-PK mTORkinase inhibitor with s of 13 nM and 21 nM respectivelyIC50CC-115 blocks both and signalingmTORC1 mTORC2

Bioactivity Compound 401 is a synthetic inhibitor of ( = 028DNA-PK IC50μM) that also targets mTOR but not PI3K in vitro

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity LTURM34 is a specific inhibitor with an of 0034DNA-PK IC50μM

Bioactivity LY3023414 potently and selectively inhibits class I PI3Kisoforms and with s of 607 nM 776DNA-PK mTORC12 IC50nM 38 nM 238 nM 424 nM and 165 nM for PI3Kα PI3KβPI3Kδ PI3Kγ DNA-PK and mTOR respectively LY3023414potently inhibits at low nanomolarhellipmTORC1 2

Bioactivity Nedisertib (M3814) is a potent and selective inhibitor of ( ) with an of lt3DNA-dependent Protein Kinase DNA-PK IC50

nM

Bioactivity NU 7026 is a novel specific inhibitor with ofDNA-PK IC50023plusmn001 μM also inhibits with of 13plusmn3 μMPI3K IC50

(R)-Nedisertib ((R)-M3814) Cat No HY-101570A

AZD-7648 Cat No HY-111783

CC-115 Cat No HY-16962

CC-115 hydrochloride Cat No HY-16962A

Compound 401 Cat No HY-19341

KU-57788 (NU7441) Cat No HY-11006

LTURM34 Cat No HY-101667

LY3023414 Cat No HY-12513

Nedisertib (M3814) Cat No HY-101570

NU 7026 (DNA-PK Inhibitor II LY293646) Cat No HY-15719

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9937Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9145Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity PI-103 is a potent and inhibitor with s of 8PI3K mTOR IC50nM 88 nM 48 nM 150 nM 20 nM and 83 nM for p110α p110β

and PI-103 also inhibitsp110δ p110γ mTORC1 mTORC2 with an of 2 nMDNA-PK IC50

Bioactivity PI-103 Hydrochloride is a dual and inhibitor withPI3K mTORs of 8 nM 88 nM 48 nM 150 nM 20 nM and 83 nM forIC50

and p110α p110β p110δ p110γ mTORC1 mTORC2PI-103 also inhibits with an of 2 nMDNA-PK IC50

Bioactivity PIK-75 is a and inhibitor which inhibits DNA-PKDNA-PK PI3K and p110γ with s of 2 58 and 76 nM respectivelyp110α IC50

PIK-75 inhibits p110α gt200-fold more potently than p110β(IC =13 μM)50

Bioactivity PIK-90 is a and inhibitor which inhibits DNA-PK PI3K p110α and with s of 11 18 and 13 nMp110γ DNA-PK IC50

respectively

Bioactivity Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib apotent inhibitor with an of lt3 nM DNA-PK IC50

[1]Bioactivity SF2523 is a highly selective and potent inhibitor of withPI3K

s of 34 nM 158 nM 9 nM 241 nM and 280 nM for IC50 PI3Kα

BRD4 and mTOR respectivelyPI3Kγ DNA-PK

Bioactivity STL127705 (Compound L) is a Ku 7080 heterodimer proteininhibitor inhibits Ku7080-DNA interaction with an ofIC5035 μM STL127705 also inhibits Ku-dependent activation ofDNA-PKCS kinase ( 25 μM) IC50

[1]

Bioactivity Torin 2 is an inhibitor with of 025 nM formTOR EC50inhibiting cellular mTOR activity and exhibits 800-foldselectivity over PI3K (EC 200 nM) Torin 2 also inhibits50

with an of 05 nM in the cell free assay TorihellipDNA-PK IC50

Bioactivity VX-984 is a potent inhibitorDNA-PK Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

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PI-103 Cat No HY-10115

PI-103 Hydrochloride Cat No HY-10115A

PIK-75 (PIK-75 Hydrochloride) Cat No HY-13281

PIK-90 Cat No HY-12030

Rac-Nedisertib (Rac-M3814) Cat No HY-101570B

SF2523 Cat No HY-101146

STL127705 Cat No HY-122727

Torin 2 Cat No HY-13002

VX-984 (M9831) Cat No HY-19939S

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

wwwMedChemExpresscom 51

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity YU238259 is an inhibitor of homology-dependent DNA repair () used for cancer researchHDR

YU238259 Cat No HY-19977

DNARNA Synthesis

RNA synthesis which is also called DNA transcription is a highlyselective process Transcription by RNA polymerase II extends beyondRNA synthesis towards a more active role in mRNA maturationsurveillance and export to the cytoplasmSingle-strand breaks are repaired by DNA ligase using thecomplementary strand of the double helix as a template with DNAligase creating the final phosphodiester bond to fully repair theDNADNA ligases discriminate against substrates containing RNAstrands or mismatched base pairs at positions near the ends of thenickedDNA Bleomycin (BLM) exerts its genotoxicity by generatingfree radicals whichattack C-4prime in the deoxyribose backbone of DNA

leading to opening of the ribose ring and strand breakage it is an S-independentradiomimetic agent that causesdouble-strand breaks in DNAFirst strand cDNA is synthesized using random hexamer primers and M-MuLV Reverse Transcriptase (RNase H)Second strand cDNA synthesis is subsequently performed using DNA Polymerase I and RNase H The remainingoverhangs are converted into blunt ends using exonucleasepolymerase activity After adenylation of the 3prime ends ofDNA fragments NEBNext Adaptor with hairpin loop structure is ligated to prepare the samples for hybridization Cellcycle and DNA replication are the top two pathways regulated by BET bromodomain inhibition Cycloheximide blocksthe translation of mRNA to protein

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wwwMedChemExpresscom 53

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 1 mg 2 mg 5 mg

Purity 9876Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9989Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 9968Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

25 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

DNARNA Synthesis Inhibitors amp Modulators

Bioactivity 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is amodified nucleoside 2-(Methylamino)-1H-purin-6(7H)-one is anendogenous methylated nucleoside found in human fluids

Bioactivity 374-Trihydroxyflavone isolated from Rhus javanica var is a flavonoid with DNA strand-scission activityroxburghiana

[1]

Bioactivity 5-Methoxyflavone belonged to Flavonoid family is a DNApolymerase-beta inhibitor and neuroprotective agent againstbeta-amyloid toxicity possess central nervous system (CNS)depressant effect mediated through the ionotropic GABA Areceptors

Bioactivity 6-Thio-2-Deoxyguanosine is a nucleoside analogue that can beincorporated into de novo-synthesized telomeres by telomerase

Bioactivity Acelarin (NUC-1031) is a ProTide transformation andenhancement of the widely-used nucleoside analoguegemcitabine

Bioactivity Actinomycin D inhibits with an of 042 μMDNA repair IC50

Bioactivity Adenine is a purine derivative and a nucleobase with a varietyof roles in biochemistry Target Nucleosideantimetaboliteanalog Adenine is a nucleobase with a varietyof roles in biochemistry including cellular respiration inthe form of both the energy-rich adenosine triphosphate (ATP)hellip

Bioactivity alpha-Amanitin is the principal toxin of several deadlypoisonous mushrooms exerting its toxic function by inhibiting

RNA-polymerase II

Bioactivity Anisomycin is a potent inhibitor whichprotein synthesisinterferes with protein and by inhibitingDNA synthesispeptidyl transferase or the 80S ribosome system Anisomycin isa JNK activator which increases phospho-JNK

Bioactivity Beaucage reagent is found to be potent in causing DNAcleavage

2-(Methylamino)-1H-purin-6(7H)-one (N2-methylguanine) Cat No HY-101412

374-Trihydroxyflavone (5-Deoxykampferol) Cat No HY-111806

5-Methoxyflavone Cat No HY-107790

6-Thio-2-Deoxyguanosine (6-thio-dG β-TGdR) Cat No HY-18762

Acelarin (NUC-1031) Cat No HY-100885

Actinomycin D (Dactinomycin Actinomycin IV) Cat No HY-17559

Adenine (6-Aminopurine Vitamin B4) Cat No HY-B0152

alpha-Amanitin (α-Amanitin α-Amatoxin) Cat No HY-19610

Anisomycin (Flagecidin Wuningmeisu C) Cat No HY-18982

Beaucage reagent Cat No HY-100951

Purity 9847Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity 9804Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9896Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Bioactivity Bleomycin sulfate is a inhibitor with potentDNA synthesisantitumor activity

Bioactivity BMH-21 is a small molecule DNA intercalator that bindsribosomal DNA and inhibits RNA polymerase I (Pol I)transcription does not cause phosphorylation of H2AX

Bioactivity Branaplam (LMI070) is a highly potent selective and orallyactive small molecule modulatorSMN2 splicing

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity CeMMEC1 is an inhibitor of and also has high affinityBRD4for with an of 09 μM for TAF1 and a of 18TAF1 IC50 KdμM for TAF1 (2)

Bioactivity CeMMEC13 is a potent inhibitor of bromodomain withTAF1 (2)an of 21 μMIC50

Bioactivity Chebulinic acid is a potent natural inhibitor of Mtuberculosis DNA gyrase also can inhibit SMAD-3phosphorylation inhibit H+ K+-ATPase activity

Bioactivity COH29 is a potent ribonucleotide reductase ( ) inhibitorRNRwith anticancer activity COH29 inhibits α and β subunit ofRNR with s of 16 μMIC50

Bioactivity CX-5461 is a potent and oral inhibitor ItrRNA synthesisinhibits RNA polymerase I-driven transcription of rRNA with

s of 142 113 and 54 nM in HCT-116 A375 and MIA PaCa-2IC50cells respectively

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Bleomycin sulfate Cat No HY-17565

BMH-21 Cat No HY-12484

Branaplam (LMI070 NVS-SM1) Cat No HY-19620

Capecitabine Cat No HY-B0016

Carboplatin (NSC 241240) Cat No HY-17393

CeMMEC1 Cat No HY-111445

CeMMEC13 Cat No HY-101088

Chebulinic acid Cat No HY-N2033

COH29 (RNR Inhibitor COH29) Cat No HY-19931

CX-5461 Cat No HY-13323

wwwMedChemExpresscom 55

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9872Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9963Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9945Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg

Bioactivity CX-5461 dihydrochloride is a potent and orally bioavailableinhibitor of Pol I-mediated with s of 142rRNA synthesis IC50nM in HCT-116 113 nM in A375 and 54 nM in MIA PaCa-2 cellsand shows little or no effect on Pol II ( ge25 μM)IC50

Bioactivity Cycloheximide (Naramycin A) is an eukaryote protein synthesisinhibitor with s of 5325 nM and 2880 nM for proteinIC50synthesis and RNA synthesis respectivelyin vivo

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Datelliptium chloride is a DNA-intercalating agent derivedfrom ellipticine with anti-tumor activities

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Didox (NSC-324360) is a synthetic (ribonucleotide reductase) inhibitorRR

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

CX-5461 dihydrochloride Cat No HY-13323A

Cycloheximide (Naramycin A Actidione CHX) Cat No HY-12320

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Datelliptium chloride Cat No HY-U00337

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Didox (NSC-324360) Cat No HY-19387

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Bioactivity Folic acid(Vitamin M Vitamin B9) is a B vitamin is necessaryfor the production and maintenance of new cells for DNAsynthesis and RNA synthesis

Bioactivity GC7 Sulfate is a ( ) inhibitordeoxyhypusine synthase DHPS

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity GNE-371 is a potent and selective chemical probe for thesecond bromodomains of human transcription-initiation-factor

subunit 1 and transcription-initiation-factor TFIID TFIIDsubunit 1-like with an of 10 nM for TAF1(2)IC50

Bioactivity Guanine is one of the fundamental components of nucleic acids( and ) Guanine is a purine derivative consistingDNA RNAof a fused pyrimidine-imidazole ring system with conjugateddouble bonds

Bioactivity Halofuginone (RU-19110) is a less-toxic form of Febrifuginewhich is isolated from the plant Dichroa febrifuga [1]

Halofuginone inhibits in anprolyl-tRNA synthetaseATP-dependent manner with a of 183 nM HalofuginhellipKi

[2]

Bioactivity Halofuginone hydrobromide (RU-19110 hydrobromide) is aless-toxic form of Febrifugine which is isolated from theplant Halofuginone inhibits Dichroa febrifuga [1] prolyl-tRNA

in an ATP-dependent manner with a of 183hellipsynthetase Ki

Bioactivity Hydroxyurea is a cell apoptosis inducer that inhibit DNAsynthesis through inhibition of ribonucleotide reductase

Bioactivity L189 is a novel human DNA ligase inhibitor inhibitshLigIIIIIV with IC50 of 595 μM

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Folic acid (Vitamin B9 Vitamin M) Cat No HY-16637

GC7 Sulfate Cat No HY-108314A

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

GNE-371 Cat No HY-112803

Guanine Cat No HY-Y1055

Halofuginone (RU-19110) Cat No HY-N1584

Halofuginone hydrobromide (RU-19110 (hydrobromide)) Cat No HY-N1584A

Hydroxyurea (Hydroxycarbamide) Cat No HY-B0313

L189 Cat No HY-15588

wwwMedChemExpresscom 57

Purity 990Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9839Clinical Data No Development ReportedSize 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9977Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9988Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity L67 is a novel competitive human DNA ligase inhibitorinhibits DNA ligases I and III with IC50 of 10 μM and 10 μM

Bioactivity Madrasin is a potent and cell penetrant splicing inhibitorthat interferes with the early stages of spliceosome assemblyMadrasin is cytotoxic at higher concentrations although atlower concentrations it induces cell cycle arrest promotes aspecific reorganization of subnuclear protein localizationhellip

Bioactivity MB-7133 is a inhibitorDNA synthesis Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Bioactivity ML216(CID-49852229) is a potent inhibitor of the DNA unwindingactivity of BLM helicase showing similar IC50s of 30 and097 μM for full length BLM and BLM636ndash1298 respectively IC50value 30097 uM(Full length636ndash1298 BLM) Target BLMhelicase inhibitor ML216 shows cell-based activity and canhellip

Bioactivity Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNAdamage agent

Bioactivity NITD008 is a potent and selective inhibitor whichflavivirusecan inhibit with an ofDengue Virus Type 2 (DENV-2) EC50064 μM

Bioactivity Oxolinic acid is a potent inhibitor of DNA gyrase and DNAsynthesis lead to DNA cleavage when extracted chromosomes areincubated with sodium dodecyl sulfate

Bioactivity Phen-DC3 is a (G4) specific ligand which canG-quadruplexinhibit and helicases with s of 65plusmn6 and 50plusmn10FANCJ DinG IC50nM respectively

Bioactivity Plicamycin is a selective specificity protein 1 ( )Sp1inhibitor Plicamycin inhibits the growth of various cancersby decreasing Sp1 protein

L67 (DNA Ligase Inhibitor) Cat No HY-15586

Madrasin (DDD00107587) Cat No HY-100236

MB-7133 Cat No HY-16311

Mitomycin C (Ametycine) Cat No HY-13316

ML216 (CID-49852229) Cat No HY-12342

Nedaplatin (NSC 375101D) Cat No HY-13700

NITD008 (7-Deaza-2-C-acetylene-adenosine) Cat No HY-12957

Oxolinic acid Cat No HY-B1002

Phen-DC3 Cat No HY-15594

Plicamycin (Mithramycin A) Cat No HY-A0122

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9762Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9931Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Quarfloxin (CX 3543) a fluoroquinolone derivative withantineoplastic activity targets and inhibits RNA pol Iactivity with IC values in the nanomolar range in50neuroblastoma cells Quarfloxin disrupts the interactionbetween the nucleolin protein and a G-quadruplex DNA structurehellip

Bioactivity RG7800 a small molecule splicing modifier to enterSMN2human clinical trials to treat spinal muscular atrophy

Bioactivity RG7800 hydrochloride is an orally active splicingSMN2modulator with s of 23 nM and 87 nM for EC15x SMN2

splicing and RG7800 hydrochloride has theSMN proteinpotential to treat spinal muscular atrophy

Bioactivity Risdiplam (RG7916 RO7034067) is an orally administeredcentrally and peripherally distributed pre-mRNASMN2splicing modifier that increases survival motor neuron (SMN)protein levels

Bioactivity Saccharin 1-methylimidazole is an activator for DNARNASynthesis

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity SMN-C3 is an orally active splicing modulator and hasSMN2the potential to treat spinal muscular atrophy (SMA)

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 valueof 08 nM less potent for MTH2 NUDT5 NUDT12 NUDT14 andNUDT16

Bioactivity TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) withan IC50 value of 08 nM less potent for MTH2 NUDT5 NUDT12NUDT14 and NUDT16

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Quarfloxin (CX 3543) Cat No HY-14776

RG7800 (RO6885247) Cat No HY-101792

RG7800 hydrochloride (RO6885247 hydrochloride) Cat No HY-101792A

Risdiplam (RG7916 RO7034067) Cat No HY-109101

Saccharin 1-methylimidazole Cat No HY-112060

SCR7 Cat No HY-12742

SMN-C3 Cat No HY-112633

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

TH287 Cat No HY-16965

TH287 hydrochloride Cat No HY-16965A

wwwMedChemExpresscom 59

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9920Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 25 mg 50 mg 100 mg

Bioactivity TH588 is first-in-class nudix hydrolase family inhibitor thatpotently and selectively engage and inhibit the (MTH1

= 5 nM)IC50

Bioactivity TH588 hydrochloride is first-in-class nudix hydrolase familyinhibitor that potently and selectively engage and inhibit the

( = 5 nM)MTH1 IC50

Bioactivity Thiarabine (OSI-7836) shows potent anti-tumor activity andinhibition of synthesisDNA

Bioactivity Triapine is a novel inhibitor of the M2 subunit of ( ) and is a potentribonucleotide reductase RR

radiosensitizer

Bioactivity Triciribine is a inhibitor also inhibits DNA synthesis Aktand with of 130 nM and 002-046 μMHIV-12 IC50respectively

Bioactivity YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding tothe oncogenic transciption factor EWS-FLI1 YK-4-279 inhibitsEwings sarcoma family tumor (ESFT) cell growth YK-4-279induces apoptosis

Bioactivity Zoliflodacin (ETX0914AZD0914) is a novelspiropyrimidinetrione bacterial DNA gyrasetopoisomeraseinhibitor Zoliflodacin has potent antibacterialin vitroactivity against Gram-positive and Gram-negative organismsincluding with the of 025 μgmLS aureus MIC90

TH588 Cat No HY-12814

TH588 hydrochloride Cat No HY-12814A

Thiarabine (OSI-7836) Cat No HY-16496

Triapine (3-AP PAN-811 OCX191 NSC663249) Cat No HY-10082

Triciribine (API-2 NSC 154020 TCN) Cat No HY-15457

YK-4-279 Cat No HY-14507

Zoliflodacin (ETX0914 AZD0914) Cat No HY-17647

Eukaryotic Initiation Factor (eIF)

Eukaryotic initiation factors (eIFs) are proteins involved in theinitiation phase of eukaryotic translation These proteins help stabilizethe formation of the functional ribosome around the start codon andalso provide regulatory mechanisms in translation initiationEukaryotic initiation factor 2B (eIF2B) is a guaninenucleotide-exchange factor which mediates the exchange of GDP(bound to initiation factor eIF2) for GTP thus regenerating the active[eIF2GTP] complex that is required for peptide-chain initiation Theactivity of eIF2B is a key control point for eukaryotic protein synthesisand is altered in response to viral infection hormones nutrientsgrowth factors and certain stresses

Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis oncapped mRNAs in the cytoplasm Eukaryotic initiation factor (elF) 4A functions as a subunit of the initiation factorcomplex elF4F which mediates the binding of mRNA to the ribosome

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Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 2 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Eukaryotic Initiation Factor (eIF) Inhibitors amp Modulators

Bioactivity 4E1RCat is an inhibitor of cap-dependent translation andinhibits interaction with an an of 4 μMeIF4EeIF4GI IC50

Bioactivity 4E2RCat is an inhibitor of interaction with an eIF4E-eIF4G IC50of 135 μM

Bioactivity 4EGI-1 is an inhibitor of interaction with a eIF4EeIF4G Kdof 25 μM against eIF4E binding

Bioactivity Briciclib is a water soluble derivative of ON 013100 and hasthe potential in targeting for solid cancerseIF4E

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic inhibitor with an of 110initiation factor 4A-3 (eIF4A3) IC50

nM

Bioactivity Episilvestrol is a derivative of silvestrol isolated from thefruits and twigs of and is a specificAglaia silvestris

-targeting translation inhibitor with antitumor activityeIF4A

Bioactivity GCN2iB is an ATP-competitive inhibitor of aserinethreonine-protein kinase general control

with an of 24 nMnonderepressible 2 (GCN2) IC50

Bioactivity SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1and disrupts the eIF4F complex

Bioactivity Silvestrol is a eukaryotic translation initiation factor 4A () inhibitor isolated from the fruits and twigs of eIF4A Aglaia

foveolata

4E1RCat Cat No HY-14427

4E2RCat Cat No HY-100733

4EGI-1 Cat No HY-19831

Briciclib (ON 014185) Cat No HY-16366

CCT020312 Cat No HY-119240

eIF4A3-IN-2 Cat No HY-101785

Episilvestrol Cat No HY-15359

GCN2iB Cat No HY-112654

SBI-0640756 (SBI-756) Cat No HY-19560

Silvestrol ((-)-Silvestrol) Cat No HY-13251

G-quadruplex

G-quadruplexes (G-tetrads or G4-DNA) are nucleic acid sequencesthat are rich in guanine and are capable of forming a four-strandedstructure Four guanine bases can associate through Hoogsteenhydrogen bonding to form a square planar structure called a guaninetetrad and two or more guanine tetrads can stack on top of eachother to form a G-quadruplex The quadruplex structure is furtherstabilized by the presence of a cation especially potassium which sitsin a central channel between each pair of tetradsThey can be formedof DNA RNA LNA and PNA and may be intramolecular bimolecularor tetramolecular Depending on the direction of the strands or partsof a strand that form the tetrads structures may be described as

parallel or antiparallel

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Purity 980Clinical Data No Development ReportedSize 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity 9680Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

G-quadruplex Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity APTO-253 is an inducer of andKruppel-like factor 4 (KLF4)also stabilizes with anti-proliferative activityGquadruplex

Bioactivity Phen-DC3 Trifluoromethanesulfonate is a (G4)G-quadruplexspecific ligand which can inhibit and helicasesFANCJ DinGwith s of 65plusmn6 and 50plusmn10 nM respectivelyIC50

Bioactivity Pyridostatin is a stabilizer with a of 490G-quadruplexe KdnM

Bioactivity Pyridostatin hydrochloride is a stabilizer withG-quadruplexea of 490 nMKd

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

APTO-253 (LOR-253 LT-253) Cat No HY-16291

Phen-DC3 Trifluoromethanesulfonate (Phen-DC3 Triflate) Cat No HY-15594A

Pyridostatin (RR82) Cat No HY-15176

Pyridostatin hydrochloride (RR-82 hydrochloride) Cat No HY-15176A

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

Haspin Kinase

Haspin is a protein kinase that regulates chromosome and spindlefunction during mitosis and meiosis Haspin expression is detected infetal liver skin kidney small intestine and in all proliferating cellsHaspin phosphorylates H3 thr3 (H3T3ph) in human cell lines anddepletion of Haspin by RNA interference reveals that Haspin isrequired for H3 thr3 phosphorylation in mitotic cells Phosphorylationof H3T3ph by Haspin is necessary for chromosomal passengercomplex (CPC) accumulation at centromeres H3T3ph then positionsthe CPC at centromeres to regulate selected targets of Aurora Bduring mitosis

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Purity 9956Clinical Data No Development ReportedSize 5 mg

Purity 9812Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Haspin Kinase Inhibitors amp Modulators

Bioactivity CHR-6494 is a potent inhibitor of inhibiting histonehaspinH3T3 phosphorylation with an of 2 nMIC50

Bioactivity LDN-192960 is a potent ( Haspin Haploid Germ Cell-Specific) inhibitor with an of 0010 microMNuclear Protein Kinase IC50

CHR-6494 Cat No HY-15217

LDN-192960 Cat No HY-13455

HDACHistone deacetylases

HDAC (Histone deacetylases) are a class of enzymes that removeacetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid onahistone allowing the histones to wrap the DNA more tightly This isimportant because DNA is wrapped around histones and DNAexpression is regulated by acetylation and de-acetylation Its action isopposite to that of histone acetyltransferase HDAC proteins are nowalso called lysine deacetylases (KDAC) to describe their functionrather than their target which also includes non-histone proteinsTogether with the acetylpolyamine amidohydrolases and the acetoinutilization proteins the histone deacetylases form an ancient proteinsuperfamily known as the histone deacetylase superfamily

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Purity 9600Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9971 Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9896Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

HDAC Inhibitors amp Modulators

Bioactivity Abexinostat (CRA 024781) is a novel pan- inhibitorHDACmostly targeting HDAC1 with of 7 nMKi

Bioactivity ACY-1083 is a selective and brain-penetrating inhibitorHDAC6with an of 3 nM and is 260-fold more selective for HDAC6IC50than all other classes of HDAC isoforms ACY-1083 effectivelyreverses chemotherapy-induced peripheral neuropathy [1]

Bioactivity ACY-738 is a potent selective and orally-bioavailable HDAC6inhibitor with an of 17 nM ACY-738 also inhibitsIC50HDAC1 HDAC2 and HDAC3 with s of 94 128 and 218 nMIC50

Bioactivity ACY-775 is a potent and selective inhibitor of the of histonedeacetylase 6 ( ) with an of 75nMHDAC6 IC50

Bioactivity ACY-957 is a selective inhibitor of and withHDAC1 HDAC2s of 7 nM 18 nM and 1300 nM against HDAC123IC50

respectively and shows no inhibition on HDAC456789

Bioactivity AES-135 is a potent inhibitor inhibits HDAC HDAC3 HDAC6 with s of 654 190 and 636 nM respectivelyHDAC11 IC50

Anti-tumor activity [1]

Bioactivity Belinostat is a potent inhibitor with an of 27 nMHDAC IC50in HeLa cell extracts

Bioactivity Benzenebutyric acid is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity BG45 is an HDAC class I inhibitor with selectivity for HDAC3(IC50 = 289 nM) It inhibits HDAC1 HDAC2 and HDAC6 withgreatly reduced potency (IC50s = 2 22 and gt20 μMrespectively) IC50 value 289 nM (HDAC3) 2 μM (HDAC1) 22μM (HDAC2) gt20 μM (HDAC6) Target HDAC At concentrationshellip

Bioactivity BML-210 is a novel HDAC inhibitor and its mechanism of actionhas not been characterized IC50 value 5 μM[1] Target HDAC4In vitro Cell cycle analysis indicated that HeLa celltreatment with 20 and 30 μM concentration of BML-210 increasedthe proportion of cells in G0G1 phase and causedhellip

Abexinostat (CRA 024781 PCI-24781) Cat No HY-10990

ACY-1083 Cat No HY-111791

ACY-738 Cat No HY-19327

ACY-775 Cat No HY-19328

ACY-957 Cat No HY-104008

AES-135 Cat No HY-114483

Belinostat (PXD101 PX105684) Cat No HY-10225

Benzenebutyric acid (4-Phenylbutyric acid) Cat No HY-A0281

BG45 Cat No HY-18712

BML-210 Cat No HY-19350

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9875Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9906Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BRD 4354 is a moderately potent inhibitor of andHDAC5 with of 085 and 188 μM respectivelyHDAC9 IC s50

Bioactivity BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitorof and with of 085 and 188 μMHDAC5 HDAC9 IC s50

respectively [1]

Bioactivity BRD73954 ia a potent and selective HDAC inhibitor with IC50 of36 nM and 120 nM for HDAC6 and HDAC8 respectively

Bioactivity Bufexamac is a class IIB histone deacetylases (HDAC6 andHDAC10) inhibitor used as an anti-inflammatory agent

Bioactivity CAY10603 (BML-281) is a potent and selective inhibitorHDAC6with an of 2 pM CAY10603 (BML-281) also inhibits HDAC1IC50HDAC2 HDAC3 HDAC8 HDAC10 with s of 271 252 042IC506851 907 nM

Bioactivity CHDI-390576 a potent cell permeable and CNS penetrant class inhibitor with s of 54 nMIIa histonedeacetylase (HDAC) IC50

60 nM 31 nM 50 nM for class IIa HDAC4 HDAC5 HDAC7 HDAC9respectively shows gt500-fold selectivity over class IHDACs (1 2 3) and ~150-fold selectivity over HDAC8 and thehellip

Bioactivity Citarinostat is a HDAC6 specific inhibitor with IC50 of 4 nMand 76 nM for HDAC6 and HDAC3 respectively IC50 value 4 nM(HDAC6) 76 nM (HDAC3) Target HDAC The detailed informationplease refer to WO2015061684A1 and 2015054197A1

Bioactivity CM-675 is a dual and phosphodiesterase 5 (PDE5) class I histone-selective inhibitor with values of 114 nMdeacetylases IC50

and 673 nM for PDE5 and HDAC1 respectively CM-675 haspotential to treat Alzheimerrsquos disease [1]

Bioactivity Corin is a dual inhibitor of histone lysine specificdemethylase and histone deacetylase with a(LSD1) (HDAC)

of 110 nM for LSD1 and an IC of 147 nM forK (inact)i 50HDAC1

Bioactivity CRA-026440 is a potent broad-spectrum inhibitor The HDAC Kivalues against recombinant HDAC isoenzymes HDAC1 HDAC2

and are 4 14 11 15 7 andHDAC3 HDAC6 HDAC8 HDAC1020 nM respectively

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BRD 4354 Cat No HY-112719

BRD 4354 ditrifluoroacetate Cat No HY-112719B

BRD73954 Cat No HY-18700

Bufexamac (Bufexamic acid) Cat No HY-B0494

CAY10603 (BML-281) Cat No HY-18613

CHDI-390576 Cat No HY-119939

Citarinostat (ACY241) Cat No HY-15994

CM-675 Cat No HY-114303

Corin Cat No HY-111048

CRA-026440 Cat No HY-19754

wwwMedChemExpresscom 69

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in Ethanol

2 mg 5 mg 10 mg 50 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9809Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9959Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity CUDC-101 is a potent inhibitor of and withHDAC EGFR HER2s of 44 24 and 157 nM respectivelyIC50

Bioactivity Dacinostat is a potent inhibitor with an of 32 nMHDAC IC50Dacinostat also inhibits with an of 9 nM and usedHDAC1 IC50in cancer research

Bioactivity Domatinostat (4SC-202 free base) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Domatinostat tosylate (4SC-202) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Droxinostat(NS41080) is a selective inhibitor of HDAC3 HDAC6and HDAC8 with IC50 of 169 247 and 146 μM respectivelygt 8-fold selective against HDAC3 and no inhibition toHDAC1 2 4 5 7 9 and 10 IC50 Value 169 μM(HDAC3) 247μM(HDAC6) 146 μM(HDAC8) Target HDAC368 in vitrohellip

Bioactivity EDO-S101 is a pan inhibitor inhibits HDAC1 HDAC2 andHDACHDAC3 with values of 9 9 and 25 nM respectivelyIC50

Bioactivity Entinostat is an oral and selective class I inhibitorHDACwith s of 243 nM 453 nM and 248 nM for IC50 HDAC1 HDAC2

and respectivelyHDAC3

Bioactivity Fimepinostat (CUDC-907) potently inhibits class I s as wellPI3Kas classes I and II enzymes with an of 195439 nMHDAC IC50and 17501828 nM for PI3KαPI3KβPI3Kδ andHDAC1HDAC2HDAC3HDAC10 respectively

Bioactivity FT895 is a potent and selective inhibitor with an HDAC11 IC50

of 3 nM [1]

Bioactivity Givinostat (ITF-2357) is a inhibitor with an of 198HDAC IC50and 157 nM for and respectivelyHDAC1 HDAC3

CUDC-101 Cat No HY-10223

Dacinostat (NVP-LAQ824 LAQ824) Cat No HY-13606

Domatinostat (4SC-202 (free base)) Cat No HY-16012A

Domatinostat tosylate (4SC-202) Cat No HY-16012

Droxinostat (NS 41080) Cat No HY-13267

EDO-S101 (Tinostamustine) Cat No HY-101780

Entinostat (MS-275 SNDX-275) Cat No HY-12163

Fimepinostat (CUDC-907) Cat No HY-13522

FT895 Cat No HY-112285

Givinostat (ITF-2357) Cat No HY-14842

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9849Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9609Clinical Data LaunchedSize 2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Bioactivity Givinostat hydrochloride (ITF-2357 hydrochloride) is a HDACinhibitor with an of 198 and 157 nM for andIC50 HDAC1

respectivelyHDAC3

Bioactivity Givinostat hydrochloride monohydrate (ITF-2357 hydrochloridemonohydrate) is a inhibitor with an of 198 and 157HDAC IC50nM for and respectivelyHDAC1 HDAC3

Bioactivity HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2008040934 A1

Bioactivity HDAC-IN-4 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2007045844 A1 20070426

Bioactivity HDAC-IN-5 is a histone deacetylase inhibitor(HDAC) Bioactivity HDAC-IN-7 (Chidamide impurity) is an impurity of ChidamideChidamide is a potent and orally bioavailable HDAC enzymesclass I (HDAC123) and class IIb (HDAC10) inhibitor

Bioactivity HDAC6-IN-1 is a potent and selective inhibitor for withHDAC6an of 17 nM and shows 25-fold and 200-fold selectivityIC50relative to ( =422 nM) and ( =3398 nM)HDAC1 IC50 HDAC8 IC50respectively

Bioactivity HDAC8-IN-1 is a inhibitor with an of 272 nMHDAC8 IC50

Bioactivity HDACsmTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs)and targetmammalian target of Rapamycin (mTOR)inhibitor for treating hematologic malignancies with ofIC s50019 nM 18 nM 12 nM and gt500 nM for HDAC1 HDAC6 mTORand PI3Kα respectively HDACsmTOR Inhibitor 1 stimulateshellip

Bioactivity HPOB is a highly potent and selective inhibitor of histonedeacetylase 6 (HDAC6) with IC50 of 56 nM gt30 fold lesspotent against other HDACs target HDAC6 [1] IC 50 56nM [1]In vitro HPOB causes growth inhibition of normal andtransformed cells but does not induce cell death HPOBhellip

70 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Givinostat hydrochloride (ITF-2357 hydrochloride) Cat No HY-14842A

Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) Cat No HY-14842B

HDAC-IN-3 Cat No HY-19772

HDAC-IN-4 (CXD101) Cat No HY-100748

HDAC-IN-5 Cat No HY-18362

HDAC-IN-7 (Chidamide impurity) Cat No HY-13592

HDAC6-IN-1 Cat No HY-18947

HDAC8-IN-1 Cat No HY-111342

HDACsmTOR Inhibitor 1 Cat No HY-114414

HPOB Cat No HY-19747

wwwMedChemExpresscom 71

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg 100 mg

Bioactivity IDO1 and HDAC1 Inhibitor (Compound 10) is a dual andIDO1 inhibitor with s of 690 nM and 665 nMHDAC1 IC50

respectively [1]

Bioactivity ITSA-1 is membrane permeable and specifically suppresses TSAinhibition of HDAC (histone deacetylase) but not other HDACinhibitors

Bioactivity J22352 is a PROTAC (proteolysis-targeting chimeras)-like andhighly selective inhibitor with an value of 47HDAC6 IC50nM J22352 promotes HDAC6 degradation and induces anticancereffects by inhibiting autophagy and eliciting the antitumorimmune response in glioblastoma cancers and leading to thehellip

Bioactivity JAKHDAC-IN-1 is a potent dual inhibitor exhibitsJAK2HDACantiproliferative and proapoptotic activities in severalhematological cell lines JAKHDAC-IN-1 shows s of 4 and 2IC50

nM for JAK2 and HDAC respectively [1]

Bioactivity LMK-235 is a potent and selective inhibitor inhibitsHDAC45HDAC5 HDAC4 HDAC6 HDAC1 HDAC2 HDAC11 and HDAC8 with

s of 422 nM 119 nM 557 nM 320 nM 881 nM 852 nM andIC501278 nM respectively and is used in cancer research

Bioactivity M344 (D 237) is an inhibitor of ( =100histone deacetylase IC50nM) and an inducer of terminal cell fifferentiation

Bioactivity MC1568 is a selective class II (IIa) histone deacetylas () inhibitor used for cancer researchHDAC II

Bioactivity Mocetinostat (MGCD0103) is a potent orally active andisotype-selective inhibitor with s ofHDAC (Class IIV) IC50015 029 166 and 059 μM for andHDAC1 HDAC2 HDAC3

respectively Mocetinostat shows no inhibition onHDAC11HDAC4 HDAC5 HDAC6 HDAC7 or HDAC8

Bioactivity Nanatinostat (CHR-3996) is a potent class I selective andorally active inhibitor with anhistone deacetylase (HDAC)

of 8 nM IC50[1]

Bioactivity Nexturastat A is a potent and selective HDAC6 inhibitor withIC50 of 5 nM no inhibition on other HDAC forms

IDO1 and HDAC1 Inhibitor Cat No HY-112147

ITSA-1 Cat No HY-100508

J22352 Cat No HY-126147

JAKHDAC-IN-1 Cat No HY-126141

LMK-235 Cat No HY-18998

M344 (D 237 MS 344) Cat No HY-13506

MC1568 Cat No HY-16914

Mocetinostat (MGCD0103) Cat No HY-12164

Nanatinostat (CHR-3996) Cat No HY-13432

Nexturastat A Cat No HY-16699

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9907Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9867Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9797Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NKL 22 is a HDAC inhibitor The value of IC 50 is 78 uM NKL 22increase frataxin protein concentrations NKL 22 inhibitorsincrease FXN mRNA in FRDA lymphocytes HDAC inhibitors actdirectly on FXN [1]

Bioactivity Oxamflatin (Metacept-3) is a potent inhibitor with anHDAC of 157 nMIC50

Bioactivity Panobinostat is a non-selective histone deacetylase ( )HDACinhibitor

Bioactivity PCI-34051 is a potent and selective inhibitor with HDAC8 IC50of 10 nM with gt200-fold selectivity over the other HDACisoforms

Bioactivity PI3KHDAC-IN-1 is a potent dual inhibitor of PI3KHDACpotently inhibits PI3Kδ and HDAC1 with s of 81 nM and 14IC50

nM respectively [1]

Bioactivity Pimelic diphenylamide 106 is a slow tight-binding inhibitorof class I HDAC (HDAC 1 2 and 3 with IC50 values of 150 nM 760nM and 370 nM respectively) demonstrating no activityagainst class II HDACs

Bioactivity Pracinostat is a potent inhibitorhistone deacetylase (HDAC)with s of 40-140 nM used for cancer researchIC50

Bioactivity PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDACPTACH exerts potent growth inhibition against various humancancer cells with EC50 values ranging from 1 to 10 μM

Bioactivity Quisinostat (JNJ-26481585) is an orally available potent inhibitor with an of 011 nM for HDAC1HDAC IC50

Bioactivity Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of which is under developmenthistone deacetylase enzymes (HDAC)

for the treatment of cutaneous T-cell lymphoma [1]

72 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NKL 22 Cat No HY-100384

Oxamflatin (Metacept-3) Cat No HY-102033

Panobinostat (LBH589 NVP-LBH589) Cat No HY-10224

PCI-34051 Cat No HY-15224

PI3KHDAC-IN-1 Cat No HY-128582

Pimelic Diphenylamide 106 (RGFA-8 TC-H 106 Histone Deacetylase Inhibitor VII) Cat No HY-19348

Pracinostat (SB939) Cat No HY-13322

PTACH (NCH-51) Cat No HY-12954

Quisinostat (JNJ-26481585) Cat No HY-15433

Remetinostat (SHP-141) Cat No HY-100365

wwwMedChemExpresscom 73

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9970Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Bioactivity Resminostat is a potent inhibitor of andHDAC1 HDAC3 with mean values of 425 501 718 nMHDAC6 IC50

respectively and shows less potent activities against HDAC8with an of 877 nMIC50

Bioactivity Resminostat hydrochloride is a potent inhibitor of HDAC1 and with mean values of 425 501 718HDAC3 HDAC6 IC50

nM respectively and shows less potent activities againstHDAC8 with an of 877 nMIC50

Bioactivity RG2833 is a brain-penetrant inhibitor with of 60 nMHDAC IC50and 50 nM for HDAC1 and HDAC3 respectively

Bioactivity RGFP966 is a highly selective inhibitor with an ofHDAC3 IC5080 nM and shows no inhibition to other HDACs at concentrationsup to 15 μM

Bioactivity Ricolinostat (ACY-1215) is a potent and selective HDAC6inhibitor with an of 5 nM ACY-1215 also inhibitsIC50

and with s of 58 48 and 51 nMHDAC1 HDAC2 HDAC3 IC50respectively

Bioactivity Romidepsin is a potent and inhibitor with sHDAC1 HDAC2 IC50of 36 and 47 nM respectively

Bioactivity RTS-V5 is a dual inhibitor with s ofHDACproteasome IC5069 18 15 027 053 μM for HDAC1 HDAC2 HDAC3 HDAC6HDAC8 respectively

Bioactivity Santacruzamate A (CAY-10683) is a potent and selective HDAC2inhibitor with an of 119 pM IC50

[1]

Bioactivity Scriptaid is a potent inhibitorhistone deacetylase (HDAC)used in cancer research

Bioactivity Sinapinic acid (Sinapic acid) is a phenolic compound isolatedfrom Jack Rhizome acts as anHydnophytum formicaruminhibitor of with an of 227 mM and alsoHDAC IC50

[1]

inhibits activity Sinapinic acid posssess pothellipACE-I [2]

Resminostat (RAS2410 4SC-201) Cat No HY-14718

Resminostat hydrochloride (RAS2410 hydrochloride 4SC-201 hydrochloride) Cat No HY-14718A

RG2833 (RGFP109) Cat No HY-16425

RGFP966 Cat No HY-13909

Ricolinostat (ACY-1215 Rocilinostat) Cat No HY-16026

Romidepsin (FK 228 FR 901228 NSC 630176) Cat No HY-15149

RTS-V5 Cat No HY-112908

Santacruzamate A (CAY-10683) Cat No HY-N0931

Scriptaid (Scriptide GCK1026) Cat No HY-15489

Sinapinic acid (Sinapic acid) Cat No HY-W009732

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg

Purity 9800Clinical Data Phase 3Size 10mM x 1mL in Water

1 g 5 g 500 g

Bioactivity Butyric acid is a inhibitor withhistone deacetylase (HDAC)anti-tumor effects in several cancers

Bioactivity Sodium phenylbutyrate is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity SR-4370 is an inhibitor of with s of 013 μM 058HDAC IC50μM 0006 μM 23 μM and 34 μM for HDAC1 HDAC2 HDAC3HDAC8 and HDAC6 respectively

Bioactivity ST8154AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity ST8155AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity Sulforaphane is an isothiocyanate present naturally in widelyconsumed vegetables has shown anticancer and cardioprotectiveactivities

Bioactivity SW-100 a selective inhibitorhistone deacetylase 6 (HDAC6)with an of 23 nM shows at least 1000-fold selectivityIC50for HDAC6 relative to all other HDAC isozymes SW-100 displaysa significantly improved ability to cross hellip

Bioactivity Tacedinaline (N-acetyldinaline) is an inhibitor of the histonedeacetylase ( ) with s of 09 09 12 μM forHDAC IC50recombinant HDAC 1 2 and 3 respectively

Bioactivity Tasquinimod is an oral antiangiogenic agent in clinical trialsfor the treatment of castration-resistant prostate cancerTasquinimod binds to the regulatory Zn binding domain of2+

with of 10-30 nMHDAC4 Kd

Bioactivity TH34 an inhibitor with s of 46 μM 19HDAC6 8 10 IC50μM and 77 μM respectively shows high selectivity overHDAC123 [1]

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Sodium Butyrate (Butanoic acid sodium salt) Cat No HY-B0350A

Sodium phenylbutyrate (Sodium 4-phenylbutyrate TriButyrate) Cat No HY-15654

SR-4370 Cat No HY-111400

ST8154AA1 Cat No HY-112805

ST8155AA1 Cat No HY-112806

Sulforaphane Cat No HY-13755

SW-100 Cat No HY-115475

Tacedinaline (N-acetyldinaline CI-994 Goe-5549) Cat No HY-50934

Tasquinimod (ABR-215050) Cat No HY-10528

TH34 Cat No HY-111818

wwwMedChemExpresscom 75

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g 25 g

Purity 9867Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g 25 g

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9887Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TMP195 is a selective class IIa histone deacetylase ( )HDACinhibitor with s of 59 60 26 15 nM for HDAC4 HDAC5KiHDAC7 and HDAC9 respectively

Bioactivity TMP269 is a novel and selective class IIa histone deacetylase inhibitor with s of 157 nM 97 nM 43 nM and 23 nM(HDAC) IC50

for HDAC4 HDAC5 HDAC7 and HDAC9 respectively

Bioactivity Trichostatin A is a potent and specific inhibitor of HDAC with an value of 18 nM for HDACclass III IC50

Bioactivity Tubacin is a potent and selective inhibitor of with anHDAC6 value of 4 nM and approximately 350-fold selectivity overIC50

HDAC1

Bioactivity Tubastatin A (Hydrochloride) is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tubastatin-A is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tucidinostat is a potent and orally bioavailable enzymesHDACclass I ( ) and class IIb ( ) inhibitor withHDAC123 HDAC10

s of 95 160 67 and 78 nM less active on HDAC8 andIC50HDAC11 ( s 733 nM 432 nM respectively) and showshellipIC50

Bioactivity UF010 is a potent and selective HDAC inhibitor with IC50 ~006μM 01 μM 05 μM and 15 μM for HDACs 3 2 1 and 8respectively It has gt 6-fold selectivity over other HDACsIC50 value 006 μM (HDAC3) 01 μM (HDAC2) 05 μM (HDAC1)15 μM(HDAC 8) Target HDAC in vitro UF010 is a competitivehellip

Bioactivity Valproic acid is an inhibitor with in the range ofHDAC IC5005 and 2 mM also inhibits ( 400 μM) andHDAC1 IC50induces proteasomal degradation of Valproic acidHDAC2sodium salt is used in the treatment of epilepsy bipohellip

Bioactivity Valproic acid sodium salt is an anticonvulsants used to treatepilepsy bipolar disorder and migraines Valproic acidinhibits with an of 04 mMhistone deacetylase 1 (HDAC1) IC50

TMP195 Cat No HY-18361

TMP269 Cat No HY-18360

Trichostatin A (TSA) Cat No HY-15144

Tubacin Cat No HY-13428

Tubastatin A Hydrochloride (Tubastatin A HCl TSA HCl) Cat No HY-13271

Tubastatin-A Cat No HY-13271A

Tucidinostat (Chidamide HBI-8000 CS 055) Cat No HY-109015

UF010 Cat No HY-18976

Valproic acid (VPA 2-Propylpentanoic Acid) Cat No HY-10585

Valproic acid sodium salt (Sodium Valproate) Cat No HY-10585A

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

250 mg 500 mg 1 g 5 g

Bioactivity Vorinostat is a potent and orally available inhibitor of and andHDAC1 HDAC2 HDAC3 (Class I) HDAC7 (Class II)

with values of 10 nM and 20 nM forHDAC11 (Class IV ) ID50HDAC1 and HDAC3 respectively

Bioactivity WT-161 is a potent and selective inhibitor with an HDAC6 IC50of 040 nM

76 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Vorinostat (SAHA) Cat No HY-10221

WT-161 Cat No HY-100871

wwwMedChemExpresscom 77

HSPHeat shock proteins

HSP (Heat shock proteins) are a group of proteins induced by heatshock the most prominent members of this group are a class offunctionally related proteins involved in the folding and unfolding ofother proteins HSP expression is increased when cells are exposed toelevated temperatures or other stress This increase in expression istranscriptionally regulated The dramatic upregulation of the heatshock proteins is a key part of the heat shock response and is inducedprimarily by heat shock factor (HSF) HSPs are found in virtually allliving organisms from bacteria to humans Heat shock proteinsappear to serve a significant cardiovascular role Hsp90 Hsp84Hsp70 Hsp27 Hsp20 and alpha B crystallin all have been reported as

having roles in the cardiovasculature

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 g

Purity 9997Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9932Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 1 mg

HSP Inhibitors amp Modulators

Bioactivity Alvespimycin is a potent inhibitor of binding to Hsp90Hsp90with an of 62 plusmn 29 nMEC50

Bioactivity Alvespimycin hydrochloride is a potent inhibitor of Hsp90binding to Hsp90 with of 62plusmn29 nMEC50

Bioactivity Apoptozole is an inhibitor of the ATPase domain of andHsc70 with s of 021 and 014 μM respectively and canHsp70 Kd

induce apoptosis

Bioactivity Arimoclomol maleate (BRX-220) is a co-inducer of heat shockproteins ( )HSP

Bioactivity BIIB021 is an orally available fully synthetic inhibitor of with and of 17 nM and 38 nM respectivelyHSP90 Ki EC50

Bioactivity Bimoclomol is a coinducer used forheat shock protein (HSP)treatment of cardiovascular diseases

Bioactivity CCT251236 is an orally available pirin ligand from a heatshock transcription factor 1 (hsf1) phenotypic screen with an

of 19 nM for inhibition of HSF1-mediated IC50 HSP72

induction

Bioactivity Col003 is a potent inhibitor of competitively binds toHsp47the collagen binding site on Hsp47 ( 18 μM) andIC50inhibits collagen secretion by destabilizing the collagentriple helix [1]

Bioactivity Debio 0932 is an orally active inhibitor with s ofHSP90 IC50100 and 103 nM for HSP90α and HSP90β respectively

Bioactivity Ethoxyquin is an antioxidant which has been used in animalfeed for many years and also an inhibitor of heat shock

( )protein 90 Hsp90

78 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Alvespimycin (17-DMAG NSC 707545) Cat No HY-10389

Alvespimycin hydrochloride (17-DMAG hydrochloride KOS-1022 BMS 826476) Cat No HY-12024

Apoptozole (Apoptosis Activator VII) Cat No HY-15098

Arimoclomol maleate (BRX-220) Cat No HY-106443A

BIIB021 (CNF2024) Cat No HY-10212

Bimoclomol Cat No HY-U00398

CCT251236 Cat No HY-101026

Col003 Cat No HY-124817

Debio 0932 (CUDC-305) Cat No HY-13469

Ethoxyquin Cat No HY-B1425

wwwMedChemExpresscom 79

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9994Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Bioactivity Feretoside a phenolic compound extracted from the barks of E is a which act as cytoprotectiveulmoides HSP inducer

agent

Bioactivity Ganetespib is a heat shock protein 90 ( ) inhibitorHSP90which exhibits potent cytotoxicity in a wide variety ofhematological and solid tumor cell lines

Bioactivity Geldanamycin is a inhibitor with antimicrobial activityHsp90against many Gram-positive and some Gram-negative bacteria

Bioactivity Grp94 Inhibitor-1 is a potent selective inhibitor withGrp94an value of 2 nM and over 1000-fold selectivity to Grp94IC50

against Hsp90α [1]

Bioactivity HA15 a molecule that targets specifically BiP GRP78 HSPA5inhibits the ATPase activity of BiP HA15 strongly increasesBiP protein expression in A375 melanoma cells [1]

Bioactivity HSF1A is a cell-permeable activator of heat shocktranscription factor 1 ( )HSF1

Bioactivity HSP70-IN-1 is a heat shock protein ( ) inhibitor inhibitsHSPthe growth of Kasumi-1 cells with an of 23 μMIC50

Bioactivity JG-98 is an allosteric heat shock protein 70 (Hsp70)inhibitor with anti-cancer activities which disrupts Hsp70

and affects signalinginteraction with a co-chaperone Bag3pathways important for cancer development [1] [2] [3]

Bioactivity KNK437 is a inhibitor and inhibits the induction ofHSPHSP105 HSP70 and HSP40

Bioactivity KRIBB11 is an inhibitor of withHeat shock factor 1 (HSF1) of 12 μMIC50

Feretoside Cat No HY-N6249

Ganetespib (STA-9090) Cat No HY-15205

Geldanamycin Cat No HY-15230

Grp94 Inhibitor-1 Cat No HY-112910

HA15 Cat No HY-100437

HSF1A Cat No HY-103000

HSP70-IN-1 Cat No HY-12622

JG-98 Cat No HY-117282

KNK437 (Heat Shock Protein Inhibitor I) Cat No HY-100110

KRIBB11 Cat No HY-100872

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 100 mg

Purity 9569Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9914Clinical Data Phase 2Size 5 mg 10 mg 25 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity KU-32 is a novel novobiocin-based inhibitor that canHsp90protect against neuronal cell death

Bioactivity KW-2478 is an inhibitor of with an of 38 nMHsp90α IC50and has antitumor activity against various human hematologicaltumor cells

Bioactivity Luminespib (NVP-AUY922) is a potent inhibitor withHSP90s of 78 and 21 nM for HSP90α and HSP90β respectivelyIC50

Bioactivity MKT-077 is a rhodacyanine dye and also a heat shock protein 70( ) inhibitor which exhibits significant antitumorHsp70activity

Bioactivity NVP-HSP990 is a potent and selective inhibitor withHsp90 values of 06 08 and 85 nM for Hsp90α Hsp90β andIC50

Grp94 respectively

Bioactivity Onalespib (AT13387) is a potent inhibitor of with aHsp90 of 071 nMKd

Bioactivity p5 Ligand for Dnak and DnaJ is a nonapeptide whichcorresponds to the main binding site for the 23-residue partof the presequence of mitochondrial aspartateaminotransferase p5 Ligand for Dnak and DnaJ is ahigh-affinity ligand for DnaK and DnaJ [1]

Bioactivity Pifithrin-μ is an inhibitor of and with antitumorp53 HSP70and neuroprotective activity

Bioactivity PU-WS13 is a selective inhibitor with an ofGrp94 EC50022 μM

Bioactivity Retaspimycin is a potent and water-soluble inhibitor of with s of 119 nM for both Hsp90 and Grp9Hsp90 EC50

80 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

KU-32 Cat No HY-108248

KW-2478 Cat No HY-13468

Luminespib (NVP-AUY922 AUY922 VER-52296) Cat No HY-10215

MKT-077 (FJ-776) Cat No HY-15096

NVP-HSP990 (HSP-990) Cat No HY-15190

Onalespib (AT13387) Cat No HY-14463

p5 Ligand for Dnak and DnaJ Cat No HY-P1887

Pifithrin-μ (PFTμ 2-Phenylethynesulfonamide) Cat No HY-10940

PU-WS13 Cat No HY-18680

Retaspimycin Cat No HY-15263

wwwMedChemExpresscom 81

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9740Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9982Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9903Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Retaspimycin Hydrochloride is a potent and water-solubleinhibitor of with s of 119 nM for both Hsp90 andHsp90 EC50Grp9

Bioactivity Shepherdin (79-87) is amino acids 79 to 87 fragment ofShepherdin Shepherdin is a peptidomimetic antagonist of thecomplex between Hsp90 and Survivin Anticancer activity [1]

Bioactivity SNX-5422 Mesylate (PF-04929113 Mesylate) a prodrug ofSNX-2112 is an orally active inhibitor with a ofHsp90 Kd41 nM and also induces Her-2 degradation with an ofIC5037nM

Bioactivity Tanespimycin (17-AAG) is a potent inhibitor with anHSP90 of 5 nM having a 100-fold higher binding affinity forIC50

tumour cell derived HSP90 than normal cell derived HSP90

Bioactivity TAS-116 is an oral bioavailable ATP-competitive highlyspecific inhibitor ( s of 347 nM and 213HSP90αHSP90β KinM respectively) without inhibiting other HSP90 familyproteins such as GRP94 TAS-116 demonstrates less ocuhellip[1]

Bioactivity Teprenone is a anti-ulcer drug and works as an inducer ofheat shock proteins ( )HSPs

Bioactivity TRC051384 is a heat shock protein 70 ( ) inducerHSP70 Bioactivity VER-155008 is an inhibitor of with s of 05 μMHsp70 IC5026 μM and 26 μM for Hsc70 and Grp7 respectivelyHsp70and with a of 03 μM for Kd Hsp70

Bioactivity VER-49009 is a inhibitor with an of 25 nM and aHsp90 IC50 of 78 nMKd

Bioactivity VER-50589 is a inhibitor with an of 21 nM and aHsp90 IC50 of 45 nMKd

Retaspimycin Hydrochloride (IPI-504) Cat No HY-10210

Shepherdin 79-87 Cat No HY-P1750

SNX-5422 Mesylate (PF-04929113 (Mesylate)) Cat No HY-10213A

Tanespimycin (17-AAG NSC 330507 CP 127374) Cat No HY-10211

TAS-116 Cat No HY-15785

Teprenone (Geranylgeranylacetone) Cat No HY-B0779

TRC051384 Cat No HY-101712

VER-155008 Cat No HY-10941

VER-49009 (CCT 129397) Cat No HY-15986

VER-50589 Cat No HY-15984

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9924Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity VER-82576 (NVP-BEP800) is a potent orally available andselective inhibitor with an of 58 nM for Hsp90βHsp90 IC50VER-82576 also slightly blocks Grp94 and Trap-1 with s ofIC5041 and 55 μM respectively

Bioactivity XL888 is a heat shock protein-90 ( ) inhibitor with anHSP90 of 24 nMIC50

Bioactivity YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathwayagainst glioblastoma directly binding to heat shock protein

with an of 820 nM on NFAT nuclear90 (HSP90) IC50translocation YZ129-induced GBM cell-cycle arrest at the G2Mphase promotes apoptosis and inhibited tumor cellhellip

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VER-82576 (NVP-BEP800) Cat No HY-10942

XL888 Cat No HY-13313

YZ129 Cat No HY-114413

wwwMedChemExpresscom 83

IRE1Inositol requiring enzyme 1

The serinethreonine-protein kinaseendoribonucleaseinositol-requiring enzyme 1 (IRE1) is an enzyme that in humans isencoded by the gene IRE1 is an endoplasmic reticulum (ER)ERN1transmembrane sensor that activates UPR to maintain ER and cellularfunction While mammalian IRE1 promotes cell survive it can initiateapoptosis via decay of anti-apoptotic microRNAsIRE1 activation is initiated by homotypic interactions of thestress-sensing lumenal domain favoring transautophosphorylation ofthe kinase-extension nuclease (KEN) domain on the cytoplasmic sideof the ER membraneIRE1XBP-1 has been shown to regulate a variety of genes in various

cell types in response to ER stress mostly related to ER function and the secretory pathway although the target genesvary depending on the cell type and nature of the stress stimuli

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9875Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg

IRE1 Inhibitors amp Modulators

Bioactivity 36-DMAD hydrochloride is a inhibitor of the pathwayIRE1α-XBP1of the unfolded protein response

Bioactivity 4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor ofIRE1α

Bioactivity 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1αinhibitor with an of 008 μM extracted from patent WOIC502008154484 A1 IRE-lα inhibitor compound 3-5

Bioactivity APY29 is an allosteric modulator of which inhibits IRE1αIRE1αautophosphorylation with of 280 nM and activates IRE1αIC50RNase activity

Bioactivity B I09 is an RNase inhibitor with an of 1230 nMIRE-1 IC50 Bioactivity GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1alpha ( ) which can inhibit and IRE1α IRE1α kinase activity RNase

with s of 20 and 200 nM respectivelyactivity IC50

Bioactivity GSK2850163 hydrochloride is a novel inhibitor ofinositol-requiring enzyme-1 alpha ( ) which can inhibitIRE1α

and with s of 20 andIRE1α kinase activity RNase activity IC50200 nM respectively

Bioactivity KIRA6 allosterically inhibits activity withIRE1α RNase kinasean of 06 microMIC50

Bioactivity Kira8 is a mono-selective inhibitor that allostericallyIRE1αattenuates with an of 59 nM IRE1α RNase activity IC50

[1]Bioactivity MKC3946 is a potent and soluble inhibitor used forIRE1α

cancer research

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36-DMAD hydrochloride Cat No HY-U00460

4μ8C (IRE1 Inhibitor III) Cat No HY-19707

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) Cat No HY-107371

APY29 Cat No HY-17537

B I09 Cat No HY-107400

GSK2850163 Cat No HY-U00459

GSK2850163 hydrochloride Cat No HY-U00459B

KIRA6 Cat No HY-19708

Kira8 Cat No HY-114368

MKC3946 Cat No HY-19710

wwwMedChemExpresscom 85

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity MKC8866 is an inhibitor with an of less thanIRE1 RNase IC5001 μM for IRE1α RNase

Bioactivity MKC9989 is a ( ) inhibitor and alsoHydroxy aryl aldehydes HAAinhibits with an of 023 to 44 μMIRE1α IC50

Bioactivity STF-083010 is an inhibitor STF-083010 inhibits Ire1Ire1endonuclease activity without affecting its kinase activityafter endoplasmic reticulum stress

MKC8866 Cat No HY-104040

MKC9989 Cat No HY-12399

STF-083010 Cat No HY-15845

Kinesin

Kinesin is a protein belonging to a class of motor proteins found ineukaryotic cells Kinesins move along microtubule filaments and arepowered by the hydrolysis of ATP (thus kinesins are ATPases) Theactive movement of kinesins supports several cellular functionsincluding mitosis meiosis and transport of cellular cargo Mostkinesins walk towards the plus end of a microtubule entailstransporting cargo from the centre of the cell towards the peripheryKinesins were discovered as microtubule (MT)-based anterogradeintracellular transport motors The founding member of thissuperfamily the genomes of mammals encode more than 40 kinesinproteins organized into at least 14 families named kinesin-1 through

kinesin-14

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wwwMedChemExpresscom 87

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9871Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9973Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Kinesin Inhibitors amp Modulators

Bioactivity (R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of ARRY-520(R)-Filanesib ((R)-ARRY-520) is a synthetic kinesin spindle

inhibitor with of 6 nMprotein (KSP) IC50

Bioactivity AZ82 is a selective kinesin-like protein KIFC1 (HSETKIFC1)inhibitor with a of 43 nM and an of 300 nM for KIFC1Ki IC50

Bioactivity CW-069 is an allosteric inhibitor of microtubule motor with an of 75 μMprotein HSET IC50

Bioactivity Dimethylenastron is a potent inhibitor with ankinesin Eg5 of 200 nMIC50

Bioactivity Eg5 Inhibitor V trans-24 is a potent and specific kinesin Eg5inhibitor with an of 065 μM and can be used in theIC50research of cancer

Bioactivity EMD534085 is a potent and selective inhibitor of the mitotic with an of 8 nMkinesin-5 IC50

Bioactivity Filanesib (ARRY-520) is a synthetic kinesin spindle protein inhibitor with of 6 nM(KSP) IC50

Bioactivity Ispinesib is a specific inhibitor of kinesin spindle protein with a of 17 nM(KSP) Ki app

Bioactivity K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5with an of 13 μMIC50

Bioactivity Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member and is used for the research of cellular15 (Kif15)

proliferative diseases

(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A

AZ82 Cat No HY-12241

CW-069 Cat No HY-15857

Dimethylenastron Cat No HY-19944

Eg5 Inhibitor V trans-24 Cat No HY-112915

EMD534085 Cat No HY-15000

Filanesib (ARRY-520) Cat No HY-15187

Ispinesib (SB-715992) Cat No HY-50759

K858 Racemic Cat No HY-19966

Kif15-IN-1 Cat No HY-15948

Purity 9731Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9705Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg

Purity 9959Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9651Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Kif15-IN-2 is an inhibitor of the mitotic and iskinesin Kif15used for the research of cellular proliferative diseases

Bioactivity Litronesib is a selective mitosis-specific kinesin Eg5inhibitor with antitumor activity

Bioactivity Litronesib (Racemate) is the racemate of litronesibLitronesib is a selective allosteric inhibitor of kinesin

Eg5

Bioactivity Monastrol is a potent and cell-permeable inhibitor of themitotic with an value of 14 μMkinesin Eg5 IC50

Bioactivity Paprotrain is a cell-permeable inhibitor of the kinesin inhibits the ATPase activity of MKLP-2 with an MKLP-2 IC50

of 135 μM and a of 336 μM and shows a moderate inhibitionKiactivity on with an of 55 μMDYRK1A IC50

Bioactivity PF-2771 is a potent and selective centromere protein E inhibitor inhibiting CENP-E motor activity with an(CENP-E)

of 161 nM PF-2771 is used as an anticancer agentIC50

Bioactivity SB-743921 is a potent inhibitor of the mitotic kinesin KSP with a of 01 nM(Eg5) Ki

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Kif15-IN-2 Cat No HY-15949

Litronesib (LY-2523355 KF-89617) Cat No HY-14846

Litronesib Racemate (LY-2523355 Racemate KF-89617 Racemate) Cat No HY-14846A

Monastrol ((plusmn)-Monastrol) Cat No HY-101071A

Paprotrain Cat No HY-101298

PF-2771 Cat No HY-19530

SB-743921 Cat No HY-12069

wwwMedChemExpresscom 89

LIM Kinase (LIMK)LIMKs

LIM kinases (LIMKs) are important cell cytoskeleton regulators thatplay a prominent role in cancer manifestation and neuronal diseasesThe LIMK family consists of two homologues LIMK1 and LIMK2which differ from one another in expression profile intercellularlocalization and function The main substrate of LIMK is cofilin amember of the actin-depolymerizing factor (ADF) protein familyWhen phosphorylated by LIMK cofilin is inactive LIMKs play acontributory role in several neurodevelopmental disorders and incancer growth and metastasisLIM domain kinases (LIMK1 and 2) are substrate for Cdc42Rac-PAKand modulate actin dynamics by phosphorylating cofilin at serine-3

This modification inactivates cofilinrsquos actin severing and depolymerizing activity LIMKs also translocate into thenucleus and regulate cell cycle progression LIMKs are potential therapeutic targets for NF2 and other merlin-deficienttumors

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

LIM Kinase (LIMK) Inhibitors amp Modulators

Bioactivity BMS-3 is a potent inhibitor with s of 5 nM and 6LIMK IC50nM for and respectivelyLIMK1 LIMK2

Bioactivity BMS-5 (LIMKi 3) is a potent inhibitor with s of 7LIMK IC50nM and 8 nM for and respectivelyLIMK1 LIMK2

Bioactivity R-10015 a broad-spectrum antiviral compound for HIVinfection acts as a potent and selective inhibitor of LIM

and binds to the ATP-binding pocketdomain kinase (LIMK)with an of 38 nM for human LIMK1 IC50

[1]

Bioactivity T56-LIMKi is a selective inhibitor of inhibits theLIMK2growth of Panc-1 cells with an of 352 μMIC50

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BMS-3 Cat No HY-18304

BMS-5 (LIMKi 3) Cat No HY-18305

R-10015 Cat No HY-120097

T56-LIMKi (T5601640) Cat No HY-19352

wwwMedChemExpresscom 91

MicrotubuleTubulin

Microtubules are a component of the cytoskeleton found throughoutthe cytoplasm These tubular polymers of tubulin can grow as long as50 micrometres with an average length of 25 microm and are highlydynamic The outer diameter of a microtubule is about 24 nm whilethe inner diameter is about 12 nm Microtubules are found ineukaryotic cells and are formed by the polymerization of a dimer oftwo globular proteins alpha and beta tubulin Tubulin is one ofseveral members of a small family of globular proteins The tubulinsuperfamily includes five distinct families the alpha- beta- gamma-delta- and epsilon-tubulins and a sixth family which is present only inkinetoplastid protozoa The most common members of the tubulin

family are α-tubulin and β-tubulin the proteins that make up microtubules Microtubules are very important in anumber of cellular processes They are involved in maintaining the structure of the cell

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9987Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9920Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9982Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

MicrotubuleTubulin Inhibitors amp Modulators

Bioactivity 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivativewith improved pharmacological features and higher watersolubility IC50 value Target Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cyclearrest and apoptosis as measured by flow cytometry DNAhellip

Bioactivity 10-Oxo Docetaxel (Docetaxel Impurity) is a novel taxoid havingremarkable anti-tumor properties and a Docetaxel intermediate

Bioactivity 2-Methoxyestradiol is an inhibitor and angiogenesis apoptosisinducer with potent antineoplastic activity2-Methoxyestradiol also destablize microtubules

Bioactivity 4-Demethylepipodophyllotoxin(4-DMEP) is a key intermediatecompound for the preparation of podophyllotoxin-typeanti-cancer drugs a potent inhibitor of microtubule assembly

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity ofdocetaxel detected by high performance liquid chromatography(HPLC)

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity C 7-Epitaxotere)is a impurity of docetaxel

Bioactivity 7-epi-Taxol is an active metabolite of taxol with activitycomparable to that of taxol against cell replicationpromoting bundle formation and againstmicrotubulemicrotubule depolymerization

Bioactivity 7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel)derivative Paclitaxel binds to tubulin and inhibits thedisassembly of microtubules

Bioactivity ABT-751(E 7010) is a novel bioavailable tubulin-binding andantimitotic sulfonamide agent with IC50 of about 15 and 34μM in neuroblastoma and non-neuroblastoma cell linesrespectively IC50 Value 15 μM(neuroblastoma) 34μM(non-neuroblastoma) Target MicrotubuleTubulin in vitrohellip

Bioactivity Amphethinile is an agent The affinity constantanti-tubulinfor the association ( ) of Amphethinile with tubulin isKa13 μM

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10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol

10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584

10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674

2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033

4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435

7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675

7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676

7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227

7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574

ABT-751 (E7010) Cat No HY-13270

Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190

wwwMedChemExpresscom 93

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9903Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9949Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9751Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ansamitocin P-3 is a inhibitor Ansamitocin P-3microtubuleis a macrocyclic antitumor antibiotic

Bioactivity Auristatin E is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAE analog and cytotoxin inAntibody-drug conjugates

Bioactivity Auristatin F is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAF analog and cytotoxin inAntibody-drug conjugates

Bioactivity BNC105 is a tubulin polymerization inhibitor with potentantiproliferative and tumor vascular disrupting properties

Bioactivity BTB-1 is a potent selective and reversible mitotic motorprotein inhibitor with an of 169 μMKif18A IC50

Bioactivity Cabazitaxel is a semi-synthetic derivative of the naturaltaxoid 10-deacetylbaccatin III with potential antineoplasticactivity

Bioactivity CCB02 is a selective inhibitor bindingCPAP-tubulin interactionto tubulin and competing for the CPAP binding site ofβ-tubulin with an of 689 nM and shows potent anti-tumorIC50activity CCB02 shows no inhibition on the cell cycle- andcentrosome-related kinases or the phosphorylation status ofhellip

Bioactivity Cephalomannine is a taxol derivative with antitumorantiproliferative properties

Bioactivity Cevipabulin (TTI-237) is an oral microtubule-active antitumorcompound and inhibits the binding of [ H] vinblastine to3

tubulin with an of 18-40 nM for cytotoxicity in humanIC50

tumor cell line [1] [2]

Bioactivity Cevipabulin fumarate (TTI-237 fumarate) is an oralmicrotubule-active antitumor compound and inhibits thebinding of [ H] vinblastine to tubulin with an of3 IC50

18-40 nM for cytotoxicity in human tumor cell line [1] [2]

Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739

Auristatin E Cat No HY-15582

Auristatin F Cat No HY-15583

BNC105 Cat No HY-16114

BTB-1 Cat No HY-101770

Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459

CCB02 Cat No HY-114302

Cephalomannine Cat No HY-77554

Cevipabulin (TTI-237) Cat No HY-14949

Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C

Purity 9828Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9956Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9831Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Bioactivity Colchicine is a inhibitor and a tubulin microtubuledisrupting agent Colchicine inhibits microtubulepolymerization with an of 3 nMIC50

Bioactivity Combretastatin A4 is a -targeting agent thatmicrotubulebinds with of 04 μMβ-tubulin Kd

Bioactivity Crolibulin is a small molecule tubulin polymerizationinhibitor

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate IC50 Value NATarget tubulin ADCs For comparison purposes the ADC A1-mc-MMAD andor A1 -vc-MMAD were used The linker payloadmc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) washellip

Bioactivity D-64131 is a novel inhibitor of Tubulin polymerization thatcompetitively binds with [(3)H]colchicine to αβ-Tubulin

Bioactivity D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule

Bioactivity D8-MMAE is a deuterated labeled MMAE a potent mitoticinhibitor

Bioactivity D8-MMAF is a deuterated form of MMAF which is a disrupting agentmicrotubule

Bioactivity D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a disrupting agentmicrotubule

Bioactivity DM4 is is an agent that inhibit cell division DM4antitubulincan be used in the preparation of antibody drug conjugate

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Colchicine Cat No HY-16569

Combretastatin A4 (CRC 87-09) Cat No HY-N2146

Crolibulin (EPC2407) Cat No HY-13603

Cys-mcMMAD Cat No HY-15750

D-64131 Cat No HY-15482

D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8

Monomethyl Dolastatin 10 D8) Cat No HY-15581S

D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A

D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S

D8-MMAF hydrochloride Cat No HY-15579AS

DM4 Cat No HY-12454

wwwMedChemExpresscom 95

Purity 9897Clinical Data LaunchedSize 500u g 1 mg

Purity gt98Clinical Data LaunchedSize 1 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Purity 9988Clinical Data Phase 3Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9555Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9983Clinical Data Phase 2Size 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg

Bioactivity Docetaxel is an antineoplastic drug by inhibiting depolymerization and attenuating of themicrotubule

effects of and gene expressionbcl-2 bcl-xL

Bioactivity Docetaxel Trihydrate is a semi-synthetic taxane analogue actsas a stabilizermicrotubule

Bioactivity Angiotensin II human is a vasoconstrictor that acts on the and the receptorAT1 AT2

Bioactivity ELR510444 is a novel microtubule disruptor inhibitsMDA-MB-231 cell proliferation with IC50 of 309 nM not asubstrate for the P-glycoprotein drug transporter and retainsactivity in βIII-tubulin-overexpressing cell lines

Bioactivity Entasobulin is a polymerization inhibitor withβ-tubulinpotential anticancer activity

Bioactivity Epothilone A is a competitive inhibitor of the binding of [H] paclitaxel to polymers with a of 06-14 μM3 tubulin Ki

Bioactivity Epothilone B is a stabilizer with a ofmicrotubule Ki071μM It acts by binding to the αβ-tubulin heterodimersubunit which causes decreasing of αβ-tubulin dissociation

Bioactivity Epothilone D (KOS 862) is a potent stabilizermicrotubule

Bioactivity Eribulin (E7389) is a targeting agent that ismicrotubuleused in the treatment of metastatic breast cancer Eribulin(E7389) inhibits the proliferation of cancer cells by bindingmicrotubule proteins and microtubules

Bioactivity Eribulin mesylate (E7389 mesylate) is a microtubuletargeting agent that is used in the treatment of metastaticbreast cancer Eribulin mesylate (E7389 mesylate) inhibits theproliferation of cancer cells by binding microtubule proteinsand microtubules

Docetaxel (RP-56976) Cat No HY-B0011

Docetaxel Trihydrate (RP-56976 (Trihydrate)) Cat No HY-B0011A

Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580

ELR510444 Cat No HY-16191

Entasobulin Cat No HY-16777

Epothilone A (Epo A) Cat No HY-13503

Epothilone B (EPO 906 Patupilone) Cat No HY-17029

Epothilone D (KOS 862) Cat No HY-15278

Eribulin (B1939 E7389 ER-086526) Cat No HY-13442

Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A

Purity 9874Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9723Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9947Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9801Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Bioactivity Estramustine phosphate sodium is an antimicrotubulechemotherapy agent arrests prostate cancer cells in the G2Mphase of the cell cycle

Bioactivity Fosbretabulin disodium(CA 4DP CA 4P) is a microtubuledestabilizing drug a type of vascular-targeting agent a drugdesigned to damage the vasculature (blood vessels) of cancertumors causing central necrosis IC50 Value 4 nM [1] Targetmicrotubule in vitro Cytotoxic IC(50) values of CA-4 in humanhellip

Bioactivity Ixabepilone is an orally bioavailable inhibitor which binds to tubulin andmicrotubule

promotes tubulin polymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of the cell cycle andinduces tumor cell apoptosis

Bioactivity Lexibulin(CYT-997) is a potent tubulin polymerisationinhibitor with IC50 of 10-100 nM in cancer cell lines withpotent cytotoxic and vascular disrupting activity in vitro andin vivo

Bioactivity Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM in cancer celllines with potent cytotoxic and vascular disrupting activityin vitro and in vivo

Bioactivity Maytansinol inhibits microtubule assembly and inducesmicrotubule disassembly in vitro Target MicrotubuleTubulinin vitro Maytansinol disrupts the mitotic spindle andprevents mitotic exit in Drosophila Maytansinol reduces thegrowth andor survival of HCT116 cells in a dose-dependenthellip

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate Mc-MMAD is aprotective group (maleimidocaproyl) -conjugated MMAD IC50Value Target tubulin ADCs For comparison purposes the ADCA1 -mc-MMAD andor A1 -vc-MMAD were used The linkerpayloadhellip

Bioactivity Mc-MMAE is a protective group (maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE) which is a potent tubulininhibitor is a toxin payload in antibody drug conjugate (

)ADC

Bioactivity Mc-MMAF is a protective group-conjugated MMAF MMAF is a morepotent drug than Monomethyl auristatin E (MMAE) but ischarged and relatively membrane-impermeable is a potenttubulin inhibitor is a toxin payload in antibody drugconjugate Target MMAF is a new auristatin derivative with ahellip

Bioactivity Mertansine (DM1) is a inhibitor and is anmicrotubulinantibody-conjugatable maytansinoid that is developed toovercome systemic toxicity associated with maytansine and toenhance tumor-specific delivery Mertansine can be attached toa monoclonal antibody with a linker to create an antibody-drughellip

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Estramustine phosphate sodium Cat No HY-13627

Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449

Ixabepilone (Azaepothilone B BMS 247550 BMS 247550-1) Cat No HY-10222

Lexibulin (CYT-997) Cat No HY-10498

Lexibulin dihydrochloride (CYT-997 dihydrochloride) Cat No HY-10498A

Maytansinol (Ansamitocin P-0) Cat No HY-19474

Mc-MMAD Cat No HY-15740

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741

McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578

Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792

wwwMedChemExpresscom 97

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9957Clinical Data Phase 3Size 10mM x 1mL in Water

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 4Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity Microtubule inhibitor 1 is an antitumor agent with inhibitory activity with anmicrotubule polymerization

value of 9-16 nM in cancer cells IC50[1]

Bioactivity MMAD is a potent inhibitor is a toxin payload intubulinantibody drug conjugates ( )ADCs

Bioactivity MMAF (Monomethylauristatin F) is an antitubulin agent thatinhibit cell division inhibits H3397 cell growth with an IC50of 105 nM

Bioactivity MMAF hydrochloride is an antitubulin agent that inhibit celldivision inhibits H3397 cell growth with an of 105 nMIC50

Bioactivity Monomethyl auristatin E (MMAE SGD-1010) is a syntheticderivative of dolastatin 10 and functions as a potent

inhibitor by inhibiting tubulin polymerizationmitoticMMAE is widely used as a cytotoxic component of antibody-drug

to treat several different cancer typesconjugates (ADCs)

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity Ombrabulin (AVE8062) is a derivative of CA-4 phosphate whichis known to exhibit antivascular effects through selectivedisruption of the cytoskeleton of endothelial cellstubulin

Bioactivity Ombrabulin hydrochloride is a derivative of CA-4 phosphatewhich is known to exhibit antivascular effects throughselective disruption of the cytoskeleton of endothelialtubulincells

Bioactivity OSIP-486823 is a novel -interfering agent withmicrotubuledistinct biological effects on both protein kinase G (PKG) andmicrotubules

Bioactivity Paclitaxel (Taxol) a naturally occurring antineoplasticagent stabilizes resulting intubulin polymerizationarrest at the G2M phase of the cell cycle and apoptotic celldeath [1] [2]

Microtubule inhibitor 1 Cat No HY-114313

MMAD (Demethyldolastatin 10 Monomethylauristatin D

Monomethyl Dolastatin 10) Cat No HY-15581

MMAF (Monomethylauristatin F) Cat No HY-15579

MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat No HY-15579A

Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162

Nocodazole (Oncodazole R17934) Cat No HY-13520

Ombrabulin (AVE8062 AC7700) Cat No HY-14797

Ombrabulin hydrochloride (AVE8062 (hydrochloride) AC7700 (hydrochloride)) Cat No HY-18256

OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004

Paclitaxel (Taxol) Cat No HY-B0015

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9979Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9344Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9968Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Bioactivity Parbendazole is a potent inhibitor of assemblymicrotubuledestabilizes tubulin with an of 879nM and exhibitsEC50a broad-spectrum anthelmintic activity

Bioactivity PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX) compound acts asa -depolymerizing agent and an apoptotic agentmicrotubule

Bioactivity PE859 is a potent inhibitor of both and aggregationtau Aβwith values of 066 and 12 μM respectivelyIC50

Bioactivity PF-06380101 is a novel cytotoxic Dolastatin 10 analogue withexcellent potencies in tumor cell proliferation assays anddifferential ADME properties when compared to other syntheticauristatin analogues that are used in the preparation of ADCsIC50 value ~02 nM(GI50 in BT474 MDA-MB-361-DYT2 and N87hellip

Bioactivity Plinabulin (NPI-2358) is a vascular disrupting agents (VDA)against tubulin-depolymerizing with IC50 of 98~18 nM in tumorcells IC50 Value 98~18 nM Target MicrotubuleTubulin invitro NPI-2358 binds to the colchicine-binding site oftubulin and has potent inhibitory to human tumor cell lineshellip

Bioactivity Podofilox (Podophyllotoxin) is a potent inhibitor ofmicrotubule assembly and DNA topoisomerase II

Bioactivity Rosabulin is a potent inhibitor withmicrotubuleanti-cancer activities

Bioactivity Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10derivative and inhibitor of polymerizationtubulin

Bioactivity SSE15206 is a polymerization inhibitor (GI microtubule 50= 197 nM in HCT116 cells) that overcomes multidrug resistanceCauses aberrant mitosis resulting in G2M arrest due toincomplete spindle formation in cancer cells [1]

Bioactivity Taltobulin (HTI-286 SPA-110) is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibitedproliferation of all three hepatic tumor cell lines (mean IC50= 2 nmolL +- 1 nmolL) in vitro Interestingly no decreasehellip

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Parbendazole (SKF 29044) Cat No HY-115364

PBOX 6 Cat No HY-U00446

PE859 Cat No HY-12662

PF-06380101 Cat No HY-12522

Plinabulin (NPI-2358) Cat No HY-14444

Podofilox (Podophyllotoxin) Cat No HY-15552

Rosabulin (STA 5312) Cat No HY-14934

Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672

SSE15206 Cat No HY-111425

Taltobulin (HTI-286 SPA-110) Cat No HY-15584

wwwMedChemExpresscom 99

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9624Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9996Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Taltobulin hydrochloride is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibits proliferationof all three hepatic tumor cell lines (mean IC50 = 2 nmolL+- 1 nmolL) Interestingly no decrease in viable primaryhellip

Bioactivity Taltobulin trifluoroacetate (HTI-286 SPA-110) is an analogueof Hemiasterlin potent tubulin inhibitor ADCs cytotoxinIC50 value Target tubulin in vitro HTI-286 significantlyinhibited proliferation of all three hepatic tumor cell lines(mean IC50 = 2 nmolL +- 1 nmolL) in vitro Interestinglyhellip

Bioactivity Tasidotin hydrochloride is a peptide analog of the antimitoticdepsipeptide dolastatin 15 as an inhibitor of microtubuleassembly and microtubule dynamics

Bioactivity Tirbanibulin (KX2-391) is an inhibitor of that targetsSrcthe peptide substrate site of Src with of 9-60 nM inGI50cancer cell lines

Bioactivity Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) isan inhibitor of that targets the peptide substrate siteSrcof Src with of 9-60 nM in cancer cell linesGI50

Bioactivity Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitorof that targets the peptide substrate site of Src withSrc

of 9-60 nM in cancer cell linesGI50

Bioactivity Triclabendazole(CGA89317) is a benzimidazole it binds totubulin impairing intracellular transport mechanisms andinterferes with protein synthesis Target MicrotubuleTubulinTriclabendazole treatment produces percentage decreases of thefluke egg output by 153 43 and 366 respectively inhellip

Bioactivity Tubulin inhibitor 1 is a inhibitor occupying thetubulincolchicine binding site inhibits tubulin polymerizationTubulin inhibitor 1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase and inducescellular apoptosis [1]

Bioactivity Tubulysin A(TubA) is a myxobacterial product that can functionas an antiangiogenic agent in many in vitro assaysanti-microtubule anti-mitotic an apoptosis induceranticancer anti-angiogenic and antiproliferative IC50value Target microtubule Tubulysin A is a novel antibiotichellip

Bioactivity Valecobulin (CKD516) a valine prodrug of (S516) and avascular disrupting agent (VDA) is a potent beta-tubulin

inhibitor with marked antitumor activitypolymerizationagainst murine and human solid tumors [1] [2]

Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A

Tasidotin hydrochloride (ILX651) Cat No HY-13760

Tirbanibulin (KX2-391 KX-01) Cat No HY-10340

Tirbanibulin dihydrochloride (KX2-391 (dihydrochloride) KX-01 (dihydrochloride)) Cat No HY-10340A

Tirbanibulin Mesylate (KX2-391 (Mesylate) KX01 (Mesylate)) Cat No HY-10340B

Triclabendazole (CGA89317) Cat No HY-B0621

Tubulin inhibitor 1 Cat No HY-112607

Tubulysin A (TubA) Cat No HY-15995

Valecobulin (CKD-516) Cat No HY-13598

Purity 9958Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9914Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data LaunchedSize 10 mg 50 mg 100 mg 200 mg

Purity 9987Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9989Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Bioactivity Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulininhibitor (MMAD) Vc-MMAD is an antibody drug conjugate IC50Valu NA Target tubulin ADCs Monomethyl auristatin D(MMAD) a potent tubulin inhibitor is a toxin payload andantibody drug conjugate For comparison purposes the ADC A1hellip

Bioactivity VcMMAE is a with potentdrug-linker conjugate for ADCantitumor activity by using the anti-mitotic agent monomethylauristatin E (MMAE) linked via the lysosomally cleavabledipeptide valine-citrulline (vc)

Bioactivity Vinblastine sulfate is a cytotoxic alkaloid used againstvarious cancer types Vinblastine sulfate inhibits theformation of microtubule and suppresses nAChR with an ofIC5089 μM

Bioactivity Vincristine sulfate is an antitumor vinca alkaloid whichinhibits formation in mitotic spindlemicrotubuleresulting in an arrest of dividing cells at the metaphasestage It binds to with a of 85 nMmicrotubule Ki

Bioactivity Vinflunine is a new vinca alkaloid uniquely fluorinated withthe properties of mitotic-arresting and tubulin-interactingactivity

Bioactivity Vinflunine Tartrat is a new vinca alkaloid uniquelyfluorinated with the properties of mitotic-arresting andtubulin-interacting activity Target MicrotubuleTubulin Themajor effects of Vinflunine on dynamic instability are aslowing of the microtubule growth rate an increase in growthhellip

Bioactivity Vinorelbine is an anti-mitotic agent which inhibits theproliferation of Hela cells with IC of 125 nM50

Bioactivity Vinorelbine (ditartrate) is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC of 12550nM

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Vc-MMAD Cat No HY-15742

VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575

Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780

Vincristine sulfate (Leurocristine sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488

Vinflunine Cat No HY-B0628

Vinflunine Tartrate Cat No HY-B0628A

Vinorelbine (KW-2307 base) Cat No HY-12053

Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A

wwwMedChemExpresscom 101

Mps1Monopolar spindle 1

Monopolar spindle 1 (Mps1) also known as TTK is a serine threoninekinase which ensures proper biorientation of sister chromatids on themitotic spindle by the activation of the spindle assembly checkpoint(SAC) Mps1 has been shown to function as the key kinase thatactivates the spindle assembly checkpoint (SAC) to secure properdistribution of chromosomes to daughter cellsMps1 is a dual specificity protein kinase that is essential for thebipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomesare properly attached Mps1 is expressed at high levels during mitosisand is abundantly expressed in cancer cells Disruption of Mps1

function induces aneuploidy and cell death

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Mps1 Inhibitors amp Modulators

Bioactivity AZ3146 is a reasonably potent and selective inhibitorMps1with of 35 nM for Mps1 IC50

CatBioactivity BAY 1217389 is a potent and selective inhibitor of the

monopolar spindle 1 ( ) kinase with an value lessMPS1 IC50than 10 nM

Bioactivity BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1)checkpoint with an of 2 nMIC50

Bioactivity CCT251455 is a potent and selective mitotic kinase monopolarspindle 1 ( ) inhibitor with an of 3 nMMPS1 IC50

Bioactivity CFI-402257 is a highly selective and orally bioavailable inhibitor with an of 17 nM for TTK in vitroTTKMps1 IC50

CFI-402257 has anti-cancer activity [1]

Bioactivity CFI-402257 hydrochloride is a highly selective and orallybioavailable inhibitor with an of 17 nM forTTKMps1 IC50TTK in vitro CFI-402257 hydrochloride has anti-canceractivity [1]

Bioactivity Empesertib (BAY 1161909) is a potent inhibitor withMps1an of lt 1 nMIC50

Bioactivity MPI-0479605 is a potent and selective ATP-competitiveinhibitor of with an of 18 nMMps1 IC50

Bioactivity Mps1-IN-1 is a potent selective and ATP-competitive Mps1kinase inhibitor with an and a of 367 nM and 27 nMIC50 Kd

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

102 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

AZ3146 Cat No HY-14710

BAY1217389 Cat No HY-12859

BOS-172722 Cat No HY-112162

CCT251455 Cat No HY-12603

CFI-402257 Cat No HY-101340

CFI-402257 hydrochloride Cat No HY-101340A

Empesertib (BAY 1161909) Cat No HY-12858

MPI-0479605 Cat No HY-12660

Mps1-IN-1 Cat No HY-13298

Mps1-IN-2 Cat No HY-13994

wwwMedChemExpresscom 103

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-3 is a potent and selective kinase inhibitorMPS1with an of 50 nMIC50

Bioactivity NMS-P715 is a selective ATP-competitive inhibitor of MPS1with an of 182 nMIC50

Bioactivity NMS-P715 analog is an inhibitor of with an of 84MPS1 IC50nM

Mps1-IN-3 Cat No HY-12401

NMS-P715 Cat No HY-12382

NMS-P715 analog Cat No HY-14712

Nucleoside AntimetaboliteAnalog

Nucleoside analogues are molecules that act like nucleosides in DNAsynthesis They include a range of antiviral products used to preventviral replication in infected cells Nucleoside analogues can be usedagainst hepatitis B virus hepatitis C virus herpes simplex and HIVOnce they are phosphorylated they work as antimetabolites by beingsimilar enough to nucleotidesto be incorporated into growing DNAstrands Less selective nucleoside analogues are used aschemotherapy agents to treat cancer eg gemcitabine and 5-FUAntimetabolite is a chemical that inhibits the use of a metabolitewhich is another chemical that is part of normal metabolism Suchsubstances are often similar in structure to the metabolite that they

interfere with such as the antifolates that interfere with the use of folic acid The presence of antimetabolites can havetoxic effects on cells such as halting cell growth and cell division so these compounds are used as chemotherapy forcancer

104 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 105

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Nucleoside AntimetaboliteAnalog Inhibitors amp Modulators

Bioactivity 1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is abicyclic nucleoside

Bioactivity 1-Methylcytosine is a methylated form of the DNA base cytosineand used as a nucleobase of hachimoji DNA in which it pairswith Isoguanine [1] [2]

Bioactivity 1-Methylinosine is a modified nucleotide found at position 37in tRNA 3 to the anticodon of eukaryotic tRNA [1]

Bioactivity 2-Deoxypseudoisocytidine is a nucleoside analogue

Bioactivity 2rsquo-O4rsquo-C-Methyleneuridine (Compound 15a) is a bicyclicnucleoside

Bioactivity 3-Azido-3-deoxy-5-fluorocytidine (Compound 12) is a cytidinederivative

Bioactivity 3-Azido-3-deoxy-beta-L-uridine (Compound 25) is a nucleosidederivative

Bioactivity 3-Methylcytidine a urinary nucleoside can be used as abiomarker of four different types of cancer lung cancergastric cancer colon cancer and breast cancer [1]

Bioactivity 5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methyluridine is a derivative of LNA-type nucleoside

Bioactivity 5-Aza-7-deazaguanine is a substrate for wild-type (WT) E coli and its Ser90Ala mutant in thepurine nucleoside phosphorylase

synthesis of base-modified nucleosides [1]

1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine Cat No HY-111638

1-Methylcytosine Cat No HY-W006395

1-Methylinosine (N1-Methylinosine) Cat No HY-113139

2-Deoxypseudoisocytidine Cat No HY-101968

2rsquo-O4rsquo-C-Methyleneuridine Cat No HY-111639

3-Azido-3-deoxy-5-fluorocytidine Cat No HY-111641

3-Azido-3-deoxy-beta-L-uridine Cat No HY-111642

3-Methylcytidine Cat No HY-111645

5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methylurid

ine

Cat No HY-111807

5-Aza-7-deazaguanine Cat No HY-111627

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9874Clinical Data Phase 4Size 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 960Clinical Data LaunchedSize 50 mg 100 mg 500 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in Water

50 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Bioactivity 5-Azacytidine is a nucleoside analogue of cytidine thatspecifically inhibits DNA methylation by trapping DNA

methyltransferases

Bioactivity 5-BrdU is a nucleoside analog that competes with thymidine forincorporation into DNA 5-BrdU is commonly used in thedetection of proliferating cells

Bioactivity 5-Fluorouracil is a potent antitumor agent that affectspyrimidine synthesis by inhibiting thymidylate synthetasethus depleting intracellular dTTP pools

Bioactivity 6-Amino-5-nitropyridin-2-one is a pyridine base and used as anucleobase of hachimoji DNA in which it pairs with5-aza-7-deazaguanine [1]

Bioactivity 6-Mercaptopurine is a purine analogue which acts as anantagonist of the and has been widely usedendogenous purinesas antileukemic agent and immunosuppressive drug

Bioactivity 6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MPhydrate) is a purine analogue which acts as an antagonist ofthe and has been widely used asendogenous purinesantileukemic agent and immunosuppressive drug

Bioactivity 6-O-Methyl Guanosine is a modified nucleoside 6-O-Methyl[1]

Guanosine (6-methylguanosine) inhibit colony-forming abilityin a malignant xeroderma pigmentosum cell line [2]

Bioactivity 7-Methylguanosine is a novel cNIIIB nucleotidase inhibitorwith IC value of 878 plusmn 75 microM50

Bioactivity 8-Azaguanine is a purine analogue which shows antineoplasticactivity

Bioactivity Adenosine is a nucleoside composed of a molecule of adenineattached to a ribose sugar molecule (ribofuranose) moiety viaa β-N9-glycosidic bond Target Nucleosideantimetaboliteanalog Adenosine plays an important role inbiochemical processes such as energy transfer mdash as adenosinehellip

106 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

5-Azacytidine (Ladakamycin 5-AzaC Azacitidine) Cat No HY-10586

5-BrdU (BUdR BRDU) Cat No HY-15910

5-Fluorouracil (5-FU) Cat No HY-90006

6-Amino-5-nitropyridin-2-one Cat No HY-50071

6-Mercaptopurine (Mercaptopurine 6-MP) Cat No HY-13677

6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MP hydrate) Cat No HY-13677A

6-O-Methyl Guanosine Cat No HY-111648

7-Methylguanosine Cat No HY-122524

8-Azaguanine Cat No HY-B1468

Adenosine (Adenine riboside D-Adenosine) Cat No HY-B0228

wwwMedChemExpresscom 107

Purity 9818Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 1 g

Purity 9897Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carmofur is a derivative of fluorouracil an antimetaboliteused as an antineoplastic agent

Bioactivity Clofarabine(Clolar Clofarex) inhibits the enzymaticactivities of ribonucleotide reductase (IC50 = 65 nM) and DNApolymerase IC50 Value 65 nM Target in vitro Clofarabine isa second generation purine nucleoside analog withantineoplastic activity It is phosphorylated intracellularlyhellip

Bioactivity CNDAC is a major metabolite of oral drug sapacitabine and anucleoside analog

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Cytidine is a nucleoside molecule that is formed when cytosineis attached to a ribose ring cytidine is a component of RNATarget Nucleoside antimetaboliteanalog Cytidine is anucleoside molecule that is formed when cytosine is attachedto a ribose ring (also known as a ribofuranose) via ahellip

Bioactivity Dacarbazine(DTIC-Dome DTIC) is an antineoplastic agent Ithas significant activity against melanomas Target Nucleosideantimetaboliteanalog Approved May 1975 Dacarbazine (DTIC) isthe only single-agent approved by the Food and DrugAdministration for treating metastatic melanoma With DTIC ashellip

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Deoxypseudouridine is a nucleotide analog

Capecitabine Cat No HY-B0016

Carmofur (HCFU) Cat No HY-B0182

Clofarabine Cat No HY-A0005

CNDAC Cat No HY-16445A

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Cytidine (Cytosine β-D-riboside Cytosine-1-β-D-ribofuranoside) Cat No HY-B0158

Dacarbazine (Imidazole Carboxamide) Cat No HY-B0078

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Deoxypseudouridine Cat No HY-101970

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in Water

1000u g 2500u g 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 2500u g 5 mg 10 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 50 mg

Bioactivity DMTr-LNA-5MeU-3-CED-phosphoramidite is a nucleoside derivative[1]

Bioactivity Doxifluridine is a thymidine phosphorylase activator forPC9-DPE2 cells with IC50 of 062 μM

Bioactivity Ethynylcytidine is a new nucleoside antimetabolite Bioactivity Floxuridine (5-fluorodeoxyuridine) is an oncology drug thatbelongs to the class known as antimetabolites with an GI50 of51 μM for the inhibition of PEPT1 IC50 value TargetNucleoside antimetaboliteanalog Floxuridine (Fludara) is aprodrug of floxuridine and an oncology agent with an GI50 ofhellip

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

Bioactivity Fludarabine (phosphate) is an analogue of adenosine anddeoxyadenosine which is able to compete with dATP forincorporation into DNA and inhibit DNA synthesis

Bioactivity Forodesine(BCX-1777 freebase Immucillin-H) is an orallybioavailable PNP inhibitor with picomolar potency inducesapoptosis mainly in T cells

Bioactivity Forodesine hydrochloride is a potent and oral purine nucleoside inhibitor with s ranging from 048 tophosphorylase (PNP) IC50

157 nM

Bioactivity Fosteabine is an oral and prodrug analogue of cytarabine whichis resistant to deoxycytidine deaminase

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

108 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

DMTr-LNA-5MeU-3-CED-phosphoramidite Cat No HY-111531

Doxifluridine (Ro 21-9738 5-Fluoro-5-deoxyuridine 5-DFUR) Cat No HY-B0021

Ethynylcytidine (ECyD TAS-106 3-C-Ethynylcytidine) Cat No HY-16200

Floxuridine (5-Fluorouracil 2-deoxyriboside) Cat No HY-B0097

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Fludarabine phosphate (NSC 118218 (phosphate)) Cat No HY-B0028

Forodesine (BCX-1777 freebase Immucillin-H) Cat No HY-16210

Forodesine hydrochloride (BCX-1777 Immucillin-H hydrochloride) Cat No HY-16209

Fosteabine (Cytarabine ocfosfate YNK 01) Cat No HY-106349

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

wwwMedChemExpresscom 109

Purity 9575Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 9971Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9829Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Gemcitabine elaidate(CP-4126 CO-101) is a lipophilicunsaturated fatty acid ester derivative of gemcitabine (dFdC)an antimetabolite deoxynucleoside analogue with potentialantineoplastic activity IC50 value Target Gemcitabineanalog Upon hydrolysis intracellularly by esterases thehellip

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity Isocytosine is a non-natural nucleobase and an isomer ofcytosine It is used in combination with Isoguanine in studiesof unnatural nucleic acid analogues of the normal base pairsin DNA and used as a nucleobase of hachimoji RNA [1] [2]

Bioactivity Isoguanine is a purine base that is an isomer of guanine Abuilding block in organic synthesis

Bioactivity LY2334737 is an orally available prodrug of gemcitabine whichis a nucleoside analog used as chemotherapy

Bioactivity N2-methylguanosine is a modified nucleoside that occurs atseveral specific locations in many tRNAs

Bioactivity N6N6-Dimethyladenosine is a modified ribonucleosidepreviously found in rRNA and also exhibits in mycobacteriumbovis Bacille Calmette-Gueacuterin tRNA [1]

Bioactivity N6-Etheno 2-deoxyadenosine is a reactive oxygen species(ROS)reactive nitrogen species (RNS)-induced DNA oxidationproduct used as a biomarker to evaluate chronic inflammationand lipid peroxidation in animal or human tissues [1]

Bioactivity Nelarabine (Arranon 506U78) is a purine nucleoside analog andDNA synthesis inhibitor with IC50 from 0067-215 μM in tumorcells Nelarabine is a chemotherapy drug used in T-cell acutelymphoblastic leukemia

Bioactivity Orotic acid (OA) is an intermediate in pyrimidine metabolismIC50 Value Target Nucleoside antimetaboliteanalog in vitroOA increases cell proliferation and decreases apoptosis inserum-starved SK-Hep1 hepatocellular carcinoma cells whichmay ascribe to the inhibition of AMP-activated protein kinasehellip

Gemcitabine elaidate (CP-4126 CO-101 Gemcitabine 5-elaidate) Cat No HY-13538

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

Isocytosine Cat No HY-W002272

Isoguanine Cat No HY-124143

LY2334737 Cat No HY-13672

N2-Methylguanosine Cat No HY-111647

N6N6-Dimethyladenosine Cat No HY-101984

N6-Etheno 2-deoxyadenosine Cat No HY-111646

Nelarabine (506U78 GW 506U78 Nelzarabine) Cat No HY-13701

Orotic acid (6-Carboxyuracil Vitamin B13) Cat No HY-N0157

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9972Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9783Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9887Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9745Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity Pseudothymidine is a C-nucleoside analog of thymidine Bioactivity Raltitrexed is an antimetabolite drug used in chemotherapyacting by inhibiting thymidylate synthase

Bioactivity RX-3117(TV-1360 Fluorocyclopentenylcytosine) is novel acytidine analog shows anticancer activity in several cancercell lines including gemcitabine-resistant variants

Bioactivity Sapacitabine is an orally available prodrugnucleoside analogthat is structurally related to cytarabine

Bioactivity Tegafur (FT 207 NSC 148958) is a chemotherapeutic 5-FUprodrug used in the treatment of cancers is a component oftegafur-uracil

Bioactivity Tipiracil is a thymidine phosphorylase ( ) inhibitorTPase

Bioactivity Tipiracil (hydrochloride) is a thymidine phosphorylaseinhibitor (TPI) used for cancer research

Bioactivity Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT)is an irreversible inhibitor andthymidylate synthasethereby suppresses Trifluridine is an antiviralDNA synthesisdrug for infectionherpes simplex virus (HSV)

Bioactivity Trifluridine-tipiracil hydrochloride mixture (TAS-102) is anovel oral combination drug that consists of an antineoplasticthymidine-based nucleoside analog trifluorothymidine and apotent inhibitor tipiracil in athymidine phosphorylase105 molar ratio

Bioactivity Vidarabine (Ara-A) an antiviral drug which is active againstherpes simplex and varicella zoster viruses

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Pseudothymidine (5-Methyl-2-Deoxypseudouridin) Cat No HY-101969

Raltitrexed (ZD1694 D1694 ICI-D1694) Cat No HY-10821

RX-3117 (TV-1360 fluorocyclopentenylcytosine) Cat No HY-15228

Sapacitabine (CS682 CYC682) Cat No HY-16445

Tegafur (FT 207NSC 148958) Cat No HY-17400

Tipiracil Cat No HY-A0063A

Tipiracil hydrochloride Cat No HY-A0063

Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT) Cat No HY-A0061

Trifluridinetipiracil hydrochloride mixture (TAS-102) Cat No HY-16478

Vidarabine (Ara-A Adenine Arabinoside

9-β-D-Arabinofuranosyladenine) Cat No HY-B0277

wwwMedChemExpresscom 111

p97VCPCdc48

p97 an abundant hexameric ATPase of the AAA family is involved inhomotypic membrane fusion It is thought to disassemble SNAREcomplexes formed during the process of membrane fusion Twostructures have been reported a crystal structure of the N-terminaland D1 ATPase domains of murine p97 at 29 A resolution and acryoelectron microscopy structure of full-length rat p97 at 18 Aresolution Together these structures show that the D1 and D2hexamers pack in a tail-to-tail arrangement and that the N domain isflexible A comparison with NSF D2 (ATP complex) reveals possibleconformational changes induced by ATP hydrolysis

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9765Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

p97 Inhibitors amp Modulators

Bioactivity CB-5083 is a potent selective and orally bioavailable p97inhibitor with an value of 11 nMIC50

Bioactivity DBeQ is a selective potent reversible and ATP-competitive inhibitor with an value of 15 μM and 16 μM forp97 IC50

p97(wt) and p97(C522A) respectively DBeQ also inhibits Vps4with an of 115 μMIC50

Bioactivity ML240 is a potent inhibitor inhibiting p97 ATPase withp97 value of 100 nMIC50

Bioactivity ML241 hydrochloride is a potent inhibitor inhibiting p97p97ATPase with value of 100 nMIC50

Bioactivity NMS-859 is a potent covalent inhibitor withVCP (p97)s of 037 and 036 μM for wild-type VCP in the presence ofIC50

60 μM and 1 mM ATP in cells respectively

Bioactivity NMS-873 is a potent selective allosteric inhibitorVCPp97with value of 30 nMIC50

112 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CB-5083 Cat No HY-12861

DBeQ (JRF 12) Cat No HY-15945

ML240 Cat No HY-19795

ML241 hydrochloride Cat No HY-19797A

NMS-859 Cat No HY-15714

NMS-873 Cat No HY-15713

wwwMedChemExpresscom 113

PAKp21 activated kinases

PAKs (p21-activated kinases) are key regulators of actin dynamics cellproliferation and cell survival PAKs are SerThr kinases that areclassified into two groups on the basis of their structural andfunctional features group I (PAK1ndash3) and group II (PAK4ndash6) Group IPAKs have an auto-inhibitory domain (also called an inhibitory switchdomain) and a kinase domain (catalytic domain CD) and are activatedby the binding of the active (that is GTP-bound) forms of RhoGTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPasesBecause the deregulation of PAKs is closely associated with varioushuman diseasessmall-molecule inhibitors of these kinases have great

potential as therapeutic agents In addition these compounds can also be used as powerful tools in studies aimed atunderstanding the PAK signaling pathwayPAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actinremodelling and their ability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role intumor cell invasion and metastasis The current evidence suggests the involvement of PAKs in motility cell survivalanchorage-independent growth angiogenesis invasion migration and regulation of cell cycle and mitosisConsequently PAKs have also been implicated in a number of pathological conditions including cancer

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9902Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 1 g 5 g

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

PAK Inhibitors amp Modulators

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Fingolimod is a ( ) antagonistsphingosine 1-phosphate S1Pwith of 0033 nM in K562 and NK cells Fingolimod also isIC50a activatorpak1

Bioactivity Fingolimod hydrochloride is a ( )sphingosine 1-phosphate S1Pantagonist with an of 0033 nM in K562 and NK cellsIC50Fingolimod hydrochloride also is a activatorpak1

Bioactivity FRAX1036 is a inhibitor with s of 233 nM 724 nM andPAK Ki24 μM for PAK1 PAK2 and PAK4 respectively

Bioactivity FRAX486 is a p21-activated kinase ( ) inhibitor with sPAK IC50of 14 33 and 39 nM for PAK1 PAK2 and PAK3 respectively

Bioactivity FRAX597 is a potent group I p21-activated Kinases ( s)PAKinhibitor with of 8 13 and 19 nM for and IC50 PAK1 2 3

Bioactivity G-5555 is a potent p21-activated kinase 1 ( ) inhibitorPAK1with s of 37 nM and 11 nM for PAK1 and PAK2 respectivelyKi

Bioactivity G-5555 hydrochloride is a potent and selective p21-activatedkinase 1 ( ) inhibitor with a of 37 nMPAK1 Ki

Bioactivity IPA-3 is a selective non-ATP competitive inhibitor withPAK1 of 25 μM and shows no inhibition to group II PAKs (PAKsIC50

4-6)

Bioactivity NVS-PAK1-1 is a potent and selective allosteric PAK1inhibitor with an of 5 nMIC50

114 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Fingolimod (FTY720 free base) Cat No HY-11063

Fingolimod hydrochloride (FTY720) Cat No HY-12005

FRAX1036 Cat No HY-19538

FRAX486 Cat No HY-15542B

FRAX597 Cat No HY-15542A

G-5555 Cat No HY-19635

G-5555 hydrochloride Cat No HY-19635A

IPA-3 Cat No HY-15663

NVS-PAK1-1 Cat No HY-100519

wwwMedChemExpresscom 115

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity PAK-IN-1 is a inhibitor that displays group IIPAKselectivity PAK-IN-1 inhibits PAK4 PAK5 and PAK6 with sIC50of 75 36 126 nM respectively

Bioactivity PF-3758309 is an inhbitor of with of 13 nM forPAK IC50PAK4

PAK-IN-1 Cat No HY-12632

PF-3758309 Cat No HY-13007

PARPpoly ADP ribose polymerase

PARP is a family of proteins involved in a number of cellular processesinvolving mainly DNA repair and programmed cell death The PARPfamily comprises 17 members They have all very different structuresand functions in the cell PARP1 PARP2 VPARP (PARP4) Tankyrase-1and -2 (PARP-5a or TNKS and PARP-5b or TNKS2) have a confirmedPARP activity Others include PARP3 PARP6 TIPARP (or PARP7)PARP8 PARP9 PARP10 PARP11 PARP12 PARP14 PARP15 andPARP16 PARP is found in the cellrsquos nucleus The main role is to detectand signal single-strand DNA breaks (SSB) to the enzymaticmachinery involved in the SSB repair

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wwwMedChemExpresscom 117

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9839Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in Water

200 mg 500 mg

PARP Inhibitors amp Modulators

Bioactivity 3-Aminobenzamide is a potent inhibitor of with of appr 50 nM in CHO cellsPARP IC50

and acts as a mediator of oxidant-induced myocyte dysfunctionduring reperfusion

Bioactivity A-966492 is a novel and potent inhibitor of and with of 1 nM andPARP1 PARP2 Ki

15 nM respectively

Bioactivity AG14361 is a potent inhibitor with a of lt 5 nMPARP-1 Kiand in permeabilized SW620 and intact SW620 cells the sIC50are 29 nM and 14 nM respectively

Bioactivity AZ6102 is a potent dual and inhibitor withTNKS1 TNKS2s of 3 nM and 1 nM respectively and alao has 100-foldIC50

selectivity against other PARP family enzymes with s ofIC5020 μM 05 μM and gt3 μM for PARP1 PARP2 and PARhellip

Bioactivity AZD-2461 is a potent inhibitor with s of 5 nM 2 nMPARP IC50and 200 nM for PARP1 PARP2 and PARP3 respectively

Bioactivity BGP-15 is a inhibitor with an and a of 120 andPARP IC50 Ki57 μM respectively

Bioactivity BRCA1-IN-1 is a novel small-molecule-like inhibitorBRCA1with and of 053 μM and 071 μM respecrivelyIC50 Ki

Bioactivity Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolatedfrom traditional Chinese herb WT WangCorydalis yanhusuoDehydrocorydaline regulates protein expression of Bax Bcl-2activates and inactivates caspase-7 caspase-8 PARP

Bioactivity E7449 is a potent and inhibitor and alsoPARP1 PARP2inhibits and with s of 20 10 50 andTNKS1 TNKS2 IC5050 nM for PARP1 PARP2 TNKS1 and TNKS2 respectively using

P-NAD as substrate32 +

Bioactivity G007-LK is a potent and selective inhibitor of andTNKS1 with s of 46 nM and 25 nM respectivelyTNKS2 IC50

3-Aminobenzamide (PARP-IN-1) Cat No HY-12022

A-966492 Cat No HY-10614

AG14361 Cat No HY-12032

AZ6102 Cat No HY-12975

AZD-2461 Cat No HY-13536

BGP-15 Cat No HY-100828

BRCA1-IN-1 Cat No HY-100863

Dehydrocorydaline (13-Methylpalmatine) Cat No HY-N0674

E7449 Cat No HY-12418

G007-LK Cat No HY-12438

Purity 9952Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Bioactivity GeA-69 is a selective highly cell permeable allostericinhibitor of poly-adenosine-diphosphate-ribose polymerase 14

targeting macrodomain 2 with a of 21 microM (PARP14) Kd[1]

Bioactivity Iniparib (BSI-201) is an irreversible inhibitor of PARP1used in the research of triple negative breast cancer

Bioactivity JW 55 is a potent and selective signaling pathwayβ-catenininhibitor which functions via inhibition of the PARP domainof tankyrase 1 and tankyrase 2 (TNKS12) JW 55 decreasesauto-PARsylation of TNKS12 in vitro with s of 19 μM andIC50830 nM respectively

Bioactivity K-756 is a direct and selective ( ) inhibitortankyrase TNKSwhich inhibits the ADP-ribosylation activity of andTNKS1

with s of 31 and 36 nM respectivelyTNKS2 IC50

Bioactivity ME0328 is a potent and selective inhibitor withARTD3 PARP3an of 089plusmn028 μMIC50

Bioactivity MN-64 is a potent inhibitor with s of 6 nMtankyrase 1 IC5072 nM 191 μM and 394 μM for TNKS2 ARTD1 andTNKS1ARTD2 respectively

Bioactivity Niraparib (MK-4827) is a highly potent and PARP1 PARP2inhibitor with s of 38 and 21 nM respectivelyIC50

Bioactivity Niraparib hydrochloride (MK-4827 hydrochloride) is anexcellent and inhibitor with of 38 and 21PARP1 PARP2 IC50nM respectively

Bioactivity Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent inhibitor with of 24 nMPARP1 IC50

Bioactivity Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1and inhibitor with an of 38 and 21 nMPARP2 IC50respectively

118 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

GeA-69 Cat No HY-108708

Iniparib (BSI-201 NSC-746045 IND-71677) Cat No HY-12015

JW 55 Cat No HY-13968

K-756 Cat No HY-U00422

ME0328 Cat No HY-100225

MN-64 Cat No HY-19351

Niraparib (MK-4827) Cat No HY-10619

Niraparib hydrochloride (MK-4827 (hydrochloride)) Cat No HY-10619A

Niraparib R-enantiomer (MK 4827 (R-enantiomer)) Cat No HY-10619D

Niraparib tosylate (MK-4827 (tosylate)) Cat No HY-10619B

wwwMedChemExpresscom 119

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg

Purity 9768Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2 g

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NMS-P118 is a potent orally available and highly selective Inhibitor for cancer therapyPARP-1

Bioactivity NMS-P515 is a potent and stereospecific inhibitorPARP-1with an of 27 nM in hela cells Anti-tumor activity IC50

[1]

Bioactivity NVP-TNKS656 is a highly potent selective and orally active inhibitor with of 6 nM and is gt 300 foldTNKS2 IC50

selectivity against and PARP1 PARP2

Bioactivity Olaparib (AZD2281KU0059436) is a potent and oral PARPinhibitor with s of 5 and 1 nM for and IC50 PARP1 PARP2

respectively

Bioactivity Pamiparib is a inhibitor which can be used for thePARPtreatment of various cancers including the solid tumorextracted from patent WO 2013097225 A1

Bioactivity PARP-2-IN-1 is a potent and selective inhibitor withPARP-2an of 115 nMIC50

Bioactivity PJ34 is a potent specific inhibitor of with ofPARPl 2 IC50110 nM and 86 nM respectively

Bioactivity PJ34 hydrochloride is an inhibitor of with of 110PARPl12 IC50nM and 86 nM respectively

Bioactivity PROTAC PARP1 degrader is a degrader based on thePARP1 technology It induces significant PARP1 cleavage andPROTAC

programmed cell death PROTAC PARP1 degrader at 10 μM at 24 hinhibits MDA-MB-231 cell line with an of 612 μMIC50

Bioactivity RK-287107 is a potent and specific inhibitor withtankyrases of 143 and 106 nM for and IC50 tankyrase-1 tankyrase-2

respectively RK-287107 blocks colorectal cancer cell growth[1]

NMS-P118 Cat No HY-18954

NMS-P515 Cat No HY-128599

NVP-TNKS656 (TNKS656) Cat No HY-13990

Olaparib (AZD2281 KU0059436) Cat No HY-10162

Pamiparib (BGB-290) Cat No HY-104044

PARP-2-IN-1 Cat No HY-102035

PJ34 Cat No HY-13688A

PJ34 hydrochloride Cat No HY-13688

PROTAC PARP1 degrader Cat No HY-114324

RK-287107 Cat No HY-123892

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9962Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9888Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9508Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9983Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9989Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9981Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity Rucaparib (AG014699) is an inhibitor of with of 14 nM for PARP1 in aPARP Ki

cell-free assay and also shows binding affinity to eightother PARP domains

Bioactivity Rucaparib Camsylate is an inhibitor of with a of 14PARP KinM for PARP1 and also shows binding affinity to eight otherPARP domains

Bioactivity Rucaparib phosphate (AG-014699 phosphate) is a potent and oral inhibitor with a of 14 nM for PARP1 in cell-freePARP Ki

assay also showing binding affinity to eight other PARPdomains

Bioactivity Talazoparib (BMN-673) is a highly potent inhibitorPARP12with s of 12 nM and 087 nM respectivelyKi

Bioactivity Talazoparib 8R9S (BMN-673 8R9S) is an enantiomer ofTalazoparib less active than Talazoparib on the inhibition of

with an of 144 nMPARP1 IC50

Bioactivity Talazoparib tosylate (BMN 673ts) is a novel potent and orallyavailable inhibitor with an of 057 nM forPARP12 IC50PARP1

Bioactivity UPF 1069 is a inhibitor with s of 8 and 03 μM forPARP IC50PARP-1 and PARP-2 respectively

Bioactivity Veliparib is a potent inhibitor inhibiting andPARP PARP1 with s of 52 and 29 nM respectivelyPARP2 Ki

Bioactivity Veliparib (dihydrochloride) is a potent inhibitor of and with s of 52PARP1 PARP2 Ki

nM and 29 nM in cell-free assays respectively

Bioactivity WD2000-012547 is a selective poly(ADP-ribose)-polymerase(PARP-1) inhibitor with a pK of 8221i

120 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Rucaparib (AG014699 PF-01367338) Cat No HY-10617A

Rucaparib Camsylate Cat No HY-102003

Rucaparib phosphate (AG-014699 phosphate PF-01367338 phosphate) Cat No HY-10617

Talazoparib (BMN-673 LT-673) Cat No HY-16106

Talazoparib 8R9S (BMN-673 (8R9S) (8R9S)-LT-673) Cat No HY-16106A

Talazoparib tosylate (BMN 673ts) Cat No HY-108413

UPF 1069 Cat No HY-14478

Veliparib (ABT-888) Cat No HY-10129

Veliparib dihydrochloride (ABT-888 dihydrochloride) Cat No HY-10130

WD2000-012547 Cat No HY-U00223

wwwMedChemExpresscom 121

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity XAV-939 is a inhibitor and an indirecttankyrase (TNKS)inhibitor of with s of 5 and 2Wntβ-catenin signaling IC50nM for TNKS1 and TNKS2 respectively

XAV-939 Cat No HY-15147

PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinase

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) isactivated in response to a variety of endoplasmic reticulum stressesimplicated in numerous disease states PERK is implicated intumorigenesis and cancer cell survival GSK2606414 is an orallyavailable potent and selective PERK inhibitor GSK2606414 inhibitsPERK activation in cells and inhibits the growth of a human tumorxenograft in mice PERK activation is independent of the largeincrease in unfolded nascent proteins within the ER followingtransient global brain ischemia

122 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 123

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

PERK Inhibitors amp Modulators

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity GSK2606414 is a cell-permeable and orally available proteinkinase R-like endoplasmic reticulum (ER) kinase (PERK)inhibitor with an of 04 nMIC50

Bioactivity GSK2656157 is a selective and ATP-competitive inhibitor ofprotein kinase R (PKR)-like endoplasmic reticulum kinase (

) with an of 09 nMPERK IC50

Bioactivity ISRIB (trans-isomer) is a potent inhibitor of with anPERK of 5 nMIC50

CCT020312 Cat No HY-119240

GSK2606414 Cat No HY-18072

GSK2656157 Cat No HY-13820

ISRIB trans-isomer Cat No HY-12495

Polo-like Kinase (PLK)

Polo-like Kinases (PLKs) are important regulators of the cell cycle Plksare involved in the formation of and the changes in the mitoticspindle and in the activation of CDKcyclin complexes duringM-phase of the cell cyclePolo-like kinases (Plks) are a family ofconserved serinethreonine kinases involved in the regulation of cellcycle progression through G2 and mitosis Mammalian polo-likekinases include Plk1 (Xenopus Plx1) Plk2Snk (Xenopus Plx2)Plk3PrkFnK (Xenopus Plx3) Plk4Sak and Plk5 Plk1 is involved in theregulation of key steps during cell division DNA damage repairpathways apoptosis and the progression of the cell cycle Plk3 is amultifunctional stress response protein that responses to signals

induced by DNA damage andor mitotic spindle disruption

124 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 125

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9982Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9897Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9857Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Polo-like Kinase (PLK) Inhibitors amp Modulators

Bioactivity BI 2536 is a dual and inhibitor with s of 083PLK1 BRD4 IC50

and 25 nM respectively BI-2536 suppresses IFNB[1]

(encoding IFN-β) gene transcription [4]

Bioactivity Centrinone (LCR-263) is a selective and reversible inhibitorof polo-like kinase 4 ( ) with a of 016 nMPlK4 Ki

Bioactivity Centrinone-B (LCR-323) is a potent and highly selective PLK4inhibitor with a of 059 nMKi

Bioactivity CFI-400945 free base is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity CFI-400945 fumarate is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity GSK461364 is a selective reversible and ATP-competitive inhibitor with a value of 22 nMPolo-like kinase 1 (PLK1) Ki

Bioactivity GW843682X is a selective ATP-competitive inhibitor of PLK1and with s of 22 nM and 91 nM respectively andPLK3 IC50is also gt100-fold selective against 30 other kinases

Bioactivity HMN-214 an orally bioavailable prodrug of HMN-176 is aninhibitor of polo-like kinase-1 ( ) with antitumorplk1activity

Bioactivity LFM-A13 is a potent inhibitor inhibitsBTK JAK2 PLKrecombinant BTK Plx1 and PLK3 with s of 25 μM 10 μM andIC5061 μM LFM-A13 shows no effects on JAK1 and JAK3 Src familykinase HCK EGFR and IRK

Bioactivity MLN0905 is a potent inhibitor with an of 2 nMPLK1 IC50

BI 2536 Cat No HY-50698

Centrinone (LCR-263) Cat No HY-18682

Centrinone-B (LCR-323) Cat No HY-18683

CFI-400945 free base Cat No HY-12300

CFI-400945 fumarate Cat No HY-12300B

GSK461364 (GSK461364A) Cat No HY-50877

GW843682X (GW843682) Cat No HY-11003

HMN-214 (IVX-214) Cat No HY-12045

LFM-A13 Cat No HY-18009

MLN0905 (PLK1 Inhibitor) Cat No HY-15155

Purity 9759Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9949Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9809Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9626Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9970Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

Bioactivity NMS-1286937 is a potent selective and orally available PLK1inhibitor with an of 2 nMIC50

Bioactivity Poloxime a hydrolysis product of poloxin is anon-ATP-competitive inhibitor with moderate Plk1Plk1inhibitory activity

Bioactivity Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1)inhibitor that targets the polo-box domain with an ofIC50appr 48 μM

Bioactivity Rigosertib (ON-01910) is a multi-kinase inhibitor and aselective anti-cancer agent which induces apoptosis byinhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib is a selective andhellip[1] [2]

Bioactivity Rigosertib sodium (ON-01910 sodium) is a multi-kinaseinhibitor and a selective anti-cancer agent which inducesapoptosis by inhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib sodium is a selective andhellip[1] [2]

Bioactivity Ro3280 is a potent highly selective inhibitor of withPLK1an and a of 3 nM and 009 nM respectively andIC50 Kdnearly has no effect on PLK2 and PLK3

Bioactivity SBE13 is a potent and selective inhibitor with an ofPlk1 IC50200 pM SBE13 poorly inhibits Plk2 (IC gt66 μM) or Plk350(IC =875 nM)50

Bioactivity SBE13 Hydrochloride is a potent and selective inhibitorPlk1with an of 200 pM SBE13 Hydrochloride poorly inhibitsIC50Plk2 (IC gt66 μM) or Plk3 (IC =875 nM)50 50

Bioactivity TAK-960 is an orally available selective inhibitor of with an of 08 nM at 10 μMpolo-like kinase 1 (PLK1) IC50

ATP TAK-960 also shows inhibitory activities against PLK2and with s of 169 and 502 nM respectivelyPLK3 IC50

126 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Mps1-IN-2 Cat No HY-13994

NMS-1286937 (NMS-P937) Cat No HY-15828

Poloxime Cat No HY-77195

Poloxin Cat No HY-12134

Rigosertib (ON-01910) Cat No HY-12037A

Rigosertib sodium (ON-01910 sodium) Cat No HY-12037

Ro3280 Cat No HY-15161

SBE13 Cat No HY-15158A

SBE13 Hydrochloride Cat No HY-15158

TAK-960 Cat No HY-15160

wwwMedChemExpresscom 127

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9955Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TAK-960 dihydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 dihydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TAK-960 hydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 hydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TC-S 7005 is a inhibitor with s ofPolo-like kinases (Plks) IC504 nM 24 nM and 214 nM for Plk2 Plk3 and Plk1 respectively

[1]

Bioactivity Volasertib is a highly potent Polo-like kinase 1 (PLK1)inhibitor with an of 087 nM as well as the two closelyIC50related kinases and with s of 5 and 56 nMPLK2 PLK3 IC50respectively

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

TAK-960 dihydrochloride Cat No HY-15160B

TAK-960 hydrochloride Cat No HY-15160A

TC-S 7005 Cat No HY-108597

Volasertib (BI 6727) Cat No HY-12137

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

PPARPeroxisome proliferator-activated receptors

PPARs (Peroxisome proliferator-activated receptors) areligand-activated transcription factors of nuclear hormone receptorsuperfamily comprising of the following three subtypes PPARαPPARγ and PPARβδ PPARs play essential roles in the regulation ofcellular differentiation development and metabolism (carbohydratelipid protein) and tumorigenesis of higher organisms All PPARsheterodimerize with the retinoid X receptor (RXR) and bind to specificregions on the DNA of target genes Activation of PPAR-α reducestriglyceride level and is involved in regulation of energy homeostasisActivation of PPAR-γ enhances glucose metabolism whereasactivation of PPAR-βδ enhances fatty acids metabolism

128 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 129

Purity 9905Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9921Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 980Clinical Data Phase 4Size 50 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg

Purity gt98Clinical Data Phase 2Size 1 mg

Purity 9900Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

PPAR Inhibitors amp Modulators

Bioactivity 4-O-Methyl honokiol is a natural neolignan isolated from acts as a agonist and inhibtisMagnolia officinalis PPARγ

activity used for cancer and inflammation researchNF-κB

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Adelmidrol exerts important anti-inflammatory effects that arepartly dependent on Adelmidrol reduces PPARγ NF-κBtranslocation and expressionCOX-2

Bioactivity Aleglitazar(R1439 RO-0728804) is a new dual PPAR-αγ agonistwith IC50 of 28 nM46 nM

Bioactivity Arhalofenate (MBX 102) is a selective partial agonist ofperoxisome proliferator-activated receptor used for(PPAR)-γthe treatment of type 2 diabetes

Bioactivity Astaxanthin a red dietary carotenoid isolated from is an inhibitor of and aHaematococcus pluvialis PPARγ

potent antioxidant with antiproliferative neuroprotective andanti-inflammatory activity Astaxanthin has potential in[1]

the treatment of various diseases such as cancers andhellip

Bioactivity Astragalus polysaccharide are active components of thepolysaccharides extract of Astragulus attenuatesTNF-α-induced insulin resistance by suppressing miR-721 andactivating and in 3T3-L1 adipocytesPPAR-γ PI3KAkt

Bioactivity AVE-8134 is a potent agonist with values of 100PPARα EC50and 3000 nM for human and rodent PPARα receptor respectively

Bioactivity Balaglitazone is a selective partial agonist with anPPARγ of 1351 μM for human EC50 PPARγ

Bioactivity Bezafibrate is an agonist of with s of 50 μM 60PPAR EC50μM 20 μM for and and 90 μMhuman PPARα PPARγ PPARδ55 μM 110 μM for and murine PPARα PPARγ PPARδrespectively Bezafibrate is used as an hypolipidemic agent

4-O-Methyl honokiol Cat No HY-U00450

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Adelmidrol Cat No HY-B1026

Aleglitazar (R1439 RO0728804) Cat No HY-14728

Arhalofenate (MBX 102 JNJ 39659100) Cat No HY-14831

Astaxanthin Cat No HY-B2163

Astragalus polysaccharide (Astragalus Polysacharin) Cat No HY-N0937

AVE-8134 Cat No HY-U00014

Balaglitazone (DRF 2593 NN 2344) Cat No HY-16086

Bezafibrate (BM15075) Cat No HY-B0637

Purity 9877Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data Phase 4Size 10mM x 1mL in DMSO

500 mg 1 g 5 g 10 g

Purity 9959Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9981Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BMS-687453 is a potent and selective agonist with anPPARα and of 10 nM and 260 nM for human and 4100EC50 IC50 PPARα

nM and gt15000 nM for PPARγ in PPAR-GAL4 transactivationassays

Bioactivity CDDO-Im (CDDO-imidazolide) is an activator of and Nrf2 PPARwith s of 232 and 344 nM for PPARα and PPARγKi

Bioactivity Chiglitazar is a dual agonist with of 12PPARαγ EC s50008 17 μM for PPARα PPARγ and PPARδ respectively

Bioactivity Choline Fenofibrate (ABT-335) is the choline salt offenofibric acid under clinical development as a combinationtherapy with rosuvastatin for the management of dyslipidemia

Bioactivity Ciprofibrate is a peroxisome proliferator-activated receptoragonist

Bioactivity Ciprofibrate D6 is deuterium labeled Ciprofibrate which is aperoxisome proliferator-activated receptor agonist

Bioactivity Clofibrate is an agonist of with s of 50 μM 500PPAR EC50μM for murine PPARα and PPARγ and 55 μM 500 μM for humanPPARα and PPARγ respectively

Bioactivity Daidzein is a soy isoflavone which acts as a activatorPPAR

Bioactivity DG172 dihydrochloride is a selective antagonist withPPARβδan of 27 nMIC50

Bioactivity Elafibranor is a agonist with s of 45 and 175PPARαδ EC50nM respectively

130 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

BMS-687453 Cat No HY-10678

CDDO-Im (RTA-403 TP-235 CDDO-Imidazolide) Cat No HY-15725

Chiglitazar Cat No HY-106266

Choline Fenofibrate (ABT-335) Cat No HY-14739

Ciprofibrate (Win35833) Cat No HY-B0664

Ciprofibrate D6 Cat No HY-B0664S

Clofibrate Cat No HY-B0287

Daidzein Cat No HY-N0019

DG172 dihydrochloride Cat No HY-19737A

Elafibranor (GFT505) Cat No HY-16737

wwwMedChemExpresscom 131

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Ertiprotafib is an inhibitor of PTP1B IkB kinase β (IKK-β)and a dual agonist with an of 16 μMPPARα and PPARβ IC50for PTP1B 400 nM for IKK-β an of ~1 μM forEC50PPARαPPARβ

Bioactivity Eupatilin a lipophilic flavonoid isolated from Artemisiaspecies is a agonist and possesses anti-apoptoticPPARαanti-oxidative and anti-inflammatory activities

Bioactivity Fenofibrate is a agonist with an of 30 μMPPARα EC50 Bioactivity Fenofibric acid an active metabolite of fenofibrate is a activitor with s of 224 microM 147 microM and 106 microMPPAR EC50

for PPARα PPARγ and PPARδ respectively Fenofibric acid alsoinhibits enzyme activity with an of 48 nMCOX-2 IC50

Bioactivity FH535 is an inhibitor of and withWntβ-catenin PPARanti-tumor activities

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Fonadelpar is a agonist used in the research ofPPARδneuroparalytic keratopathy

Bioactivity Gemfibrozil is an activator of used as aPPAR-αlipid-lowering drug Gemfibrozil is also a nonselectiveinhibitor of several isoforms with values forP450 KiCYP2C9 2C19 2C8 and 1A2 of 58 24 69 and 82 μMrespectively

Bioactivity Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2Sanchinoside Rh1) is isolated from the root of Panax GinsengGinsenoside Rh1 inhibits the expression of PPAR-γ TNF-α

and IL-6 IL-1β

Bioactivity Glabridin is a natural isoflavan from bindsGlycyrrhiza glabrato and activates with an of 6115 nM GlabridinPPARγ EC50exhibits antioxidant anti-bacterial anti-nephriticanti-diabetic anti-fungal antitumor anti-inflammatoryantiosteoporotic cardiovascular protective neuroprotectivehellip

Ertiprotafib (PTP 112) Cat No HY-19383

Eupatilin Cat No HY-N0783

Fenofibrate Cat No HY-17356

Fenofibric acid (FNF acid) Cat No HY-B0760

FH535 Cat No HY-15721

Fisetin Cat No HY-N0182

Fonadelpar (NPS-005 SJP-0035) Cat No HY-17633

Gemfibrozil (CI-719) Cat No HY-B0258

Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2 Sanchinoside Rh1) Cat No HY-N0604

Glabridin Cat No HY-N0393

Purity 9875Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9727Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9667Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity GSK0660 is a potent antagonist of and withPPARβ PPARδs of 155 nM for both isoformsIC50

Bioactivity GSK376501A is a selective peroxisome proliferator-activatedreceptor gamma ( ) modulator for the treatment of type 2PPARγdiabetes mellitus

Bioactivity GSK3787 is a selective and irreversible peroxisomeproliferator-activated receptor δ ( ) antagonist withPPARδ

of 66pIC50

Bioactivity GW 501516 is a agonist with an of 11 nMPPARδ EC50

Bioactivity GW 6471 is a potent antagonistPPARα Bioactivity GW0742 is a potent and agonist with an ofPPARβ PPARδ IC501 nM for human in binding assay and s of 1 nMPPARδ EC5011 μM and 2 μM for human PPARα and PPARγPPARδrespectively

Bioactivity GW1929 is a potent agonist with a of 884 forPPAR-γ pKihuman and s of 856 and 827 for human PPAR-γ pEC50 PPAR-γ

and murine respectivelyPPAR-γ

Bioactivity GW7647 is a potent agonist with s of 6 nM 11PPARα EC50μM and 62 μM for human PPARα PPARγ and PPARδ respectively

Bioactivity GW9662 is a potent and selective antagonist with anPPARγ of 33 nM showing 10 and 1000-fold selectivity overIC50

PPARα and PPARδ respectively

Bioactivity Icariin is a flavonol glycoside Icariin inhibits andPDE5 activities with s of 432 nM and 7350 μMPDE4 IC50

respectively Icariin also is a activatorPPARα

132 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

GSK0660 Cat No HY-12377

GSK376501A Cat No HY-101746

GSK3787 Cat No HY-15577

GW 501516 (GW 1516 GSK-516) Cat No HY-10838

GW 6471 Cat No HY-15372

GW0742 (GW610742) Cat No HY-13928

GW1929 Cat No HY-15655

GW7647 Cat No HY-13861

GW9662 Cat No HY-16578

Icariin (Ieariline) Cat No HY-N0014

wwwMedChemExpresscom 133

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9889Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9921Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 2Size 5 mg

Purity 9942Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Bioactivity Imiglitazar (TAK559) is a potent and dual human andPPARα agonist with values of 67 and 31 nMPPARγ1 EC50

Bioactivity Indeglitazar is an orally available peroxisomeproliferator-activated receptor ( ) pan-agonist for allPPARthree PPAR subtypes alpha (α) delta (δ) and gamma (γ)

Bioactivity Inolitazone a novel high-affinity agonist that isPPARγdependent upon PPARγ for its biological activity with ofIC5008 nM for growth inhibition

Bioactivity Inolitazone dihydrochloride is a novel high-affinity PPARγagonist that is dependent upon PPARγ for its biologicalactivity with of 08 nM for growth inhibitionIC50

Bioactivity KD3010 is a potent orally active and selective PPARδagonist

Bioactivity L-165041 is a cell permeable agonist with s of 6 nMPPARδ Kiand appr 730 nM for PPARδ and PPARγ respectively and inducesadipocyte differentiation in NIH-PPARδ cells

Bioactivity Lanifibranor is a pan peroxisome proliferator-activated ( ) agonist with s of 15 087 and 021receptor PPAR EC50

μM for human and respectivelyPPARα PPARσ PPARγ

Bioactivity LJ570 is a dual agonist with s of 105PPARα PPARγ EC50

and 012 μM respectively [1]

Bioactivity MA-0204 is a potent highly selective and orally availableperoxisome proliferator activated receptor δ ( )PPARδmodulator with s of 04 nM 79 nM and 10 nM for humanEC50mouse and rat PPARδ respectively Potential treatment hellip

Bioactivity Magnolol a natural lignan isolated from the stem bark of is a dual agonist of both andMagnolia officinalis RXRα

with values of 104 microM and 177 microMPPARγ EC50respectively

Imiglitazar (TAK-559) Cat No HY-101649

Indeglitazar (PPM 204) Cat No HY-14817

Inolitazone (Efatutazone CS-7017 RS5444) Cat No HY-14792

Inolitazone dihydrochloride (Efatutazone (dihydrochloride)

CS-7017 (dihydrochloride) RS5444 (dihydrochloride)) Cat No HY-14792B

KD-3010 Cat No HY-111068

L-165041 Cat No HY-20019

Lanifibranor (IVA337) Cat No HY-104049

LJ570 Cat No HY-111775

MA-0204 Cat No HY-114739

Magnolol Cat No HY-N0163

Purity 9639Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9918Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in Ethanol

10 mg

Purity gt98Clinical DataSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9872Clinical Data Phase 1Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Bioactivity Naringenin is the predominant flavanone in grapefruitdisplays strong anti-inflammatory and antioxidant activities

Bioactivity Naveglitazar racemate is the racemate of NaveglitazarNaveglitazar is a nonthiozolidinedione peroxisomeproliferator-activated receptor ( ) α-γ dual γ-dominantPPARagonist that has shown glucose-lowering potential in animalmodels and in the clinic

Bioactivity NXT629 is a potent selective and competitive PPAR-αantagonist with an of 77 nM for human PPARα shows highIC50selectivity over other nuclear hormone receptor such asPPARδ PPARγ ERβ GR and TRβ s are 60 15 152 3hellipIC50

Bioactivity Oleoylethanolamide is a high affinity endogenous PPAR-αagonist which plays an important role in the treatment ofobesity and arteriosclerosis

Bioactivity Palmitelaidic acid is the trans isomer of palmitoleic acidPalmitoleic acid is one of the most abundant fatty acids inserum and tissue

Bioactivity Peliglitazar racemate is the racemate of PeliglitazarPeliglitazar is a novel dual αγ PPAR activator

Bioactivity Pemafibrate is a highly selective agonist with anPPARα of 1 nMEC50

Bioactivity Pemafibrate racemate is the racemate of pemafibrate andactivates activity with s of 1 nM gt10 μM andPPARα EC5017 μM for h-PPARα h-PPARγ and h-PPARδ respectively

Bioactivity Pioglitazone is a potent and selective agonist withPPARγhigh affinity binding to the PPARγ ligand-binding domain with

of 093 and 099 μM for human and mouse PPARγEC50respectively

Bioactivity Pioglitazone hydrochloride is a potent and selective PPARγagonist with s of 093 and 099 μM for human and mouseEC50PPARγ respectively

134 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Naringenin Cat No HY-N0100

Naveglitazar racemate Cat No HY-U00036

NXT629 Cat No HY-114263

Oleoylethanolamide (N-(2-Hydroxyethyl)oleamide

N-Oleoyl-2-aminoethanol N-Oleoylethanolamide hellip) Cat No HY-107542

Palmitelaidic Acid (9-trans-Hexadecenoic acid trans-Palmitoleic acid) Cat No HY-N2341

Peliglitazar racemate (BMS 426707-01 racemate) Cat No HY-101738A

Pemafibrate ((R)-K-13675) Cat No HY-17618

Pemafibrate racemate (K13675 (racemate)) Cat No HY-17618A

Pioglitazone (U 72107) Cat No HY-13956

Pioglitazone hydrochloride (U 72107A AD 4833) Cat No HY-14601

wwwMedChemExpresscom 135

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9836Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 250 mg

Bioactivity Pirinixic acid (Wy-14643) is a potent agonist of withPPARαs of 063 μM 32 μM for murine and PPARγ and 50EC50 PPARα

μM 60 μM 35 μM for human PPARγ and PPARδPPARαrespectively

Bioactivity PPAR agonist 1 is an agonist of and usedPPAR α PPAR γfor reducing blood glucose lipid levels lowering cholesteroland reducing body weight

Bioactivity PPARα-MO-1 is a potent modulator extracted from patentPPARαWO2004110982A1 formula I

Bioactivity PPARδ agonist is a agonist extracted from patentPPARδUS20180071304 compound example 10

Bioactivity Pparδ agonist 1 is a agonist with an of 506PPAR-δ EC50nM used in the research of PPAR-delta related diseases suchas mitochondrial diseases muscular diseases vasculardiseases demyelinating diseases and metabolic diseases

Bioactivity Pparδ agonist 2 is a agonist extracted from patent WOPPARδ2016057656 A1

Bioactivity Raspberry ketone is a major aromatic compound of redraspberry widely used as a fragrance in cosmetics and as aflavoring agent in foodstuff also shows agonisticPPAR-αactivity

Bioactivity Retinoic acid is a metabolite of vitamin A that playsimportant roles in cell growth differentiation andorganogenesis Retinoic acid is a natural agonist of RARnuclear receptors with s of 14 nM for RARαβγ RetinhellipIC50

Bioactivity RG-12525 is a a specific competitive and orally effectiveantagonist of the and peptidoleukotrienes LTC4 LTD4 LTE4inhibiting LTC4- LTD4- and LTE4-inducd guinea pig parenchymalstrips contractions with s of 26 nM 25 nM and 7 nMIC50respectively RG-12525 is also a peroxisomehellip

Bioactivity Rosiglitazone (BRL49653) is a selective agonist withPPARγs of 30 nM 100 nM and 60 nM for andEC50 PPARγ1 PPARγ2

respectivelyPPARγ

Pirinixic acid (Wy-14643) Cat No HY-16995

PPAR agonist 1 Cat No HY-U00340

PPARα-MO-1 Cat No HY-U00068

Pparδ agonist Cat No HY-112597

Pparδ agonist 1 Cat No HY-107901

Pparδ agonist 2 Cat No HY-100120

Raspberry ketone (Frambione 4-(4-Hydroxyphenyl)-2-butanone) Cat No HY-N1426

Retinoic acid (ATRA Tretinoin Vitamin A acid all-trans-Retinoic acid) Cat No HY-14649

RG-12525 (NID 525) Cat No HY-101676

Rosiglitazone (BRL49653) Cat No HY-17386

Purity 9953Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9852Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9885Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9803Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9925Clinical Data LaunchedSize 100 mg 500 mg

Bioactivity Rosiglitazone maleate is a potent and selective activator of with s of 30 nM 100 nM and 60 nM for PPARγ EC50 PPARγ1

and respectively and a of appr 40 nMPPARγ2 PPARγ Kdfor Rosiglitazone maleate is also an modulator of PPARγ hellip

Bioactivity Saroglitazar is a novel peroxisome proliferator-activatedreceptor ( ) agonist with predominant PPARα and moderatePPARPPARγ activity with values of 065 pM and 3 nM in HepG2EC50cells respectively

Bioactivity Saroglitazar magnesium is a novel peroxisomeproliferator-activated receptor ( ) agonist withPPARpredominant PPARα and moderate PPARγ activity with EC50values of 065 pM and 3 nM in HepG2 cells respectively

Bioactivity Seladelpar is an orally active potent (50 effectconcentration 2 nM) and specific agonistEC50 PPAR-δ

Bioactivity Seladelpar sodium salt (MBX-8025) is an orally active potentand specific agonist with an of 2 nM showingPPARδ EC50more than 750-fold and 2500-fold selectivity over the PPARαand PPARγ receptors respectively

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

Bioactivity Troglitazone is a agonist with s of 550 nM andPPARγ EC50780 nM for human and murinePPARγ receptor respectively

136 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Rosiglitazone maleate (BRL 49653C) Cat No HY-14600

Saroglitazar Cat No HY-19937

Saroglitazar Magnesium Cat No HY-19937A

Seladelpar (MBX-8025) Cat No HY-19522

Seladelpar sodium salt (MBX-8025 sodium salt RWJ-800025 sodium salt) Cat No HY-19522A

T0070907 Cat No HY-13202

Troglitazone (CS-045) Cat No HY-50935

wwwMedChemExpresscom 137

RAD51

RAD51 protein family assist in repair of DNA double strand breaksRAD51 family members are homologous to the bacterial RecA andyeast Rad51 In humans RAD51 is a 339-amino acid protein that playsa major role in homologous recombination of DNA during doublestrand break repair RAD51 is involved in the search for homologyand strand pairing stages of the process RAD51 can interact with thessDNA-binding protein RPA BRCA2 PALB2 and RAD52 Recentstudies using fluorescent labeled Rad5 has indicated that Rad51fragments elongate via multiple nucleation events followed bygrowth with the total fragment terminating when it reaches about 2μm in length

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

500 mg

RAD51 Inhibitors amp Modulators

Bioactivity Harmine is a natural dual-specificity tyrosinephosphorylation-regulated kinase ( ) inhibitor with(DYRK)anticancer and anti-inflammatory activities

Bioactivity IBR2 is a specific inhibitorRAD51

Bioactivity RAD51 Inhibitor B02 (B02) is an inhibitor of human withRAD51an of 274 μMIC50

Bioactivity RAD51-IN-2 (compound example 67A) is a inhibitorRAD51extracted from patent WO2019051465A1 [1]

Bioactivity RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM Bioactivity RI-2 is a reversible inhibitor with an of 4417RAD51 IC50μM and specifically inhibits homologous recombination repairin human cells

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

138 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Harmine (Telepathine) Cat No HY-N0737A

IBR2 Cat No HY-103710

RAD51 Inhibitor B02 (B02) Cat No HY-101462

RAD51-IN-2 Cat No HY-111887

RI-1 Cat No HY-15317

RI-2 Cat No HY-16904

RS-1 Cat No HY-19793

T0070907 Cat No HY-13202

wwwMedChemExpresscom 139

ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROK

ROCK (Rho-associated protein kinase) is a kinase belonging to theAGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopusinvertebrates and chicken Human ROCK1 has a molecular mass of158 kDa and is a major downstream effector of the small GTPaseRhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces thekinase activity of ROCKs by an autoinhibitory intramolecular fold ifRhoA-GTP is not present ROCK plays a role in a wide range ofdifferent cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators

of the cytoskeleton

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9954Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

ROCK Inhibitors amp Modulators

Bioactivity AT13148 is an orally active and ATP-competitive multi- AGC inhibitor with s of 38 nM402 nM50 nM 8 nM 3 nMkinase IC50

and 6 nM4 nM for Akt123 p70S6K PKA and ROCKIIIrespectively

Bioactivity Azaindole 1 is an orally active and ATP-competitive ROCKinhibitor with s of 06 and 11nM for human andIC50 ROCK-1

respectivelyROCK-2

Bioactivity BDP5290 is a potent inhibitor of both and withROCK MRCKs of 5 nM 50 nM 10 nM and 100 nM for IC50 ROCK1 ROCK2

and respectivelyMRCKα MRCKβ

Bioactivity Chroman 1 is a highly potent inhibitor with an ofROCK2 IC501 nM

Bioactivity Fasudil (HA-1077 AT877) a potent inhibitor of with aROCK of 033 μM for ROCK1 which is also a potent Ki Ca channel2+

antagonist and vasodilator

Bioactivity Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877Hydrochloride) a potent inhibitor of with a of 033ROCK Ki

μM for ROCK1 which is also a potent antagonistCa channel2+

and vasodilator

Bioactivity GSK180736A is a G protein-coupled receptor kinase 2 ( )GRK2inhibitor with an of 077 μMIC50

Bioactivity GSK269962A is a potent inhibitor with s of 16 and 4ROCK IC50nM for recombinant human and respectivelyROCK1 ROCK2

Bioactivity GSK429286A is a selective inhibitor of with an ROCK1 IC50value of 14 nM

Bioactivity H-1152 is a membrane-permeable and selective inhibitorROCKwith a value of 16 nM and an value of 12 nM forKi IC50

ROCK2

140 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

AT13148 Cat No HY-16071

Azaindole 1 (TC-S 7001) Cat No HY-10319

BDP5290 Cat No HY-12437

Chroman 1 Cat No HY-15392

Fasudil (HA-1077 AT877) Cat No HY-10341A

Fasudil Hydrochloride (HA-1077 (Hydrochloride) AT-877 (Hydrochloride)) Cat No HY-10341

GSK180736A Cat No HY-18990

GSK269962A (GSK 269962) Cat No HY-15556

GSK429286A Cat No HY-11000

H-1152 Cat No HY-15720

wwwMedChemExpresscom 141

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9726Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical DataSize 10 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9929Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9940Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9813Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity H-1152 dihydrochloride is a membrane-permeable and selective inhibitor with a value of 16 nM and an valueROCK Ki IC50

of 12 nM for ROCK2

Bioactivity Hydroxyfasudil is a inhibitor with s of 073 andROCK IC50072 μM for and respectivelyROCK1 ROCK2

Bioactivity Hydroxyfasudil hydrochloride is a inhibitor with sROCK IC50of 073 and 072 μM for and respectivelyROCK1 ROCK2

Bioactivity LX7101 is a potent inhibitor of and with LIMK ROCK2 IC50values of 24 16 and 10 nM for LIMK1 LIMK2 and ROCK2respectively also inhibits with an less than 1 nMPKA IC50

Bioactivity Narciclasine is a plant growth modulator Narciclasinemodulates the RhoRho kinaseLIM kinasecofilin signalingpathway greatly increasing GTPase RhoA activity as well asinducing actin stress fiber formation in a RhoA-dependentmanner

Bioactivity Pentanoic acid a short-chain fatty acid is a product ofbacterial metabolism and are associated with allergic skindisorders Pentanoic acid activates signaling pathwayROCK

Bioactivity Ripasudil (K-115) is a specific inhibitor of with sROCK IC50of 19 and 51 nM for and respectivelyROCK2 ROCK1

Bioactivity Ripasudil free base (K-115 free base) is a specific inhibitorof with s of 19 and 51 nM for and ROCK IC50 ROCK2 ROCK1

respectively

Bioactivity RKI-1447 is a potent small molecule inhibitor of andROCK1 with values of 145 nM and 62 nM respectivelyROCK2 IC50

Bioactivity ROCK inhibitor-2 is a selective dual and ROCK1 ROCK2inhibitor with s of 17 nM and 2 nM respectively IC50

[1]

H-1152 dihydrochloride Cat No HY-15720A

Hydroxyfasudil (HA-1100) Cat No HY-13911

Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100

hydrochloride HA1100 hydrochloride) Cat No HY-13911A

LX7101 Cat No HY-12659

Narciclasine (Lycoricidinol) Cat No HY-16563

Pentanoic acid Cat No HY-N6056

Ripasudil (K-115) Cat No HY-15685

Ripasudil free base (K-115 (free base)) Cat No HY-15685A

RKI-1447 Cat No HY-15755

ROCK inhibitor-2 Cat No HY-119937

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2g

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9843Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Bioactivity ROCK-IN-1 is a potent inhibitor of with an of 12ROCK IC50nM for ROCK2

Bioactivity ROCK2-IN-2 is a selective inhibitor extracted fromROCK2patent US20180093978A1 Compound A-30 has an of lt1IC50μM

Bioactivity SAR407899 is a selective potent and ATP-competitive ROCKinhibitor with an of 135 nM for and s of 36IC50 ROCK-2 KinM and 41 nM for human and rat respectivelyROCK-2

Bioactivity SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an of 135 nM forROCK IC50

and s of 36 nM and 41 nM for human and rat ROCK-2 Ki ROCK-2

respectively

Bioactivity SB-772077B dihydrochloride is an aminofurazan-based Rho inhibitor with s of 56 nM and 6 nM towardkinase( ROCK) IC50

ROCK1 and ROCK2 respevtively [1]

Bioactivity SLx-2119 (KD-025) is a selective inhibitor of with anROCK2 of 105 nMIC50

Bioactivity SR-3677 is a potent and selective inhibitor with anROCK-II of ~3 nMIC50

Bioactivity Thiazovivin is a potent inhibitor which can protectROCKhuman embryonic stem cells

Bioactivity Y-27632 is an ATP-competitive inhibitor of and ROCK-I ROCK-IIwith of 220 nM and 300 nM for and Ki ROCK-I ROCK-II

respectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

Bioactivity Y-27632 dihydrochloride is a cell-permeable ATP-competitiveinhibitor of and with s of 220 and 300 nMROCK-I ROCK-II Kirespectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

142 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

ROCK-IN-1 Cat No HY-U00351

ROCK2-IN-2 Cat No HY-103620

SAR407899 Cat No HY-15687A

SAR407899 hydrochloride Cat No HY-15687

SB-772077B dihydrochloride Cat No HY-108518

SLx-2119 (KD-025) Cat No HY-15307

SR-3677 Cat No HY-13300

Thiazovivin Cat No HY-13257

Y-27632 Cat No HY-10071

Y-27632 dihydrochloride Cat No HY-10583

wwwMedChemExpresscom 143

Purity 9923Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity Y-33075 is a selective inhibitor derived from Y-27632ROCKand is more potent than Y-27632 with an of 36 nMIC50

Bioactivity Y-33075 dihydrochloride is a selective inhibitor with anROCK of 36 nMIC50

Bioactivity ZINC00881524 is a inhibitorROCK

Y-33075 (Y 39983) Cat No HY-10067

Y-33075 dihydrochloride Cat No HY-10069

ZINC00881524 Cat No HY-101244

Sirtuin

Sirtuin (Sir2 proteins) are a class of proteins that possess eithermono-ADP-ribosyltransferase or deacylase activity includingdeacetylase desuccinylase demalonylase demyristoylase anddepalmitoylase activity Sirtuins regulate important biologicalpathways in bacteria archaeaand eukaryotes Sirtuins have beenimplicated in influencing a wide range of cellular processes like agingtranscription apoptosis inflammation and stress resistance as well asenergy efficiency and alertness during low-calorie situations Sirtuinscan also control circadian clocks and mitochondrial biogenesis

144 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 145

Purity 9891Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9909Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Sirtuin Inhibitors amp Modulators

Bioactivity 3-TYP is a selective inhibitor with an of 16 nMSIRT3 IC50more potent over SIRT1 ( =88 nM) SIRT2 ( =92 nM)IC50 IC50

Bioactivity AGK2 is a selective inhibitor with of 35 μM AGK2SIRT2 IC50can also inhibit and with of 30 and 91 μMSIRT1 SIRT3 IC50respectively

Bioactivity AK-1 is a potent specific and cell-permeable inhibitorSIRT2with an of 125 μMIC50

Bioactivity AK-7 is a selective cell- and brain-permeable inhibitorSIRT2with an of 155 μMIC50

Bioactivity Cambinol is a and inhibitor with values of 56SIRT1 SIRT2 IC50and 59 μM respectively

Bioactivity CAY10602 is a activatorSIRT1

Bioactivity Dihydrocoumarin is a compound found in Melilotus Dihydrocoumarin is a inhibitorofficinalis yeast Sir2p

Dihydrocoumarin also inhibits and withhuman SIRT1 SIRT2s of 208 μM and 295 μM respectively IC50

[1]

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Ginkgolide C is a flavone isolated from leavesGinkgo bilobapossessing multiple biological functions such as decreasingplatelet aggregation and ameliorating Alzheimer disease

Bioactivity Inauhzin is a dual inhibitor and acts as anSirT1IMPDH2activator used in the research of cancerp53

3-TYP Cat No HY-108331

AGK2 Cat No HY-100578

AK-1 Cat No HY-101465

AK-7 Cat No HY-16691

Cambinol Cat No HY-100732

CAY10602 Cat No HY-104073

Dihydrocoumarin (Hydrocoumarin Chroman-2-one) Cat No HY-N1926

Fisetin Cat No HY-N0182

Ginkgolide C (BN-52022 Ginkgolide-C) Cat No HY-N0785

Inauhzin (INZ) Cat No HY-15869

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9876Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity MC3482 is a specific sirtuin5 ( ) inhibitorSIRT5 Bioactivity Nicotinamide is a form of vitamin B3 that plays essentialroles in cell physiology through facilitating NAD+ redoxhomeostasis and providing NAD+ as a substrate to a class ofenzymes that catalyze non-redox reactions Nicotinamide is aninhibitor of SIRT1

Bioactivity OSS_128167 is a selective inhibitor with s of 89SIRT6 IC501578 and 751 μM for and respectivelySIRT6 SIRT1 SIRT2

Bioactivity PROTAC Sirt2 Degrader-1 is a SirReal-based acts as aPROTAC degrader composed of a highly potent andSirt2

isotype-selective inhibitor a linker and a bona fideSirt2cereblon ligand for E3 ubiquitin ligase PROTAC Sirt2Degrader-1 shows an of 025 μM for Sirt2 with no effecthellipIC50

Bioactivity Salermide is an inhibitor of and can cause strongSirt1 Sirt2cancer-specific apoptotic cell death

Bioactivity Selisistat (EX-527) is a potent and selective inhibitorSIRT1with of 98 nMIC50

Bioactivity Selisistat S-enantiomer (EX-527 S-enantiomer) is theS-enantiomer of Selisistat with an of 123 nM for SIRT1IC50Selisistat S-enantiomer is much more potent than SelisistatR-enantiomer

Bioactivity SIRT-IN-1 is a potent inhibitor of with of 15SIRT123 IC s5010 33 μM respectively

Bioactivity SIRT-IN-2 is a potent inhibitor of with of 4SIRT123 IC s504 7 μM respectively

Bioactivity Sirt2-IN-1 (Compound 9) is a ( ) inhibitor withsirtuin 2 Sirt2an of 163 nM IC50

[1]

146 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

MC3482 Cat No HY-112587

Nicotinamide (Niacinamide Nicotinic acid amide Vitamin B3) Cat No HY-B0150

OSS_128167 Cat No HY-107454

PROTAC Sirt2 Degrader-1 Cat No HY-103636

Salermide Cat No HY-101073

Selisistat (EX-527) Cat No HY-15452

Selisistat S-enantiomer (EX-527 (S-enantiomer)) Cat No HY-15452A

SIRT-IN-1 Cat No HY-16615

SIRT-IN-2 Cat No HY-16616

Sirt2-IN-1 Cat No HY-112427

wwwMedChemExpresscom 147

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9939Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9887Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9944Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity SIRT5 inhibitor 1 is a potent Human deacylaseSirtuin 5inhibitor with an of 011 μMIC50

Bioactivity Sirtinol is a inhibitor with s of 48 μM 577 μMsirtuin IC50and 131 μM for ySir2 hSIRT2 and hSIRT2 respectively

Bioactivity Sirtuin modulator 1 is a modulator of a homolog of SIRTl SIRT3with EC of lt 1 μM extracted from patent WO 201007185315A1 Compound No4

Bioactivity SRT 1460 a potent activator with an Sirtuin-1 (SIRT1) EC15value of 29 μM shows good selectivity for activation ofSIRT1 versus SIRT2 and SIRT3 (EC15 gt 300 μM) and is morepotent than Resveratrol and the closest sirtuin homologhellip

Bioactivity SRT 1720 is a selective activator of human with anSIRT1 of 016 μM and shows less potent activities agaiinstEC15

SIRT2 and SIRT3 with EC s of 37 μM and gt 300 μM15respectively

Bioactivity SRT 1720 Hydrochloride is a selective activator of withSIRT1an of 016 μM and shows less potent activities onEC15SIRT2 and SIRT3 with EC s of 37 μM and 300 μM15respectively

Bioactivity SRT 2104 is a first-in-class highly selective andbrain-permeable activator of the NAD dependent deacetylase+

increases Sirt1 protein but shows no effect on Sirt1Sirt1mRNA Used in the research of diabetes mellitus hellip

Bioactivity SRT 2183 is a selective activator with anSirtuin-1 (SIRT1) value of 036 μM SRT 2183 induces growth arrestEC15

[1]

and apoptosis concomitant with deacetylation of STAT3 andNF-κB and reduction of c-Myc protein levels [2]

Bioactivity Tenovin-1 is an inhibitor of and ansirtuin 1 sirtuin 2activator of and may have potential in the management ofp53cancer

Bioactivity Tenovin-6 is an inhibitor of and slightly inhibitsSIRT1 SIRT2 and is also a potent activator of with s ofHDAC8 p53 IC50

21 μM 10 μM and 67 μM for SirT1 SirT2 and SirT3respectively

SIRT5 inhibitor 1 Cat No HY-112634

Sirtinol Cat No HY-13515

Sirtuin modulator 1 Cat No HY-19758A

SRT 1460 Cat No HY-124037

SRT 1720 Cat No HY-10532

SRT 1720 Hydrochloride Cat No HY-15145

SRT 2104 Cat No HY-15262

SRT 2183 Cat No HY-19759

Tenovin-1 Cat No HY-13423

Tenovin-6 Cat No HY-15510

Purity 9855Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Tenovin-6 Hydrochloride is an inhibitor of and SIRT1 SIRT2slightly inhibits and is also a potent activator ofHDAC8

with s of 21 μM 10 μM and 67 μM for SirT1 SirT2p53 IC50and SirT3 respectively

Bioactivity Thiomyristoyl is a potent and specific inhibitor with anSIRT2 of 28 nMIC50

Bioactivity UBCS039 is the first synthetic specific Sirtuin 6 (SIRT6)activator inducing autophagy in human tumor cells with an

of 38 μM EC50[1]

148 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Tenovin-6 Hydrochloride Cat No HY-15510B

Thiomyristoyl Cat No HY-101278

UBCS039 Cat No HY-115453

wwwMedChemExpresscom 149

SRPKSerine-arginine protein kinases

SRPKs is a critical enzyme family that regulates splicing activity in thecell The first serine-arginine (SR) protein kinase identified is SRPK1which is isolated from mitotic cells and it is described tophosphorylate SR proteins and to promote their release from nuclearspeckles during the G2M phase of the cell cycle SRPK1 is theprototype of the SRPK family which also includes the twohomologous SRPK2 and SRPK3 proteins SRPKs are characterized by abipartite catalytic domain separated by a unique spacer sequence andare mainly localized in the cytoplasm of mammalian cellsSRPKs can translocate into the nucleus of cells under severalconditions such as during the G2M phase of the cell cycle or after

osmotic stress or as a consequence of activation of the epidermal growth factor (EGF) signal transduction pathway

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9917Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

SRPK Inhibitors amp Modulators

Bioactivity SPHINX31 is a potent and selective inhibitor of with an ofserinearginine-rich protein kinase 1 (SRPK1) IC50

59 nM SPHINX31 inhibits phosphorylation ofserinearginine-rich splicing factor 1 (SRSF1) SPHINX31 is apotential topical therapeutic for neovascular eye diseasehellip

Bioactivity SRPIN340 is an ATP-competitive serine-arginine-rich proteinkinase ( ) inhibitor with a of 089 μM for SRPK1SRPK Ki

Bioactivity SRPKIN-1 is a covalent and irreversible inhibitorSRPK12with s of 356 and 98 nM respectively Anti-angiogenesisIC50

effect [1]

150 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SPHINX31 Cat No HY-117661

SRPIN340 (SRPK inhibitor) Cat No HY-13949

SRPKIN-1 Cat No HY-116856

wwwMedChemExpresscom 151

Telomerase

Telomerase is a ribonucleoprotein that is an enzyme that adds DNAsequence repeats (TTAGGG in all vertebrates) to the 3 end of DNAstrands in the telomere regions which are found at the ends ofeukaryotic chromosomes This region of repeated nucleotide calledtelomeres contains noncoding DNA and hinders the loss of importantDNA from chromosome ends As a result every time the chromosomeis copied only 100ndash200 nucleotides are lost which causes no damageto the organisms DNA Telomerase is a reverse transcriptase thatcarries its own RNA molecule which is used as a template when itelongates telomeres which are shortened after each replication cycleTelomerase a eukaryotic ribonucleoprotein (RNP) complex contains

both an essential RNA and a protein reverse transcriptase subunit By reverse transcription the telomerase RNPmaintains telomere length stability in almost all cancer cells

Purity 980Clinical Data No Development ReportedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Telomerase Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity BIBR 1532 is a potent selective and non-competitive inhibitor with of 100 nM intelomerase IC50

a cell-free assay

Bioactivity Telomerase-IN-1 is a inhibitor with an ofTelomerase IC50019 μM

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

152 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

BIBR 1532 Cat No HY-17353

Telomerase-IN-1 Cat No HY-U00268

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

wwwMedChemExpresscom 153

TOPKT-LAK cell-originated protein kinase

TOPK (T-lymphokine-activated killer cellndashoriginated protein kinasealso known as PBK or PDZ-binding kinase) is a SerThr protein kinasethat is highly expressed in many types of human cancer includingbreast and lung cancers TOPK is included in the ldquoconsensus stemnessranking signaturerdquo gene list that is up-regulated in cancer stemcell-enriched tumors and is associated with poor prognosis inmultiple types of cancerTOPKPBK is an oncogenic kinase upregulated in most humancancers TOPK is important for mitotic cell division and thatphosphorylation by Cdk1 is needed for its activationTOPK a member of the MEK36-related MAPKK family is expressed in

a wide range of proliferating cells and tissues including cancer cells and testis TOPK negatively regulates the activityof p38α by phosphorylating the p38α-specific phosphatase MKP1 and enhancing the stability of MKP1 The MAPKphosphatase MKP1 an archetypal member of the MKP family plays a pivotal role in the deactivation of p38 through adephosphorylation reaction

Purity 9563Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

TOPK Inhibitors amp Modulators

Bioactivity HI-TOPK-032 is a potent and specific inhibitorTOPK Bioactivity OTS-964 is a potent T-lymphokine-activated killer inhibitor ( =28cell-originated protein kinase (TOPK) IC50

nM) which inhibits TOPK kinase activity with high affinityand selectivity

Bioactivity OTS514 is a highly potent inhibitor which inhibits TOPKTOPKkinase activity with a median inhibitory concentration ( )IC50value of 26 nM

154 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

HI-TOPK-032 Cat No HY-101550

OTS-964 Cat No HY-12467

OTS514 Cat No HY-18621

wwwMedChemExpresscom 155

Topoisomerase

Topoisomerases are enzymes that regulate the overwinding orunderwinding of DNA The winding problem of DNA arises due to theintertwined nature of its double-helical structure Topoisomerases areisomerase enzymes that act on the topology of DNA Type Itopoisomerase cuts one strand of a DNA double helix relaxationoccurs and then the cut strand is reannealed Type I topoisomerasesare subdivided into two subclasses type IA topoisomerases whichshare many structural and mechanistic features with the type IItopoisomerases and type IB topoisomerases which utilize acontrolled rotary mechanism Type II topoisomerase cuts both strandsof one DNA double helix pass another unbroken DNA helix through

it and then reanneal the cut strands This class is also split into two subclasses type IIA and type IIB topoisomeraseswhich possess similar structure and mechanisms

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 1 mg 5 mg

Purity 980Clinical Data LaunchedSize 1 mg 5 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9243Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 9808Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9889Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Topoisomerase Inhibitors amp Modulators

Bioactivity 9-Aminocamptothecin is a inhibitor withtopoisomerase Ipotent anticancer activity

Bioactivity Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) afluorescent molecule and the first described non-peptidicinhibitor showing discrete specificity for the CTRL(chymotrypsin-like) activity of the 20S proteasome [1]

Aclacinomycin A hydrochloride is also a dual inhibitor ofhellip

Bioactivity Aldoxorubicin (INNO-206) is an albumin-binding prodrug ofdoxorubicin which is released from albumin under acidicconditions Aldoxorubicin (INNO-206) has potent antitumoractivities in various cancer cell lines and in murine tumormodels

Bioactivity Amonafide is a inhibitor and DNAtopoisomerase IIintercalator that induces apoptotic signaling by blocking thebinding of Topo II to DNA

Bioactivity Amrubicin (SM-5887) is a DNA inhibitortopoisomerase IIused for the research of cancer

Bioactivity Amrubicin (hydrochloride) (SM-5887 (hydrochloride)) is a DNA inhibitor used for the research of cancertopoisomerase II

Bioactivity Amsacrine (m-AMSA) is an inhibitor of andtopoisomerase IIacts as an antineoplastic agent which can intercalates intothe DNA of tumor cells

Bioactivity Amsacrine hydrochloride (mAMSA hydrochloride) is an inhibitorof and acts as an antineoplastic agenttopoisomerase IIwhich can intercalates into the DNA of tumor cells

Bioactivity Banoxantrone D12 (AQ4N D12) is the deuterium labeledbanoxantrone Banoxantrone is a novel bioreductive agent thatcan be reduced to a stable DNA-affinic compound AQ4 which isa potent inhibitortopoisomerase II

Bioactivity Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) isthe deuterium labeled banoxantrone dihydrochlorideBanoxantrone is a novel bioreductive agent that can be reducedto a stable DNA-affinic compound AQ4 which is a potent

inhibitortopoisomerase II

156 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

9-amino-CPT (9-amino-20(S)-camptothecin) Cat No HY-100309

Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) Cat No HY-N2306A

Aldoxorubicin (INNO-206 DOXO-EMCH) Cat No HY-16261

Amonafide (AS1413) Cat No HY-10982

Amrubicin (SM-5887 AMR) Cat No HY-B0067

Amrubicin hydrochloride (SM-5887 (hydrochloride) AMR (hydrochloride)) Cat No HY-B0067A

Amsacrine (m-AMSA acridinyl anisidide) Cat No HY-13551

Amsacrine hydrochloride (m-AMSA hydrochloride acridinyl anisidide hydrochloride) Cat No HY-13551A

Banoxantrone D12 (AQ4N D12) Cat No HY-13562S

Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) Cat No HY-13562AS

wwwMedChemExpresscom 157

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity 9826Clinical Data Phase 4Size 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9635Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg

Purity 9818Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9880Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg

Bioactivity Banoxantrone dihydrochloride is a novel bioreductive agentthat can be reduced to a stable DNA-affinic compound AQ4which is a potent inhibitortopoisomerase II

Bioactivity Belotecan hydrochloride (CKD-602 hydrochloride) a inhibitor is a synthetic and water-solubleTopoisomerase I

camptothecin derivative

Bioactivity Berberine chloride is an alkaloid isolated from the Chineseherbal medicine Huanglian as an Berberine chlorideantibioticinduces reactive oxygen species ( ) generation andROSinhibits Antineoplastic propertiesDNA topoisomerase

[1]

Bioactivity Berberine chloride hydrate is an alkaloid isolated from theChinese herbal medicine Huanglian as an Berberineantibioticchloride hydrate induces reactive oxygen species ( )ROSgeneration and inhibits AntineoplasticDNA topoisomeraseproperties [1]

Bioactivity Betulinic acid is a natural pentacyclic triterpenoid acts asa eukaryotic inhibitor with an of 5topoisomerase I IC50μM and possesses anti-HIV anti-malarial anti-inflammatoryand anti-tumor properties

Bioactivity Bisantrene is a highly effective antitumor drug targetseukaryotic type II topoisomerases

Bioactivity Campathecin is a potent DNA enzyme topoisomerase Iinhibitor with an of 679 nMIC50

Bioactivity Daun02 is a prodrug of the inhibitortopoisomeraseDaunorubicin

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Banoxantrone dihydrochloride (AQ4N dihydrochloride) Cat No HY-13562A

Belotecan hydrochloride (CKD-602) Cat No HY-13566A

Berberine chloride (Natural Yellow 18 (chloride)) Cat No HY-18258

Berberine chloride hydrate (Natural Yellow 18 (chloride hydrate)) Cat No HY-17577

Betulinic acid (Lupatic acid Betulic acid) Cat No HY-10529

Bisantrene (CL216942) Cat No HY-100875

Campathecin (Camptothecin (S)-(+)-Camptothecin CPT) Cat No HY-16560

Daun02 Cat No HY-13061

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9965Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9888Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9839Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9947Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Doxorubicin is a cytotoxic anthracycline antibiotic for thetreatment of multiple cancers The possible mechanisms bywhich doxorubicin acts in the cancer cell are intercalationinto DNA and disruption of -mediated DNAtopoisomerase-IIrepair

Bioactivity Doxorubicin hydrochloride is a cytotoxic anthracyclineantibiotic for the treatment of multiple cancers The possiblemechanisms by which doxorubicin acts in the cancer cell areintercalation into DNA and disruption of

-mediated DNA repairtopoisomerase-II

Bioactivity Dxd is a potent inhibitor with an ofDNA topoisomerase I IC50031 μM used as a conjugated drug of HER2-targeting ADC(DS-8201a)

Bioactivity Edotecarin is a potent inhibitor of that cantopoisomerase Iinduces single-strand DNA cleavage with of 50 nMIC50

Bioactivity Ellipticine (NSC 71795) is a potent antineoplastic agentinhibits activitiesDNA topoisomerase II

Bioactivity Ellipticine (NSC 71795) hydrochloride is a potentantineoplastic agent inhibits DNA topoisomerase IIactivities

Bioactivity Epirubicin is a semisynthetic L-arabino derivative ofdoxorubicin and an antineoplastic agent by inhibiting

Topoisomerase

Bioactivity Epirubicin (hydrochloride) is a semisynthetic L-arabinoderivative of doxorubicin and an antineoplastic agent byinhibiting Topoisomerase

Bioactivity Etoposide (VP-16 VP-16-213) a chemotherapy medication usedfor the treatments of a number of types of cancer inhibits

by forming a complex with topoisomerase II andDNA synthesisDNA Etoposide arrests cell cycle in G2 and induces apoptoshellip

Bioactivity Exatecan is a water soluble inhibitor withtopoisomerase Ian of 22 μM (0975 μgmL) and can be used in cancerIC50research

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Doxorubicin (Hydroxydaunorubicin) Cat No HY-15142A

Doxorubicin hydrochloride (Hydroxydaunorubicin (hydrochloride)) Cat No HY-15142

Dxd (Exatecan derivative for ADC) Cat No HY-13631D

Edotecarin (J 107088 PF 804950) Cat No HY-13618

Ellipticine (NSC 71795) Cat No HY-15753

Ellipticine hydrochloride (NSC 71795 (hydrochloride)) Cat No HY-15753A

Epirubicin Cat No HY-13624

Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride) Cat No HY-13624A

Etoposide (VP-16 VP-16-213) Cat No HY-13629

Exatecan (DX-8951) Cat No HY-13631

wwwMedChemExpresscom 159

Purity 9830Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9803Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9912Clinical Data Phase 3Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg 500 mg

Bioactivity Exatecan Mesylate is a water soluble topoisomerase Iinhibitor with an of 22 μM (0975 μgmL) and can beIC50used in cancer research

Bioactivity Flumequine (R-802) is a quinolone antibiotic and acts as a inhibitor with an of 15 μM (392topoisomerase II IC50

μgmL)

Bioactivity Genz-644282 is a non-camptothecin inhibitortopoisomerase Iused for cancer research

Bioactivity Idarubicin hydrochloride is an anthracycline antileukemicdrug It inhibits the interfering with thetopoisomerase IIreplication of DNA and RNA transcription

Bioactivity Indotecan (LMP-400) is a potent topoisomerase 1(Top1)inhibitor with values of 300 1200 560 nM for P388IC50HCT116 MCF-7 cell lines respectively

Bioactivity Intoplicine is a and inhibitorDNA topoisomerase I II

Bioactivity Irinotecan is a water soluble inhibitortopoisomerase Ipreventing religation of the DNA strand by binding totopoisomerase I-DNA complex

Bioactivity Irinotecan hydrochloride is a water soluble topoisomerase Iinhibitor mainly used to treat colon cancer and rectal cancer

Bioactivity Irinotecan hydrochloride trihydrate is a water soluble inhibitor with antitumor activitytopoisomerase I

Bioactivity Karenitecin (Cositecan) is a inhibitor withtopoisomerase Ipotent anti-cancer activity

Exatecan Mesylate (DX8951f) Cat No HY-13631A

Flumequine (R-802) Cat No HY-B0526

Genz-644282 Cat No HY-16228

Idarubicin hydrochloride (4-Demethoxydaunorubicin hydrochloride) Cat No HY-17381

Indotecan (LMP-400 NSC-724998) Cat No HY-18351

Intoplicine Cat No HY-101647

Irinotecan ((+)-Irinotecan CPT-11) Cat No HY-16562

Irinotecan hydrochloride (CPT-11 hydrochloride Camptothecin 11 hydrochloride) Cat No HY-16562A

Irinotecan hydrochloride trihydrate Cat No HY-16568

Karenitecin (Cositecan BNP 1350) Cat No HY-14812

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9690Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9902Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9702Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg

Bioactivity LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I inhibitor with antitumor activity (Top1) [1]

Bioactivity LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNAintercalator and inhibitor withTopoisomerase I (Top1)antitumor activity [1]

Bioactivity MC-DOXHZN is an albumin-binding prodrug of Doxorubicin withacid-sensitive properties [1]

Bioactivity MC-DOXHZN hydrochloride is an albumin-binding prodrug ofDoxorubicin with acid-sensitive properties [1]

Bioactivity Mitoxantrone is a inhibitor also inhibitstopoisomerase IIprotein kinase C ( ) activity with an of 85 μMPKC IC50

Bioactivity Mitoxantrone dihydrochloride is a topoisomerase IIinhibitor also inhibits protein kinase C ( ) activityPKCwith an of 85 μMIC50

Bioactivity Namitecan is a potent inhibitor withtopoisomerase Iantitumor property

Bioactivity Pirarubicin is an anthracycline antibiotics acts as a inhibitor and is a widely used fortopoisomerase II

treatment of various cancers in particular solid tumors

Bioactivity Pirarubicin Hydrochloride is an anthracycline antibioticsacts as a inhibitor and is a widely usedtopoisomerase IIfor treatment of various cancers in particular solid tumors

Bioactivity Pixantrone is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

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LMP744 (MJ-III65 NSC706744) Cat No HY-U00248

LMP744 hydrochloride (MJ-III65 hydrochloride NSC706744 hydrochloride) Cat No HY-U00248A

MC-DOXHZN (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat No HY-16261A

MC-DOXHZN hydrochloride (Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat No HY-16261B

Mitoxantrone (mitozantrone) Cat No HY-13502

Mitoxantrone dihydrochloride (mitozantrone dihydrochloride) Cat No HY-13502A

Namitecan (ST-1968) Cat No HY-14821

Pirarubicin (THP) Cat No HY-13725

Pirarubicin Hydrochloride (THP Hydrochloride) Cat No HY-13725A

Pixantrone (BBR 2778) Cat No HY-13727

wwwMedChemExpresscom 161

Purity 9920Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 100 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 50 mg 100 mg 200 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9960Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Pixantrone dimaleate is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

Bioactivity Podocarpusflavone A is a DNA topoisomerase I inhibitor havemoderated anti-proliferative activity induce cell apoptosis inMCF-7 is developing anti-tumor drugs target DNAtopoisomerase I In vitro podocarpusflavone-A show significantinhibitions against DLD KB MCF-7 HEp-2 tumor cell lineshellip

Bioactivity SN-38 (NK012) is an active metabolite of the Topoisomerase Iinhibitor Irinotecan SN-38 (NK012) inhibits and DNA RNA

with s of 0077 and 13 μM respectivelysynthesis IC50

Bioactivity SW044248 is a non-canonical inhibitor andtopoisomerase Iselectively toxic for certain non-small cell lung cancer(NSCLC) cell lines

Bioactivity TAS-103 is a dual inhibitor of DNA usedtopoisomerase IIIfor cancer research

Bioactivity TAS-103 dihydrochloride is a dual inhibitor of DNA used for cancer researchtopoisomerase III

Bioactivity Teniposide is a podophyllotoxin derivative acts as a inhibitor and used as a chemotherapeutictopoisomerase II

agent

Bioactivity Top1 inhibitor 1 (compound 28) is a potent human inhibitor with an value of 29topoisomerase I (Top1) IC50

nM [1]

Bioactivity Topotecan (SKF 104864A NSC 609669) is a Topoisomerase Iinhibitor The values of Topotecan at 24 h are 273plusmn025IC50μM of U251 cells 295plusmn023 μM of U87 cells 546plusmn041 μM ofGSCs-U251 and 595plusmn024 μM of GSCs-U87

Bioactivity Topotecan Hydrochloride (SKF 104864A Hydrochloride NSC 609669Hydrochloride) is a inhibitor with potentTopoisomerase Iantineoplastic activities

Pixantrone dimaleate (BBR 2778 dimaleate) Cat No HY-13727A

Podocarpusflavone A Cat No HY-N2198

SN-38 (NK012) Cat No HY-13704

SW044248 Cat No HY-19637

TAS-103 (BMS-247615) Cat No HY-13758

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) Cat No HY-13758A

Teniposide (VM26) Cat No HY-13761

Top1 inhibitor 1 Cat No HY-126142

Topotecan (SKF 104864A NSC 609669) Cat No HY-13768

Topotecan Hydrochloride (SKF 104864A (Hydrochloride) NSC 609669 (Hydrochloride)) Cat No HY-13768A

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Bioactivity Voreloxin is a first-in-class inhibitortopoisomerase IIthat intercalates DNA and induces site-selective DNA DSB G2arrest and apoptosis

Bioactivity Voreloxin Hydrochloride is a first-in-class topoisomerase IIinhibitor that intercalates DNA and induces site-selective DNADSB G2 arrest and apoptosis

Bioactivity β-Lapachone is a naturally occurring O-naphthoquinone acts asa inhibitor and induces apoptosis bytopoisomerase Iinhibiting cell cycle progression

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Voreloxin (SNS-595 Vosaroxin AG 7352) Cat No HY-10534

Voreloxin Hydrochloride (SNS-595 Hydrochloride Vosaroxin

Hydrochloride AG 7352 Hydrochloride) Cat No HY-16518

β-Lapachone (ARQ-501 NSC-26326) Cat No HY-13555

wwwMedChemExpresscom 163

Wee1

Wee1 is a nuclear kinase belonging to the SerThr family of proteinkinases in the fission yeast ( )Schizosaccharomyces pombe S pombeWee1 has amolecular mass of 96 kDa and it is a key regulator of cellcycle progression Wee1 influences cell size by inhibiting the entryinto mitosis through inhibiting Cdk1 Wee1 has homologues in manyother organisms including mammals Wee1 inhibits Cdk1 byphosphorylating it on two different sites Tyr15 and Thr14 Cdk1 iscrucial for the cyclin-dependent passage of the various cell cyclecheckpoints At least three checkpoints exist for which the inhibitionof Cdk1 by Wee1 is important G M checkpoint Cell size checkpoint2DNA damage checkpoint Wee1 is shown to phosphorylate histone

H2B at tyrosine 37 residue which regulates global expression of histones

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Wee1 Inhibitors amp Modulators

Bioactivity Adavosertib (AZD-1775 MK-1775) is a potent inhibitorWee1with an of 52 nMIC50

Bioactivity PD0166285 is a inhibitor and a weak inhibitorWEE1 Myt1with s of 24 and 72 nM respectivelyIC50

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Adavosertib (AZD1775 MK-1775) Cat No HY-10993

PD0166285 Cat No HY-13925

Page 3: Cell Cycle/DNA Damage - MedchemExpress.com · 2019. 7. 2. · G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition,

wwwMedChemExpresscom 3

bull Nucleoside AntimetaboliteAnalog 104

bull p97 111

bull PAK 113

bull PARP 116

bull PERK 122

bull Polo-like Kinase (PLK) 124

bull PPAR 128

bull RAD51 137

bull ROCK 139

bull Sirtuin 144

bull SRPK 149

bull Telomerase 151

bull TOPK 153

bull Topoisomerase 155

bull Wee1 163

bull Antifolate 3

bull APC 7

bull ATMATR 9

bull Aurora Kinase 12

bull Casein Kinase 17

bull CDK 20

bull Checkpoint Kinase (Chk) 34

bull CRISPRCas9 37

bull Deubiquitinase 39

bull DNA AlkylatorCrosslinker 43

bull DNA-PK 48

bull DNARNA Synthesis 52

bull Eukaryotic Initiation Factor (eIF) 60

bull G-quadruplex 62

bull Haspin Kinase 64

bull HDAC 66

bull HSP 77

bull IRE1 83

bull Kinesin 86

bull LIM Kinase (LIMK) 89

bull MicrotubuleTubulin 91

bull Mps1 101

Inhibitors Agonists Screening LibrarieswwwMedChemExpresscom

Target List in Cell CycleDNA Damage

Antifolate

Antifolates are compounds that antagonise the actions of folic acid(vitamin B9) Folic acids primary function in the body is as a cofactorto various methyltransferases involved in serine methioninethymidine and purine biosynthesis Consequently antifolates inhibitcell division DNARNA synthesis and repair and protein synthesisSome such as Proguanil Pyrimethamine and Trimethoprim selectivelyinhibit folates actions in microbial organisms such as bacteriaprotozoa and fungi The majority of antifolates work by inhibitingdihydrofolate reductase (DHFR) Many are primarily DHFR inhibitorsbut Raltitrexed is an inhibitor of thymidylate synthase andPemetrexed inhibits both and a third enzyme Antifolates act

specifically during DNA and RNA synthesis and thus are cytotoxic during the S-phase of the cell cycle Thus they havea greater toxic effect on rapidly dividing cells

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Purity 9517Clinical Data LaunchedSize 10 mg 50 mg

Purity 9524Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg 1 g 2 g

Purity 9973Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9973Clinical Data LaunchedSize 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Antifolate Inhibitors amp Modulators

Bioactivity Calcium N5-methyltetrahydrofolate(NSC173328) is the calciumsalt of levomefolic acid which has been proposed fortreatment of cardiovascular disease and advanced cancers suchas breast and colorectal cancers

Bioactivity Cycloguanil D6 is the deuterium labeled Cycloguanil which isa dihydrofolate reductase inhibitor

Bioactivity Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanilwhich is a dihydrofolate reductase inhibitor

Bioactivity Diaveridine (EGIS-5645) is a ( )dihydrofolate reductase DHFRinhibitor with a of 115 nM for the wild type DHFR and alsoKian antibacterial agent

Bioactivity EC0489 a conjugate of folic acid and desacetyl vinblastinehydrazide is a high-affinity ligand for the folate receptor(FR) Refractory or metastatic Tumor Small molecule-drug[1]

conjugate (SMDC) [2]

Bioactivity Folinic acid is an adjuvant used in cancer chemotherapyinvolving the drug methotrexate Target Antifolate Folinicacid is a 5-formyl derivative of tetrahydrofolic acid It isreadily converted to other reduced folic acid derivatives(eg tetrahydrofolate) and thus has vitamin activity thathellip

Bioactivity Leucovorin Calcium is a reduced folic acid IC50 Value 30 μMfor zcSHMT and70 μM for zmSHMT [2] Target Antifolate invitro Increasing concentrations of leucovorin (N5-CHO-THF)inhibit both zcSHMT and hcSHMT activities substantially yetto a lesser extent than zmSHMT The IC50 of leucovorin ishellip

Bioactivity Folinic Acid is a reduced folic acid which is used incombination with other chemotherapy drugs Target Folateanalog Approved 2008 Folinic acid (calcium salt pentahydrate)is the calcium salt form of folinic acid which is one of theforms of folate found naturally in foods Folate deficiency ishellip

Bioactivity Levoleucovorin calcium is the calcium salt of Levoleucovorinwhich is the enantiomerically active form of folinic acidIC50 value Target Levoleucovorin is used to treat or preventtoxic effects of methotrexate in people who have receivedmethotrexate to treat bone cancer Levoleucovorin is also usedhellip

Bioactivity Levomefolate is an artificial form of folate IC50 ValueTarget Antifolate The calcium salt ofL-5-methyltetrahydrofolic acid which belongs to the group offolate vitamins (Vitamin B9 Folacin) It is a coenzymatedform of folic acid and a more bioavailable alternative inhellip

Calcium N5-methyltetrahydrofolate (NSC173328) Cat No HY-17557

Cycloguanil D6 (Chlorguanide triazine D6) Cat No HY-12784S

Cycloguanil D6 Nitrate (Chlorguanide triazine D6 Nitrate) Cat No HY-12784S1

Diaveridine (EGIS-5645) Cat No HY-B1902

EC0489 Cat No HY-114306

Folinic acid (leucovorin) Cat No HY-17556

Folinic acid Calcium (Leucovorin Calcium Calcium Folinate) Cat No HY-13664

Folinic acid calcium salt pentahydrate (Leucovorin calcium salt pentahydrate) Cat No HY-B0080

Levoleucovorin Calcium (Calcium levofolinate CL307782) Cat No HY-13667

Levomefolate calcium Cat No HY-17383

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9923Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg

Purity 9977Clinical Data LaunchedSize 10mM x 1mL in Water

50 mg 100 mg 200 mg

Purity 9930Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity LY 254155 an antifolate inhibits and binds tohGARFT with s of 21plusmn02 and 17plusmn01 nM respectivelymFBP Ki

Bioactivity LY309887 is a potent inhibitor of glycinamide ribonucleotideformyltransferase ( ) with a of 65 nM and hasGARFT Kiantitumor activity

Bioactivity Methotrexate is a antagonist with median of 78 nMfolate IC50in assayin vitro

Bioactivity Pemetrexed is a novel the values of theantifolate Kipentaglutamate of LY231514 are 13 72 and 65 nM forinhibits thymidylate synthase ( ) dihydrofolate reductaseTS( ) and glycinamide ribonucleotide formyltransferase (DHFR

) respectivelyGARFT

Bioactivity Pemetrexed disodium is a novel that inhibits theantifolatefolatedependent enzymes thymidylate synthase dihydrofolate

and reductase glycinamide ribonucleotide with s of 13 72 and 65 nMformyltransferase Ki

respectively

Bioactivity Pemetrexed disodium hemipenta hydrate is a novel antifolatethe values of the pentaglutamate of LY231514 are 13 72Kiand 65 nM for inhibits thymidylate synthase ( )TSdihydrofolate reductase ( ) and glycinamideDHFRribonucleotide formyltransferase ( ) respectivelyGARFT

Bioactivity Pralatrexate(Folotyn) is an antifolate and structurally afolate analog Its IC50 is lt 300 nM in some cell linesIC50 Value lt 300 nM Target Antifolate Pralatrexate is anantifolate (a folate analogue metabolic inhibitor) designed toaccumulate preferentially in cancer cells Based onhellip

Bioactivity Pyrimethamine(RP4753) is a medication used for protozoalinfections interferes with tetrahydrofolic acid synthesisfrom folic acid by inhibiting the enzyme dihydrofolatereductase (DHFR) IC50 Value 154 nM (Plasmodium falciparum)[1] Target DHFR antifolate in vitro Three susceptibilityhellip

Bioactivity Trimethoprim is a bacteriostatic antibiotic used mainly in theprophylaxis and treatment of urinary tract infections

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LY 254155 Cat No HY-14523

LY309887 Cat No HY-10818

Methotrexate (Amethopterin CL14377 WR19039) Cat No HY-14519

Pemetrexed (LY231514) Cat No HY-10820

Pemetrexed disodium (LY231514 disodium) Cat No HY-10820A

Pemetrexed disodium hemipenta hydrate (LY231514 (disodium hemipenta hydrate)) Cat No HY-13781

Pralatrexate Cat No HY-10446

Pyrimethamine (Pirimecidan Pirimetamin RP 4753) Cat No HY-18062

Trimethoprim Cat No HY-B0510

wwwMedChemExpresscom 7

APCAnaphase promoting complex

APC (Anaphase-Promoting Complex) is an E3 ubiquitin ligase thatmarks target cell cycle proteins for degradation by the 26Sproteasome The APCC is a large complex of 11ndash13 subunit proteinsincluding a cullin (Apc2) and RING (Apc11) subunit much like SCF TheAPCCs main function is to trigger the transition from metaphase toanaphase by tagging specific proteins for degradation The twoproteins of most importance that get degraded in this process assubstrates of the APCC are securin and S and M cyclins Securinreleases separase a protease after being degraded which in turntriggers the cleavage of cohesin the protein complex that binds sisterchromatids together During metaphase sister chromatids are linked

by intact cohesin complexes When securin undergoes ubiquitination by the APCC and releases separase whichdegrades cohesin sister chromatids become free to move to opposite poles for anaphase The APCC also targets themitotic cyclins for degradation resulting in the inactivation of M-CdK (mitotic cyclin-dependent kinase) complexespromoting exit from mitosis and cytokinesis

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9911Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

APC Inhibitors amp Modulators

Bioactivity TAME is a inhibitor and can be also utilizedserine proteaseas a substrate for the serine proteases trypsin plasmin andthrombin TAME is an inhibitor of[1] [2] [3]

which binds to the hellipanaphase-promoting complex (APC)

Bioactivity TAME hydrochloride is a inhibitor and can beserine proteasealso utilized as a substrate for the serine proteases trypsinplasmin and thrombin TAME hydrochloride is an[1] [2] [3]

inhibitor of which bihellipanaphase-promoting complex (APC)

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TAME Cat No HY-13255

TAME hydrochloride Cat No HY-13255A

wwwMedChemExpresscom 9

ATMATRAtaxia telangiectasia mutatedATM and RAD3 related

ATMATR are members of the PI3 family of serine-threonine kinasesand function as essential links between the sensors and effectors ofthe DNA damage response The roles of ATM and ATR partiallyoverlap and are cooperative however they are also known to playdistinct roles in protecting the cell from DNA damage ATM is mostlyresponsible for sending signals from DSBs (double-strand breaks)induced by ionizing radiation while the closely related ATR respondsto UV damage or stalled replication forks ATM and ATR are known tophosphorylate common as well as specific substrates to activatecheckpoint signaling The G1 S and G2 cell cycle checkpoints areprimarily regulated by the ATM (ataxia telangiectasia mutated) and

ATR (ATM and Rad3-related) protein kinases

Purity 9976Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9904Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9960Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

ATMATR Inhibitors amp Modulators

Bioactivity ATM Inhibitor-1 is a highly potent selective and orallyactive inhibitor with an of 07 nM shows weakATM IC50activity against mTOR (IC 21 μM) DNAPK (IC 28 μM)50 50PI3Kα (IC 38 μM) PI3Kβ (IC 103 μM) PI3Kγ hellip50 50

Bioactivity ATR inhibitor 1 is a inhibitor extracted from patentATRWO2015187451A1 compound I-l has a value below 1 microΜ Ki

[1]

Bioactivity AZ20 is a potent and selective inhibitor of with an ATR IC50of 5 nM and has 8-fold selectivity against (IC =38mTOR 50nM)

Bioactivity AZ32 is an orally bioavailable and blood-brainbarrier-penetrating inhibitor with an of lt62ATM IC50nM for ATM enzyme and an of 031 μM for ATM in cellIC50

Bioactivity AZD0156 is an oral potent and selective inhibitor withATMan of 058 nMIC50

Bioactivity AZD1390 is an inhibitorATM

Bioactivity BAY-1895344 is a potent orally available and selective ATRinhibitor with of 7 nM Anti-tumor activity IC50

[1]Bioactivity BAY-1895344 hydrochloride is a potent orally available and

selective inhibitor with of 7 nM Anti-tumorATR IC50

activity [1]

Bioactivity Berzosertib (VE-822) is an inhibitor with a value ofATR Kiless than 02 nM It also inhibits with a of 34 nMATM Ki

Bioactivity Ceralasertib (AZD6738) is a potent inhibitor of kinaseATRwith an of 1 nMIC50

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ATM Inhibitor-1 Cat No HY-112614

ATR inhibitor 1 Cat No HY-111451

AZ20 Cat No HY-15557

AZ32 Cat No HY-112305

AZD0156 Cat No HY-100016

AZD1390 Cat No HY-109566

BAY-1895344 Cat No HY-101566

BAY-1895344 hydrochloride Cat No HY-101566A

Berzosertib (VE-822 VX-970) Cat No HY-13902

Ceralasertib (AZD6738) Cat No HY-19323

wwwMedChemExpresscom 11

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9947Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9988Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9840Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity CGK733 is a potent inhibitor used for the researchATMATRof cancer

Bioactivity CP-466722 is a rapidly reversible inhibitor of with anATM of 41 μM and has no effects on PI3K or closely relatedIC50

PI3K-like protein kinase (PIKK) family members

Bioactivity ETP-46464 is an effective and inhibitor withmTOR ATRs of 06 and 14 nM respectivelyIC50

Bioactivity KU 59403 is a potent inhibitor with an of 3 nMATM IC50

Bioactivity KU-55933 is a potent inhibitor with an and ofATM IC50 Ki129 and 22 nM respectively and is highly selective for ATMas compared to DNA-PK PI3KPI4K ATR and mTOR

Bioactivity KU-60019 is an improved kinase-specific inhibitor withATM of 63 nMIC50

Bioactivity VE-821 is a potent ATP-competitive inhibitor of with ATR Ki of 13 nM26 nMIC50

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

CGK733 Cat No HY-15520

CP-466722 Cat No HY-11002

ETP-46464 Cat No HY-15521

KU 59403 Cat No HY-18650

KU-55933 Cat No HY-12016

KU-60019 Cat No HY-12061

VE-821 Cat No HY-14731

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

Aurora Kinase

Aurora kinases are serinethreonine kinases that are essential for cellproliferation Aurora kinase helps the dividing cell dispense its geneticmaterials to its daughter cells More specifically Aurora kinases play acrucial role in cellular division by controlling chromatid segregationDefects in this segregation can cause genetic instability a conditionwhich is highly associated with tumorigenesis Three Aurora kinaseshave been identified in mammalian cells to date Aurora A Aurora BAurora C Besides being implicated as mitotic regulators these threekinases have generated significant interest in the cancer research fielddue to their elevated expression profiles in many human cancers Thehuman Aurora kinases present a similar domain organization with a

N-terminal domain of 39 to 129 residues in length a protein kinase domain and a short C-terminal domain containing15 to 20 residues The N-terminal domain of three proteins share low sequence conservation which determinesselectivity during protein-protein interactions

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Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9895Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9874Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Aurora Kinase Inhibitors amp Modulators

Bioactivity Alisertib (MLN 8237) is an oral active and selective Aurora A inhibitor with an of 12 nMkinase IC50

Bioactivity AMG 900 is a potent and highly selective kinasespan-Aurorainhibitor with of 5 nM 4 nM and 1 nM for IC50 Aurora A B

and respectivelyC

Bioactivity AT9283 is a multitargeted kinase inhibitor which potentlyinhibits ( =12 nM 11 nM)aurora kinase AB JAK23 IC50

Bioactivity Aurora A inhibitor I is a potent and highly selective Aurora inhibitor with with an of 34 nMA IC50

Bioactivity Aurora B inhibitor 1 is an (Aurora-1) inhibitorAurora Bextracted from patent WO2007059299A1 compound 1-3 has a Kivalue of lt0010 uM

Bioactivity Aurora inhibitor 1 is a potent inhibitor with an Aurora IC50of le 4 nM and le13 nM for and kinaseAurora A Aurora Brespectively [1]

Bioactivity AZD1152 is a pro-drug of Barasertib-hQPA which is a highlyselective inhibitor with of 037 nM in aAurora B IC50cell-free assay

Bioactivity AZD1152-HQPA is a highly selective Aurora inhibitor with an of 037 nM in aB IC50

cell-free assay and shows 3700-fold selectivity for Aurora Bover Aurora A

Bioactivity BI-847325 is an ATP competitive dual inhibitor of andMEKaurora kinases ( ) with values of 4 and 15 nM forAK IC50human MEK2 and AK-C respectively

Bioactivity CCT 137690 is a potent and orally available kinaseaurorainhibitor with s of 15 25 and 19 nM for aurora A B andIC50C respectively

Alisertib (MLN 8237) Cat No HY-10971

AMG 900 Cat No HY-13253

AT9283 Cat No HY-50514

Aurora A inhibitor I Cat No HY-70061

Aurora B inhibitor 1 Cat No HY-U00304

Aurora inhibitor 1 Cat No HY-111506

AZD1152 (Barasertib) Cat No HY-10127

Barasertib-HQPA (AZD2811 INH-34 AZD1152-HQPA) Cat No HY-10126

BI-847325 Cat No HY-18955

CCT 137690 Cat No HY-10804

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 1 mg 5 mg 10 mg 20 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9859Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9923Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9944Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data Phase 1Size 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 950Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity CCT129202 is an kinase inhibitor with s of 42aurora IC50198 and 227 nM for aurora A B and C respectively

Bioactivity CCT241736 is a potent and orally bioavailable dual andFLT3 inhibitor which inhibits Aurora kinasesAurora kinase

(Aurora-A 75 nM 38 nM Aurora-B 48 nM)Kd IC50 KdFLT3 kinase ( 62 nM) and FLT3 mutants includhellipKd

Bioactivity CYC-116 is a potent and inhibitor withaurora A aurora Bs of 8 and 9 nM respectivelyKi

Bioactivity Danusertib is a pyrrolo-pyrazole and inhibitoraurora kinasewith of 13 79 and 61 nM for Aurora A B and CIC50respectively

Bioactivity ENMD-2076 is a multi-targeted kinase inhibitor with s ofIC50186 14 582 159 927 708 564 nM for Aurora A Flt3

KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src PDGFRαrespectively

Bioactivity ENMD-2076 Tartrate is a multi-targeted kinase inhibitor withs of 186 14 582 159 927 708 564 nM for IC50 Aurora

A Flt3 KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src respectivelyPDGFRα

Bioactivity GSK-1070916 is a potent and selective ATP-competitiveinhibitor of and with s of 038 andaurora B aurora C Ki15 nM respectively and is gt250- fold selective overAurora A

Bioactivity Hesperadin is an ATP-competitive inhibitor of aurora Bkinase with an of 250 nMIC50

Bioactivity Ilorasertib (ABT-348) is an ATP-competitive multitargetedkinase inhibitor with s for inhibiting binding Aurora B (7IC50nM) C (1 nM) and A (120 nM) and also inhibits RET tyrosinekinase PDGFRβ and Flt1 with s of 7 nM 3 nM and 32 nMIC50

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

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CCT129202 Cat No HY-12049

CCT241736 Cat No HY-18161

CYC-116 Cat No HY-10558

Danusertib (PHA-739358) Cat No HY-10179

ENMD-2076 Cat No HY-10987A

ENMD-2076 Tartrate Cat No HY-10987

GSK-1070916 (GSK-1070916A) Cat No HY-70044

Hesperadin Cat No HY-12054

Ilorasertib (ABT-348) Cat No HY-16018

JNJ-7706621 Cat No HY-10329

wwwMedChemExpresscom 15

Purity 9820Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9928Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9911Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity KW-2449 is a multi-targeted kinase inhibitor of FLT3 ABL and with s of 66 14 4 and 48 nMABLT315I Aurora kinase IC50

respectively

Bioactivity LY3295668 is a potent orally active and highly specific inhibitor with values of 08 nM and 1038Aurora-A kinase Ki

nM for AurA and AurB respectively

Bioactivity MK-5108 is a highly potent and specific inhibitor of Aurora A with an value of 0064 nMkinase IC50

Bioactivity MK-8745 is an kinase inhibitor with an of 06aurora A IC50nM

Bioactivity MLN8054 is a potent selective and orally available aurora Akinase inhibitor with an of 4 nMIC50

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity PF-03814735 is a potent orally available and reversible and inhibitor with s of 08 and 05aurora A aurora B IC50

nM respectively

Bioactivity PHA-680632 is an kinase inhibitor with s of 27aurora IC50135 and 120 nM for aurora A B and C respectively

Bioactivity Reversine is a novel class of ATP-competitive Aurora kinaseinhibitor with s of 400 500 and 400 nM for IC50 Aurora A

and respectivelyAurora B Aurora C

Bioactivity SCH-1473759 is an inhibitor with s of 4 and 13 nMaurora IC50for aurora A and B respectively

KW-2449 Cat No HY-10339

LY3295668 (AK-01) Cat No HY-114258

MK-5108 (VX-689) Cat No HY-13252

MK-8745 Cat No HY-13819

MLN8054 Cat No HY-10180

NU6140 Cat No HY-107419

PF-03814735 Cat No HY-14574

PHA-680632 Cat No HY-10178

Reversine Cat No HY-14711

SCH-1473759 Cat No HY-10482

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg

Purity 9980Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity SCH-1473759 hydrochloride is an inhibitor with saurora IC50of 4 and 13 nM for aurora A and B respectively

Bioactivity SNS-314 is a potent and selective kinase inhibitoraurorawith s of 9 31 and 6 nM for aurora A B and CIC50respectively

Bioactivity TAK-632 is a potent inhibitor with of 14 24pan-RAF IC50

and 83 nM for respectivelyCRAF BRAFV600E BRAFWT

Bioactivity TAK-901 is a multi-targeted inhibitor with s of 21aurora IC50and 15 nM for aurora A and B respectively

Bioactivity Tozasertib (VX 680 MK-0457) is an inhibitor of Aurora ABC with s of 06 18 46 nM respectivelykinases Ki

Bioactivity XL228 is a multi-targeted tyrosine kinase inhibitor with sIC50of 5 31 16 61 2 nM for Bcr-Abl Aurora A IGF-1R Srcand respectivelyLyn

Bioactivity ZM-447439 is an kinase inhibitor with s of 110 andaurora IC50130 nM for aurora A and B respectively

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SCH-1473759 hydrochloride Cat No HY-10483

SNS-314 (SNS-314 Mesylate) Cat No HY-12003

TAK-632 Cat No HY-15767

TAK-901 Cat No HY-12201

Tozasertib (VX 680 MK-0457) Cat No HY-10161

XL228 Cat No HY-15749

ZM-447439 Cat No HY-10128

wwwMedChemExpresscom 17

Casein Kinase

Casein Kinases (CKs) are serinethreonine-selective enzymes thatfunction as regulators of signal transduction pathways in mosteukaryotic cell types

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9992Clinical Data Phase 2Size 1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Casein Kinase Inhibitors amp Modulators

Bioactivity Casein Kinase II Inhibitor IV is a small-molecule inducer ofepidermal keratinocyte differentiation

Bioactivity Casein Kinase II Inhibitor IV Hydrochloride is asmall-molecule inducer of epidermal keratinocytedifferentiation

Bioactivity CK1-IN-1 is a inhibitor extracted fromcasein kinase 1 (CK1)patent WO2015119579A1 compound 1c has s of 15 nM 16 nMIC50

73 nM for CK1δ and CK1ε p38σ MAPK respectively [1]

Bioactivity D4476 is a potent selective and cell-permeable inhibitor ofcasein kinase 1( ) with an value of 03 μM CK1 IC50 in vitro

Bioactivity DMAT is a potent and specific inhibitor with an CK2 IC50value of 130 nM

Bioactivity Ellagic acid is a natural antioxidant and acts as a potentand ATP-competitive inhibitor with an of 40 nM andCK2 IC50a of 20 nMKi

Bioactivity Emodin is a broad-spectrum anticancer agent Emodin inhibits II (CKII) activity with of 2 μMcasein kinase IC50

Bioactivity IC261 is a selective ATP-competitive inhibitor withCK1s of 1 μM 1 μM 16 μM for and Ckiα1IC50 Ckiδ Ckiε

respectively

Bioactivity LH846 is a selective inhibitor of with an of 290 nMCKIδ IC50and less potently inhibits CKIα and CKIε with s of 25 μMIC50and 13 μM respectively

Bioactivity Longdaysin is a and CK1α CK1δ extracellular inhibitor with s of  56signal-regulated kinase 2 (ERK2) IC50

microM 88 microM and 52 microM respectively [1] [2]

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Casein Kinase II Inhibitor IV Cat No HY-111378

Casein Kinase II Inhibitor IV Hydrochloride Cat No HY-111378A

CK1-IN-1 Cat No HY-111820

D4476 (Casein Kinase I Inhibitor) Cat No HY-10324

DMAT (Casein kinase II Inhibitor CK2 Inhibitor) Cat No HY-15535

Ellagic acid Cat No HY-B0183

Emodin (Frangula emodin) Cat No HY-14393

IC261 Cat No HY-12774

LH846 Cat No HY-15704

Longdaysin Cat No HY-18285

wwwMedChemExpresscom 19

Purity 9701Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9827Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Bioactivity NCC007 is a dual and inhibitorcasein kinase Iα (CKIα) δ (CKIδ)with s of 18 and 36 μM respectively and can be used inIC50

research of modulating mammalian circadian rhythms [1]

Bioactivity PF-4800567 is a potent and selective inhibitor of caseinkinase 1ϵ ( ) with an of 32 nM which is greaterCK1ϵ IC50than 20-fold selectivity over CK1δ ( 711 nM)IC50

Bioactivity PF-670462 is a potent and selective inhibitor of casein kinase with s of 77 nM and 14 nM( and )CK1ε CK1δ IC50

respectively

Bioactivity Silmitasertib (CX-4945) is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity Silmitasertib sodium salt is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity SR-3029 is a potent and ATP competitive and CK1δ CK1εinhibitor with s of 44 nM and 260 nM respectively andIC50

s of 97 nM for both kinasesKi

Bioactivity TA-01 is a potent and inhibitor with sCK1 p38 MAPK IC50of 64 nM 68 nM 67 nM for CK1ε CK1δ and p38 MAPKrespectively

Bioactivity TBB is a cell-permeable and ATP-competitive inhibitorCK2with an of 015 μM for rat liver CK2IC50

Bioactivity TTP 22 is a potent inhibitor with an of 100 nM andCK2 IC50a of 40 nMKi

NCC007 Cat No HY-128677

PF-4800567 Cat No HY-12470

PF-670462 Cat No HY-15490

Silmitasertib (CX-4945) Cat No HY-50855

Silmitasertib sodium salt (CX-4945 (sodium salt)) Cat No HY-50855B

SR-3029 Cat No HY-100011

TA-01 Cat No HY-100114

TBB (NSC 231634 Casein Kinase II Inhibitor I) Cat No HY-14394

TTP 22 Cat No HY-15479

CDKCyclin dependent kinase

CDKs (Cyclin-dependent kinases) are serine-threonine kinases firstdiscovered for their role in regulating the cell cycle They are alsoinvolved in regulating transcription mRNA processing and thedifferentiation of nerve cells CDKs are relatively small proteins withmolecular weights ranging from 34 to 40 kDa and contain little morethan the kinase domain In fact yeast cells can proliferate normallywhen their CDK gene has been replaced with the homologous humangene By definition a CDK binds a regulatory protein called a cyclinWithout cyclin CDK has little kinase activity only the cyclin-CDKcomplex is an active kinaseThere are around 20 Cyclin-dependent kinases (CDK1-20) known till

date CDK1 4 and 5 are involved in cell cycle and CDK 7 8 9 and 11 are associated with transcriptionCDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational Mostknowledge of CDK structure and function is based on CDKs of (Cdc2) (CDC28) and vertebratesS pombe S cerevisia(CDC2 and CDK2) The four major mechanisms of CDK regulation are cyclin binding CAK phosphorylation regulatoryinhibitory phosphorylation and binding of CDK inhibitory subunits (CKIs)

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Purity 9815Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9969Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9973Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

CDK Inhibitors amp Modulators

Bioactivity (+)-BAY-1251152 is a inhibitor extracted from patent WOCDK92014076091 A1 example 1

Bioactivity (-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation(-) BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity (plusmn)-BAY-1251152 is a racemic mixture of BAY-1251152BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity 5-Iodo-indirubin-3-monoxime is a potent GSK-3β CDK5P25and inhibitor competing with ATP for binding toCDK1cyclin Bthe catalytic site of the kinase with s of 9 20 and 25IC50

nM respectively [1]

Bioactivity Abemaciclib (LY2835219) is a selective inhibitor withCDK46 values of 2 nM and 10 nM for CDK4 and CDK6 respectivelyIC50

Bioactivity Abemaciclib Metabolites M2 is a metabolite of abemaciclibacts as a potent and inhibitor with s in theCDK4 CDK6 IC50

range of 1-3 nM Anti-cancer activity [1]

Bioactivity Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is aselective inhibitor with s of 2 nM and 10 nM forCDK46 IC50CDK4 and CDK6 respectively

Bioactivity AMG 925 is a potent selective and orally available FLT3 dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMCDK4 IC50

respectively

Bioactivity AMG 925 HCl is a potent selective and orally available dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMFLT3 CDK4 IC50

respectively

Bioactivity AT7519 as a potent inhibitor of with s of 210 47CDKs IC50100 13 170 and lt10 nM for CDK1 CDK2 CDK4 to CDK6 andCDK9 respectively

(+)-BAY-1251152 Cat No HY-103019

(-)-BAY-1251152 Cat No HY-103019B

(plusmn)-BAY-1251152 Cat No HY-103019A

5-Iodo-indirubin-3-monoxime Cat No HY-111930

Abemaciclib (LY2835219) Cat No HY-16297A

Abemaciclib Metabolites M2 Cat No HY-128669

Abemaciclib methanesulfonate (LY2835219 (methanesulfonate)) Cat No HY-16297

AMG 925 Cat No HY-15889

AMG 925 HCl Cat No HY-15889A

AT7519 Cat No HY-50940

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 1Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9999Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9700Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9848Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9816Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity AT7519 Hydrochloride is a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity AT7519 trifluoroacetate as a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity Atuveciclib (BAY-1143572) is a potent and highly selectiveoral inhibitor Atuveciclib (BAY-1143572)PTEFb CDK9inhibits with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib Racemate (BAY-1143572 Racemate) is the racematemixture of Atuveciclib Atuveciclib is a potent and highlyselective oral inhibitor which supressesP-TEFb CDK9

with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is apotent and selective inhibitor which inhibits CDK9 CDK9

with an of 16 nMCycT1 IC50

Bioactivity AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 82nM AUZ 454 (K03861) inhibits CDK2 activity by competing withbinding of activating cyclins

Bioactivity AZD-5438 is a potent inhibitor of with of 16CDK129 IC50nM6 nM20 nM in cell-free assays AZD-5438 shows lessinhibition activity against GSK3β CDK5 and CDK6

Bioactivity AZD4573 is a inhibitor with an of lt3 nMCDK9 IC50extracted from patent US 20160376287 A1 example 14

Bioactivity BGG463 is a inhibitorCDK2 Bioactivity BI-1347 is a potent inhibitor extracted from patentCDK8WO2017202719A1 product I-003 has an of 11 nM IC50

[1]

22 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

AT7519 Hydrochloride Cat No HY-50943

AT7519 trifluoroacetate Cat No HY-50940A

Atuveciclib (BAY-1143572) Cat No HY-12871B

Atuveciclib Racemate (BAY-1143572 Racemate) Cat No HY-12871

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) Cat No HY-12871C

AUZ 454 (K03861) Cat No HY-15004

AZD-5438 Cat No HY-10012

AZD4573 Cat No HY-112088

BGG463 Cat No HY-100600

BI-1347 Cat No HY-120350

wwwMedChemExpresscom 23

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9754Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9747Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity BMS-265246 is a potent and selective CDK12 inhibitor forCDK1cyclin B and CDK2cyclin E with IC50 of 6 nM and 9 nMrespectively

Bioactivity BS-181 is a highly selective inhibitor with an ofCDK7 IC5021 nM showing 40-fold selective over CDK1 2 4 5 6 or 9

Bioactivity BS-181 hydrochloride is a highly selective inhibitorCDK7with of 21 nM and gt 40-fold selective for CDK7 thanIC50CDK1 2 4 5 6 or 9

Bioactivity BSJ-03-123 is a potent and novel -selective small-moleculeCDK6degrader

Bioactivity Ca channel agonist 1 is an agonist of 2+ N-type Ca channel2+

and an inhibitor of with s of 1423 μM and 334Cdk2 EC50μM respectively and is used as a potential treatment formotor nerve terminal dysfunction

Bioactivity CC-671 is a dual ( )TTK protein kinase CDC2-like kinase CLK2inhibitor with s of 0005 and 0006 μM for TTK and CLK2IC50respectively

Bioactivity CCT-251921 is a potent selective and orally bioavailable inhibitor with an of 23 nMCDK8 IC50

Bioactivity CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 oflt8 nM extracted from reference 1 example 4 IC50 Valuelt8 nM [1] Target CDK9 In vitro In vivo

Bioactivity CDK46-IN-2 is a potent and inhibitor extractedCDK4 CDK6from patent US20180000819A1 Compound 1 has s of 27 andIC50

16 nM for CDK4 and CDK6 respectively [1]

Bioactivity CDK461 Inhibitor is a inhibitor with s of 3 andCDK46 IC501 nM respectively

BMS-265246 Cat No HY-15275

BS-181 Cat No HY-13266

BS-181 hydrochloride Cat No HY-13266A

BSJ-03-123 Cat No HY-111556

Ca2+ channel agonist 1 Cat No HY-41076

CC-671 Cat No HY-108709

CCT-251921 Cat No HY-19984

CDK-IN-2 (CDK inhibitor II) Cat No HY-13033

CDK46-IN-2 Cat No HY-114339

CDK461 Inhibitor Cat No HY-112280

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9548Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CDK8-IN-1 is a potent and selective inhibitor with anCDK8 of 3 nMIC50

Bioactivity CDK8-IN-3 is an inhibitor of extracted from patentCDK8WO2016041618A1 compound example 17

Bioactivity CDK8-IN-4 is an inhibitor of extracted from patentCDK8WO2014090692A1 compound example 16 with an of 02 nMIC50

Bioactivity CDK819-IN-1 is a potent selective and oral bioavailable dual inhibitor with s of 046 nM 099 nM andCDK819 IC50

270 nM for CDK8 CDK19 and CDK9 respectively

Bioactivity CDK9 Antagonist-1 (compounds 11c) is a potent and selective degrader based on PROTAC with an of 17 μM in MCF-7CDK9 IC50

cell lines Natural product Wogonin binds ubiquitin E3 ligasecereblon (CRBN) via a linker to form PROTAC [1]

Bioactivity CDK9-IN-1 is a novel selective inhibitor for theCDK9treatment of HIV infection with an of 39 nM forIC50CDK9CycT1 extracted from reference compound 87

Bioactivity CDK9-IN-2 is a special cyclin-dependent kinase 9 ( )CDK9inhibitor extracted from patent WO2012131594A1 compoundCDKI(8) has an of 5 nM and 7 nM in H929 multipleIC50myeloma(MM) cell line (72 hours) and A2058 skin cell line (72hours) respectively

Bioactivity CDK9-IN-8 is a highly effective and selective inhibitorCDK9with an of 12 nMIC50

Bioactivity CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM showsselective toxicity to CLL cells(LD50=80 nM) versus normal Bcell and normal CD34+ cell(LD50gt20 uM) IC50 value 4 nM80nM(KiLD50) [1] Target CDK9 inhibitor in vitro CDKI-73 wascytotoxic to all of the CLL samples tested (n = 38) with ahellip

Bioactivity CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 () inhibitor with an IC of 2 nMCLK1 50

24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CDK8-IN-1 Cat No HY-103492

CDK8-IN-3 Cat No HY-111463

CDK8-IN-4 Cat No HY-111465

CDK819-IN-1 Cat No HY-111427

CDK9 Antagonist-1 Cat No HY-112811

CDK9-IN-1 Cat No HY-13231

CDK9-IN-2 Cat No HY-16462

CDK9-IN-8 Cat No HY-102039

CDKI-73 Cat No HY-12445

CLK1-IN-1 Cat No HY-103082

wwwMedChemExpresscom 25

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9900Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9973Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9998Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CMPD 7 is a potent and selective inhibitor with an CDK12 IC50of 491 nM in enzymatic assay

Bioactivity CT7001 hydrochloride is a selective inhibitor withCDK7s of 41 nM and 578 nM for andIC50 CDK7CycHMAT1

respectivelyCDK2cycE1

Bioactivity Cucurbitacin E is a natural compound which from the climbingstem of Cucurbitacin E significantlyCucumic melo Lsuppresses the activity of the complexcyclin B1 CDC2

Bioactivity CVT-313 is a potent selective reversible andATP-competitive inhibitor of with of 05 μMCDK2 IC50

Bioactivity CYC065 is a second-generation orally availableATP-competitive inhibitor of kinasesCDK2 CDK 9

Bioactivity Dinaciclib is a potent inhibitor of with s of 1 1CDK IC503 and 4 nM for and respectivelyCDK2 CDK5 CDK1 CDK9

Bioactivity EHT 5372 is a strong inhibitor of family kinases withDYRKrsquos of 022 028 nM for DYRK1A and DYRK1B respectivelyIC s50

Bioactivity Flavopiridol is a broad spectrum and competitive inhibitor of inhibiting CDK1 CDK2 CDK4 with s of 30 170 100CDKs IC50

nM respectively

Bioactivity Flavopiridol Hydrochloride is a broad inhibitor of CDKcompeting with ATP to inhibit CDKs including CDK1 CDK2 CDK4with s of 30 170 100 nM respectivelyIC50

Bioactivity FMF-04-159-2 is a covalent inhibitor FMF-04-159-2CDK14inhibits CDK14 and CDK2 with s of 396 nM and 256 nM inIC50

NanoBRET assay respectively [1]

CMPD 7 Cat No HY-112261

CT7001 hydrochloride (ICEC0942 hydrochloride) Cat No HY-103712A

Cucurbitacin E (α-Elaterin α-Elaterine) Cat No HY-N0417

CVT-313 (Cdk2 Inhibitor III) Cat No HY-15339

CYC065 Cat No HY-101212

Dinaciclib (SCH 727965) Cat No HY-10492

EHT 5372 Cat No HY-111380

Flavopiridol (L868275 HMR-1275 Alvocidib) Cat No HY-10005

Flavopiridol Hydrochloride (HL 275 NSC 649890 MDL 107826A

FLAVOPIRIDOL HCL Alvocidib Hydrochloride) Cat No HY-10006

FMF-04-159-2 Cat No HY-127104

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9204Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 251 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9841Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity FN-1501 is a potent inhibitor of and with s ofFLT3 CDK IC50247 085 196 and 028 nM for CDK2cyclin A CDK4cyclinD1 CDK6cyclin D1 and FLT3 respectively FN-1501 hasanticancer activity

Bioactivity GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO) is apotent selective reversible and ATP-competitive inhibitor of

and complex with s of 5 nM320GSK-3αβ CDK1-cyclinB IC50nM80nM for (GSK-3αβ)CDK1CDK5 respectively

Bioactivity GSK3186899 is an inhibitor of cdc-2-related kinase 12 () with an of 14 μM for in anCRK12 EC50 L donovani

intra-macrophage assay

Bioactivity IIIM-290 is a potent and oral inhibitor with s of 90CDK IC50and 94 nM for CDK2A and CDK9T1

Bioactivity Indirubin-3-monoxime-5-sulphonic acid is a potent andselective inhibitor of and with s ofCDK1 CDK5 GSK-3β IC50

5 nM 7 nM and 80 nM respectively [1]

Bioactivity Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK)inhibitor with values of 55 nM 35 nM 150 nM 300 nMIC50and 65 nM for CDK1cyclin B CDK2cyclin A CDK2cyclin ECDK4cyclin D1 and CDK5p35 respectively [1]

Bioactivity JH-XI-10-02 is a potent and selective degrader of withCDK8an of 159 nM based on JH-XI-10-02 causesIC50 PROTAC

proteasomal degradation does not affect CDK8 mRNA levelsJH-XI-10-02 shows no effect on CDK19 [1]

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

Bioactivity JSH-150 is a highly selective and potent inhibitor withCDK9an IC of 1 nM50

Bioactivity Kenpaullone is a potent inhibitor of andCDK1cyclin B with s of 04 μM and 23 nM and also inhibitsGSK-3β IC50

CDK2cyclin A CDK2cyclin E and CDK5p25 with s of 068IC50μM 75 μM 085 μM respectively

26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

FN-1501 Cat No HY-111361

GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO MLS 2052) Cat No HY-10580

GSK3186899 (DDD-853651) Cat No HY-112622

IIIM-290 Cat No HY-111356

Indirubin-3-monoxime-5-sulphonic acid Cat No HY-111931

Indirubin-5-sulfonate Cat No HY-111932

JH-XI-10-02 Cat No HY-111518

JNJ-7706621 Cat No HY-10329

JSH-150 Cat No HY-X0150

Kenpaullone (9-Bromopaullone NSC-664704) Cat No HY-12302

wwwMedChemExpresscom 27

Purity 9861Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9847Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Bioactivity KH-CB19 is a potent and highly specific inhibitor of theCDC2-like kinase isoforms 1 and 4 (CLK1CLK4) IC50 value 20nM (CLK1) [1] Target CLK14 inhibitor in vitro KH-CB19showed potent inhibition of CLK1 with an IC50 of 20 nM andfor the pure isomer KH-CB19 almost 100-fold selectivityhellip

Bioactivity LDC000067 is a highly specific inhibitor with an CDK9 IC50value of 44plusmn10 nM in vitro

Bioactivity LDC4297 is a potent and selective inhibitor with an CDK7 IC50of 013 nM

Bioactivity Lerociclib (G1T38) is a potent and selective inhibitor of with of 1 nM 2 nM for CDK4CyclinD1 andCDK46 IC s50

CDK6CyclinD3 respectively

Bioactivity Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potentand selective inhibitor of with of 1 nMCDK4 CDK6 IC s50and 2 nM for and respectivelyCDK4 CyclinD1 CDK6 CyclinD3

Bioactivity LY2857785 is a type I reversible and competitive ATP kinaseinhibitor against ( 11 nM) and other transcriptionCDK9 IC50kinases ( 16 nM) and ( 246 nM)CDK8 IC50 CDK7 IC50

Bioactivity LY3177833 is an and inhibitor extracted fromCDC7 pMCM2patent US 20140275131and patent WO 2014143601 A1 compoundexample 4 has values of 33 nM and 290 nM respectivelyIC50

Bioactivity MBQ-167 is a dual inhibitor with of 103 nMRacCdc42 IC s50for Rac 123 and 78 nM for Cdc42 in MDA-MB-231 cellsrespectively

Bioactivity MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin inhibitor with an of 5 nM at least 22-fold moreT1 IC50

selective for CDK9 over other CDKs MC180295 also inhibitsGSK-3α and GSK-3β MC180295 ((rel)-MC180295) has pothellip

Bioactivity Milciclib (PHA-848125) is a potent dual inhibitor of andCDK with s of 45 150Tropomyosin receptor kinase (TRK) IC50

160 363 398 nM and 53 nM for cyclin ACDK2 cyclin HCDK7cyclin D1CDK4 cyclin ECDK2 cyclin BCDK1 and TRKArespectively

KH-CB19 Cat No HY-12828

LDC000067 (LDC067) Cat No HY-15878

LDC4297 Cat No HY-12653

Lerociclib (G1T38) Cat No HY-112272

Lerociclib dihydrochloride (G1T38 dihydrochloride) Cat No HY-112272A

LY2857785 Cat No HY-12293

LY3177833 Cat No HY-100023

MBQ-167 Cat No HY-112842

MC180295 ((rel)-MC180295) Cat No HY-119940

Milciclib (PHA-848125) Cat No HY-10424

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9703Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9851Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Bioactivity ML167 is a highly selective Cdc2-like kinase 4 ( )Clk4inhibitor with of 136 nM gt10-fold selectivity forIC50closely related kinases Clk1 Clk2 Clk3 and Dyrk1A1B

Bioactivity MSC2530818 is a potent selective and orally available CDK8inhibitor with an of 26 nM for CDK8IC50

Bioactivity NG 52 (Compound 52 ) is a potent cell-permeable reversibleselective and ATP-compatible inhibitor of the cellcycle-regulating kinase Cdc28p (IC50 = 7 μM) and the relatedPho85p kinase (IC50 = 2 μM)

Bioactivity Nimbolide is a triterpene derived from the leaves and flowersof neem ( L) Nimbolide induces apoptosisAzadirachta indicathrough inactivation of Nimbolide inhibits NF-κB CDK4

kinase activity Nimbolide suppresses the NF-κB WntCDK6PI3K-Akt MAPK and JAK-STAT signaling pathways [1]

Bioactivity NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and26 μM for CDK2 and CDK1 IC50 value 17μM (CDK2) 26μM (CDK1)Target CDK in vitro NU2058 is a competitive inhibitor ofCDK2 with respect to ATP (Ki value CDK2 12 3 μM) that bindsin the ATP binding pocket in a different orientation fromhellip

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity NU6300 is the first covalent ATP-competitive CDK2 inhibitorIC50 value Target CDK2 in vitro NU6300 is a covalent CDK2inhibitor that illustrates the potential of using vinylsulfones to mediate irreversible inhibition NU6300 blocks theinhibitor binding site The effect was time dependent andhellip

Bioactivity NVP-2 is a inhibitor with an of 05 nMCDK9 IC50

Bioactivity NVP-LCQ195 (AT9311 LCQ195) is a small molecule heterocyclicinhibitor of CDK1 CDK2 CDK3 and CDK5 with IC50 of 1-42 nM

Bioactivity ON-013100 an antineoplastic drug acts a mitotic inhibitorthat could inhibit expressionCyclin D1

28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

ML167 (CID44968231 NCGC00188654) Cat No HY-15951

MSC2530818 Cat No HY-101611

NG 52 (Compound 52) Cat No HY-15154

Nimbolide Cat No HY-116035

NU2058 (O6-(Cyclohexylmethyl)guanine) Cat No HY-19316

NU6140 Cat No HY-107419

NU6300 Cat No HY-18930

NVP-2 Cat No HY-12214A

NVP-LCQ195 (LCQ-195 AT9311) Cat No HY-15241

ON-013100 Cat No HY-112822

wwwMedChemExpresscom 29

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9996Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity ON123300 is a potent inhibitor of CDK4 with an IC50 of 38nM with little inhibitory activity against CDKs 125 and 8

Bioactivity Palbociclib (PD 0332991) is a selective and CDK4 CDK6inhibitor with s of 11 and 16 nM respectivelyIC50Palbociclib is a drug for the treatment of ER-positive andHER2-negative breast cancer

Bioactivity Palbociclib hydrochloride is a highly selective CDK46inhibitor with s of 11 nM and 16 nM respectivelyIC50

Bioactivity Palbociclib isethionate is a highly selective inhibitorof with s of 11 nM16 nMCDK46 IC50respectively

Bioactivity PF-06873600 is a selective and orally bioavailable inhibitorof cyclin-dependent kinase with values of 009 nM(CDK) Ki013 nM and 016 nM for CDK2 CDK4 and CDK6 respectivelyPF-06873600 has potential antineoplastic activity [1] [2]

Bioactivity PHA-767491 is a dual inhibitor with s of 10 nMCdc7Cdk9 IC50and 34 nM respectively

Bioactivity PHA-767491 hydrochloride is a dual inhibitor withCdc7Cdk9s of 10 nM and 34 nM respectivelyIC50

Bioactivity PHA-793887 is a potent ATP-competitive inhibitor canCDKinhibit Cdk2 Cdk1 Cdk4 and Cdk9 with s of 8 nM 60 nMIC5062 nM and 138 nM respectively and also inhibits glycogensynthase kinase 3β with an of 79 nMIC50

Bioactivity PROTAC CDK9 Degrader-1 is a selective degraderCDK9 Bioactivity Purvalanol A is a potent inhibitor which inhibitsCDKcdc2-cyclin B cdk2-cyclin A cdk2-cyclin E cdk4-cyclin D1and cdk5-p35 with s of 4 70 35 850 75 nMIC50resepctively

ON123300 Cat No HY-12624

Palbociclib (PD 0332991) Cat No HY-50767

Palbociclib hydrochloride (PD 0332991 hydrochloride) Cat No HY-50767A

Palbociclib isethionate (PD 0332991 isethionate) Cat No HY-A0065

PF-06873600 Cat No HY-114177

PHA-767491 (CAY10572) Cat No HY-13461

PHA-767491 hydrochloride (CAY-10572 hydrochloride) Cat No HY-13461A

PHA-793887 Cat No HY-11001

PROTAC CDK9 Degrader-1 Cat No HY-103628

Purvalanol A (NG-60) Cat No HY-18299A

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9900Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9983Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitorwith IC50 values of 6 6 9 gt 10000 and 6 nM forcdc2cyclin B cdk2cyclin A cdk2cyclin E cdk4cyclin D1and cdk5-p35 respectively

Bioactivity R547 is a potent ATP-competitive inhibitor of CDK124 with Kiof 2 nM3 nM1 nM

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity Ribociclib (LEE011) is a highly specific inhibitorCDK46with s of 10 nM and 39 nM respectivelyIC50

Bioactivity Ribociclib hydrochloride (LEE011 hydrochloride) is a highlyspecific inhibitor with values of 10 nM and 39CDK46 IC50nM respectively and is over 1000-fold less potent againstthe cyclin BCDK1 complex

Bioactivity Ribociclib succinate (LEE011 succinate) is a highly specific inhibitor with values of 10 nM and 39 nMCDK46 IC50

respectively and is over 1000-fold less potent against thecyclin BCDK1 complex

Bioactivity Ribociclib succinate hydrate (LEE011 succinate hydrate) is ahighly specific inhibitor with values of 10 nMCDK46 IC50and 39 nM respectively and is over 1000-fold less potentagainst the cyclin BCDK1 complex

Bioactivity Riviciclib (P276-00 free base) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib shows antituhellip[1] [2]

Bioactivity Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib hydrochlorhellip[1] [2]

30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Purvalanol B (NG 95) Cat No HY-18299

R547 Cat No HY-10014

RGB-286638 Cat No HY-15504

RGB-286638 free base Cat No HY-15504A

Ribociclib (LEE011) Cat No HY-15777

Ribociclib hydrochloride (LEE011 (hydrochloride)) Cat No HY-15777A

Ribociclib succinate (LEE011 (succinate)) Cat No HY-15777B

Ribociclib succinate hydrate (LEE011 (succinate hydrate)) Cat No HY-15777C

Riviciclib (P276-00 (free base)) Cat No HY-16559A

Riviciclib hydrochloride (P276-00) Cat No HY-16559

wwwMedChemExpresscom 31

Purity 9850Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9907Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9677Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ro-3306 is a potent and selective inhibitor of with sCDK1 Kiof 20 nM 35 nM and 340 nM for CDK1 CDK1cyclin B1 andCDK2cyclin E respectively

Bioactivity Roniciclib is an orally bioavailable pan-cyclin dependentkinase inhibitor with of 5-25 nM for CDK1 CDK2(CDK) IC s50CDK3 CDK4 CDK7 and CDK9

Bioactivity SB1317 is a potent inhibitor of and forCDK2 JAK2 FLT3the treatment of cancer with of 13 73 and 56 nM forIC50CDK2 JAK2 and FLT3 respectively

Bioactivity SEL120-34A is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A HCl is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A monohydrochloride is an ATP-competitive andselective inhibitor inhibits kinase activities ofCDK8CDK8CycC and CDK19CycC complexes with s of 44 nM andIC50104 nM respectively with a of 3 nM for CDhellipKd

Bioactivity Seliciclib (Roscovitine) is a potent and selective CDKsinhibitor with s of 02 μM 065 μM and 07 μM for IC50 CDK5

and respectivelyCdc2 CDK2

Bioactivity Senexin A is a inhibitor with an of 280 nMCDK8 IC50

Bioactivity Simurosertib (TAK-931) is a selective cycle 7 kinase(CDC7)inhibitor with an lt03 nMIC50

Bioactivity SNS-032 (BMS-387032) is a selective inhibitor of CDK2 and with s of 38 nM 62 nM and 4CDK7 CDK9 IC50

nM respectively

Ro-3306 Cat No HY-12529

Roniciclib (BAY 1000394) Cat No HY-13914

SB1317 (TG02) Cat No HY-15166

SEL120-34A Cat No HY-111388

SEL120-34A HCl Cat No HY-111388B

SEL120-34A monohydrochloride Cat No HY-111388A

Seliciclib (Roscovitine CYC202 R-roscovitine) Cat No HY-30237

Senexin A Cat No HY-15681

Simurosertib (TAK-931) Cat No HY-100888

SNS-032 (BMS-387032) Cat No HY-10008

Purity 9846Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9796Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9882Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity SU9516 is a potent inhibitor with an of 22 nM andCDK2 IC50also shows inhibitory effects on CDK1 and CDK4 with s ofIC5040 200 nM respectively

Bioactivity SY-1365 is a highly selective covalent inhibitor of CDK7SY-1365 possesses therapeutic potential in both hematologicaland solid tumors [1]

Bioactivity T025 is an orally available and highly potent Cdc2-like kinase inhibitor with s of 48 0096 65 and 061 nM(CLK) Kd

for CLK1 CLK2 CLK3 and CLK4 respectively

Bioactivity THAL-SNS-032 is a selective degrader PROTAC consistingCDK9of a CDK-binding SNS-032 ligand linked to a thalidomidederivative that binds the E3 ubiquitin ligase Cereblon (CRBN)

[1]

Bioactivity THZ1 is a selective and potent covalent inhibitor withCDK7an of 32 nMIC50

Bioactivity THZ1 Hydrochloride is a selective and potent inhibitorCDK7with an of 32 nMIC50

Bioactivity THZ1-R is a non-cysteine reactive analog of THZ1 whichdisplays diminished activity for inhibition THZ1-RCDK7binds to with a of 142 nMCDK7 Kd

Bioactivity THZ2 is a potent and selective inhibitor with an ofCDK7 IC50139 nM

Bioactivity THZ531 is a covalent inhibitor of both and withCDK12 CDK13s of 158 nM and 69 nM respectivelyIC50

Bioactivity Trilaciclib is a inhibitor with s of 1 nM and 4 nMCDK46 IC50for CDK4 and CDK6 respectively

32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SU9516 Cat No HY-18629

SY-1365 Cat No HY-128587

T025 Cat No HY-112296

THAL-SNS-032 Cat No HY-123937

THZ1 Cat No HY-80013

THZ1 Hydrochloride Cat No HY-80013A

THZ1-R Cat No HY-19988

THZ2 Cat No HY-12280

THZ531 Cat No HY-103618

Trilaciclib (G1T28) Cat No HY-101467

wwwMedChemExpresscom 33

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Trilaciclib hydrochloride is a inhibitor with s ofCDK46 IC501 nM and 4 nM for CDK4 and CDK6 respectively

Bioactivity Voruciclib hydrochloride is a clinical stage oral CDK9inhibitor Voruciclib hydrochloride represses expression ofMCL-1 in multiple models of diffuse large B-cell lymphoma(DLBCL) [1]

Bioactivity Wogonin is a naturally occurring mono-flavonoid can inhibitthe activity of and and exhibitsCDK8 Wntanti-inflammatory and anti-tumor effects

Bioactivity XL413 is a potent selective and ATP competitive inhibitor of with an of 34 nM and also shows potent effectCdc7 IC50

with s of 215 42 nM on CK2 PIM1 respectively and anIC50 of 118 nM on pMCMEC50

Bioactivity XL413 hydrochloride is a potent selective and ATP competitiveinhibitor of with an of 34 nM and also showsCdc7 IC50potent effect with s of 215 42 nM on CK2 PIM1IC50respectively and an of 118 nM on pMCMEC50

Trilaciclib hydrochloride (G1T28 hydrochloride) Cat No HY-101467A

Voruciclib hydrochloride Cat No HY-12422A

Wogonin Cat No HY-N0400

XL413 Cat No HY-15260

XL413 hydrochloride Cat No HY-15260A

Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) are protein kinases that are involved in cellcycle control Two checkpoint kinase subtypes have been identifiedChk1 and Chk2 Chk1 is a central component of genome surveillancepathways and is a key regulator of the cell cycle and cell survivalChk1 is required for the initiation of DNA damage checkpoints andhas recently been shown to play a role in the normal (unperturbed)cell cycle Chk1 impacts various stages of the cell cycle including the Sphase G2M transition and M phase In addition to mediating cellcycle checkpoints Chk1 also contributes to DNA repair processesgene transcription embryo development cellular responses to HIVinfection and somatic cell viability Chk2 is a protein kinase that is

activated in response to DNA damage and is involved in cell cycle arrest In response to DNA damage and replicationblocks cell cycle progression is halted through the control of cell cycle regulators The protein encoded by this gene isa cell cycle checkpoint regulator and putative tumor suppressor

34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 35

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9877Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9990Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Checkpoint Kinase (Chk) Inhibitors amp Modulators

Bioactivity AZD-7762 is a potent ATP-competitive checkpoint kinase ( )Chkinhibitor in with an of 5 nM for Chk1IC50

Bioactivity BML-277 is a selective checkpoint kinase 2 ( ) inhibitorChk2with an of 15 nMIC50

Bioactivity CCT241533 is a potent and selective ATP competitive inhibitorof with an of 3 nM and of 116 nMCHK2 IC50 Ki

Bioactivity CCT241533 hydrochloride is a potent and selective CHK2inhibitor with an of 3 nM and a of 116 nMIC50 Ki

Bioactivity CCT244747 is a potent orally bioavailable and highlyselective inhibitor with an of 77 nM CCT244747CHK1 IC50also abrogates G2 checkpoint with an of 29 nMIC50

Bioactivity CCT245737 is a orally active and seletive inhibitorChk1with an of 13 nMIC50

Bioactivity CHIR-124 is a potent and selective inhibitor with Chk1 IC50of 03 nM and also potently targets and withPDGFR FLT3

s of 66 nM and 58 nMIC50

Bioactivity CHK-IN-1 is an inhibitor of and withCHK1 CHK2anti-proliferative activities

Bioactivity CHK1 inhibitor is an inhibitor of CHK1 Bioactivity CHK1-IN-2 is a checkpoint kinase 1 inhibitor with an(CHK1) of 6 nMIC50

AZD-7762 Cat No HY-10992

BML-277 (Chk2 Inhibitor II) Cat No HY-13946

CCT241533 Cat No HY-14715

CCT241533 hydrochloride Cat No HY-14715B

CCT244747 Cat No HY-18175

CCT245737 Cat No HY-18958

CHIR-124 Cat No HY-13263

CHK-IN-1 Cat No HY-U00345

CHK1 inhibitor Cat No HY-104022

CHK1-IN-2 Cat No HY-111369

Purity 9965Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9791Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity CHK1-IN-3 is a inhibitor with anCheckpoint Kinase 1 (CHK1) of 04 nM IC50

[1]Bioactivity GDC-0575 (ARRY-575 RG7741) is a highly-selective oral

small-molecule inhibitor with an of 12nMChk1 IC50

Bioactivity GDC-0575 dihydrochloride is an orally bioavailable CHK1inhibitor with an of 12 nM and has antitumor activityIC50

Bioactivity PF 477736 is a potent selective ATP-competitive inhibitor of with a of 049 nM 100-fold selectivity versus Chk1 Ki Chk2

( 47 nM)Ki

Bioactivity Prexasertib (LY2606368) is a potent selective andATP-competitive inhibitor with ancheckpoint kinase 1 (Chk1)

and a of lt1 nM and 09 nM respectivelyIC50 Ki

Bioactivity Prexasertib dihydrochloride (LY2606368 dihydrochloride) is apotent and selective ATP competitive inhibitor of the Chk1protein kinase with s of lt1 nM and 8 nM for CHK1 andIC50CHK2 respectively and a of 09 nM against purified CHK1Ki

Bioactivity Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is apotent selective ATP competitive and inhibitorCHK1 CHK2with a of 09 nM for CHK1 and s of lt1 nM 8 nM forKi IC50CHK1 and CHK2 respectively Prexasertib Mesylate Hydrateinhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2hellip

Bioactivity Rabusertib (LY2603618) is a potent and selective inhibitor of with an of 7 nMChk1 IC50

Bioactivity SCH900776 is a potent selective and oral inhibitor ofcheckpoint kinase1 ( ) with an of 3 nM It shows 50-Chk1 IC50and 500-fold selectivity over CDK2 andChk2 respectively

36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CHK1-IN-3 Cat No HY-128601

GDC-0575 (ARRY-575 RG7741) Cat No HY-112167

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride RG7741 dihydrochloride) Cat No HY-112167A

PF 477736 (PF 00477736) Cat No HY-10032

Prexasertib (LY2606368) Cat No HY-18174

Prexasertib dihydrochloride (LY2606368 (dihydrochloride)) Cat No HY-18174A

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate LY2940930) Cat No HY-18174B

Rabusertib (LY2603618 IC-83) Cat No HY-14720

SCH900776 (MK-8776) Cat No HY-15532

wwwMedChemExpresscom 37

CRISPRCas9

CRISPRCas9 (Clustered Regularly-Interspaced Short PalindromicRepeatsCas9) is a bacterial immune system that has been adaptedfor genome editing in mammalian cells Cas9 is a programmablenuclease that generates double-stranded breaks (DSB) in DNAdictated by binding of a ~20 nucleotide recombinant ldquoguide RNArdquo(gRNA) to the target site DSBrsquos produced by Cas9 are most oftenrepaired through the cellrsquos error-prone non-homologous end joining(NHEJ) pathway resulting in small insertions or deletions (indels) Thevast majority of indels shift the reading frame introducing apremature stop codon or resulting in nonsense mediated decay ofthe mRNA-effectively ldquoknocking outrdquo a gene

The CRISPRCas9 system has substantially advanced efforts in specific gene editing and has been successfully appliedto modify the episomal genomes of human and other organisms The CRISPRCas9 system utilizes a prokaryoticRNA-guided programmable nuclease that can make a double-strand DNA break (DSB) at a specific site under theguidance of a leading RNA This DSB process depends on the co-expression of two basic components a guide RNA(gRNA) and Cas9 nuclease Making a specific DSB can trigger DNA repair via either error-prone non-homologous endjoining (NHEJ) or homology-directed repair (HDR) In the presence of the CRISPRCas9 system the NHEJ inhibitorSCR7 is proven to increase the efficiency of Cas9-mediated HDR by at least by 7-fold in mammalian cells Genomeediting via CRISPRCas9 has become an efficient and reliable way to make precise targeted changes to the genome ofliving cells

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

CRISPRCas9 Inhibitors amp Modulators

Bioactivity Brefeldin A is a specific inhibitor of whichprotein traffickingblocks the protein transport from the endoplasmic reticulum tothe Golgi complex

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity L755507 is a potent selective agonist of with an β -AR3 IC50of 35 nM

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity Zidovudine is a nucleoside reverse transcriptase inhibitor () widely used to treat HIV infection Zidovudine increasesNRTI

CRISPRCas9-mediated editing frequency

38 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Brefeldin A (BFA Cyanein Decumbin) Cat No HY-16592

KU-57788 (NU7441) Cat No HY-11006

L755507 Cat No HY-19334

Nocodazole (Oncodazole R17934) Cat No HY-13520

RS-1 Cat No HY-19793

SCR7 Cat No HY-12742

Zidovudine (Azidothymidine AZT ZDV) Cat No HY-17413

wwwMedChemExpresscom 39

DeubiquitinaseDUBs

Deubiquitinases (DUBs) are a large group of proteases that cleaveubiquitin from proteins and other molecules Ubiquitin is attached toproteins in order to regulate the degradation of proteins via theproteasome and lysosome coordinate thecellular localisation ofproteins activate and inactivate proteins and modulateprotein-protein interactions DUBs can reverse these effects bycleaving the peptide or isopeptide bond between ubiquitin and itssubstrate protein In humans there are nearly 100 DUB genes whichcan be classified into two main classes cysteine proteases andmetalloproteases The cysteine proteases comprise ubiquitin-specificproteases (USPs) ubiquitin C-terminal hydrolases (UCHs)

Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU) The metalloprotease groupcontains only the Jab1Mov34Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases DUBs play several roles inthe ubiquitin pathway One of the best characterised functions of DUBs is the removal of monoubiqutin andpolyubiquitin chainsfrom proteins

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9940Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9892Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9893Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Deubiquitinase Inhibitors amp Modulators

Bioactivity 6-Thioguanine (Thioguanine) is an anti-leukemia andimmunosuppressant agent acts as an inhibitor of SARS and MERScoronavirus papain-like proteases ( ) and also potentlyPLprosinhibits activity with s of 25 μM and 40 μM forUSP2 IC50Plpros and recombinant human USP2 respectively

Bioactivity b-AP15 is a specific inhibitor of the enzymesdeubiquitinating and UCHL5 Usp14

Bioactivity BAY 11-7082 is a inhibitor which decreases NF-κB byNF-κBinhibiting TNF-α-induced phosphorylation of IκB-α BAY 11-7082inhibits ubiquitin-specific protease and withUSP7 USP21

s of 019 μM and 096 μM respectivelyIC50

Bioactivity C527 is a is a pan inhibitor with a highDUB enzymepotency for the complex ( =088 μM)USP1UAF1 IC50

Bioactivity Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB)inhibitor directly inhibiting DUB activity of USP9x USP5USP14 and UCH37 Degrasyn has been shown to downregulate theantiapoptotic proteins and Bcr-Abl JAK2

Bioactivity DUBs-IN-1 is an active inhibitor of ubiquitin-specific with an of 024 μM for USP8proteases (USPs) IC50

Bioactivity DUBs-IN-2 is a potent inhibitor with an ofdeubiquitinase IC50028 μM for USP8

Bioactivity DUBs-IN-3 is a potent enzyme inhibitordeubiquitinase (USP)extracted from reference compound 22c with an of 056 μMIC50for USP8

Bioactivity EOAI3402143 is a ( ) inhibitor whichdeubiquitinase DUBinhibits dose-dependently inhibits and Usp9x Usp24 Usp5

Bioactivity FT671 is a potent non-covalent and selective inhibitorUSP7with an of 52 nM and binds to the USP7 catalytic domainIC50with a of 65 nMKd

40 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

6-Thioguanine (Thioguanine2-Amino-6-purinethiol) Cat No HY-13765

b-AP15 (NSC 687852) Cat No HY-13989

BAY 11-7082 (BAY 11-7821) Cat No HY-13453

C527 Cat No HY-12988

Degrasyn (WP1130) Cat No HY-13264

DUBs-IN-1 Cat No HY-50736

DUBs-IN-2 Cat No HY-50737A

DUBs-IN-3 Cat No HY-50737

EOAI3402143 Cat No HY-111408

FT671 Cat No HY-107985

wwwMedChemExpresscom 41

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9773Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9684Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity FT827 is a selective and covalent ubiquitin-specific protease7 ( ) inhibitor with an of 52 nMUSP7 IC50

Bioactivity GNE-6640 is a selective and non-covalent inhibitor ofubiquitin epecific peptidase 7 with values of(USP7) IC50075 μM 043 μM 203 μM and 023 μM for full length USP7USP7 catalytic domain full length USP43 and Ub-MDM2respectively

Bioactivity GNE-6776 is a selective inhibitorUSP7 Bioactivity HBX 19818 is a specific inhibitor of ubiquitin-specific with an of 281 μMprotease 7 (USP7) IC50

Bioactivity IU1 is a special inhibitor with of 4-5 μMUsp14 IC50 Bioactivity IU1-47 is a potent inhibitor with an of 06 μMUSP14 IC50

IU1-47 induces tau elimination in cultured neurons [1]

Bioactivity LDN-57444 is a reversible competitive and site-directedinhibitor of withubiquitin C-terminal hydrolase L1 (UCH-L1)an of 088 μM and a of 040 μM LDN-57444 alsoIC50 Kisuppresses UCH-L3 activity with an of 25 μMIC50

Bioactivity MF-094 is a potent and selective inhibitor with an USP30 IC50of 120 nM

Bioactivity ML-323 is a reversible potent inhibitor with USP1-UAF1 IC50of 76 nM in a Ub-Rho assay The measured inhibition constantsof ML-323 for the free enzyme ( ) is 68 nMKi

Bioactivity ML364 is an inhibitor of ubiquitin specific peptidase 2 and can be used for the research of breast cancer(USP2)

extracted from patent WO 2016134026 A1 compound Figure 10G

FT827 Cat No HY-111350

GNE-6640 Cat No HY-112937

GNE-6776 Cat No HY-107986

HBX 19818 Cat No HY-17540

IU1 Cat No HY-13817

IU1-47 Cat No HY-122243

LDN-57444 Cat No HY-18637

MF-094 Cat No HY-112438

ML-323 Cat No HY-17543

ML364 Cat No HY-100900

Purity 9800Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9737Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9843Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NSC632839 is a nonselective isopeptidase inhibitor whichinhibits and with s of 45plusmn4 μMUSP2 USP7 SENP2 EC5037plusmn1 μM and 98plusmn18 μM respectively

Bioactivity P 22077 is a cell-permeable ubiquitin-specific protease 7 inhibitor with an of 801 μM It also inhibits(USP7) EC50

USP47 with an of 874 μMEC50

Bioactivity P005091 is a selective and potent inhibitor of with anubiquitin-specific protease 7 (USP7)

of 42 μMEC50

Bioactivity PR-619 is a broad-range inhibitor with of 393DUB EC5049 686 72 and 861 μM for USP4 USP8 USP7 USP2and respectivelyUSP5

Bioactivity SJB2-043 is an inhibitor of the native complex withUSP1UAF1 of 544 nMIC50

Bioactivity SJB3-019A is a potent and novel inhibitor 5 times moreUSP1potent than SJB2-043 in promoting ID1 degradation andcytoxicity in K562 cells with of 00781 μMIC50

Bioactivity USP7-IN-1 is a selective and reversible inhibitor of with an of 77 μMubiquitin-specific protease 7 (USP7) IC50

and can be used for the research of cancer

Bioactivity USP7-IN-3 (Compound 5) is a potent and selective allostericubiquitin-specific protease 7 ( ) inhibitor USP7 [1]

Bioactivity USP7USP47 inhibitor is a selective ubiquitin-specific protease inhibitor with s of 042 μM and 10747 (USP7USP47) EC50

μM respectively

Bioactivity VLX1570 is a competitive inhibitor of proteasomedeubiquitinases ( ) with an of approximate 10 μMDUBs IC50

42 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NSC632839 Cat No HY-100708

P 22077 Cat No HY-13865

P005091 (P5091) Cat No HY-15667

PR-619 Cat No HY-13814

SJB2-043 Cat No HY-15757

SJB3-019A Cat No HY-80012

USP7-IN-1 Cat No HY-16709

USP7-IN-3 Cat No HY-112128

USP7USP47 inhibitor Cat No HY-13487

VLX1570 Cat No HY-12471

wwwMedChemExpresscom 43

DNA AlkylatorCrosslinker

DNA alkylatorcrosslinker is a molecule that alkylates DNA or cancross link with DNA DNA alkylatorcrosslinker can have mutagenicpharmaceutical or other effects Alkylation is the transfer of an alkylgroup from one molecule to another The alkyl group may betransferred as an alkyl carbocation a free radical a carbanion or acarbene Alkylating agents are widely used in chemistry because thealkyl group is probably the most common group encountered inorganic molecules Selective alkylation or adding parts to the chainwith the desired functional groups is used especially if there is nocommonly available biological precursor Alkylation with only onecarbon is termed methylation In medicine alkylation of DNA is used

in chemotherapy to damage the DNA of cancer cells Alkylation is accomplished with the class of drugs calledalkylating antineoplastic agents Crosslinking of DNA occurs when various exogenous or endogenous agents reactwith two different positions in the DNA This can either occur in the same strand (intrastrand crosslink) or in theopposite strands of the DNA (interstrand crosslink) Crosslinks also occur between DNA and protein DNA replicationis blocked by crosslinks which causes replication arrest and cell death if the crosslink is not repaired The RAD51family plays a role in repair

Purity 990Clinical Data LaunchedSize 100 mg 500 mg

Purity 9879Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9844Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9961Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

DNA AlkylatorCrosslinker Inhibitors amp Modulators

Bioactivity Altretamine is an antineoplastic agentalkylating Bioactivity Altretamine hydrochloride is an antineoplasticalkylatingagent

Bioactivity Bendamustine D4 is the deuterium labeled BendamustineBendamustine is a agent that causes DNADNA cross-linkingbreaks with alkylating and antimetabolite properties

Bioactivity Bendamustine hydrochloride is a agent thatDNA cross-linkingcauses DNA breaks with alkylating and antimetaboliteproperties

Bioactivity Busulfan is a potent with selective immunosuppressivealkylatoreffect on bone marrow

Bioactivity Calicheamicin is a cytotoxic agent that causes double-strandDNA breaks

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity Carmustine is an antitumor chemotherapeutic agent which worksby akylating DNA and RNA

Bioactivity Chlorambucil is an agent with antitumor activityalkylating Bioactivity Cisplatin is a antineoplastic chemotherapy drug which works bycross-linking with and causing DNA damage in cancerDNAcells

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Altretamine (ENT-50852 RB-1515 WR-95704) Cat No HY-B0181

Altretamine hydrochloride (ENT-50852 hydrochloride RB-1515

hydrochloride WR-95704 hydrochloride) Cat No HY-B0181A

Bendamustine D4 (SDX-105 D4) Cat No HY-13567S

Bendamustine hydrochloride (SDX-105 EP-3101) Cat No HY-B0077

Busulfan Cat No HY-B0245

Calicheamicin (Calicheamicin γ1) Cat No HY-19609

Carboplatin (NSC 241240) Cat No HY-17393

Carmustine Cat No HY-13585

Chlorambucil (CB-1348 WR-139013) Cat No HY-13593

Cisplatin (CDDP cis-Diaminodichloroplatinum) Cat No HY-17394

wwwMedChemExpresscom 45

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 980Clinical Data LaunchedSize 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Bioactivity Cyclophosphamide is a synthetic agent chemicallyalkylatingrelated to the nitrogen mustards with antineoplastic andimmunosuppressive activities

Bioactivity Cyclophosphamide hydrate is a synthetic agentalkylatingchemically related to the nitrogen mustards withantineoplastic and immunosuppressive activities

Bioactivity Fotemustine is a agent with antitumor activityDNA-alkylating Bioactivity Ifosfamide is an chemotherapeutic agent withalkylatingactivity against a wide range of tumors

Bioactivity Lomustine (CCNU) is a agent with antitumorDNA alkylatingactivity

Bioactivity Melphalan is an effective agent with potentDNA alkylatingantitumor activity

Bioactivity Methylnitronitrosoguanidine (MNNG) is an agent withalkylatingtoxic and mutagenic effects [1]

Bioactivity Miriplatin is a chemotherapy agent which belongs to the classof agentsalkylating

Bioactivity Miriplatin hydrate is a chemotherapy agent which belongs tothe class of agentsalkylating

Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Cyclophosphamide Cat No HY-17420

Cyclophosphamide hydrate (Cyclophosphamide monohydrate) Cat No HY-17420A

Fotemustine (S10036) Cat No HY-B0733

Ifosfamide Cat No HY-17419

Lomustine (CCNU NSC 79037) Cat No HY-13669

Melphalan (L-PAM) Cat No HY-17575

Methylnitronitrosoguanidine (MNNG) Cat No HY-128612

Miriplatin (SM-11355) Cat No HY-16325A

Miriplatin hydrate (SM-11355 (hydrate)) Cat No HY-16325

Mitomycin C (Ametycine) Cat No HY-13316

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9926Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9986Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Oxaliplatin is a inhibitor It causes DNADNA synthesiscrosslinking damage prevents DNA replication andtranscription and causes cell death

Bioactivity Palifosfamide is a novel DNA alkylator and the activemetabolite of ifosfamide with antitumor activity

Bioactivity Procarbazine Hydrochloride is an agent withalkylatinganticancer activity

Bioactivity RITA is an inhibitor of binds top53-HDM-2 interactionp53dN with a of 15 nM and also induces Kd DNA-DNA

cross-links

Bioactivity Satraplatin is an agent with potent antitumoralkylatingeffect

Bioactivity SJG-136 is a agent with an of 45 nMDNA cross-linking XL50for pBR322 DNA SJG-136 has potent antitumor activity

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity Temozolomide (NSC 362856 CCRG 81045) is an oral DNA agent used to treat some brain cancersalkylating

Bioactivity Thio-TEPA is a agent with antitumor activityDNA alkylating Bioactivity Treosulfan (NSC 39069Treosulphan) is an agent withalkylatingactivity in ovarian cancer and other solid tumor types

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Oxaliplatin Cat No HY-17371

Palifosfamide (Isophosphoramide mustard IPM ZIO-201) Cat No HY-14798

Procarbazine Hydrochloride Cat No HY-13733

RITA (NSC 652287) Cat No HY-13424

Satraplatin (BMS182751 BMY45594 JM216) Cat No HY-17576

SJG-136 (NSC-694501) Cat No HY-14573

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

Temozolomide (NSC 362856 CCRG 81045 TMZ) Cat No HY-17364

Thio-TEPA Cat No HY-17574

Treosulfan (NSC 39069 Treosulphan) Cat No HY-16503

wwwMedChemExpresscom 47

Purity 980Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Uramustine is an oral agent effective in thealkylatingtreatment of lymphosarcoma chronic lymphatic leukaemia andthrombocythemia

Bioactivity VAL-083 is an agent that creates N7 methylation onalkylatingDNA with antitumor activity

Uramustine (Uracil mustard) Cat No HY-13544

VAL-083 (Dianhydrodulcitol Dianhydrogalactitol) Cat No HY-16513

DNA-PKDNA-dependent protein kinase

DNA-PKcs (DNA-dependent protein kinase catalytic subunit) is anenzyme that in humans is encoded by the PRKDC gene DNA-PKcsbelongs to the phosphatidylinositol 3-kinase-related kinase proteinfamily DNA-PKcs is the catalytic subunit of a nuclear DNA-dependentserinethreonine protein kinase called DNA-PK The secondcomponent is the autoimmune antigen Ku On its own DNA-PKcs isinactive and relies on Ku to direct it to DNA ends and trigger itskinase activity DNA-PKcs is required for the non-homologous endjoining (NHEJ) pathway of DNA repair Many proteins have beenidentified as substrates for the kinase activity of DNA-PKAutophosphorylation of DNA-PKcs appears to play a key role in NHEJ

and is thought to induce a conformational change that allows end processing enzymes to access the ends of thedouble-strand break DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNAdamage checkpoint

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wwwMedChemExpresscom 49

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9943Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9722Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9664Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9239Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

DNA-PK Inhibitors amp Modulators

Bioactivity (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer ofNedisertib with an in the range of 7-30 nM for IC50 DNA-PK

[1]

Bioactivity AZD-7648 is a potent and selective inhibitorDNA-PKAnti-tumor activity [1]

Bioactivity CC-115 is a potent and dual and kinaseDNA-PK mTORinhibitor with s of 13 nM and 21 nM respectively CC-115IC50blocks both and signalingmTORC1 mTORC2

Bioactivity CC-115 hydrochloride is a potent and dual and DNA-PK mTORkinase inhibitor with s of 13 nM and 21 nM respectivelyIC50CC-115 blocks both and signalingmTORC1 mTORC2

Bioactivity Compound 401 is a synthetic inhibitor of ( = 028DNA-PK IC50μM) that also targets mTOR but not PI3K in vitro

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity LTURM34 is a specific inhibitor with an of 0034DNA-PK IC50μM

Bioactivity LY3023414 potently and selectively inhibits class I PI3Kisoforms and with s of 607 nM 776DNA-PK mTORC12 IC50nM 38 nM 238 nM 424 nM and 165 nM for PI3Kα PI3KβPI3Kδ PI3Kγ DNA-PK and mTOR respectively LY3023414potently inhibits at low nanomolarhellipmTORC1 2

Bioactivity Nedisertib (M3814) is a potent and selective inhibitor of ( ) with an of lt3DNA-dependent Protein Kinase DNA-PK IC50

nM

Bioactivity NU 7026 is a novel specific inhibitor with ofDNA-PK IC50023plusmn001 μM also inhibits with of 13plusmn3 μMPI3K IC50

(R)-Nedisertib ((R)-M3814) Cat No HY-101570A

AZD-7648 Cat No HY-111783

CC-115 Cat No HY-16962

CC-115 hydrochloride Cat No HY-16962A

Compound 401 Cat No HY-19341

KU-57788 (NU7441) Cat No HY-11006

LTURM34 Cat No HY-101667

LY3023414 Cat No HY-12513

Nedisertib (M3814) Cat No HY-101570

NU 7026 (DNA-PK Inhibitor II LY293646) Cat No HY-15719

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9937Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9145Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity PI-103 is a potent and inhibitor with s of 8PI3K mTOR IC50nM 88 nM 48 nM 150 nM 20 nM and 83 nM for p110α p110β

and PI-103 also inhibitsp110δ p110γ mTORC1 mTORC2 with an of 2 nMDNA-PK IC50

Bioactivity PI-103 Hydrochloride is a dual and inhibitor withPI3K mTORs of 8 nM 88 nM 48 nM 150 nM 20 nM and 83 nM forIC50

and p110α p110β p110δ p110γ mTORC1 mTORC2PI-103 also inhibits with an of 2 nMDNA-PK IC50

Bioactivity PIK-75 is a and inhibitor which inhibits DNA-PKDNA-PK PI3K and p110γ with s of 2 58 and 76 nM respectivelyp110α IC50

PIK-75 inhibits p110α gt200-fold more potently than p110β(IC =13 μM)50

Bioactivity PIK-90 is a and inhibitor which inhibits DNA-PK PI3K p110α and with s of 11 18 and 13 nMp110γ DNA-PK IC50

respectively

Bioactivity Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib apotent inhibitor with an of lt3 nM DNA-PK IC50

[1]Bioactivity SF2523 is a highly selective and potent inhibitor of withPI3K

s of 34 nM 158 nM 9 nM 241 nM and 280 nM for IC50 PI3Kα

BRD4 and mTOR respectivelyPI3Kγ DNA-PK

Bioactivity STL127705 (Compound L) is a Ku 7080 heterodimer proteininhibitor inhibits Ku7080-DNA interaction with an ofIC5035 μM STL127705 also inhibits Ku-dependent activation ofDNA-PKCS kinase ( 25 μM) IC50

[1]

Bioactivity Torin 2 is an inhibitor with of 025 nM formTOR EC50inhibiting cellular mTOR activity and exhibits 800-foldselectivity over PI3K (EC 200 nM) Torin 2 also inhibits50

with an of 05 nM in the cell free assay TorihellipDNA-PK IC50

Bioactivity VX-984 is a potent inhibitorDNA-PK Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

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PI-103 Cat No HY-10115

PI-103 Hydrochloride Cat No HY-10115A

PIK-75 (PIK-75 Hydrochloride) Cat No HY-13281

PIK-90 Cat No HY-12030

Rac-Nedisertib (Rac-M3814) Cat No HY-101570B

SF2523 Cat No HY-101146

STL127705 Cat No HY-122727

Torin 2 Cat No HY-13002

VX-984 (M9831) Cat No HY-19939S

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

wwwMedChemExpresscom 51

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity YU238259 is an inhibitor of homology-dependent DNA repair () used for cancer researchHDR

YU238259 Cat No HY-19977

DNARNA Synthesis

RNA synthesis which is also called DNA transcription is a highlyselective process Transcription by RNA polymerase II extends beyondRNA synthesis towards a more active role in mRNA maturationsurveillance and export to the cytoplasmSingle-strand breaks are repaired by DNA ligase using thecomplementary strand of the double helix as a template with DNAligase creating the final phosphodiester bond to fully repair theDNADNA ligases discriminate against substrates containing RNAstrands or mismatched base pairs at positions near the ends of thenickedDNA Bleomycin (BLM) exerts its genotoxicity by generatingfree radicals whichattack C-4prime in the deoxyribose backbone of DNA

leading to opening of the ribose ring and strand breakage it is an S-independentradiomimetic agent that causesdouble-strand breaks in DNAFirst strand cDNA is synthesized using random hexamer primers and M-MuLV Reverse Transcriptase (RNase H)Second strand cDNA synthesis is subsequently performed using DNA Polymerase I and RNase H The remainingoverhangs are converted into blunt ends using exonucleasepolymerase activity After adenylation of the 3prime ends ofDNA fragments NEBNext Adaptor with hairpin loop structure is ligated to prepare the samples for hybridization Cellcycle and DNA replication are the top two pathways regulated by BET bromodomain inhibition Cycloheximide blocksthe translation of mRNA to protein

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wwwMedChemExpresscom 53

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 1 mg 2 mg 5 mg

Purity 9876Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9989Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 9968Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

25 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

DNARNA Synthesis Inhibitors amp Modulators

Bioactivity 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is amodified nucleoside 2-(Methylamino)-1H-purin-6(7H)-one is anendogenous methylated nucleoside found in human fluids

Bioactivity 374-Trihydroxyflavone isolated from Rhus javanica var is a flavonoid with DNA strand-scission activityroxburghiana

[1]

Bioactivity 5-Methoxyflavone belonged to Flavonoid family is a DNApolymerase-beta inhibitor and neuroprotective agent againstbeta-amyloid toxicity possess central nervous system (CNS)depressant effect mediated through the ionotropic GABA Areceptors

Bioactivity 6-Thio-2-Deoxyguanosine is a nucleoside analogue that can beincorporated into de novo-synthesized telomeres by telomerase

Bioactivity Acelarin (NUC-1031) is a ProTide transformation andenhancement of the widely-used nucleoside analoguegemcitabine

Bioactivity Actinomycin D inhibits with an of 042 μMDNA repair IC50

Bioactivity Adenine is a purine derivative and a nucleobase with a varietyof roles in biochemistry Target Nucleosideantimetaboliteanalog Adenine is a nucleobase with a varietyof roles in biochemistry including cellular respiration inthe form of both the energy-rich adenosine triphosphate (ATP)hellip

Bioactivity alpha-Amanitin is the principal toxin of several deadlypoisonous mushrooms exerting its toxic function by inhibiting

RNA-polymerase II

Bioactivity Anisomycin is a potent inhibitor whichprotein synthesisinterferes with protein and by inhibitingDNA synthesispeptidyl transferase or the 80S ribosome system Anisomycin isa JNK activator which increases phospho-JNK

Bioactivity Beaucage reagent is found to be potent in causing DNAcleavage

2-(Methylamino)-1H-purin-6(7H)-one (N2-methylguanine) Cat No HY-101412

374-Trihydroxyflavone (5-Deoxykampferol) Cat No HY-111806

5-Methoxyflavone Cat No HY-107790

6-Thio-2-Deoxyguanosine (6-thio-dG β-TGdR) Cat No HY-18762

Acelarin (NUC-1031) Cat No HY-100885

Actinomycin D (Dactinomycin Actinomycin IV) Cat No HY-17559

Adenine (6-Aminopurine Vitamin B4) Cat No HY-B0152

alpha-Amanitin (α-Amanitin α-Amatoxin) Cat No HY-19610

Anisomycin (Flagecidin Wuningmeisu C) Cat No HY-18982

Beaucage reagent Cat No HY-100951

Purity 9847Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity 9804Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9896Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Bioactivity Bleomycin sulfate is a inhibitor with potentDNA synthesisantitumor activity

Bioactivity BMH-21 is a small molecule DNA intercalator that bindsribosomal DNA and inhibits RNA polymerase I (Pol I)transcription does not cause phosphorylation of H2AX

Bioactivity Branaplam (LMI070) is a highly potent selective and orallyactive small molecule modulatorSMN2 splicing

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity CeMMEC1 is an inhibitor of and also has high affinityBRD4for with an of 09 μM for TAF1 and a of 18TAF1 IC50 KdμM for TAF1 (2)

Bioactivity CeMMEC13 is a potent inhibitor of bromodomain withTAF1 (2)an of 21 μMIC50

Bioactivity Chebulinic acid is a potent natural inhibitor of Mtuberculosis DNA gyrase also can inhibit SMAD-3phosphorylation inhibit H+ K+-ATPase activity

Bioactivity COH29 is a potent ribonucleotide reductase ( ) inhibitorRNRwith anticancer activity COH29 inhibits α and β subunit ofRNR with s of 16 μMIC50

Bioactivity CX-5461 is a potent and oral inhibitor ItrRNA synthesisinhibits RNA polymerase I-driven transcription of rRNA with

s of 142 113 and 54 nM in HCT-116 A375 and MIA PaCa-2IC50cells respectively

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Bleomycin sulfate Cat No HY-17565

BMH-21 Cat No HY-12484

Branaplam (LMI070 NVS-SM1) Cat No HY-19620

Capecitabine Cat No HY-B0016

Carboplatin (NSC 241240) Cat No HY-17393

CeMMEC1 Cat No HY-111445

CeMMEC13 Cat No HY-101088

Chebulinic acid Cat No HY-N2033

COH29 (RNR Inhibitor COH29) Cat No HY-19931

CX-5461 Cat No HY-13323

wwwMedChemExpresscom 55

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9872Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9963Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9945Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg

Bioactivity CX-5461 dihydrochloride is a potent and orally bioavailableinhibitor of Pol I-mediated with s of 142rRNA synthesis IC50nM in HCT-116 113 nM in A375 and 54 nM in MIA PaCa-2 cellsand shows little or no effect on Pol II ( ge25 μM)IC50

Bioactivity Cycloheximide (Naramycin A) is an eukaryote protein synthesisinhibitor with s of 5325 nM and 2880 nM for proteinIC50synthesis and RNA synthesis respectivelyin vivo

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Datelliptium chloride is a DNA-intercalating agent derivedfrom ellipticine with anti-tumor activities

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Didox (NSC-324360) is a synthetic (ribonucleotide reductase) inhibitorRR

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

CX-5461 dihydrochloride Cat No HY-13323A

Cycloheximide (Naramycin A Actidione CHX) Cat No HY-12320

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Datelliptium chloride Cat No HY-U00337

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Didox (NSC-324360) Cat No HY-19387

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Bioactivity Folic acid(Vitamin M Vitamin B9) is a B vitamin is necessaryfor the production and maintenance of new cells for DNAsynthesis and RNA synthesis

Bioactivity GC7 Sulfate is a ( ) inhibitordeoxyhypusine synthase DHPS

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity GNE-371 is a potent and selective chemical probe for thesecond bromodomains of human transcription-initiation-factor

subunit 1 and transcription-initiation-factor TFIID TFIIDsubunit 1-like with an of 10 nM for TAF1(2)IC50

Bioactivity Guanine is one of the fundamental components of nucleic acids( and ) Guanine is a purine derivative consistingDNA RNAof a fused pyrimidine-imidazole ring system with conjugateddouble bonds

Bioactivity Halofuginone (RU-19110) is a less-toxic form of Febrifuginewhich is isolated from the plant Dichroa febrifuga [1]

Halofuginone inhibits in anprolyl-tRNA synthetaseATP-dependent manner with a of 183 nM HalofuginhellipKi

[2]

Bioactivity Halofuginone hydrobromide (RU-19110 hydrobromide) is aless-toxic form of Febrifugine which is isolated from theplant Halofuginone inhibits Dichroa febrifuga [1] prolyl-tRNA

in an ATP-dependent manner with a of 183hellipsynthetase Ki

Bioactivity Hydroxyurea is a cell apoptosis inducer that inhibit DNAsynthesis through inhibition of ribonucleotide reductase

Bioactivity L189 is a novel human DNA ligase inhibitor inhibitshLigIIIIIV with IC50 of 595 μM

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Folic acid (Vitamin B9 Vitamin M) Cat No HY-16637

GC7 Sulfate Cat No HY-108314A

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

GNE-371 Cat No HY-112803

Guanine Cat No HY-Y1055

Halofuginone (RU-19110) Cat No HY-N1584

Halofuginone hydrobromide (RU-19110 (hydrobromide)) Cat No HY-N1584A

Hydroxyurea (Hydroxycarbamide) Cat No HY-B0313

L189 Cat No HY-15588

wwwMedChemExpresscom 57

Purity 990Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9839Clinical Data No Development ReportedSize 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9977Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9988Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity L67 is a novel competitive human DNA ligase inhibitorinhibits DNA ligases I and III with IC50 of 10 μM and 10 μM

Bioactivity Madrasin is a potent and cell penetrant splicing inhibitorthat interferes with the early stages of spliceosome assemblyMadrasin is cytotoxic at higher concentrations although atlower concentrations it induces cell cycle arrest promotes aspecific reorganization of subnuclear protein localizationhellip

Bioactivity MB-7133 is a inhibitorDNA synthesis Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Bioactivity ML216(CID-49852229) is a potent inhibitor of the DNA unwindingactivity of BLM helicase showing similar IC50s of 30 and097 μM for full length BLM and BLM636ndash1298 respectively IC50value 30097 uM(Full length636ndash1298 BLM) Target BLMhelicase inhibitor ML216 shows cell-based activity and canhellip

Bioactivity Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNAdamage agent

Bioactivity NITD008 is a potent and selective inhibitor whichflavivirusecan inhibit with an ofDengue Virus Type 2 (DENV-2) EC50064 μM

Bioactivity Oxolinic acid is a potent inhibitor of DNA gyrase and DNAsynthesis lead to DNA cleavage when extracted chromosomes areincubated with sodium dodecyl sulfate

Bioactivity Phen-DC3 is a (G4) specific ligand which canG-quadruplexinhibit and helicases with s of 65plusmn6 and 50plusmn10FANCJ DinG IC50nM respectively

Bioactivity Plicamycin is a selective specificity protein 1 ( )Sp1inhibitor Plicamycin inhibits the growth of various cancersby decreasing Sp1 protein

L67 (DNA Ligase Inhibitor) Cat No HY-15586

Madrasin (DDD00107587) Cat No HY-100236

MB-7133 Cat No HY-16311

Mitomycin C (Ametycine) Cat No HY-13316

ML216 (CID-49852229) Cat No HY-12342

Nedaplatin (NSC 375101D) Cat No HY-13700

NITD008 (7-Deaza-2-C-acetylene-adenosine) Cat No HY-12957

Oxolinic acid Cat No HY-B1002

Phen-DC3 Cat No HY-15594

Plicamycin (Mithramycin A) Cat No HY-A0122

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9762Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9931Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Quarfloxin (CX 3543) a fluoroquinolone derivative withantineoplastic activity targets and inhibits RNA pol Iactivity with IC values in the nanomolar range in50neuroblastoma cells Quarfloxin disrupts the interactionbetween the nucleolin protein and a G-quadruplex DNA structurehellip

Bioactivity RG7800 a small molecule splicing modifier to enterSMN2human clinical trials to treat spinal muscular atrophy

Bioactivity RG7800 hydrochloride is an orally active splicingSMN2modulator with s of 23 nM and 87 nM for EC15x SMN2

splicing and RG7800 hydrochloride has theSMN proteinpotential to treat spinal muscular atrophy

Bioactivity Risdiplam (RG7916 RO7034067) is an orally administeredcentrally and peripherally distributed pre-mRNASMN2splicing modifier that increases survival motor neuron (SMN)protein levels

Bioactivity Saccharin 1-methylimidazole is an activator for DNARNASynthesis

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity SMN-C3 is an orally active splicing modulator and hasSMN2the potential to treat spinal muscular atrophy (SMA)

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 valueof 08 nM less potent for MTH2 NUDT5 NUDT12 NUDT14 andNUDT16

Bioactivity TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) withan IC50 value of 08 nM less potent for MTH2 NUDT5 NUDT12NUDT14 and NUDT16

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Quarfloxin (CX 3543) Cat No HY-14776

RG7800 (RO6885247) Cat No HY-101792

RG7800 hydrochloride (RO6885247 hydrochloride) Cat No HY-101792A

Risdiplam (RG7916 RO7034067) Cat No HY-109101

Saccharin 1-methylimidazole Cat No HY-112060

SCR7 Cat No HY-12742

SMN-C3 Cat No HY-112633

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

TH287 Cat No HY-16965

TH287 hydrochloride Cat No HY-16965A

wwwMedChemExpresscom 59

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9920Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 25 mg 50 mg 100 mg

Bioactivity TH588 is first-in-class nudix hydrolase family inhibitor thatpotently and selectively engage and inhibit the (MTH1

= 5 nM)IC50

Bioactivity TH588 hydrochloride is first-in-class nudix hydrolase familyinhibitor that potently and selectively engage and inhibit the

( = 5 nM)MTH1 IC50

Bioactivity Thiarabine (OSI-7836) shows potent anti-tumor activity andinhibition of synthesisDNA

Bioactivity Triapine is a novel inhibitor of the M2 subunit of ( ) and is a potentribonucleotide reductase RR

radiosensitizer

Bioactivity Triciribine is a inhibitor also inhibits DNA synthesis Aktand with of 130 nM and 002-046 μMHIV-12 IC50respectively

Bioactivity YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding tothe oncogenic transciption factor EWS-FLI1 YK-4-279 inhibitsEwings sarcoma family tumor (ESFT) cell growth YK-4-279induces apoptosis

Bioactivity Zoliflodacin (ETX0914AZD0914) is a novelspiropyrimidinetrione bacterial DNA gyrasetopoisomeraseinhibitor Zoliflodacin has potent antibacterialin vitroactivity against Gram-positive and Gram-negative organismsincluding with the of 025 μgmLS aureus MIC90

TH588 Cat No HY-12814

TH588 hydrochloride Cat No HY-12814A

Thiarabine (OSI-7836) Cat No HY-16496

Triapine (3-AP PAN-811 OCX191 NSC663249) Cat No HY-10082

Triciribine (API-2 NSC 154020 TCN) Cat No HY-15457

YK-4-279 Cat No HY-14507

Zoliflodacin (ETX0914 AZD0914) Cat No HY-17647

Eukaryotic Initiation Factor (eIF)

Eukaryotic initiation factors (eIFs) are proteins involved in theinitiation phase of eukaryotic translation These proteins help stabilizethe formation of the functional ribosome around the start codon andalso provide regulatory mechanisms in translation initiationEukaryotic initiation factor 2B (eIF2B) is a guaninenucleotide-exchange factor which mediates the exchange of GDP(bound to initiation factor eIF2) for GTP thus regenerating the active[eIF2GTP] complex that is required for peptide-chain initiation Theactivity of eIF2B is a key control point for eukaryotic protein synthesisand is altered in response to viral infection hormones nutrientsgrowth factors and certain stresses

Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis oncapped mRNAs in the cytoplasm Eukaryotic initiation factor (elF) 4A functions as a subunit of the initiation factorcomplex elF4F which mediates the binding of mRNA to the ribosome

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Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 2 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Eukaryotic Initiation Factor (eIF) Inhibitors amp Modulators

Bioactivity 4E1RCat is an inhibitor of cap-dependent translation andinhibits interaction with an an of 4 μMeIF4EeIF4GI IC50

Bioactivity 4E2RCat is an inhibitor of interaction with an eIF4E-eIF4G IC50of 135 μM

Bioactivity 4EGI-1 is an inhibitor of interaction with a eIF4EeIF4G Kdof 25 μM against eIF4E binding

Bioactivity Briciclib is a water soluble derivative of ON 013100 and hasthe potential in targeting for solid cancerseIF4E

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic inhibitor with an of 110initiation factor 4A-3 (eIF4A3) IC50

nM

Bioactivity Episilvestrol is a derivative of silvestrol isolated from thefruits and twigs of and is a specificAglaia silvestris

-targeting translation inhibitor with antitumor activityeIF4A

Bioactivity GCN2iB is an ATP-competitive inhibitor of aserinethreonine-protein kinase general control

with an of 24 nMnonderepressible 2 (GCN2) IC50

Bioactivity SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1and disrupts the eIF4F complex

Bioactivity Silvestrol is a eukaryotic translation initiation factor 4A () inhibitor isolated from the fruits and twigs of eIF4A Aglaia

foveolata

4E1RCat Cat No HY-14427

4E2RCat Cat No HY-100733

4EGI-1 Cat No HY-19831

Briciclib (ON 014185) Cat No HY-16366

CCT020312 Cat No HY-119240

eIF4A3-IN-2 Cat No HY-101785

Episilvestrol Cat No HY-15359

GCN2iB Cat No HY-112654

SBI-0640756 (SBI-756) Cat No HY-19560

Silvestrol ((-)-Silvestrol) Cat No HY-13251

G-quadruplex

G-quadruplexes (G-tetrads or G4-DNA) are nucleic acid sequencesthat are rich in guanine and are capable of forming a four-strandedstructure Four guanine bases can associate through Hoogsteenhydrogen bonding to form a square planar structure called a guaninetetrad and two or more guanine tetrads can stack on top of eachother to form a G-quadruplex The quadruplex structure is furtherstabilized by the presence of a cation especially potassium which sitsin a central channel between each pair of tetradsThey can be formedof DNA RNA LNA and PNA and may be intramolecular bimolecularor tetramolecular Depending on the direction of the strands or partsof a strand that form the tetrads structures may be described as

parallel or antiparallel

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Purity 980Clinical Data No Development ReportedSize 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity 9680Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

G-quadruplex Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity APTO-253 is an inducer of andKruppel-like factor 4 (KLF4)also stabilizes with anti-proliferative activityGquadruplex

Bioactivity Phen-DC3 Trifluoromethanesulfonate is a (G4)G-quadruplexspecific ligand which can inhibit and helicasesFANCJ DinGwith s of 65plusmn6 and 50plusmn10 nM respectivelyIC50

Bioactivity Pyridostatin is a stabilizer with a of 490G-quadruplexe KdnM

Bioactivity Pyridostatin hydrochloride is a stabilizer withG-quadruplexea of 490 nMKd

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

APTO-253 (LOR-253 LT-253) Cat No HY-16291

Phen-DC3 Trifluoromethanesulfonate (Phen-DC3 Triflate) Cat No HY-15594A

Pyridostatin (RR82) Cat No HY-15176

Pyridostatin hydrochloride (RR-82 hydrochloride) Cat No HY-15176A

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

Haspin Kinase

Haspin is a protein kinase that regulates chromosome and spindlefunction during mitosis and meiosis Haspin expression is detected infetal liver skin kidney small intestine and in all proliferating cellsHaspin phosphorylates H3 thr3 (H3T3ph) in human cell lines anddepletion of Haspin by RNA interference reveals that Haspin isrequired for H3 thr3 phosphorylation in mitotic cells Phosphorylationof H3T3ph by Haspin is necessary for chromosomal passengercomplex (CPC) accumulation at centromeres H3T3ph then positionsthe CPC at centromeres to regulate selected targets of Aurora Bduring mitosis

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Purity 9956Clinical Data No Development ReportedSize 5 mg

Purity 9812Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Haspin Kinase Inhibitors amp Modulators

Bioactivity CHR-6494 is a potent inhibitor of inhibiting histonehaspinH3T3 phosphorylation with an of 2 nMIC50

Bioactivity LDN-192960 is a potent ( Haspin Haploid Germ Cell-Specific) inhibitor with an of 0010 microMNuclear Protein Kinase IC50

CHR-6494 Cat No HY-15217

LDN-192960 Cat No HY-13455

HDACHistone deacetylases

HDAC (Histone deacetylases) are a class of enzymes that removeacetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid onahistone allowing the histones to wrap the DNA more tightly This isimportant because DNA is wrapped around histones and DNAexpression is regulated by acetylation and de-acetylation Its action isopposite to that of histone acetyltransferase HDAC proteins are nowalso called lysine deacetylases (KDAC) to describe their functionrather than their target which also includes non-histone proteinsTogether with the acetylpolyamine amidohydrolases and the acetoinutilization proteins the histone deacetylases form an ancient proteinsuperfamily known as the histone deacetylase superfamily

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Purity 9600Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9971 Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9896Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

HDAC Inhibitors amp Modulators

Bioactivity Abexinostat (CRA 024781) is a novel pan- inhibitorHDACmostly targeting HDAC1 with of 7 nMKi

Bioactivity ACY-1083 is a selective and brain-penetrating inhibitorHDAC6with an of 3 nM and is 260-fold more selective for HDAC6IC50than all other classes of HDAC isoforms ACY-1083 effectivelyreverses chemotherapy-induced peripheral neuropathy [1]

Bioactivity ACY-738 is a potent selective and orally-bioavailable HDAC6inhibitor with an of 17 nM ACY-738 also inhibitsIC50HDAC1 HDAC2 and HDAC3 with s of 94 128 and 218 nMIC50

Bioactivity ACY-775 is a potent and selective inhibitor of the of histonedeacetylase 6 ( ) with an of 75nMHDAC6 IC50

Bioactivity ACY-957 is a selective inhibitor of and withHDAC1 HDAC2s of 7 nM 18 nM and 1300 nM against HDAC123IC50

respectively and shows no inhibition on HDAC456789

Bioactivity AES-135 is a potent inhibitor inhibits HDAC HDAC3 HDAC6 with s of 654 190 and 636 nM respectivelyHDAC11 IC50

Anti-tumor activity [1]

Bioactivity Belinostat is a potent inhibitor with an of 27 nMHDAC IC50in HeLa cell extracts

Bioactivity Benzenebutyric acid is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity BG45 is an HDAC class I inhibitor with selectivity for HDAC3(IC50 = 289 nM) It inhibits HDAC1 HDAC2 and HDAC6 withgreatly reduced potency (IC50s = 2 22 and gt20 μMrespectively) IC50 value 289 nM (HDAC3) 2 μM (HDAC1) 22μM (HDAC2) gt20 μM (HDAC6) Target HDAC At concentrationshellip

Bioactivity BML-210 is a novel HDAC inhibitor and its mechanism of actionhas not been characterized IC50 value 5 μM[1] Target HDAC4In vitro Cell cycle analysis indicated that HeLa celltreatment with 20 and 30 μM concentration of BML-210 increasedthe proportion of cells in G0G1 phase and causedhellip

Abexinostat (CRA 024781 PCI-24781) Cat No HY-10990

ACY-1083 Cat No HY-111791

ACY-738 Cat No HY-19327

ACY-775 Cat No HY-19328

ACY-957 Cat No HY-104008

AES-135 Cat No HY-114483

Belinostat (PXD101 PX105684) Cat No HY-10225

Benzenebutyric acid (4-Phenylbutyric acid) Cat No HY-A0281

BG45 Cat No HY-18712

BML-210 Cat No HY-19350

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9875Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9906Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BRD 4354 is a moderately potent inhibitor of andHDAC5 with of 085 and 188 μM respectivelyHDAC9 IC s50

Bioactivity BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitorof and with of 085 and 188 μMHDAC5 HDAC9 IC s50

respectively [1]

Bioactivity BRD73954 ia a potent and selective HDAC inhibitor with IC50 of36 nM and 120 nM for HDAC6 and HDAC8 respectively

Bioactivity Bufexamac is a class IIB histone deacetylases (HDAC6 andHDAC10) inhibitor used as an anti-inflammatory agent

Bioactivity CAY10603 (BML-281) is a potent and selective inhibitorHDAC6with an of 2 pM CAY10603 (BML-281) also inhibits HDAC1IC50HDAC2 HDAC3 HDAC8 HDAC10 with s of 271 252 042IC506851 907 nM

Bioactivity CHDI-390576 a potent cell permeable and CNS penetrant class inhibitor with s of 54 nMIIa histonedeacetylase (HDAC) IC50

60 nM 31 nM 50 nM for class IIa HDAC4 HDAC5 HDAC7 HDAC9respectively shows gt500-fold selectivity over class IHDACs (1 2 3) and ~150-fold selectivity over HDAC8 and thehellip

Bioactivity Citarinostat is a HDAC6 specific inhibitor with IC50 of 4 nMand 76 nM for HDAC6 and HDAC3 respectively IC50 value 4 nM(HDAC6) 76 nM (HDAC3) Target HDAC The detailed informationplease refer to WO2015061684A1 and 2015054197A1

Bioactivity CM-675 is a dual and phosphodiesterase 5 (PDE5) class I histone-selective inhibitor with values of 114 nMdeacetylases IC50

and 673 nM for PDE5 and HDAC1 respectively CM-675 haspotential to treat Alzheimerrsquos disease [1]

Bioactivity Corin is a dual inhibitor of histone lysine specificdemethylase and histone deacetylase with a(LSD1) (HDAC)

of 110 nM for LSD1 and an IC of 147 nM forK (inact)i 50HDAC1

Bioactivity CRA-026440 is a potent broad-spectrum inhibitor The HDAC Kivalues against recombinant HDAC isoenzymes HDAC1 HDAC2

and are 4 14 11 15 7 andHDAC3 HDAC6 HDAC8 HDAC1020 nM respectively

68 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

BRD 4354 Cat No HY-112719

BRD 4354 ditrifluoroacetate Cat No HY-112719B

BRD73954 Cat No HY-18700

Bufexamac (Bufexamic acid) Cat No HY-B0494

CAY10603 (BML-281) Cat No HY-18613

CHDI-390576 Cat No HY-119939

Citarinostat (ACY241) Cat No HY-15994

CM-675 Cat No HY-114303

Corin Cat No HY-111048

CRA-026440 Cat No HY-19754

wwwMedChemExpresscom 69

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in Ethanol

2 mg 5 mg 10 mg 50 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9809Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9959Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity CUDC-101 is a potent inhibitor of and withHDAC EGFR HER2s of 44 24 and 157 nM respectivelyIC50

Bioactivity Dacinostat is a potent inhibitor with an of 32 nMHDAC IC50Dacinostat also inhibits with an of 9 nM and usedHDAC1 IC50in cancer research

Bioactivity Domatinostat (4SC-202 free base) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Domatinostat tosylate (4SC-202) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Droxinostat(NS41080) is a selective inhibitor of HDAC3 HDAC6and HDAC8 with IC50 of 169 247 and 146 μM respectivelygt 8-fold selective against HDAC3 and no inhibition toHDAC1 2 4 5 7 9 and 10 IC50 Value 169 μM(HDAC3) 247μM(HDAC6) 146 μM(HDAC8) Target HDAC368 in vitrohellip

Bioactivity EDO-S101 is a pan inhibitor inhibits HDAC1 HDAC2 andHDACHDAC3 with values of 9 9 and 25 nM respectivelyIC50

Bioactivity Entinostat is an oral and selective class I inhibitorHDACwith s of 243 nM 453 nM and 248 nM for IC50 HDAC1 HDAC2

and respectivelyHDAC3

Bioactivity Fimepinostat (CUDC-907) potently inhibits class I s as wellPI3Kas classes I and II enzymes with an of 195439 nMHDAC IC50and 17501828 nM for PI3KαPI3KβPI3Kδ andHDAC1HDAC2HDAC3HDAC10 respectively

Bioactivity FT895 is a potent and selective inhibitor with an HDAC11 IC50

of 3 nM [1]

Bioactivity Givinostat (ITF-2357) is a inhibitor with an of 198HDAC IC50and 157 nM for and respectivelyHDAC1 HDAC3

CUDC-101 Cat No HY-10223

Dacinostat (NVP-LAQ824 LAQ824) Cat No HY-13606

Domatinostat (4SC-202 (free base)) Cat No HY-16012A

Domatinostat tosylate (4SC-202) Cat No HY-16012

Droxinostat (NS 41080) Cat No HY-13267

EDO-S101 (Tinostamustine) Cat No HY-101780

Entinostat (MS-275 SNDX-275) Cat No HY-12163

Fimepinostat (CUDC-907) Cat No HY-13522

FT895 Cat No HY-112285

Givinostat (ITF-2357) Cat No HY-14842

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9849Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9609Clinical Data LaunchedSize 2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Bioactivity Givinostat hydrochloride (ITF-2357 hydrochloride) is a HDACinhibitor with an of 198 and 157 nM for andIC50 HDAC1

respectivelyHDAC3

Bioactivity Givinostat hydrochloride monohydrate (ITF-2357 hydrochloridemonohydrate) is a inhibitor with an of 198 and 157HDAC IC50nM for and respectivelyHDAC1 HDAC3

Bioactivity HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2008040934 A1

Bioactivity HDAC-IN-4 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2007045844 A1 20070426

Bioactivity HDAC-IN-5 is a histone deacetylase inhibitor(HDAC) Bioactivity HDAC-IN-7 (Chidamide impurity) is an impurity of ChidamideChidamide is a potent and orally bioavailable HDAC enzymesclass I (HDAC123) and class IIb (HDAC10) inhibitor

Bioactivity HDAC6-IN-1 is a potent and selective inhibitor for withHDAC6an of 17 nM and shows 25-fold and 200-fold selectivityIC50relative to ( =422 nM) and ( =3398 nM)HDAC1 IC50 HDAC8 IC50respectively

Bioactivity HDAC8-IN-1 is a inhibitor with an of 272 nMHDAC8 IC50

Bioactivity HDACsmTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs)and targetmammalian target of Rapamycin (mTOR)inhibitor for treating hematologic malignancies with ofIC s50019 nM 18 nM 12 nM and gt500 nM for HDAC1 HDAC6 mTORand PI3Kα respectively HDACsmTOR Inhibitor 1 stimulateshellip

Bioactivity HPOB is a highly potent and selective inhibitor of histonedeacetylase 6 (HDAC6) with IC50 of 56 nM gt30 fold lesspotent against other HDACs target HDAC6 [1] IC 50 56nM [1]In vitro HPOB causes growth inhibition of normal andtransformed cells but does not induce cell death HPOBhellip

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Givinostat hydrochloride (ITF-2357 hydrochloride) Cat No HY-14842A

Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) Cat No HY-14842B

HDAC-IN-3 Cat No HY-19772

HDAC-IN-4 (CXD101) Cat No HY-100748

HDAC-IN-5 Cat No HY-18362

HDAC-IN-7 (Chidamide impurity) Cat No HY-13592

HDAC6-IN-1 Cat No HY-18947

HDAC8-IN-1 Cat No HY-111342

HDACsmTOR Inhibitor 1 Cat No HY-114414

HPOB Cat No HY-19747

wwwMedChemExpresscom 71

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg 100 mg

Bioactivity IDO1 and HDAC1 Inhibitor (Compound 10) is a dual andIDO1 inhibitor with s of 690 nM and 665 nMHDAC1 IC50

respectively [1]

Bioactivity ITSA-1 is membrane permeable and specifically suppresses TSAinhibition of HDAC (histone deacetylase) but not other HDACinhibitors

Bioactivity J22352 is a PROTAC (proteolysis-targeting chimeras)-like andhighly selective inhibitor with an value of 47HDAC6 IC50nM J22352 promotes HDAC6 degradation and induces anticancereffects by inhibiting autophagy and eliciting the antitumorimmune response in glioblastoma cancers and leading to thehellip

Bioactivity JAKHDAC-IN-1 is a potent dual inhibitor exhibitsJAK2HDACantiproliferative and proapoptotic activities in severalhematological cell lines JAKHDAC-IN-1 shows s of 4 and 2IC50

nM for JAK2 and HDAC respectively [1]

Bioactivity LMK-235 is a potent and selective inhibitor inhibitsHDAC45HDAC5 HDAC4 HDAC6 HDAC1 HDAC2 HDAC11 and HDAC8 with

s of 422 nM 119 nM 557 nM 320 nM 881 nM 852 nM andIC501278 nM respectively and is used in cancer research

Bioactivity M344 (D 237) is an inhibitor of ( =100histone deacetylase IC50nM) and an inducer of terminal cell fifferentiation

Bioactivity MC1568 is a selective class II (IIa) histone deacetylas () inhibitor used for cancer researchHDAC II

Bioactivity Mocetinostat (MGCD0103) is a potent orally active andisotype-selective inhibitor with s ofHDAC (Class IIV) IC50015 029 166 and 059 μM for andHDAC1 HDAC2 HDAC3

respectively Mocetinostat shows no inhibition onHDAC11HDAC4 HDAC5 HDAC6 HDAC7 or HDAC8

Bioactivity Nanatinostat (CHR-3996) is a potent class I selective andorally active inhibitor with anhistone deacetylase (HDAC)

of 8 nM IC50[1]

Bioactivity Nexturastat A is a potent and selective HDAC6 inhibitor withIC50 of 5 nM no inhibition on other HDAC forms

IDO1 and HDAC1 Inhibitor Cat No HY-112147

ITSA-1 Cat No HY-100508

J22352 Cat No HY-126147

JAKHDAC-IN-1 Cat No HY-126141

LMK-235 Cat No HY-18998

M344 (D 237 MS 344) Cat No HY-13506

MC1568 Cat No HY-16914

Mocetinostat (MGCD0103) Cat No HY-12164

Nanatinostat (CHR-3996) Cat No HY-13432

Nexturastat A Cat No HY-16699

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9907Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9867Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9797Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NKL 22 is a HDAC inhibitor The value of IC 50 is 78 uM NKL 22increase frataxin protein concentrations NKL 22 inhibitorsincrease FXN mRNA in FRDA lymphocytes HDAC inhibitors actdirectly on FXN [1]

Bioactivity Oxamflatin (Metacept-3) is a potent inhibitor with anHDAC of 157 nMIC50

Bioactivity Panobinostat is a non-selective histone deacetylase ( )HDACinhibitor

Bioactivity PCI-34051 is a potent and selective inhibitor with HDAC8 IC50of 10 nM with gt200-fold selectivity over the other HDACisoforms

Bioactivity PI3KHDAC-IN-1 is a potent dual inhibitor of PI3KHDACpotently inhibits PI3Kδ and HDAC1 with s of 81 nM and 14IC50

nM respectively [1]

Bioactivity Pimelic diphenylamide 106 is a slow tight-binding inhibitorof class I HDAC (HDAC 1 2 and 3 with IC50 values of 150 nM 760nM and 370 nM respectively) demonstrating no activityagainst class II HDACs

Bioactivity Pracinostat is a potent inhibitorhistone deacetylase (HDAC)with s of 40-140 nM used for cancer researchIC50

Bioactivity PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDACPTACH exerts potent growth inhibition against various humancancer cells with EC50 values ranging from 1 to 10 μM

Bioactivity Quisinostat (JNJ-26481585) is an orally available potent inhibitor with an of 011 nM for HDAC1HDAC IC50

Bioactivity Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of which is under developmenthistone deacetylase enzymes (HDAC)

for the treatment of cutaneous T-cell lymphoma [1]

72 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NKL 22 Cat No HY-100384

Oxamflatin (Metacept-3) Cat No HY-102033

Panobinostat (LBH589 NVP-LBH589) Cat No HY-10224

PCI-34051 Cat No HY-15224

PI3KHDAC-IN-1 Cat No HY-128582

Pimelic Diphenylamide 106 (RGFA-8 TC-H 106 Histone Deacetylase Inhibitor VII) Cat No HY-19348

Pracinostat (SB939) Cat No HY-13322

PTACH (NCH-51) Cat No HY-12954

Quisinostat (JNJ-26481585) Cat No HY-15433

Remetinostat (SHP-141) Cat No HY-100365

wwwMedChemExpresscom 73

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9970Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Bioactivity Resminostat is a potent inhibitor of andHDAC1 HDAC3 with mean values of 425 501 718 nMHDAC6 IC50

respectively and shows less potent activities against HDAC8with an of 877 nMIC50

Bioactivity Resminostat hydrochloride is a potent inhibitor of HDAC1 and with mean values of 425 501 718HDAC3 HDAC6 IC50

nM respectively and shows less potent activities againstHDAC8 with an of 877 nMIC50

Bioactivity RG2833 is a brain-penetrant inhibitor with of 60 nMHDAC IC50and 50 nM for HDAC1 and HDAC3 respectively

Bioactivity RGFP966 is a highly selective inhibitor with an ofHDAC3 IC5080 nM and shows no inhibition to other HDACs at concentrationsup to 15 μM

Bioactivity Ricolinostat (ACY-1215) is a potent and selective HDAC6inhibitor with an of 5 nM ACY-1215 also inhibitsIC50

and with s of 58 48 and 51 nMHDAC1 HDAC2 HDAC3 IC50respectively

Bioactivity Romidepsin is a potent and inhibitor with sHDAC1 HDAC2 IC50of 36 and 47 nM respectively

Bioactivity RTS-V5 is a dual inhibitor with s ofHDACproteasome IC5069 18 15 027 053 μM for HDAC1 HDAC2 HDAC3 HDAC6HDAC8 respectively

Bioactivity Santacruzamate A (CAY-10683) is a potent and selective HDAC2inhibitor with an of 119 pM IC50

[1]

Bioactivity Scriptaid is a potent inhibitorhistone deacetylase (HDAC)used in cancer research

Bioactivity Sinapinic acid (Sinapic acid) is a phenolic compound isolatedfrom Jack Rhizome acts as anHydnophytum formicaruminhibitor of with an of 227 mM and alsoHDAC IC50

[1]

inhibits activity Sinapinic acid posssess pothellipACE-I [2]

Resminostat (RAS2410 4SC-201) Cat No HY-14718

Resminostat hydrochloride (RAS2410 hydrochloride 4SC-201 hydrochloride) Cat No HY-14718A

RG2833 (RGFP109) Cat No HY-16425

RGFP966 Cat No HY-13909

Ricolinostat (ACY-1215 Rocilinostat) Cat No HY-16026

Romidepsin (FK 228 FR 901228 NSC 630176) Cat No HY-15149

RTS-V5 Cat No HY-112908

Santacruzamate A (CAY-10683) Cat No HY-N0931

Scriptaid (Scriptide GCK1026) Cat No HY-15489

Sinapinic acid (Sinapic acid) Cat No HY-W009732

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg

Purity 9800Clinical Data Phase 3Size 10mM x 1mL in Water

1 g 5 g 500 g

Bioactivity Butyric acid is a inhibitor withhistone deacetylase (HDAC)anti-tumor effects in several cancers

Bioactivity Sodium phenylbutyrate is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity SR-4370 is an inhibitor of with s of 013 μM 058HDAC IC50μM 0006 μM 23 μM and 34 μM for HDAC1 HDAC2 HDAC3HDAC8 and HDAC6 respectively

Bioactivity ST8154AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity ST8155AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity Sulforaphane is an isothiocyanate present naturally in widelyconsumed vegetables has shown anticancer and cardioprotectiveactivities

Bioactivity SW-100 a selective inhibitorhistone deacetylase 6 (HDAC6)with an of 23 nM shows at least 1000-fold selectivityIC50for HDAC6 relative to all other HDAC isozymes SW-100 displaysa significantly improved ability to cross hellip

Bioactivity Tacedinaline (N-acetyldinaline) is an inhibitor of the histonedeacetylase ( ) with s of 09 09 12 μM forHDAC IC50recombinant HDAC 1 2 and 3 respectively

Bioactivity Tasquinimod is an oral antiangiogenic agent in clinical trialsfor the treatment of castration-resistant prostate cancerTasquinimod binds to the regulatory Zn binding domain of2+

with of 10-30 nMHDAC4 Kd

Bioactivity TH34 an inhibitor with s of 46 μM 19HDAC6 8 10 IC50μM and 77 μM respectively shows high selectivity overHDAC123 [1]

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Sodium Butyrate (Butanoic acid sodium salt) Cat No HY-B0350A

Sodium phenylbutyrate (Sodium 4-phenylbutyrate TriButyrate) Cat No HY-15654

SR-4370 Cat No HY-111400

ST8154AA1 Cat No HY-112805

ST8155AA1 Cat No HY-112806

Sulforaphane Cat No HY-13755

SW-100 Cat No HY-115475

Tacedinaline (N-acetyldinaline CI-994 Goe-5549) Cat No HY-50934

Tasquinimod (ABR-215050) Cat No HY-10528

TH34 Cat No HY-111818

wwwMedChemExpresscom 75

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g 25 g

Purity 9867Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g 25 g

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9887Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TMP195 is a selective class IIa histone deacetylase ( )HDACinhibitor with s of 59 60 26 15 nM for HDAC4 HDAC5KiHDAC7 and HDAC9 respectively

Bioactivity TMP269 is a novel and selective class IIa histone deacetylase inhibitor with s of 157 nM 97 nM 43 nM and 23 nM(HDAC) IC50

for HDAC4 HDAC5 HDAC7 and HDAC9 respectively

Bioactivity Trichostatin A is a potent and specific inhibitor of HDAC with an value of 18 nM for HDACclass III IC50

Bioactivity Tubacin is a potent and selective inhibitor of with anHDAC6 value of 4 nM and approximately 350-fold selectivity overIC50

HDAC1

Bioactivity Tubastatin A (Hydrochloride) is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tubastatin-A is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tucidinostat is a potent and orally bioavailable enzymesHDACclass I ( ) and class IIb ( ) inhibitor withHDAC123 HDAC10

s of 95 160 67 and 78 nM less active on HDAC8 andIC50HDAC11 ( s 733 nM 432 nM respectively) and showshellipIC50

Bioactivity UF010 is a potent and selective HDAC inhibitor with IC50 ~006μM 01 μM 05 μM and 15 μM for HDACs 3 2 1 and 8respectively It has gt 6-fold selectivity over other HDACsIC50 value 006 μM (HDAC3) 01 μM (HDAC2) 05 μM (HDAC1)15 μM(HDAC 8) Target HDAC in vitro UF010 is a competitivehellip

Bioactivity Valproic acid is an inhibitor with in the range ofHDAC IC5005 and 2 mM also inhibits ( 400 μM) andHDAC1 IC50induces proteasomal degradation of Valproic acidHDAC2sodium salt is used in the treatment of epilepsy bipohellip

Bioactivity Valproic acid sodium salt is an anticonvulsants used to treatepilepsy bipolar disorder and migraines Valproic acidinhibits with an of 04 mMhistone deacetylase 1 (HDAC1) IC50

TMP195 Cat No HY-18361

TMP269 Cat No HY-18360

Trichostatin A (TSA) Cat No HY-15144

Tubacin Cat No HY-13428

Tubastatin A Hydrochloride (Tubastatin A HCl TSA HCl) Cat No HY-13271

Tubastatin-A Cat No HY-13271A

Tucidinostat (Chidamide HBI-8000 CS 055) Cat No HY-109015

UF010 Cat No HY-18976

Valproic acid (VPA 2-Propylpentanoic Acid) Cat No HY-10585

Valproic acid sodium salt (Sodium Valproate) Cat No HY-10585A

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

250 mg 500 mg 1 g 5 g

Bioactivity Vorinostat is a potent and orally available inhibitor of and andHDAC1 HDAC2 HDAC3 (Class I) HDAC7 (Class II)

with values of 10 nM and 20 nM forHDAC11 (Class IV ) ID50HDAC1 and HDAC3 respectively

Bioactivity WT-161 is a potent and selective inhibitor with an HDAC6 IC50of 040 nM

76 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Vorinostat (SAHA) Cat No HY-10221

WT-161 Cat No HY-100871

wwwMedChemExpresscom 77

HSPHeat shock proteins

HSP (Heat shock proteins) are a group of proteins induced by heatshock the most prominent members of this group are a class offunctionally related proteins involved in the folding and unfolding ofother proteins HSP expression is increased when cells are exposed toelevated temperatures or other stress This increase in expression istranscriptionally regulated The dramatic upregulation of the heatshock proteins is a key part of the heat shock response and is inducedprimarily by heat shock factor (HSF) HSPs are found in virtually allliving organisms from bacteria to humans Heat shock proteinsappear to serve a significant cardiovascular role Hsp90 Hsp84Hsp70 Hsp27 Hsp20 and alpha B crystallin all have been reported as

having roles in the cardiovasculature

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 g

Purity 9997Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9932Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 1 mg

HSP Inhibitors amp Modulators

Bioactivity Alvespimycin is a potent inhibitor of binding to Hsp90Hsp90with an of 62 plusmn 29 nMEC50

Bioactivity Alvespimycin hydrochloride is a potent inhibitor of Hsp90binding to Hsp90 with of 62plusmn29 nMEC50

Bioactivity Apoptozole is an inhibitor of the ATPase domain of andHsc70 with s of 021 and 014 μM respectively and canHsp70 Kd

induce apoptosis

Bioactivity Arimoclomol maleate (BRX-220) is a co-inducer of heat shockproteins ( )HSP

Bioactivity BIIB021 is an orally available fully synthetic inhibitor of with and of 17 nM and 38 nM respectivelyHSP90 Ki EC50

Bioactivity Bimoclomol is a coinducer used forheat shock protein (HSP)treatment of cardiovascular diseases

Bioactivity CCT251236 is an orally available pirin ligand from a heatshock transcription factor 1 (hsf1) phenotypic screen with an

of 19 nM for inhibition of HSF1-mediated IC50 HSP72

induction

Bioactivity Col003 is a potent inhibitor of competitively binds toHsp47the collagen binding site on Hsp47 ( 18 μM) andIC50inhibits collagen secretion by destabilizing the collagentriple helix [1]

Bioactivity Debio 0932 is an orally active inhibitor with s ofHSP90 IC50100 and 103 nM for HSP90α and HSP90β respectively

Bioactivity Ethoxyquin is an antioxidant which has been used in animalfeed for many years and also an inhibitor of heat shock

( )protein 90 Hsp90

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Alvespimycin (17-DMAG NSC 707545) Cat No HY-10389

Alvespimycin hydrochloride (17-DMAG hydrochloride KOS-1022 BMS 826476) Cat No HY-12024

Apoptozole (Apoptosis Activator VII) Cat No HY-15098

Arimoclomol maleate (BRX-220) Cat No HY-106443A

BIIB021 (CNF2024) Cat No HY-10212

Bimoclomol Cat No HY-U00398

CCT251236 Cat No HY-101026

Col003 Cat No HY-124817

Debio 0932 (CUDC-305) Cat No HY-13469

Ethoxyquin Cat No HY-B1425

wwwMedChemExpresscom 79

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9994Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Bioactivity Feretoside a phenolic compound extracted from the barks of E is a which act as cytoprotectiveulmoides HSP inducer

agent

Bioactivity Ganetespib is a heat shock protein 90 ( ) inhibitorHSP90which exhibits potent cytotoxicity in a wide variety ofhematological and solid tumor cell lines

Bioactivity Geldanamycin is a inhibitor with antimicrobial activityHsp90against many Gram-positive and some Gram-negative bacteria

Bioactivity Grp94 Inhibitor-1 is a potent selective inhibitor withGrp94an value of 2 nM and over 1000-fold selectivity to Grp94IC50

against Hsp90α [1]

Bioactivity HA15 a molecule that targets specifically BiP GRP78 HSPA5inhibits the ATPase activity of BiP HA15 strongly increasesBiP protein expression in A375 melanoma cells [1]

Bioactivity HSF1A is a cell-permeable activator of heat shocktranscription factor 1 ( )HSF1

Bioactivity HSP70-IN-1 is a heat shock protein ( ) inhibitor inhibitsHSPthe growth of Kasumi-1 cells with an of 23 μMIC50

Bioactivity JG-98 is an allosteric heat shock protein 70 (Hsp70)inhibitor with anti-cancer activities which disrupts Hsp70

and affects signalinginteraction with a co-chaperone Bag3pathways important for cancer development [1] [2] [3]

Bioactivity KNK437 is a inhibitor and inhibits the induction ofHSPHSP105 HSP70 and HSP40

Bioactivity KRIBB11 is an inhibitor of withHeat shock factor 1 (HSF1) of 12 μMIC50

Feretoside Cat No HY-N6249

Ganetespib (STA-9090) Cat No HY-15205

Geldanamycin Cat No HY-15230

Grp94 Inhibitor-1 Cat No HY-112910

HA15 Cat No HY-100437

HSF1A Cat No HY-103000

HSP70-IN-1 Cat No HY-12622

JG-98 Cat No HY-117282

KNK437 (Heat Shock Protein Inhibitor I) Cat No HY-100110

KRIBB11 Cat No HY-100872

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 100 mg

Purity 9569Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9914Clinical Data Phase 2Size 5 mg 10 mg 25 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity KU-32 is a novel novobiocin-based inhibitor that canHsp90protect against neuronal cell death

Bioactivity KW-2478 is an inhibitor of with an of 38 nMHsp90α IC50and has antitumor activity against various human hematologicaltumor cells

Bioactivity Luminespib (NVP-AUY922) is a potent inhibitor withHSP90s of 78 and 21 nM for HSP90α and HSP90β respectivelyIC50

Bioactivity MKT-077 is a rhodacyanine dye and also a heat shock protein 70( ) inhibitor which exhibits significant antitumorHsp70activity

Bioactivity NVP-HSP990 is a potent and selective inhibitor withHsp90 values of 06 08 and 85 nM for Hsp90α Hsp90β andIC50

Grp94 respectively

Bioactivity Onalespib (AT13387) is a potent inhibitor of with aHsp90 of 071 nMKd

Bioactivity p5 Ligand for Dnak and DnaJ is a nonapeptide whichcorresponds to the main binding site for the 23-residue partof the presequence of mitochondrial aspartateaminotransferase p5 Ligand for Dnak and DnaJ is ahigh-affinity ligand for DnaK and DnaJ [1]

Bioactivity Pifithrin-μ is an inhibitor of and with antitumorp53 HSP70and neuroprotective activity

Bioactivity PU-WS13 is a selective inhibitor with an ofGrp94 EC50022 μM

Bioactivity Retaspimycin is a potent and water-soluble inhibitor of with s of 119 nM for both Hsp90 and Grp9Hsp90 EC50

80 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

KU-32 Cat No HY-108248

KW-2478 Cat No HY-13468

Luminespib (NVP-AUY922 AUY922 VER-52296) Cat No HY-10215

MKT-077 (FJ-776) Cat No HY-15096

NVP-HSP990 (HSP-990) Cat No HY-15190

Onalespib (AT13387) Cat No HY-14463

p5 Ligand for Dnak and DnaJ Cat No HY-P1887

Pifithrin-μ (PFTμ 2-Phenylethynesulfonamide) Cat No HY-10940

PU-WS13 Cat No HY-18680

Retaspimycin Cat No HY-15263

wwwMedChemExpresscom 81

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9740Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9982Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9903Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Retaspimycin Hydrochloride is a potent and water-solubleinhibitor of with s of 119 nM for both Hsp90 andHsp90 EC50Grp9

Bioactivity Shepherdin (79-87) is amino acids 79 to 87 fragment ofShepherdin Shepherdin is a peptidomimetic antagonist of thecomplex between Hsp90 and Survivin Anticancer activity [1]

Bioactivity SNX-5422 Mesylate (PF-04929113 Mesylate) a prodrug ofSNX-2112 is an orally active inhibitor with a ofHsp90 Kd41 nM and also induces Her-2 degradation with an ofIC5037nM

Bioactivity Tanespimycin (17-AAG) is a potent inhibitor with anHSP90 of 5 nM having a 100-fold higher binding affinity forIC50

tumour cell derived HSP90 than normal cell derived HSP90

Bioactivity TAS-116 is an oral bioavailable ATP-competitive highlyspecific inhibitor ( s of 347 nM and 213HSP90αHSP90β KinM respectively) without inhibiting other HSP90 familyproteins such as GRP94 TAS-116 demonstrates less ocuhellip[1]

Bioactivity Teprenone is a anti-ulcer drug and works as an inducer ofheat shock proteins ( )HSPs

Bioactivity TRC051384 is a heat shock protein 70 ( ) inducerHSP70 Bioactivity VER-155008 is an inhibitor of with s of 05 μMHsp70 IC5026 μM and 26 μM for Hsc70 and Grp7 respectivelyHsp70and with a of 03 μM for Kd Hsp70

Bioactivity VER-49009 is a inhibitor with an of 25 nM and aHsp90 IC50 of 78 nMKd

Bioactivity VER-50589 is a inhibitor with an of 21 nM and aHsp90 IC50 of 45 nMKd

Retaspimycin Hydrochloride (IPI-504) Cat No HY-10210

Shepherdin 79-87 Cat No HY-P1750

SNX-5422 Mesylate (PF-04929113 (Mesylate)) Cat No HY-10213A

Tanespimycin (17-AAG NSC 330507 CP 127374) Cat No HY-10211

TAS-116 Cat No HY-15785

Teprenone (Geranylgeranylacetone) Cat No HY-B0779

TRC051384 Cat No HY-101712

VER-155008 Cat No HY-10941

VER-49009 (CCT 129397) Cat No HY-15986

VER-50589 Cat No HY-15984

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9924Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity VER-82576 (NVP-BEP800) is a potent orally available andselective inhibitor with an of 58 nM for Hsp90βHsp90 IC50VER-82576 also slightly blocks Grp94 and Trap-1 with s ofIC5041 and 55 μM respectively

Bioactivity XL888 is a heat shock protein-90 ( ) inhibitor with anHSP90 of 24 nMIC50

Bioactivity YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathwayagainst glioblastoma directly binding to heat shock protein

with an of 820 nM on NFAT nuclear90 (HSP90) IC50translocation YZ129-induced GBM cell-cycle arrest at the G2Mphase promotes apoptosis and inhibited tumor cellhellip

82 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

VER-82576 (NVP-BEP800) Cat No HY-10942

XL888 Cat No HY-13313

YZ129 Cat No HY-114413

wwwMedChemExpresscom 83

IRE1Inositol requiring enzyme 1

The serinethreonine-protein kinaseendoribonucleaseinositol-requiring enzyme 1 (IRE1) is an enzyme that in humans isencoded by the gene IRE1 is an endoplasmic reticulum (ER)ERN1transmembrane sensor that activates UPR to maintain ER and cellularfunction While mammalian IRE1 promotes cell survive it can initiateapoptosis via decay of anti-apoptotic microRNAsIRE1 activation is initiated by homotypic interactions of thestress-sensing lumenal domain favoring transautophosphorylation ofthe kinase-extension nuclease (KEN) domain on the cytoplasmic sideof the ER membraneIRE1XBP-1 has been shown to regulate a variety of genes in various

cell types in response to ER stress mostly related to ER function and the secretory pathway although the target genesvary depending on the cell type and nature of the stress stimuli

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9875Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg

IRE1 Inhibitors amp Modulators

Bioactivity 36-DMAD hydrochloride is a inhibitor of the pathwayIRE1α-XBP1of the unfolded protein response

Bioactivity 4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor ofIRE1α

Bioactivity 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1αinhibitor with an of 008 μM extracted from patent WOIC502008154484 A1 IRE-lα inhibitor compound 3-5

Bioactivity APY29 is an allosteric modulator of which inhibits IRE1αIRE1αautophosphorylation with of 280 nM and activates IRE1αIC50RNase activity

Bioactivity B I09 is an RNase inhibitor with an of 1230 nMIRE-1 IC50 Bioactivity GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1alpha ( ) which can inhibit and IRE1α IRE1α kinase activity RNase

with s of 20 and 200 nM respectivelyactivity IC50

Bioactivity GSK2850163 hydrochloride is a novel inhibitor ofinositol-requiring enzyme-1 alpha ( ) which can inhibitIRE1α

and with s of 20 andIRE1α kinase activity RNase activity IC50200 nM respectively

Bioactivity KIRA6 allosterically inhibits activity withIRE1α RNase kinasean of 06 microMIC50

Bioactivity Kira8 is a mono-selective inhibitor that allostericallyIRE1αattenuates with an of 59 nM IRE1α RNase activity IC50

[1]Bioactivity MKC3946 is a potent and soluble inhibitor used forIRE1α

cancer research

84 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

36-DMAD hydrochloride Cat No HY-U00460

4μ8C (IRE1 Inhibitor III) Cat No HY-19707

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) Cat No HY-107371

APY29 Cat No HY-17537

B I09 Cat No HY-107400

GSK2850163 Cat No HY-U00459

GSK2850163 hydrochloride Cat No HY-U00459B

KIRA6 Cat No HY-19708

Kira8 Cat No HY-114368

MKC3946 Cat No HY-19710

wwwMedChemExpresscom 85

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity MKC8866 is an inhibitor with an of less thanIRE1 RNase IC5001 μM for IRE1α RNase

Bioactivity MKC9989 is a ( ) inhibitor and alsoHydroxy aryl aldehydes HAAinhibits with an of 023 to 44 μMIRE1α IC50

Bioactivity STF-083010 is an inhibitor STF-083010 inhibits Ire1Ire1endonuclease activity without affecting its kinase activityafter endoplasmic reticulum stress

MKC8866 Cat No HY-104040

MKC9989 Cat No HY-12399

STF-083010 Cat No HY-15845

Kinesin

Kinesin is a protein belonging to a class of motor proteins found ineukaryotic cells Kinesins move along microtubule filaments and arepowered by the hydrolysis of ATP (thus kinesins are ATPases) Theactive movement of kinesins supports several cellular functionsincluding mitosis meiosis and transport of cellular cargo Mostkinesins walk towards the plus end of a microtubule entailstransporting cargo from the centre of the cell towards the peripheryKinesins were discovered as microtubule (MT)-based anterogradeintracellular transport motors The founding member of thissuperfamily the genomes of mammals encode more than 40 kinesinproteins organized into at least 14 families named kinesin-1 through

kinesin-14

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wwwMedChemExpresscom 87

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9871Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9973Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Kinesin Inhibitors amp Modulators

Bioactivity (R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of ARRY-520(R)-Filanesib ((R)-ARRY-520) is a synthetic kinesin spindle

inhibitor with of 6 nMprotein (KSP) IC50

Bioactivity AZ82 is a selective kinesin-like protein KIFC1 (HSETKIFC1)inhibitor with a of 43 nM and an of 300 nM for KIFC1Ki IC50

Bioactivity CW-069 is an allosteric inhibitor of microtubule motor with an of 75 μMprotein HSET IC50

Bioactivity Dimethylenastron is a potent inhibitor with ankinesin Eg5 of 200 nMIC50

Bioactivity Eg5 Inhibitor V trans-24 is a potent and specific kinesin Eg5inhibitor with an of 065 μM and can be used in theIC50research of cancer

Bioactivity EMD534085 is a potent and selective inhibitor of the mitotic with an of 8 nMkinesin-5 IC50

Bioactivity Filanesib (ARRY-520) is a synthetic kinesin spindle protein inhibitor with of 6 nM(KSP) IC50

Bioactivity Ispinesib is a specific inhibitor of kinesin spindle protein with a of 17 nM(KSP) Ki app

Bioactivity K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5with an of 13 μMIC50

Bioactivity Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member and is used for the research of cellular15 (Kif15)

proliferative diseases

(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A

AZ82 Cat No HY-12241

CW-069 Cat No HY-15857

Dimethylenastron Cat No HY-19944

Eg5 Inhibitor V trans-24 Cat No HY-112915

EMD534085 Cat No HY-15000

Filanesib (ARRY-520) Cat No HY-15187

Ispinesib (SB-715992) Cat No HY-50759

K858 Racemic Cat No HY-19966

Kif15-IN-1 Cat No HY-15948

Purity 9731Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9705Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg

Purity 9959Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9651Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Kif15-IN-2 is an inhibitor of the mitotic and iskinesin Kif15used for the research of cellular proliferative diseases

Bioactivity Litronesib is a selective mitosis-specific kinesin Eg5inhibitor with antitumor activity

Bioactivity Litronesib (Racemate) is the racemate of litronesibLitronesib is a selective allosteric inhibitor of kinesin

Eg5

Bioactivity Monastrol is a potent and cell-permeable inhibitor of themitotic with an value of 14 μMkinesin Eg5 IC50

Bioactivity Paprotrain is a cell-permeable inhibitor of the kinesin inhibits the ATPase activity of MKLP-2 with an MKLP-2 IC50

of 135 μM and a of 336 μM and shows a moderate inhibitionKiactivity on with an of 55 μMDYRK1A IC50

Bioactivity PF-2771 is a potent and selective centromere protein E inhibitor inhibiting CENP-E motor activity with an(CENP-E)

of 161 nM PF-2771 is used as an anticancer agentIC50

Bioactivity SB-743921 is a potent inhibitor of the mitotic kinesin KSP with a of 01 nM(Eg5) Ki

88 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Kif15-IN-2 Cat No HY-15949

Litronesib (LY-2523355 KF-89617) Cat No HY-14846

Litronesib Racemate (LY-2523355 Racemate KF-89617 Racemate) Cat No HY-14846A

Monastrol ((plusmn)-Monastrol) Cat No HY-101071A

Paprotrain Cat No HY-101298

PF-2771 Cat No HY-19530

SB-743921 Cat No HY-12069

wwwMedChemExpresscom 89

LIM Kinase (LIMK)LIMKs

LIM kinases (LIMKs) are important cell cytoskeleton regulators thatplay a prominent role in cancer manifestation and neuronal diseasesThe LIMK family consists of two homologues LIMK1 and LIMK2which differ from one another in expression profile intercellularlocalization and function The main substrate of LIMK is cofilin amember of the actin-depolymerizing factor (ADF) protein familyWhen phosphorylated by LIMK cofilin is inactive LIMKs play acontributory role in several neurodevelopmental disorders and incancer growth and metastasisLIM domain kinases (LIMK1 and 2) are substrate for Cdc42Rac-PAKand modulate actin dynamics by phosphorylating cofilin at serine-3

This modification inactivates cofilinrsquos actin severing and depolymerizing activity LIMKs also translocate into thenucleus and regulate cell cycle progression LIMKs are potential therapeutic targets for NF2 and other merlin-deficienttumors

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

LIM Kinase (LIMK) Inhibitors amp Modulators

Bioactivity BMS-3 is a potent inhibitor with s of 5 nM and 6LIMK IC50nM for and respectivelyLIMK1 LIMK2

Bioactivity BMS-5 (LIMKi 3) is a potent inhibitor with s of 7LIMK IC50nM and 8 nM for and respectivelyLIMK1 LIMK2

Bioactivity R-10015 a broad-spectrum antiviral compound for HIVinfection acts as a potent and selective inhibitor of LIM

and binds to the ATP-binding pocketdomain kinase (LIMK)with an of 38 nM for human LIMK1 IC50

[1]

Bioactivity T56-LIMKi is a selective inhibitor of inhibits theLIMK2growth of Panc-1 cells with an of 352 μMIC50

90 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

BMS-3 Cat No HY-18304

BMS-5 (LIMKi 3) Cat No HY-18305

R-10015 Cat No HY-120097

T56-LIMKi (T5601640) Cat No HY-19352

wwwMedChemExpresscom 91

MicrotubuleTubulin

Microtubules are a component of the cytoskeleton found throughoutthe cytoplasm These tubular polymers of tubulin can grow as long as50 micrometres with an average length of 25 microm and are highlydynamic The outer diameter of a microtubule is about 24 nm whilethe inner diameter is about 12 nm Microtubules are found ineukaryotic cells and are formed by the polymerization of a dimer oftwo globular proteins alpha and beta tubulin Tubulin is one ofseveral members of a small family of globular proteins The tubulinsuperfamily includes five distinct families the alpha- beta- gamma-delta- and epsilon-tubulins and a sixth family which is present only inkinetoplastid protozoa The most common members of the tubulin

family are α-tubulin and β-tubulin the proteins that make up microtubules Microtubules are very important in anumber of cellular processes They are involved in maintaining the structure of the cell

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9987Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9920Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9982Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

MicrotubuleTubulin Inhibitors amp Modulators

Bioactivity 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivativewith improved pharmacological features and higher watersolubility IC50 value Target Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cyclearrest and apoptosis as measured by flow cytometry DNAhellip

Bioactivity 10-Oxo Docetaxel (Docetaxel Impurity) is a novel taxoid havingremarkable anti-tumor properties and a Docetaxel intermediate

Bioactivity 2-Methoxyestradiol is an inhibitor and angiogenesis apoptosisinducer with potent antineoplastic activity2-Methoxyestradiol also destablize microtubules

Bioactivity 4-Demethylepipodophyllotoxin(4-DMEP) is a key intermediatecompound for the preparation of podophyllotoxin-typeanti-cancer drugs a potent inhibitor of microtubule assembly

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity ofdocetaxel detected by high performance liquid chromatography(HPLC)

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity C 7-Epitaxotere)is a impurity of docetaxel

Bioactivity 7-epi-Taxol is an active metabolite of taxol with activitycomparable to that of taxol against cell replicationpromoting bundle formation and againstmicrotubulemicrotubule depolymerization

Bioactivity 7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel)derivative Paclitaxel binds to tubulin and inhibits thedisassembly of microtubules

Bioactivity ABT-751(E 7010) is a novel bioavailable tubulin-binding andantimitotic sulfonamide agent with IC50 of about 15 and 34μM in neuroblastoma and non-neuroblastoma cell linesrespectively IC50 Value 15 μM(neuroblastoma) 34μM(non-neuroblastoma) Target MicrotubuleTubulin in vitrohellip

Bioactivity Amphethinile is an agent The affinity constantanti-tubulinfor the association ( ) of Amphethinile with tubulin isKa13 μM

92 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol

10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584

10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674

2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033

4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435

7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675

7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676

7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227

7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574

ABT-751 (E7010) Cat No HY-13270

Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190

wwwMedChemExpresscom 93

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9903Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9949Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9751Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ansamitocin P-3 is a inhibitor Ansamitocin P-3microtubuleis a macrocyclic antitumor antibiotic

Bioactivity Auristatin E is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAE analog and cytotoxin inAntibody-drug conjugates

Bioactivity Auristatin F is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAF analog and cytotoxin inAntibody-drug conjugates

Bioactivity BNC105 is a tubulin polymerization inhibitor with potentantiproliferative and tumor vascular disrupting properties

Bioactivity BTB-1 is a potent selective and reversible mitotic motorprotein inhibitor with an of 169 μMKif18A IC50

Bioactivity Cabazitaxel is a semi-synthetic derivative of the naturaltaxoid 10-deacetylbaccatin III with potential antineoplasticactivity

Bioactivity CCB02 is a selective inhibitor bindingCPAP-tubulin interactionto tubulin and competing for the CPAP binding site ofβ-tubulin with an of 689 nM and shows potent anti-tumorIC50activity CCB02 shows no inhibition on the cell cycle- andcentrosome-related kinases or the phosphorylation status ofhellip

Bioactivity Cephalomannine is a taxol derivative with antitumorantiproliferative properties

Bioactivity Cevipabulin (TTI-237) is an oral microtubule-active antitumorcompound and inhibits the binding of [ H] vinblastine to3

tubulin with an of 18-40 nM for cytotoxicity in humanIC50

tumor cell line [1] [2]

Bioactivity Cevipabulin fumarate (TTI-237 fumarate) is an oralmicrotubule-active antitumor compound and inhibits thebinding of [ H] vinblastine to tubulin with an of3 IC50

18-40 nM for cytotoxicity in human tumor cell line [1] [2]

Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739

Auristatin E Cat No HY-15582

Auristatin F Cat No HY-15583

BNC105 Cat No HY-16114

BTB-1 Cat No HY-101770

Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459

CCB02 Cat No HY-114302

Cephalomannine Cat No HY-77554

Cevipabulin (TTI-237) Cat No HY-14949

Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C

Purity 9828Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9956Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9831Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Bioactivity Colchicine is a inhibitor and a tubulin microtubuledisrupting agent Colchicine inhibits microtubulepolymerization with an of 3 nMIC50

Bioactivity Combretastatin A4 is a -targeting agent thatmicrotubulebinds with of 04 μMβ-tubulin Kd

Bioactivity Crolibulin is a small molecule tubulin polymerizationinhibitor

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate IC50 Value NATarget tubulin ADCs For comparison purposes the ADC A1-mc-MMAD andor A1 -vc-MMAD were used The linker payloadmc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) washellip

Bioactivity D-64131 is a novel inhibitor of Tubulin polymerization thatcompetitively binds with [(3)H]colchicine to αβ-Tubulin

Bioactivity D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule

Bioactivity D8-MMAE is a deuterated labeled MMAE a potent mitoticinhibitor

Bioactivity D8-MMAF is a deuterated form of MMAF which is a disrupting agentmicrotubule

Bioactivity D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a disrupting agentmicrotubule

Bioactivity DM4 is is an agent that inhibit cell division DM4antitubulincan be used in the preparation of antibody drug conjugate

94 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Colchicine Cat No HY-16569

Combretastatin A4 (CRC 87-09) Cat No HY-N2146

Crolibulin (EPC2407) Cat No HY-13603

Cys-mcMMAD Cat No HY-15750

D-64131 Cat No HY-15482

D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8

Monomethyl Dolastatin 10 D8) Cat No HY-15581S

D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A

D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S

D8-MMAF hydrochloride Cat No HY-15579AS

DM4 Cat No HY-12454

wwwMedChemExpresscom 95

Purity 9897Clinical Data LaunchedSize 500u g 1 mg

Purity gt98Clinical Data LaunchedSize 1 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Purity 9988Clinical Data Phase 3Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9555Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9983Clinical Data Phase 2Size 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg

Bioactivity Docetaxel is an antineoplastic drug by inhibiting depolymerization and attenuating of themicrotubule

effects of and gene expressionbcl-2 bcl-xL

Bioactivity Docetaxel Trihydrate is a semi-synthetic taxane analogue actsas a stabilizermicrotubule

Bioactivity Angiotensin II human is a vasoconstrictor that acts on the and the receptorAT1 AT2

Bioactivity ELR510444 is a novel microtubule disruptor inhibitsMDA-MB-231 cell proliferation with IC50 of 309 nM not asubstrate for the P-glycoprotein drug transporter and retainsactivity in βIII-tubulin-overexpressing cell lines

Bioactivity Entasobulin is a polymerization inhibitor withβ-tubulinpotential anticancer activity

Bioactivity Epothilone A is a competitive inhibitor of the binding of [H] paclitaxel to polymers with a of 06-14 μM3 tubulin Ki

Bioactivity Epothilone B is a stabilizer with a ofmicrotubule Ki071μM It acts by binding to the αβ-tubulin heterodimersubunit which causes decreasing of αβ-tubulin dissociation

Bioactivity Epothilone D (KOS 862) is a potent stabilizermicrotubule

Bioactivity Eribulin (E7389) is a targeting agent that ismicrotubuleused in the treatment of metastatic breast cancer Eribulin(E7389) inhibits the proliferation of cancer cells by bindingmicrotubule proteins and microtubules

Bioactivity Eribulin mesylate (E7389 mesylate) is a microtubuletargeting agent that is used in the treatment of metastaticbreast cancer Eribulin mesylate (E7389 mesylate) inhibits theproliferation of cancer cells by binding microtubule proteinsand microtubules

Docetaxel (RP-56976) Cat No HY-B0011

Docetaxel Trihydrate (RP-56976 (Trihydrate)) Cat No HY-B0011A

Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580

ELR510444 Cat No HY-16191

Entasobulin Cat No HY-16777

Epothilone A (Epo A) Cat No HY-13503

Epothilone B (EPO 906 Patupilone) Cat No HY-17029

Epothilone D (KOS 862) Cat No HY-15278

Eribulin (B1939 E7389 ER-086526) Cat No HY-13442

Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A

Purity 9874Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9723Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9947Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9801Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Bioactivity Estramustine phosphate sodium is an antimicrotubulechemotherapy agent arrests prostate cancer cells in the G2Mphase of the cell cycle

Bioactivity Fosbretabulin disodium(CA 4DP CA 4P) is a microtubuledestabilizing drug a type of vascular-targeting agent a drugdesigned to damage the vasculature (blood vessels) of cancertumors causing central necrosis IC50 Value 4 nM [1] Targetmicrotubule in vitro Cytotoxic IC(50) values of CA-4 in humanhellip

Bioactivity Ixabepilone is an orally bioavailable inhibitor which binds to tubulin andmicrotubule

promotes tubulin polymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of the cell cycle andinduces tumor cell apoptosis

Bioactivity Lexibulin(CYT-997) is a potent tubulin polymerisationinhibitor with IC50 of 10-100 nM in cancer cell lines withpotent cytotoxic and vascular disrupting activity in vitro andin vivo

Bioactivity Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM in cancer celllines with potent cytotoxic and vascular disrupting activityin vitro and in vivo

Bioactivity Maytansinol inhibits microtubule assembly and inducesmicrotubule disassembly in vitro Target MicrotubuleTubulinin vitro Maytansinol disrupts the mitotic spindle andprevents mitotic exit in Drosophila Maytansinol reduces thegrowth andor survival of HCT116 cells in a dose-dependenthellip

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate Mc-MMAD is aprotective group (maleimidocaproyl) -conjugated MMAD IC50Value Target tubulin ADCs For comparison purposes the ADCA1 -mc-MMAD andor A1 -vc-MMAD were used The linkerpayloadhellip

Bioactivity Mc-MMAE is a protective group (maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE) which is a potent tubulininhibitor is a toxin payload in antibody drug conjugate (

)ADC

Bioactivity Mc-MMAF is a protective group-conjugated MMAF MMAF is a morepotent drug than Monomethyl auristatin E (MMAE) but ischarged and relatively membrane-impermeable is a potenttubulin inhibitor is a toxin payload in antibody drugconjugate Target MMAF is a new auristatin derivative with ahellip

Bioactivity Mertansine (DM1) is a inhibitor and is anmicrotubulinantibody-conjugatable maytansinoid that is developed toovercome systemic toxicity associated with maytansine and toenhance tumor-specific delivery Mertansine can be attached toa monoclonal antibody with a linker to create an antibody-drughellip

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Estramustine phosphate sodium Cat No HY-13627

Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449

Ixabepilone (Azaepothilone B BMS 247550 BMS 247550-1) Cat No HY-10222

Lexibulin (CYT-997) Cat No HY-10498

Lexibulin dihydrochloride (CYT-997 dihydrochloride) Cat No HY-10498A

Maytansinol (Ansamitocin P-0) Cat No HY-19474

Mc-MMAD Cat No HY-15740

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741

McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578

Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792

wwwMedChemExpresscom 97

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9957Clinical Data Phase 3Size 10mM x 1mL in Water

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 4Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity Microtubule inhibitor 1 is an antitumor agent with inhibitory activity with anmicrotubule polymerization

value of 9-16 nM in cancer cells IC50[1]

Bioactivity MMAD is a potent inhibitor is a toxin payload intubulinantibody drug conjugates ( )ADCs

Bioactivity MMAF (Monomethylauristatin F) is an antitubulin agent thatinhibit cell division inhibits H3397 cell growth with an IC50of 105 nM

Bioactivity MMAF hydrochloride is an antitubulin agent that inhibit celldivision inhibits H3397 cell growth with an of 105 nMIC50

Bioactivity Monomethyl auristatin E (MMAE SGD-1010) is a syntheticderivative of dolastatin 10 and functions as a potent

inhibitor by inhibiting tubulin polymerizationmitoticMMAE is widely used as a cytotoxic component of antibody-drug

to treat several different cancer typesconjugates (ADCs)

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity Ombrabulin (AVE8062) is a derivative of CA-4 phosphate whichis known to exhibit antivascular effects through selectivedisruption of the cytoskeleton of endothelial cellstubulin

Bioactivity Ombrabulin hydrochloride is a derivative of CA-4 phosphatewhich is known to exhibit antivascular effects throughselective disruption of the cytoskeleton of endothelialtubulincells

Bioactivity OSIP-486823 is a novel -interfering agent withmicrotubuledistinct biological effects on both protein kinase G (PKG) andmicrotubules

Bioactivity Paclitaxel (Taxol) a naturally occurring antineoplasticagent stabilizes resulting intubulin polymerizationarrest at the G2M phase of the cell cycle and apoptotic celldeath [1] [2]

Microtubule inhibitor 1 Cat No HY-114313

MMAD (Demethyldolastatin 10 Monomethylauristatin D

Monomethyl Dolastatin 10) Cat No HY-15581

MMAF (Monomethylauristatin F) Cat No HY-15579

MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat No HY-15579A

Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162

Nocodazole (Oncodazole R17934) Cat No HY-13520

Ombrabulin (AVE8062 AC7700) Cat No HY-14797

Ombrabulin hydrochloride (AVE8062 (hydrochloride) AC7700 (hydrochloride)) Cat No HY-18256

OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004

Paclitaxel (Taxol) Cat No HY-B0015

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9979Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9344Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9968Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Bioactivity Parbendazole is a potent inhibitor of assemblymicrotubuledestabilizes tubulin with an of 879nM and exhibitsEC50a broad-spectrum anthelmintic activity

Bioactivity PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX) compound acts asa -depolymerizing agent and an apoptotic agentmicrotubule

Bioactivity PE859 is a potent inhibitor of both and aggregationtau Aβwith values of 066 and 12 μM respectivelyIC50

Bioactivity PF-06380101 is a novel cytotoxic Dolastatin 10 analogue withexcellent potencies in tumor cell proliferation assays anddifferential ADME properties when compared to other syntheticauristatin analogues that are used in the preparation of ADCsIC50 value ~02 nM(GI50 in BT474 MDA-MB-361-DYT2 and N87hellip

Bioactivity Plinabulin (NPI-2358) is a vascular disrupting agents (VDA)against tubulin-depolymerizing with IC50 of 98~18 nM in tumorcells IC50 Value 98~18 nM Target MicrotubuleTubulin invitro NPI-2358 binds to the colchicine-binding site oftubulin and has potent inhibitory to human tumor cell lineshellip

Bioactivity Podofilox (Podophyllotoxin) is a potent inhibitor ofmicrotubule assembly and DNA topoisomerase II

Bioactivity Rosabulin is a potent inhibitor withmicrotubuleanti-cancer activities

Bioactivity Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10derivative and inhibitor of polymerizationtubulin

Bioactivity SSE15206 is a polymerization inhibitor (GI microtubule 50= 197 nM in HCT116 cells) that overcomes multidrug resistanceCauses aberrant mitosis resulting in G2M arrest due toincomplete spindle formation in cancer cells [1]

Bioactivity Taltobulin (HTI-286 SPA-110) is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibitedproliferation of all three hepatic tumor cell lines (mean IC50= 2 nmolL +- 1 nmolL) in vitro Interestingly no decreasehellip

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Parbendazole (SKF 29044) Cat No HY-115364

PBOX 6 Cat No HY-U00446

PE859 Cat No HY-12662

PF-06380101 Cat No HY-12522

Plinabulin (NPI-2358) Cat No HY-14444

Podofilox (Podophyllotoxin) Cat No HY-15552

Rosabulin (STA 5312) Cat No HY-14934

Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672

SSE15206 Cat No HY-111425

Taltobulin (HTI-286 SPA-110) Cat No HY-15584

wwwMedChemExpresscom 99

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9624Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9996Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Taltobulin hydrochloride is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibits proliferationof all three hepatic tumor cell lines (mean IC50 = 2 nmolL+- 1 nmolL) Interestingly no decrease in viable primaryhellip

Bioactivity Taltobulin trifluoroacetate (HTI-286 SPA-110) is an analogueof Hemiasterlin potent tubulin inhibitor ADCs cytotoxinIC50 value Target tubulin in vitro HTI-286 significantlyinhibited proliferation of all three hepatic tumor cell lines(mean IC50 = 2 nmolL +- 1 nmolL) in vitro Interestinglyhellip

Bioactivity Tasidotin hydrochloride is a peptide analog of the antimitoticdepsipeptide dolastatin 15 as an inhibitor of microtubuleassembly and microtubule dynamics

Bioactivity Tirbanibulin (KX2-391) is an inhibitor of that targetsSrcthe peptide substrate site of Src with of 9-60 nM inGI50cancer cell lines

Bioactivity Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) isan inhibitor of that targets the peptide substrate siteSrcof Src with of 9-60 nM in cancer cell linesGI50

Bioactivity Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitorof that targets the peptide substrate site of Src withSrc

of 9-60 nM in cancer cell linesGI50

Bioactivity Triclabendazole(CGA89317) is a benzimidazole it binds totubulin impairing intracellular transport mechanisms andinterferes with protein synthesis Target MicrotubuleTubulinTriclabendazole treatment produces percentage decreases of thefluke egg output by 153 43 and 366 respectively inhellip

Bioactivity Tubulin inhibitor 1 is a inhibitor occupying thetubulincolchicine binding site inhibits tubulin polymerizationTubulin inhibitor 1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase and inducescellular apoptosis [1]

Bioactivity Tubulysin A(TubA) is a myxobacterial product that can functionas an antiangiogenic agent in many in vitro assaysanti-microtubule anti-mitotic an apoptosis induceranticancer anti-angiogenic and antiproliferative IC50value Target microtubule Tubulysin A is a novel antibiotichellip

Bioactivity Valecobulin (CKD516) a valine prodrug of (S516) and avascular disrupting agent (VDA) is a potent beta-tubulin

inhibitor with marked antitumor activitypolymerizationagainst murine and human solid tumors [1] [2]

Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A

Tasidotin hydrochloride (ILX651) Cat No HY-13760

Tirbanibulin (KX2-391 KX-01) Cat No HY-10340

Tirbanibulin dihydrochloride (KX2-391 (dihydrochloride) KX-01 (dihydrochloride)) Cat No HY-10340A

Tirbanibulin Mesylate (KX2-391 (Mesylate) KX01 (Mesylate)) Cat No HY-10340B

Triclabendazole (CGA89317) Cat No HY-B0621

Tubulin inhibitor 1 Cat No HY-112607

Tubulysin A (TubA) Cat No HY-15995

Valecobulin (CKD-516) Cat No HY-13598

Purity 9958Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9914Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data LaunchedSize 10 mg 50 mg 100 mg 200 mg

Purity 9987Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9989Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Bioactivity Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulininhibitor (MMAD) Vc-MMAD is an antibody drug conjugate IC50Valu NA Target tubulin ADCs Monomethyl auristatin D(MMAD) a potent tubulin inhibitor is a toxin payload andantibody drug conjugate For comparison purposes the ADC A1hellip

Bioactivity VcMMAE is a with potentdrug-linker conjugate for ADCantitumor activity by using the anti-mitotic agent monomethylauristatin E (MMAE) linked via the lysosomally cleavabledipeptide valine-citrulline (vc)

Bioactivity Vinblastine sulfate is a cytotoxic alkaloid used againstvarious cancer types Vinblastine sulfate inhibits theformation of microtubule and suppresses nAChR with an ofIC5089 μM

Bioactivity Vincristine sulfate is an antitumor vinca alkaloid whichinhibits formation in mitotic spindlemicrotubuleresulting in an arrest of dividing cells at the metaphasestage It binds to with a of 85 nMmicrotubule Ki

Bioactivity Vinflunine is a new vinca alkaloid uniquely fluorinated withthe properties of mitotic-arresting and tubulin-interactingactivity

Bioactivity Vinflunine Tartrat is a new vinca alkaloid uniquelyfluorinated with the properties of mitotic-arresting andtubulin-interacting activity Target MicrotubuleTubulin Themajor effects of Vinflunine on dynamic instability are aslowing of the microtubule growth rate an increase in growthhellip

Bioactivity Vinorelbine is an anti-mitotic agent which inhibits theproliferation of Hela cells with IC of 125 nM50

Bioactivity Vinorelbine (ditartrate) is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC of 12550nM

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Vc-MMAD Cat No HY-15742

VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575

Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780

Vincristine sulfate (Leurocristine sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488

Vinflunine Cat No HY-B0628

Vinflunine Tartrate Cat No HY-B0628A

Vinorelbine (KW-2307 base) Cat No HY-12053

Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A

wwwMedChemExpresscom 101

Mps1Monopolar spindle 1

Monopolar spindle 1 (Mps1) also known as TTK is a serine threoninekinase which ensures proper biorientation of sister chromatids on themitotic spindle by the activation of the spindle assembly checkpoint(SAC) Mps1 has been shown to function as the key kinase thatactivates the spindle assembly checkpoint (SAC) to secure properdistribution of chromosomes to daughter cellsMps1 is a dual specificity protein kinase that is essential for thebipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomesare properly attached Mps1 is expressed at high levels during mitosisand is abundantly expressed in cancer cells Disruption of Mps1

function induces aneuploidy and cell death

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Mps1 Inhibitors amp Modulators

Bioactivity AZ3146 is a reasonably potent and selective inhibitorMps1with of 35 nM for Mps1 IC50

CatBioactivity BAY 1217389 is a potent and selective inhibitor of the

monopolar spindle 1 ( ) kinase with an value lessMPS1 IC50than 10 nM

Bioactivity BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1)checkpoint with an of 2 nMIC50

Bioactivity CCT251455 is a potent and selective mitotic kinase monopolarspindle 1 ( ) inhibitor with an of 3 nMMPS1 IC50

Bioactivity CFI-402257 is a highly selective and orally bioavailable inhibitor with an of 17 nM for TTK in vitroTTKMps1 IC50

CFI-402257 has anti-cancer activity [1]

Bioactivity CFI-402257 hydrochloride is a highly selective and orallybioavailable inhibitor with an of 17 nM forTTKMps1 IC50TTK in vitro CFI-402257 hydrochloride has anti-canceractivity [1]

Bioactivity Empesertib (BAY 1161909) is a potent inhibitor withMps1an of lt 1 nMIC50

Bioactivity MPI-0479605 is a potent and selective ATP-competitiveinhibitor of with an of 18 nMMps1 IC50

Bioactivity Mps1-IN-1 is a potent selective and ATP-competitive Mps1kinase inhibitor with an and a of 367 nM and 27 nMIC50 Kd

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

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AZ3146 Cat No HY-14710

BAY1217389 Cat No HY-12859

BOS-172722 Cat No HY-112162

CCT251455 Cat No HY-12603

CFI-402257 Cat No HY-101340

CFI-402257 hydrochloride Cat No HY-101340A

Empesertib (BAY 1161909) Cat No HY-12858

MPI-0479605 Cat No HY-12660

Mps1-IN-1 Cat No HY-13298

Mps1-IN-2 Cat No HY-13994

wwwMedChemExpresscom 103

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-3 is a potent and selective kinase inhibitorMPS1with an of 50 nMIC50

Bioactivity NMS-P715 is a selective ATP-competitive inhibitor of MPS1with an of 182 nMIC50

Bioactivity NMS-P715 analog is an inhibitor of with an of 84MPS1 IC50nM

Mps1-IN-3 Cat No HY-12401

NMS-P715 Cat No HY-12382

NMS-P715 analog Cat No HY-14712

Nucleoside AntimetaboliteAnalog

Nucleoside analogues are molecules that act like nucleosides in DNAsynthesis They include a range of antiviral products used to preventviral replication in infected cells Nucleoside analogues can be usedagainst hepatitis B virus hepatitis C virus herpes simplex and HIVOnce they are phosphorylated they work as antimetabolites by beingsimilar enough to nucleotidesto be incorporated into growing DNAstrands Less selective nucleoside analogues are used aschemotherapy agents to treat cancer eg gemcitabine and 5-FUAntimetabolite is a chemical that inhibits the use of a metabolitewhich is another chemical that is part of normal metabolism Suchsubstances are often similar in structure to the metabolite that they

interfere with such as the antifolates that interfere with the use of folic acid The presence of antimetabolites can havetoxic effects on cells such as halting cell growth and cell division so these compounds are used as chemotherapy forcancer

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wwwMedChemExpresscom 105

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Nucleoside AntimetaboliteAnalog Inhibitors amp Modulators

Bioactivity 1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is abicyclic nucleoside

Bioactivity 1-Methylcytosine is a methylated form of the DNA base cytosineand used as a nucleobase of hachimoji DNA in which it pairswith Isoguanine [1] [2]

Bioactivity 1-Methylinosine is a modified nucleotide found at position 37in tRNA 3 to the anticodon of eukaryotic tRNA [1]

Bioactivity 2-Deoxypseudoisocytidine is a nucleoside analogue

Bioactivity 2rsquo-O4rsquo-C-Methyleneuridine (Compound 15a) is a bicyclicnucleoside

Bioactivity 3-Azido-3-deoxy-5-fluorocytidine (Compound 12) is a cytidinederivative

Bioactivity 3-Azido-3-deoxy-beta-L-uridine (Compound 25) is a nucleosidederivative

Bioactivity 3-Methylcytidine a urinary nucleoside can be used as abiomarker of four different types of cancer lung cancergastric cancer colon cancer and breast cancer [1]

Bioactivity 5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methyluridine is a derivative of LNA-type nucleoside

Bioactivity 5-Aza-7-deazaguanine is a substrate for wild-type (WT) E coli and its Ser90Ala mutant in thepurine nucleoside phosphorylase

synthesis of base-modified nucleosides [1]

1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine Cat No HY-111638

1-Methylcytosine Cat No HY-W006395

1-Methylinosine (N1-Methylinosine) Cat No HY-113139

2-Deoxypseudoisocytidine Cat No HY-101968

2rsquo-O4rsquo-C-Methyleneuridine Cat No HY-111639

3-Azido-3-deoxy-5-fluorocytidine Cat No HY-111641

3-Azido-3-deoxy-beta-L-uridine Cat No HY-111642

3-Methylcytidine Cat No HY-111645

5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methylurid

ine

Cat No HY-111807

5-Aza-7-deazaguanine Cat No HY-111627

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9874Clinical Data Phase 4Size 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 960Clinical Data LaunchedSize 50 mg 100 mg 500 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in Water

50 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Bioactivity 5-Azacytidine is a nucleoside analogue of cytidine thatspecifically inhibits DNA methylation by trapping DNA

methyltransferases

Bioactivity 5-BrdU is a nucleoside analog that competes with thymidine forincorporation into DNA 5-BrdU is commonly used in thedetection of proliferating cells

Bioactivity 5-Fluorouracil is a potent antitumor agent that affectspyrimidine synthesis by inhibiting thymidylate synthetasethus depleting intracellular dTTP pools

Bioactivity 6-Amino-5-nitropyridin-2-one is a pyridine base and used as anucleobase of hachimoji DNA in which it pairs with5-aza-7-deazaguanine [1]

Bioactivity 6-Mercaptopurine is a purine analogue which acts as anantagonist of the and has been widely usedendogenous purinesas antileukemic agent and immunosuppressive drug

Bioactivity 6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MPhydrate) is a purine analogue which acts as an antagonist ofthe and has been widely used asendogenous purinesantileukemic agent and immunosuppressive drug

Bioactivity 6-O-Methyl Guanosine is a modified nucleoside 6-O-Methyl[1]

Guanosine (6-methylguanosine) inhibit colony-forming abilityin a malignant xeroderma pigmentosum cell line [2]

Bioactivity 7-Methylguanosine is a novel cNIIIB nucleotidase inhibitorwith IC value of 878 plusmn 75 microM50

Bioactivity 8-Azaguanine is a purine analogue which shows antineoplasticactivity

Bioactivity Adenosine is a nucleoside composed of a molecule of adenineattached to a ribose sugar molecule (ribofuranose) moiety viaa β-N9-glycosidic bond Target Nucleosideantimetaboliteanalog Adenosine plays an important role inbiochemical processes such as energy transfer mdash as adenosinehellip

106 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

5-Azacytidine (Ladakamycin 5-AzaC Azacitidine) Cat No HY-10586

5-BrdU (BUdR BRDU) Cat No HY-15910

5-Fluorouracil (5-FU) Cat No HY-90006

6-Amino-5-nitropyridin-2-one Cat No HY-50071

6-Mercaptopurine (Mercaptopurine 6-MP) Cat No HY-13677

6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MP hydrate) Cat No HY-13677A

6-O-Methyl Guanosine Cat No HY-111648

7-Methylguanosine Cat No HY-122524

8-Azaguanine Cat No HY-B1468

Adenosine (Adenine riboside D-Adenosine) Cat No HY-B0228

wwwMedChemExpresscom 107

Purity 9818Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 1 g

Purity 9897Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carmofur is a derivative of fluorouracil an antimetaboliteused as an antineoplastic agent

Bioactivity Clofarabine(Clolar Clofarex) inhibits the enzymaticactivities of ribonucleotide reductase (IC50 = 65 nM) and DNApolymerase IC50 Value 65 nM Target in vitro Clofarabine isa second generation purine nucleoside analog withantineoplastic activity It is phosphorylated intracellularlyhellip

Bioactivity CNDAC is a major metabolite of oral drug sapacitabine and anucleoside analog

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Cytidine is a nucleoside molecule that is formed when cytosineis attached to a ribose ring cytidine is a component of RNATarget Nucleoside antimetaboliteanalog Cytidine is anucleoside molecule that is formed when cytosine is attachedto a ribose ring (also known as a ribofuranose) via ahellip

Bioactivity Dacarbazine(DTIC-Dome DTIC) is an antineoplastic agent Ithas significant activity against melanomas Target Nucleosideantimetaboliteanalog Approved May 1975 Dacarbazine (DTIC) isthe only single-agent approved by the Food and DrugAdministration for treating metastatic melanoma With DTIC ashellip

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Deoxypseudouridine is a nucleotide analog

Capecitabine Cat No HY-B0016

Carmofur (HCFU) Cat No HY-B0182

Clofarabine Cat No HY-A0005

CNDAC Cat No HY-16445A

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Cytidine (Cytosine β-D-riboside Cytosine-1-β-D-ribofuranoside) Cat No HY-B0158

Dacarbazine (Imidazole Carboxamide) Cat No HY-B0078

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Deoxypseudouridine Cat No HY-101970

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in Water

1000u g 2500u g 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 2500u g 5 mg 10 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 50 mg

Bioactivity DMTr-LNA-5MeU-3-CED-phosphoramidite is a nucleoside derivative[1]

Bioactivity Doxifluridine is a thymidine phosphorylase activator forPC9-DPE2 cells with IC50 of 062 μM

Bioactivity Ethynylcytidine is a new nucleoside antimetabolite Bioactivity Floxuridine (5-fluorodeoxyuridine) is an oncology drug thatbelongs to the class known as antimetabolites with an GI50 of51 μM for the inhibition of PEPT1 IC50 value TargetNucleoside antimetaboliteanalog Floxuridine (Fludara) is aprodrug of floxuridine and an oncology agent with an GI50 ofhellip

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

Bioactivity Fludarabine (phosphate) is an analogue of adenosine anddeoxyadenosine which is able to compete with dATP forincorporation into DNA and inhibit DNA synthesis

Bioactivity Forodesine(BCX-1777 freebase Immucillin-H) is an orallybioavailable PNP inhibitor with picomolar potency inducesapoptosis mainly in T cells

Bioactivity Forodesine hydrochloride is a potent and oral purine nucleoside inhibitor with s ranging from 048 tophosphorylase (PNP) IC50

157 nM

Bioactivity Fosteabine is an oral and prodrug analogue of cytarabine whichis resistant to deoxycytidine deaminase

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

108 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

DMTr-LNA-5MeU-3-CED-phosphoramidite Cat No HY-111531

Doxifluridine (Ro 21-9738 5-Fluoro-5-deoxyuridine 5-DFUR) Cat No HY-B0021

Ethynylcytidine (ECyD TAS-106 3-C-Ethynylcytidine) Cat No HY-16200

Floxuridine (5-Fluorouracil 2-deoxyriboside) Cat No HY-B0097

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Fludarabine phosphate (NSC 118218 (phosphate)) Cat No HY-B0028

Forodesine (BCX-1777 freebase Immucillin-H) Cat No HY-16210

Forodesine hydrochloride (BCX-1777 Immucillin-H hydrochloride) Cat No HY-16209

Fosteabine (Cytarabine ocfosfate YNK 01) Cat No HY-106349

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

wwwMedChemExpresscom 109

Purity 9575Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 9971Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9829Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Gemcitabine elaidate(CP-4126 CO-101) is a lipophilicunsaturated fatty acid ester derivative of gemcitabine (dFdC)an antimetabolite deoxynucleoside analogue with potentialantineoplastic activity IC50 value Target Gemcitabineanalog Upon hydrolysis intracellularly by esterases thehellip

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity Isocytosine is a non-natural nucleobase and an isomer ofcytosine It is used in combination with Isoguanine in studiesof unnatural nucleic acid analogues of the normal base pairsin DNA and used as a nucleobase of hachimoji RNA [1] [2]

Bioactivity Isoguanine is a purine base that is an isomer of guanine Abuilding block in organic synthesis

Bioactivity LY2334737 is an orally available prodrug of gemcitabine whichis a nucleoside analog used as chemotherapy

Bioactivity N2-methylguanosine is a modified nucleoside that occurs atseveral specific locations in many tRNAs

Bioactivity N6N6-Dimethyladenosine is a modified ribonucleosidepreviously found in rRNA and also exhibits in mycobacteriumbovis Bacille Calmette-Gueacuterin tRNA [1]

Bioactivity N6-Etheno 2-deoxyadenosine is a reactive oxygen species(ROS)reactive nitrogen species (RNS)-induced DNA oxidationproduct used as a biomarker to evaluate chronic inflammationand lipid peroxidation in animal or human tissues [1]

Bioactivity Nelarabine (Arranon 506U78) is a purine nucleoside analog andDNA synthesis inhibitor with IC50 from 0067-215 μM in tumorcells Nelarabine is a chemotherapy drug used in T-cell acutelymphoblastic leukemia

Bioactivity Orotic acid (OA) is an intermediate in pyrimidine metabolismIC50 Value Target Nucleoside antimetaboliteanalog in vitroOA increases cell proliferation and decreases apoptosis inserum-starved SK-Hep1 hepatocellular carcinoma cells whichmay ascribe to the inhibition of AMP-activated protein kinasehellip

Gemcitabine elaidate (CP-4126 CO-101 Gemcitabine 5-elaidate) Cat No HY-13538

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

Isocytosine Cat No HY-W002272

Isoguanine Cat No HY-124143

LY2334737 Cat No HY-13672

N2-Methylguanosine Cat No HY-111647

N6N6-Dimethyladenosine Cat No HY-101984

N6-Etheno 2-deoxyadenosine Cat No HY-111646

Nelarabine (506U78 GW 506U78 Nelzarabine) Cat No HY-13701

Orotic acid (6-Carboxyuracil Vitamin B13) Cat No HY-N0157

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9972Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9783Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9887Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9745Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity Pseudothymidine is a C-nucleoside analog of thymidine Bioactivity Raltitrexed is an antimetabolite drug used in chemotherapyacting by inhibiting thymidylate synthase

Bioactivity RX-3117(TV-1360 Fluorocyclopentenylcytosine) is novel acytidine analog shows anticancer activity in several cancercell lines including gemcitabine-resistant variants

Bioactivity Sapacitabine is an orally available prodrugnucleoside analogthat is structurally related to cytarabine

Bioactivity Tegafur (FT 207 NSC 148958) is a chemotherapeutic 5-FUprodrug used in the treatment of cancers is a component oftegafur-uracil

Bioactivity Tipiracil is a thymidine phosphorylase ( ) inhibitorTPase

Bioactivity Tipiracil (hydrochloride) is a thymidine phosphorylaseinhibitor (TPI) used for cancer research

Bioactivity Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT)is an irreversible inhibitor andthymidylate synthasethereby suppresses Trifluridine is an antiviralDNA synthesisdrug for infectionherpes simplex virus (HSV)

Bioactivity Trifluridine-tipiracil hydrochloride mixture (TAS-102) is anovel oral combination drug that consists of an antineoplasticthymidine-based nucleoside analog trifluorothymidine and apotent inhibitor tipiracil in athymidine phosphorylase105 molar ratio

Bioactivity Vidarabine (Ara-A) an antiviral drug which is active againstherpes simplex and varicella zoster viruses

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Pseudothymidine (5-Methyl-2-Deoxypseudouridin) Cat No HY-101969

Raltitrexed (ZD1694 D1694 ICI-D1694) Cat No HY-10821

RX-3117 (TV-1360 fluorocyclopentenylcytosine) Cat No HY-15228

Sapacitabine (CS682 CYC682) Cat No HY-16445

Tegafur (FT 207NSC 148958) Cat No HY-17400

Tipiracil Cat No HY-A0063A

Tipiracil hydrochloride Cat No HY-A0063

Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT) Cat No HY-A0061

Trifluridinetipiracil hydrochloride mixture (TAS-102) Cat No HY-16478

Vidarabine (Ara-A Adenine Arabinoside

9-β-D-Arabinofuranosyladenine) Cat No HY-B0277

wwwMedChemExpresscom 111

p97VCPCdc48

p97 an abundant hexameric ATPase of the AAA family is involved inhomotypic membrane fusion It is thought to disassemble SNAREcomplexes formed during the process of membrane fusion Twostructures have been reported a crystal structure of the N-terminaland D1 ATPase domains of murine p97 at 29 A resolution and acryoelectron microscopy structure of full-length rat p97 at 18 Aresolution Together these structures show that the D1 and D2hexamers pack in a tail-to-tail arrangement and that the N domain isflexible A comparison with NSF D2 (ATP complex) reveals possibleconformational changes induced by ATP hydrolysis

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9765Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

p97 Inhibitors amp Modulators

Bioactivity CB-5083 is a potent selective and orally bioavailable p97inhibitor with an value of 11 nMIC50

Bioactivity DBeQ is a selective potent reversible and ATP-competitive inhibitor with an value of 15 μM and 16 μM forp97 IC50

p97(wt) and p97(C522A) respectively DBeQ also inhibits Vps4with an of 115 μMIC50

Bioactivity ML240 is a potent inhibitor inhibiting p97 ATPase withp97 value of 100 nMIC50

Bioactivity ML241 hydrochloride is a potent inhibitor inhibiting p97p97ATPase with value of 100 nMIC50

Bioactivity NMS-859 is a potent covalent inhibitor withVCP (p97)s of 037 and 036 μM for wild-type VCP in the presence ofIC50

60 μM and 1 mM ATP in cells respectively

Bioactivity NMS-873 is a potent selective allosteric inhibitorVCPp97with value of 30 nMIC50

112 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CB-5083 Cat No HY-12861

DBeQ (JRF 12) Cat No HY-15945

ML240 Cat No HY-19795

ML241 hydrochloride Cat No HY-19797A

NMS-859 Cat No HY-15714

NMS-873 Cat No HY-15713

wwwMedChemExpresscom 113

PAKp21 activated kinases

PAKs (p21-activated kinases) are key regulators of actin dynamics cellproliferation and cell survival PAKs are SerThr kinases that areclassified into two groups on the basis of their structural andfunctional features group I (PAK1ndash3) and group II (PAK4ndash6) Group IPAKs have an auto-inhibitory domain (also called an inhibitory switchdomain) and a kinase domain (catalytic domain CD) and are activatedby the binding of the active (that is GTP-bound) forms of RhoGTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPasesBecause the deregulation of PAKs is closely associated with varioushuman diseasessmall-molecule inhibitors of these kinases have great

potential as therapeutic agents In addition these compounds can also be used as powerful tools in studies aimed atunderstanding the PAK signaling pathwayPAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actinremodelling and their ability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role intumor cell invasion and metastasis The current evidence suggests the involvement of PAKs in motility cell survivalanchorage-independent growth angiogenesis invasion migration and regulation of cell cycle and mitosisConsequently PAKs have also been implicated in a number of pathological conditions including cancer

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9902Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 1 g 5 g

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

PAK Inhibitors amp Modulators

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Fingolimod is a ( ) antagonistsphingosine 1-phosphate S1Pwith of 0033 nM in K562 and NK cells Fingolimod also isIC50a activatorpak1

Bioactivity Fingolimod hydrochloride is a ( )sphingosine 1-phosphate S1Pantagonist with an of 0033 nM in K562 and NK cellsIC50Fingolimod hydrochloride also is a activatorpak1

Bioactivity FRAX1036 is a inhibitor with s of 233 nM 724 nM andPAK Ki24 μM for PAK1 PAK2 and PAK4 respectively

Bioactivity FRAX486 is a p21-activated kinase ( ) inhibitor with sPAK IC50of 14 33 and 39 nM for PAK1 PAK2 and PAK3 respectively

Bioactivity FRAX597 is a potent group I p21-activated Kinases ( s)PAKinhibitor with of 8 13 and 19 nM for and IC50 PAK1 2 3

Bioactivity G-5555 is a potent p21-activated kinase 1 ( ) inhibitorPAK1with s of 37 nM and 11 nM for PAK1 and PAK2 respectivelyKi

Bioactivity G-5555 hydrochloride is a potent and selective p21-activatedkinase 1 ( ) inhibitor with a of 37 nMPAK1 Ki

Bioactivity IPA-3 is a selective non-ATP competitive inhibitor withPAK1 of 25 μM and shows no inhibition to group II PAKs (PAKsIC50

4-6)

Bioactivity NVS-PAK1-1 is a potent and selective allosteric PAK1inhibitor with an of 5 nMIC50

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5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Fingolimod (FTY720 free base) Cat No HY-11063

Fingolimod hydrochloride (FTY720) Cat No HY-12005

FRAX1036 Cat No HY-19538

FRAX486 Cat No HY-15542B

FRAX597 Cat No HY-15542A

G-5555 Cat No HY-19635

G-5555 hydrochloride Cat No HY-19635A

IPA-3 Cat No HY-15663

NVS-PAK1-1 Cat No HY-100519

wwwMedChemExpresscom 115

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity PAK-IN-1 is a inhibitor that displays group IIPAKselectivity PAK-IN-1 inhibits PAK4 PAK5 and PAK6 with sIC50of 75 36 126 nM respectively

Bioactivity PF-3758309 is an inhbitor of with of 13 nM forPAK IC50PAK4

PAK-IN-1 Cat No HY-12632

PF-3758309 Cat No HY-13007

PARPpoly ADP ribose polymerase

PARP is a family of proteins involved in a number of cellular processesinvolving mainly DNA repair and programmed cell death The PARPfamily comprises 17 members They have all very different structuresand functions in the cell PARP1 PARP2 VPARP (PARP4) Tankyrase-1and -2 (PARP-5a or TNKS and PARP-5b or TNKS2) have a confirmedPARP activity Others include PARP3 PARP6 TIPARP (or PARP7)PARP8 PARP9 PARP10 PARP11 PARP12 PARP14 PARP15 andPARP16 PARP is found in the cellrsquos nucleus The main role is to detectand signal single-strand DNA breaks (SSB) to the enzymaticmachinery involved in the SSB repair

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wwwMedChemExpresscom 117

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9839Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in Water

200 mg 500 mg

PARP Inhibitors amp Modulators

Bioactivity 3-Aminobenzamide is a potent inhibitor of with of appr 50 nM in CHO cellsPARP IC50

and acts as a mediator of oxidant-induced myocyte dysfunctionduring reperfusion

Bioactivity A-966492 is a novel and potent inhibitor of and with of 1 nM andPARP1 PARP2 Ki

15 nM respectively

Bioactivity AG14361 is a potent inhibitor with a of lt 5 nMPARP-1 Kiand in permeabilized SW620 and intact SW620 cells the sIC50are 29 nM and 14 nM respectively

Bioactivity AZ6102 is a potent dual and inhibitor withTNKS1 TNKS2s of 3 nM and 1 nM respectively and alao has 100-foldIC50

selectivity against other PARP family enzymes with s ofIC5020 μM 05 μM and gt3 μM for PARP1 PARP2 and PARhellip

Bioactivity AZD-2461 is a potent inhibitor with s of 5 nM 2 nMPARP IC50and 200 nM for PARP1 PARP2 and PARP3 respectively

Bioactivity BGP-15 is a inhibitor with an and a of 120 andPARP IC50 Ki57 μM respectively

Bioactivity BRCA1-IN-1 is a novel small-molecule-like inhibitorBRCA1with and of 053 μM and 071 μM respecrivelyIC50 Ki

Bioactivity Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolatedfrom traditional Chinese herb WT WangCorydalis yanhusuoDehydrocorydaline regulates protein expression of Bax Bcl-2activates and inactivates caspase-7 caspase-8 PARP

Bioactivity E7449 is a potent and inhibitor and alsoPARP1 PARP2inhibits and with s of 20 10 50 andTNKS1 TNKS2 IC5050 nM for PARP1 PARP2 TNKS1 and TNKS2 respectively using

P-NAD as substrate32 +

Bioactivity G007-LK is a potent and selective inhibitor of andTNKS1 with s of 46 nM and 25 nM respectivelyTNKS2 IC50

3-Aminobenzamide (PARP-IN-1) Cat No HY-12022

A-966492 Cat No HY-10614

AG14361 Cat No HY-12032

AZ6102 Cat No HY-12975

AZD-2461 Cat No HY-13536

BGP-15 Cat No HY-100828

BRCA1-IN-1 Cat No HY-100863

Dehydrocorydaline (13-Methylpalmatine) Cat No HY-N0674

E7449 Cat No HY-12418

G007-LK Cat No HY-12438

Purity 9952Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Bioactivity GeA-69 is a selective highly cell permeable allostericinhibitor of poly-adenosine-diphosphate-ribose polymerase 14

targeting macrodomain 2 with a of 21 microM (PARP14) Kd[1]

Bioactivity Iniparib (BSI-201) is an irreversible inhibitor of PARP1used in the research of triple negative breast cancer

Bioactivity JW 55 is a potent and selective signaling pathwayβ-catenininhibitor which functions via inhibition of the PARP domainof tankyrase 1 and tankyrase 2 (TNKS12) JW 55 decreasesauto-PARsylation of TNKS12 in vitro with s of 19 μM andIC50830 nM respectively

Bioactivity K-756 is a direct and selective ( ) inhibitortankyrase TNKSwhich inhibits the ADP-ribosylation activity of andTNKS1

with s of 31 and 36 nM respectivelyTNKS2 IC50

Bioactivity ME0328 is a potent and selective inhibitor withARTD3 PARP3an of 089plusmn028 μMIC50

Bioactivity MN-64 is a potent inhibitor with s of 6 nMtankyrase 1 IC5072 nM 191 μM and 394 μM for TNKS2 ARTD1 andTNKS1ARTD2 respectively

Bioactivity Niraparib (MK-4827) is a highly potent and PARP1 PARP2inhibitor with s of 38 and 21 nM respectivelyIC50

Bioactivity Niraparib hydrochloride (MK-4827 hydrochloride) is anexcellent and inhibitor with of 38 and 21PARP1 PARP2 IC50nM respectively

Bioactivity Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent inhibitor with of 24 nMPARP1 IC50

Bioactivity Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1and inhibitor with an of 38 and 21 nMPARP2 IC50respectively

118 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

GeA-69 Cat No HY-108708

Iniparib (BSI-201 NSC-746045 IND-71677) Cat No HY-12015

JW 55 Cat No HY-13968

K-756 Cat No HY-U00422

ME0328 Cat No HY-100225

MN-64 Cat No HY-19351

Niraparib (MK-4827) Cat No HY-10619

Niraparib hydrochloride (MK-4827 (hydrochloride)) Cat No HY-10619A

Niraparib R-enantiomer (MK 4827 (R-enantiomer)) Cat No HY-10619D

Niraparib tosylate (MK-4827 (tosylate)) Cat No HY-10619B

wwwMedChemExpresscom 119

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg

Purity 9768Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2 g

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NMS-P118 is a potent orally available and highly selective Inhibitor for cancer therapyPARP-1

Bioactivity NMS-P515 is a potent and stereospecific inhibitorPARP-1with an of 27 nM in hela cells Anti-tumor activity IC50

[1]

Bioactivity NVP-TNKS656 is a highly potent selective and orally active inhibitor with of 6 nM and is gt 300 foldTNKS2 IC50

selectivity against and PARP1 PARP2

Bioactivity Olaparib (AZD2281KU0059436) is a potent and oral PARPinhibitor with s of 5 and 1 nM for and IC50 PARP1 PARP2

respectively

Bioactivity Pamiparib is a inhibitor which can be used for thePARPtreatment of various cancers including the solid tumorextracted from patent WO 2013097225 A1

Bioactivity PARP-2-IN-1 is a potent and selective inhibitor withPARP-2an of 115 nMIC50

Bioactivity PJ34 is a potent specific inhibitor of with ofPARPl 2 IC50110 nM and 86 nM respectively

Bioactivity PJ34 hydrochloride is an inhibitor of with of 110PARPl12 IC50nM and 86 nM respectively

Bioactivity PROTAC PARP1 degrader is a degrader based on thePARP1 technology It induces significant PARP1 cleavage andPROTAC

programmed cell death PROTAC PARP1 degrader at 10 μM at 24 hinhibits MDA-MB-231 cell line with an of 612 μMIC50

Bioactivity RK-287107 is a potent and specific inhibitor withtankyrases of 143 and 106 nM for and IC50 tankyrase-1 tankyrase-2

respectively RK-287107 blocks colorectal cancer cell growth[1]

NMS-P118 Cat No HY-18954

NMS-P515 Cat No HY-128599

NVP-TNKS656 (TNKS656) Cat No HY-13990

Olaparib (AZD2281 KU0059436) Cat No HY-10162

Pamiparib (BGB-290) Cat No HY-104044

PARP-2-IN-1 Cat No HY-102035

PJ34 Cat No HY-13688A

PJ34 hydrochloride Cat No HY-13688

PROTAC PARP1 degrader Cat No HY-114324

RK-287107 Cat No HY-123892

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9962Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9888Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9508Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9983Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9989Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9981Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity Rucaparib (AG014699) is an inhibitor of with of 14 nM for PARP1 in aPARP Ki

cell-free assay and also shows binding affinity to eightother PARP domains

Bioactivity Rucaparib Camsylate is an inhibitor of with a of 14PARP KinM for PARP1 and also shows binding affinity to eight otherPARP domains

Bioactivity Rucaparib phosphate (AG-014699 phosphate) is a potent and oral inhibitor with a of 14 nM for PARP1 in cell-freePARP Ki

assay also showing binding affinity to eight other PARPdomains

Bioactivity Talazoparib (BMN-673) is a highly potent inhibitorPARP12with s of 12 nM and 087 nM respectivelyKi

Bioactivity Talazoparib 8R9S (BMN-673 8R9S) is an enantiomer ofTalazoparib less active than Talazoparib on the inhibition of

with an of 144 nMPARP1 IC50

Bioactivity Talazoparib tosylate (BMN 673ts) is a novel potent and orallyavailable inhibitor with an of 057 nM forPARP12 IC50PARP1

Bioactivity UPF 1069 is a inhibitor with s of 8 and 03 μM forPARP IC50PARP-1 and PARP-2 respectively

Bioactivity Veliparib is a potent inhibitor inhibiting andPARP PARP1 with s of 52 and 29 nM respectivelyPARP2 Ki

Bioactivity Veliparib (dihydrochloride) is a potent inhibitor of and with s of 52PARP1 PARP2 Ki

nM and 29 nM in cell-free assays respectively

Bioactivity WD2000-012547 is a selective poly(ADP-ribose)-polymerase(PARP-1) inhibitor with a pK of 8221i

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Rucaparib (AG014699 PF-01367338) Cat No HY-10617A

Rucaparib Camsylate Cat No HY-102003

Rucaparib phosphate (AG-014699 phosphate PF-01367338 phosphate) Cat No HY-10617

Talazoparib (BMN-673 LT-673) Cat No HY-16106

Talazoparib 8R9S (BMN-673 (8R9S) (8R9S)-LT-673) Cat No HY-16106A

Talazoparib tosylate (BMN 673ts) Cat No HY-108413

UPF 1069 Cat No HY-14478

Veliparib (ABT-888) Cat No HY-10129

Veliparib dihydrochloride (ABT-888 dihydrochloride) Cat No HY-10130

WD2000-012547 Cat No HY-U00223

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Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity XAV-939 is a inhibitor and an indirecttankyrase (TNKS)inhibitor of with s of 5 and 2Wntβ-catenin signaling IC50nM for TNKS1 and TNKS2 respectively

XAV-939 Cat No HY-15147

PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinase

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) isactivated in response to a variety of endoplasmic reticulum stressesimplicated in numerous disease states PERK is implicated intumorigenesis and cancer cell survival GSK2606414 is an orallyavailable potent and selective PERK inhibitor GSK2606414 inhibitsPERK activation in cells and inhibits the growth of a human tumorxenograft in mice PERK activation is independent of the largeincrease in unfolded nascent proteins within the ER followingtransient global brain ischemia

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Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

PERK Inhibitors amp Modulators

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity GSK2606414 is a cell-permeable and orally available proteinkinase R-like endoplasmic reticulum (ER) kinase (PERK)inhibitor with an of 04 nMIC50

Bioactivity GSK2656157 is a selective and ATP-competitive inhibitor ofprotein kinase R (PKR)-like endoplasmic reticulum kinase (

) with an of 09 nMPERK IC50

Bioactivity ISRIB (trans-isomer) is a potent inhibitor of with anPERK of 5 nMIC50

CCT020312 Cat No HY-119240

GSK2606414 Cat No HY-18072

GSK2656157 Cat No HY-13820

ISRIB trans-isomer Cat No HY-12495

Polo-like Kinase (PLK)

Polo-like Kinases (PLKs) are important regulators of the cell cycle Plksare involved in the formation of and the changes in the mitoticspindle and in the activation of CDKcyclin complexes duringM-phase of the cell cyclePolo-like kinases (Plks) are a family ofconserved serinethreonine kinases involved in the regulation of cellcycle progression through G2 and mitosis Mammalian polo-likekinases include Plk1 (Xenopus Plx1) Plk2Snk (Xenopus Plx2)Plk3PrkFnK (Xenopus Plx3) Plk4Sak and Plk5 Plk1 is involved in theregulation of key steps during cell division DNA damage repairpathways apoptosis and the progression of the cell cycle Plk3 is amultifunctional stress response protein that responses to signals

induced by DNA damage andor mitotic spindle disruption

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Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9982Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9897Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9857Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Polo-like Kinase (PLK) Inhibitors amp Modulators

Bioactivity BI 2536 is a dual and inhibitor with s of 083PLK1 BRD4 IC50

and 25 nM respectively BI-2536 suppresses IFNB[1]

(encoding IFN-β) gene transcription [4]

Bioactivity Centrinone (LCR-263) is a selective and reversible inhibitorof polo-like kinase 4 ( ) with a of 016 nMPlK4 Ki

Bioactivity Centrinone-B (LCR-323) is a potent and highly selective PLK4inhibitor with a of 059 nMKi

Bioactivity CFI-400945 free base is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity CFI-400945 fumarate is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity GSK461364 is a selective reversible and ATP-competitive inhibitor with a value of 22 nMPolo-like kinase 1 (PLK1) Ki

Bioactivity GW843682X is a selective ATP-competitive inhibitor of PLK1and with s of 22 nM and 91 nM respectively andPLK3 IC50is also gt100-fold selective against 30 other kinases

Bioactivity HMN-214 an orally bioavailable prodrug of HMN-176 is aninhibitor of polo-like kinase-1 ( ) with antitumorplk1activity

Bioactivity LFM-A13 is a potent inhibitor inhibitsBTK JAK2 PLKrecombinant BTK Plx1 and PLK3 with s of 25 μM 10 μM andIC5061 μM LFM-A13 shows no effects on JAK1 and JAK3 Src familykinase HCK EGFR and IRK

Bioactivity MLN0905 is a potent inhibitor with an of 2 nMPLK1 IC50

BI 2536 Cat No HY-50698

Centrinone (LCR-263) Cat No HY-18682

Centrinone-B (LCR-323) Cat No HY-18683

CFI-400945 free base Cat No HY-12300

CFI-400945 fumarate Cat No HY-12300B

GSK461364 (GSK461364A) Cat No HY-50877

GW843682X (GW843682) Cat No HY-11003

HMN-214 (IVX-214) Cat No HY-12045

LFM-A13 Cat No HY-18009

MLN0905 (PLK1 Inhibitor) Cat No HY-15155

Purity 9759Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9949Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9809Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9626Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9970Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

Bioactivity NMS-1286937 is a potent selective and orally available PLK1inhibitor with an of 2 nMIC50

Bioactivity Poloxime a hydrolysis product of poloxin is anon-ATP-competitive inhibitor with moderate Plk1Plk1inhibitory activity

Bioactivity Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1)inhibitor that targets the polo-box domain with an ofIC50appr 48 μM

Bioactivity Rigosertib (ON-01910) is a multi-kinase inhibitor and aselective anti-cancer agent which induces apoptosis byinhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib is a selective andhellip[1] [2]

Bioactivity Rigosertib sodium (ON-01910 sodium) is a multi-kinaseinhibitor and a selective anti-cancer agent which inducesapoptosis by inhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib sodium is a selective andhellip[1] [2]

Bioactivity Ro3280 is a potent highly selective inhibitor of withPLK1an and a of 3 nM and 009 nM respectively andIC50 Kdnearly has no effect on PLK2 and PLK3

Bioactivity SBE13 is a potent and selective inhibitor with an ofPlk1 IC50200 pM SBE13 poorly inhibits Plk2 (IC gt66 μM) or Plk350(IC =875 nM)50

Bioactivity SBE13 Hydrochloride is a potent and selective inhibitorPlk1with an of 200 pM SBE13 Hydrochloride poorly inhibitsIC50Plk2 (IC gt66 μM) or Plk3 (IC =875 nM)50 50

Bioactivity TAK-960 is an orally available selective inhibitor of with an of 08 nM at 10 μMpolo-like kinase 1 (PLK1) IC50

ATP TAK-960 also shows inhibitory activities against PLK2and with s of 169 and 502 nM respectivelyPLK3 IC50

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Mps1-IN-2 Cat No HY-13994

NMS-1286937 (NMS-P937) Cat No HY-15828

Poloxime Cat No HY-77195

Poloxin Cat No HY-12134

Rigosertib (ON-01910) Cat No HY-12037A

Rigosertib sodium (ON-01910 sodium) Cat No HY-12037

Ro3280 Cat No HY-15161

SBE13 Cat No HY-15158A

SBE13 Hydrochloride Cat No HY-15158

TAK-960 Cat No HY-15160

wwwMedChemExpresscom 127

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9955Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TAK-960 dihydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 dihydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TAK-960 hydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 hydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TC-S 7005 is a inhibitor with s ofPolo-like kinases (Plks) IC504 nM 24 nM and 214 nM for Plk2 Plk3 and Plk1 respectively

[1]

Bioactivity Volasertib is a highly potent Polo-like kinase 1 (PLK1)inhibitor with an of 087 nM as well as the two closelyIC50related kinases and with s of 5 and 56 nMPLK2 PLK3 IC50respectively

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

TAK-960 dihydrochloride Cat No HY-15160B

TAK-960 hydrochloride Cat No HY-15160A

TC-S 7005 Cat No HY-108597

Volasertib (BI 6727) Cat No HY-12137

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

PPARPeroxisome proliferator-activated receptors

PPARs (Peroxisome proliferator-activated receptors) areligand-activated transcription factors of nuclear hormone receptorsuperfamily comprising of the following three subtypes PPARαPPARγ and PPARβδ PPARs play essential roles in the regulation ofcellular differentiation development and metabolism (carbohydratelipid protein) and tumorigenesis of higher organisms All PPARsheterodimerize with the retinoid X receptor (RXR) and bind to specificregions on the DNA of target genes Activation of PPAR-α reducestriglyceride level and is involved in regulation of energy homeostasisActivation of PPAR-γ enhances glucose metabolism whereasactivation of PPAR-βδ enhances fatty acids metabolism

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Purity 9905Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9921Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 980Clinical Data Phase 4Size 50 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg

Purity gt98Clinical Data Phase 2Size 1 mg

Purity 9900Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

PPAR Inhibitors amp Modulators

Bioactivity 4-O-Methyl honokiol is a natural neolignan isolated from acts as a agonist and inhibtisMagnolia officinalis PPARγ

activity used for cancer and inflammation researchNF-κB

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Adelmidrol exerts important anti-inflammatory effects that arepartly dependent on Adelmidrol reduces PPARγ NF-κBtranslocation and expressionCOX-2

Bioactivity Aleglitazar(R1439 RO-0728804) is a new dual PPAR-αγ agonistwith IC50 of 28 nM46 nM

Bioactivity Arhalofenate (MBX 102) is a selective partial agonist ofperoxisome proliferator-activated receptor used for(PPAR)-γthe treatment of type 2 diabetes

Bioactivity Astaxanthin a red dietary carotenoid isolated from is an inhibitor of and aHaematococcus pluvialis PPARγ

potent antioxidant with antiproliferative neuroprotective andanti-inflammatory activity Astaxanthin has potential in[1]

the treatment of various diseases such as cancers andhellip

Bioactivity Astragalus polysaccharide are active components of thepolysaccharides extract of Astragulus attenuatesTNF-α-induced insulin resistance by suppressing miR-721 andactivating and in 3T3-L1 adipocytesPPAR-γ PI3KAkt

Bioactivity AVE-8134 is a potent agonist with values of 100PPARα EC50and 3000 nM for human and rodent PPARα receptor respectively

Bioactivity Balaglitazone is a selective partial agonist with anPPARγ of 1351 μM for human EC50 PPARγ

Bioactivity Bezafibrate is an agonist of with s of 50 μM 60PPAR EC50μM 20 μM for and and 90 μMhuman PPARα PPARγ PPARδ55 μM 110 μM for and murine PPARα PPARγ PPARδrespectively Bezafibrate is used as an hypolipidemic agent

4-O-Methyl honokiol Cat No HY-U00450

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Adelmidrol Cat No HY-B1026

Aleglitazar (R1439 RO0728804) Cat No HY-14728

Arhalofenate (MBX 102 JNJ 39659100) Cat No HY-14831

Astaxanthin Cat No HY-B2163

Astragalus polysaccharide (Astragalus Polysacharin) Cat No HY-N0937

AVE-8134 Cat No HY-U00014

Balaglitazone (DRF 2593 NN 2344) Cat No HY-16086

Bezafibrate (BM15075) Cat No HY-B0637

Purity 9877Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data Phase 4Size 10mM x 1mL in DMSO

500 mg 1 g 5 g 10 g

Purity 9959Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9981Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BMS-687453 is a potent and selective agonist with anPPARα and of 10 nM and 260 nM for human and 4100EC50 IC50 PPARα

nM and gt15000 nM for PPARγ in PPAR-GAL4 transactivationassays

Bioactivity CDDO-Im (CDDO-imidazolide) is an activator of and Nrf2 PPARwith s of 232 and 344 nM for PPARα and PPARγKi

Bioactivity Chiglitazar is a dual agonist with of 12PPARαγ EC s50008 17 μM for PPARα PPARγ and PPARδ respectively

Bioactivity Choline Fenofibrate (ABT-335) is the choline salt offenofibric acid under clinical development as a combinationtherapy with rosuvastatin for the management of dyslipidemia

Bioactivity Ciprofibrate is a peroxisome proliferator-activated receptoragonist

Bioactivity Ciprofibrate D6 is deuterium labeled Ciprofibrate which is aperoxisome proliferator-activated receptor agonist

Bioactivity Clofibrate is an agonist of with s of 50 μM 500PPAR EC50μM for murine PPARα and PPARγ and 55 μM 500 μM for humanPPARα and PPARγ respectively

Bioactivity Daidzein is a soy isoflavone which acts as a activatorPPAR

Bioactivity DG172 dihydrochloride is a selective antagonist withPPARβδan of 27 nMIC50

Bioactivity Elafibranor is a agonist with s of 45 and 175PPARαδ EC50nM respectively

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BMS-687453 Cat No HY-10678

CDDO-Im (RTA-403 TP-235 CDDO-Imidazolide) Cat No HY-15725

Chiglitazar Cat No HY-106266

Choline Fenofibrate (ABT-335) Cat No HY-14739

Ciprofibrate (Win35833) Cat No HY-B0664

Ciprofibrate D6 Cat No HY-B0664S

Clofibrate Cat No HY-B0287

Daidzein Cat No HY-N0019

DG172 dihydrochloride Cat No HY-19737A

Elafibranor (GFT505) Cat No HY-16737

wwwMedChemExpresscom 131

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Ertiprotafib is an inhibitor of PTP1B IkB kinase β (IKK-β)and a dual agonist with an of 16 μMPPARα and PPARβ IC50for PTP1B 400 nM for IKK-β an of ~1 μM forEC50PPARαPPARβ

Bioactivity Eupatilin a lipophilic flavonoid isolated from Artemisiaspecies is a agonist and possesses anti-apoptoticPPARαanti-oxidative and anti-inflammatory activities

Bioactivity Fenofibrate is a agonist with an of 30 μMPPARα EC50 Bioactivity Fenofibric acid an active metabolite of fenofibrate is a activitor with s of 224 microM 147 microM and 106 microMPPAR EC50

for PPARα PPARγ and PPARδ respectively Fenofibric acid alsoinhibits enzyme activity with an of 48 nMCOX-2 IC50

Bioactivity FH535 is an inhibitor of and withWntβ-catenin PPARanti-tumor activities

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Fonadelpar is a agonist used in the research ofPPARδneuroparalytic keratopathy

Bioactivity Gemfibrozil is an activator of used as aPPAR-αlipid-lowering drug Gemfibrozil is also a nonselectiveinhibitor of several isoforms with values forP450 KiCYP2C9 2C19 2C8 and 1A2 of 58 24 69 and 82 μMrespectively

Bioactivity Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2Sanchinoside Rh1) is isolated from the root of Panax GinsengGinsenoside Rh1 inhibits the expression of PPAR-γ TNF-α

and IL-6 IL-1β

Bioactivity Glabridin is a natural isoflavan from bindsGlycyrrhiza glabrato and activates with an of 6115 nM GlabridinPPARγ EC50exhibits antioxidant anti-bacterial anti-nephriticanti-diabetic anti-fungal antitumor anti-inflammatoryantiosteoporotic cardiovascular protective neuroprotectivehellip

Ertiprotafib (PTP 112) Cat No HY-19383

Eupatilin Cat No HY-N0783

Fenofibrate Cat No HY-17356

Fenofibric acid (FNF acid) Cat No HY-B0760

FH535 Cat No HY-15721

Fisetin Cat No HY-N0182

Fonadelpar (NPS-005 SJP-0035) Cat No HY-17633

Gemfibrozil (CI-719) Cat No HY-B0258

Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2 Sanchinoside Rh1) Cat No HY-N0604

Glabridin Cat No HY-N0393

Purity 9875Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9727Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9667Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity GSK0660 is a potent antagonist of and withPPARβ PPARδs of 155 nM for both isoformsIC50

Bioactivity GSK376501A is a selective peroxisome proliferator-activatedreceptor gamma ( ) modulator for the treatment of type 2PPARγdiabetes mellitus

Bioactivity GSK3787 is a selective and irreversible peroxisomeproliferator-activated receptor δ ( ) antagonist withPPARδ

of 66pIC50

Bioactivity GW 501516 is a agonist with an of 11 nMPPARδ EC50

Bioactivity GW 6471 is a potent antagonistPPARα Bioactivity GW0742 is a potent and agonist with an ofPPARβ PPARδ IC501 nM for human in binding assay and s of 1 nMPPARδ EC5011 μM and 2 μM for human PPARα and PPARγPPARδrespectively

Bioactivity GW1929 is a potent agonist with a of 884 forPPAR-γ pKihuman and s of 856 and 827 for human PPAR-γ pEC50 PPAR-γ

and murine respectivelyPPAR-γ

Bioactivity GW7647 is a potent agonist with s of 6 nM 11PPARα EC50μM and 62 μM for human PPARα PPARγ and PPARδ respectively

Bioactivity GW9662 is a potent and selective antagonist with anPPARγ of 33 nM showing 10 and 1000-fold selectivity overIC50

PPARα and PPARδ respectively

Bioactivity Icariin is a flavonol glycoside Icariin inhibits andPDE5 activities with s of 432 nM and 7350 μMPDE4 IC50

respectively Icariin also is a activatorPPARα

132 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

GSK0660 Cat No HY-12377

GSK376501A Cat No HY-101746

GSK3787 Cat No HY-15577

GW 501516 (GW 1516 GSK-516) Cat No HY-10838

GW 6471 Cat No HY-15372

GW0742 (GW610742) Cat No HY-13928

GW1929 Cat No HY-15655

GW7647 Cat No HY-13861

GW9662 Cat No HY-16578

Icariin (Ieariline) Cat No HY-N0014

wwwMedChemExpresscom 133

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9889Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9921Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 2Size 5 mg

Purity 9942Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Bioactivity Imiglitazar (TAK559) is a potent and dual human andPPARα agonist with values of 67 and 31 nMPPARγ1 EC50

Bioactivity Indeglitazar is an orally available peroxisomeproliferator-activated receptor ( ) pan-agonist for allPPARthree PPAR subtypes alpha (α) delta (δ) and gamma (γ)

Bioactivity Inolitazone a novel high-affinity agonist that isPPARγdependent upon PPARγ for its biological activity with ofIC5008 nM for growth inhibition

Bioactivity Inolitazone dihydrochloride is a novel high-affinity PPARγagonist that is dependent upon PPARγ for its biologicalactivity with of 08 nM for growth inhibitionIC50

Bioactivity KD3010 is a potent orally active and selective PPARδagonist

Bioactivity L-165041 is a cell permeable agonist with s of 6 nMPPARδ Kiand appr 730 nM for PPARδ and PPARγ respectively and inducesadipocyte differentiation in NIH-PPARδ cells

Bioactivity Lanifibranor is a pan peroxisome proliferator-activated ( ) agonist with s of 15 087 and 021receptor PPAR EC50

μM for human and respectivelyPPARα PPARσ PPARγ

Bioactivity LJ570 is a dual agonist with s of 105PPARα PPARγ EC50

and 012 μM respectively [1]

Bioactivity MA-0204 is a potent highly selective and orally availableperoxisome proliferator activated receptor δ ( )PPARδmodulator with s of 04 nM 79 nM and 10 nM for humanEC50mouse and rat PPARδ respectively Potential treatment hellip

Bioactivity Magnolol a natural lignan isolated from the stem bark of is a dual agonist of both andMagnolia officinalis RXRα

with values of 104 microM and 177 microMPPARγ EC50respectively

Imiglitazar (TAK-559) Cat No HY-101649

Indeglitazar (PPM 204) Cat No HY-14817

Inolitazone (Efatutazone CS-7017 RS5444) Cat No HY-14792

Inolitazone dihydrochloride (Efatutazone (dihydrochloride)

CS-7017 (dihydrochloride) RS5444 (dihydrochloride)) Cat No HY-14792B

KD-3010 Cat No HY-111068

L-165041 Cat No HY-20019

Lanifibranor (IVA337) Cat No HY-104049

LJ570 Cat No HY-111775

MA-0204 Cat No HY-114739

Magnolol Cat No HY-N0163

Purity 9639Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9918Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in Ethanol

10 mg

Purity gt98Clinical DataSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9872Clinical Data Phase 1Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Bioactivity Naringenin is the predominant flavanone in grapefruitdisplays strong anti-inflammatory and antioxidant activities

Bioactivity Naveglitazar racemate is the racemate of NaveglitazarNaveglitazar is a nonthiozolidinedione peroxisomeproliferator-activated receptor ( ) α-γ dual γ-dominantPPARagonist that has shown glucose-lowering potential in animalmodels and in the clinic

Bioactivity NXT629 is a potent selective and competitive PPAR-αantagonist with an of 77 nM for human PPARα shows highIC50selectivity over other nuclear hormone receptor such asPPARδ PPARγ ERβ GR and TRβ s are 60 15 152 3hellipIC50

Bioactivity Oleoylethanolamide is a high affinity endogenous PPAR-αagonist which plays an important role in the treatment ofobesity and arteriosclerosis

Bioactivity Palmitelaidic acid is the trans isomer of palmitoleic acidPalmitoleic acid is one of the most abundant fatty acids inserum and tissue

Bioactivity Peliglitazar racemate is the racemate of PeliglitazarPeliglitazar is a novel dual αγ PPAR activator

Bioactivity Pemafibrate is a highly selective agonist with anPPARα of 1 nMEC50

Bioactivity Pemafibrate racemate is the racemate of pemafibrate andactivates activity with s of 1 nM gt10 μM andPPARα EC5017 μM for h-PPARα h-PPARγ and h-PPARδ respectively

Bioactivity Pioglitazone is a potent and selective agonist withPPARγhigh affinity binding to the PPARγ ligand-binding domain with

of 093 and 099 μM for human and mouse PPARγEC50respectively

Bioactivity Pioglitazone hydrochloride is a potent and selective PPARγagonist with s of 093 and 099 μM for human and mouseEC50PPARγ respectively

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Naringenin Cat No HY-N0100

Naveglitazar racemate Cat No HY-U00036

NXT629 Cat No HY-114263

Oleoylethanolamide (N-(2-Hydroxyethyl)oleamide

N-Oleoyl-2-aminoethanol N-Oleoylethanolamide hellip) Cat No HY-107542

Palmitelaidic Acid (9-trans-Hexadecenoic acid trans-Palmitoleic acid) Cat No HY-N2341

Peliglitazar racemate (BMS 426707-01 racemate) Cat No HY-101738A

Pemafibrate ((R)-K-13675) Cat No HY-17618

Pemafibrate racemate (K13675 (racemate)) Cat No HY-17618A

Pioglitazone (U 72107) Cat No HY-13956

Pioglitazone hydrochloride (U 72107A AD 4833) Cat No HY-14601

wwwMedChemExpresscom 135

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9836Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 250 mg

Bioactivity Pirinixic acid (Wy-14643) is a potent agonist of withPPARαs of 063 μM 32 μM for murine and PPARγ and 50EC50 PPARα

μM 60 μM 35 μM for human PPARγ and PPARδPPARαrespectively

Bioactivity PPAR agonist 1 is an agonist of and usedPPAR α PPAR γfor reducing blood glucose lipid levels lowering cholesteroland reducing body weight

Bioactivity PPARα-MO-1 is a potent modulator extracted from patentPPARαWO2004110982A1 formula I

Bioactivity PPARδ agonist is a agonist extracted from patentPPARδUS20180071304 compound example 10

Bioactivity Pparδ agonist 1 is a agonist with an of 506PPAR-δ EC50nM used in the research of PPAR-delta related diseases suchas mitochondrial diseases muscular diseases vasculardiseases demyelinating diseases and metabolic diseases

Bioactivity Pparδ agonist 2 is a agonist extracted from patent WOPPARδ2016057656 A1

Bioactivity Raspberry ketone is a major aromatic compound of redraspberry widely used as a fragrance in cosmetics and as aflavoring agent in foodstuff also shows agonisticPPAR-αactivity

Bioactivity Retinoic acid is a metabolite of vitamin A that playsimportant roles in cell growth differentiation andorganogenesis Retinoic acid is a natural agonist of RARnuclear receptors with s of 14 nM for RARαβγ RetinhellipIC50

Bioactivity RG-12525 is a a specific competitive and orally effectiveantagonist of the and peptidoleukotrienes LTC4 LTD4 LTE4inhibiting LTC4- LTD4- and LTE4-inducd guinea pig parenchymalstrips contractions with s of 26 nM 25 nM and 7 nMIC50respectively RG-12525 is also a peroxisomehellip

Bioactivity Rosiglitazone (BRL49653) is a selective agonist withPPARγs of 30 nM 100 nM and 60 nM for andEC50 PPARγ1 PPARγ2

respectivelyPPARγ

Pirinixic acid (Wy-14643) Cat No HY-16995

PPAR agonist 1 Cat No HY-U00340

PPARα-MO-1 Cat No HY-U00068

Pparδ agonist Cat No HY-112597

Pparδ agonist 1 Cat No HY-107901

Pparδ agonist 2 Cat No HY-100120

Raspberry ketone (Frambione 4-(4-Hydroxyphenyl)-2-butanone) Cat No HY-N1426

Retinoic acid (ATRA Tretinoin Vitamin A acid all-trans-Retinoic acid) Cat No HY-14649

RG-12525 (NID 525) Cat No HY-101676

Rosiglitazone (BRL49653) Cat No HY-17386

Purity 9953Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9852Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9885Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9803Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9925Clinical Data LaunchedSize 100 mg 500 mg

Bioactivity Rosiglitazone maleate is a potent and selective activator of with s of 30 nM 100 nM and 60 nM for PPARγ EC50 PPARγ1

and respectively and a of appr 40 nMPPARγ2 PPARγ Kdfor Rosiglitazone maleate is also an modulator of PPARγ hellip

Bioactivity Saroglitazar is a novel peroxisome proliferator-activatedreceptor ( ) agonist with predominant PPARα and moderatePPARPPARγ activity with values of 065 pM and 3 nM in HepG2EC50cells respectively

Bioactivity Saroglitazar magnesium is a novel peroxisomeproliferator-activated receptor ( ) agonist withPPARpredominant PPARα and moderate PPARγ activity with EC50values of 065 pM and 3 nM in HepG2 cells respectively

Bioactivity Seladelpar is an orally active potent (50 effectconcentration 2 nM) and specific agonistEC50 PPAR-δ

Bioactivity Seladelpar sodium salt (MBX-8025) is an orally active potentand specific agonist with an of 2 nM showingPPARδ EC50more than 750-fold and 2500-fold selectivity over the PPARαand PPARγ receptors respectively

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

Bioactivity Troglitazone is a agonist with s of 550 nM andPPARγ EC50780 nM for human and murinePPARγ receptor respectively

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Rosiglitazone maleate (BRL 49653C) Cat No HY-14600

Saroglitazar Cat No HY-19937

Saroglitazar Magnesium Cat No HY-19937A

Seladelpar (MBX-8025) Cat No HY-19522

Seladelpar sodium salt (MBX-8025 sodium salt RWJ-800025 sodium salt) Cat No HY-19522A

T0070907 Cat No HY-13202

Troglitazone (CS-045) Cat No HY-50935

wwwMedChemExpresscom 137

RAD51

RAD51 protein family assist in repair of DNA double strand breaksRAD51 family members are homologous to the bacterial RecA andyeast Rad51 In humans RAD51 is a 339-amino acid protein that playsa major role in homologous recombination of DNA during doublestrand break repair RAD51 is involved in the search for homologyand strand pairing stages of the process RAD51 can interact with thessDNA-binding protein RPA BRCA2 PALB2 and RAD52 Recentstudies using fluorescent labeled Rad5 has indicated that Rad51fragments elongate via multiple nucleation events followed bygrowth with the total fragment terminating when it reaches about 2μm in length

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

500 mg

RAD51 Inhibitors amp Modulators

Bioactivity Harmine is a natural dual-specificity tyrosinephosphorylation-regulated kinase ( ) inhibitor with(DYRK)anticancer and anti-inflammatory activities

Bioactivity IBR2 is a specific inhibitorRAD51

Bioactivity RAD51 Inhibitor B02 (B02) is an inhibitor of human withRAD51an of 274 μMIC50

Bioactivity RAD51-IN-2 (compound example 67A) is a inhibitorRAD51extracted from patent WO2019051465A1 [1]

Bioactivity RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM Bioactivity RI-2 is a reversible inhibitor with an of 4417RAD51 IC50μM and specifically inhibits homologous recombination repairin human cells

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

138 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Harmine (Telepathine) Cat No HY-N0737A

IBR2 Cat No HY-103710

RAD51 Inhibitor B02 (B02) Cat No HY-101462

RAD51-IN-2 Cat No HY-111887

RI-1 Cat No HY-15317

RI-2 Cat No HY-16904

RS-1 Cat No HY-19793

T0070907 Cat No HY-13202

wwwMedChemExpresscom 139

ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROK

ROCK (Rho-associated protein kinase) is a kinase belonging to theAGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopusinvertebrates and chicken Human ROCK1 has a molecular mass of158 kDa and is a major downstream effector of the small GTPaseRhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces thekinase activity of ROCKs by an autoinhibitory intramolecular fold ifRhoA-GTP is not present ROCK plays a role in a wide range ofdifferent cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators

of the cytoskeleton

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9954Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

ROCK Inhibitors amp Modulators

Bioactivity AT13148 is an orally active and ATP-competitive multi- AGC inhibitor with s of 38 nM402 nM50 nM 8 nM 3 nMkinase IC50

and 6 nM4 nM for Akt123 p70S6K PKA and ROCKIIIrespectively

Bioactivity Azaindole 1 is an orally active and ATP-competitive ROCKinhibitor with s of 06 and 11nM for human andIC50 ROCK-1

respectivelyROCK-2

Bioactivity BDP5290 is a potent inhibitor of both and withROCK MRCKs of 5 nM 50 nM 10 nM and 100 nM for IC50 ROCK1 ROCK2

and respectivelyMRCKα MRCKβ

Bioactivity Chroman 1 is a highly potent inhibitor with an ofROCK2 IC501 nM

Bioactivity Fasudil (HA-1077 AT877) a potent inhibitor of with aROCK of 033 μM for ROCK1 which is also a potent Ki Ca channel2+

antagonist and vasodilator

Bioactivity Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877Hydrochloride) a potent inhibitor of with a of 033ROCK Ki

μM for ROCK1 which is also a potent antagonistCa channel2+

and vasodilator

Bioactivity GSK180736A is a G protein-coupled receptor kinase 2 ( )GRK2inhibitor with an of 077 μMIC50

Bioactivity GSK269962A is a potent inhibitor with s of 16 and 4ROCK IC50nM for recombinant human and respectivelyROCK1 ROCK2

Bioactivity GSK429286A is a selective inhibitor of with an ROCK1 IC50value of 14 nM

Bioactivity H-1152 is a membrane-permeable and selective inhibitorROCKwith a value of 16 nM and an value of 12 nM forKi IC50

ROCK2

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AT13148 Cat No HY-16071

Azaindole 1 (TC-S 7001) Cat No HY-10319

BDP5290 Cat No HY-12437

Chroman 1 Cat No HY-15392

Fasudil (HA-1077 AT877) Cat No HY-10341A

Fasudil Hydrochloride (HA-1077 (Hydrochloride) AT-877 (Hydrochloride)) Cat No HY-10341

GSK180736A Cat No HY-18990

GSK269962A (GSK 269962) Cat No HY-15556

GSK429286A Cat No HY-11000

H-1152 Cat No HY-15720

wwwMedChemExpresscom 141

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9726Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical DataSize 10 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9929Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9940Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9813Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity H-1152 dihydrochloride is a membrane-permeable and selective inhibitor with a value of 16 nM and an valueROCK Ki IC50

of 12 nM for ROCK2

Bioactivity Hydroxyfasudil is a inhibitor with s of 073 andROCK IC50072 μM for and respectivelyROCK1 ROCK2

Bioactivity Hydroxyfasudil hydrochloride is a inhibitor with sROCK IC50of 073 and 072 μM for and respectivelyROCK1 ROCK2

Bioactivity LX7101 is a potent inhibitor of and with LIMK ROCK2 IC50values of 24 16 and 10 nM for LIMK1 LIMK2 and ROCK2respectively also inhibits with an less than 1 nMPKA IC50

Bioactivity Narciclasine is a plant growth modulator Narciclasinemodulates the RhoRho kinaseLIM kinasecofilin signalingpathway greatly increasing GTPase RhoA activity as well asinducing actin stress fiber formation in a RhoA-dependentmanner

Bioactivity Pentanoic acid a short-chain fatty acid is a product ofbacterial metabolism and are associated with allergic skindisorders Pentanoic acid activates signaling pathwayROCK

Bioactivity Ripasudil (K-115) is a specific inhibitor of with sROCK IC50of 19 and 51 nM for and respectivelyROCK2 ROCK1

Bioactivity Ripasudil free base (K-115 free base) is a specific inhibitorof with s of 19 and 51 nM for and ROCK IC50 ROCK2 ROCK1

respectively

Bioactivity RKI-1447 is a potent small molecule inhibitor of andROCK1 with values of 145 nM and 62 nM respectivelyROCK2 IC50

Bioactivity ROCK inhibitor-2 is a selective dual and ROCK1 ROCK2inhibitor with s of 17 nM and 2 nM respectively IC50

[1]

H-1152 dihydrochloride Cat No HY-15720A

Hydroxyfasudil (HA-1100) Cat No HY-13911

Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100

hydrochloride HA1100 hydrochloride) Cat No HY-13911A

LX7101 Cat No HY-12659

Narciclasine (Lycoricidinol) Cat No HY-16563

Pentanoic acid Cat No HY-N6056

Ripasudil (K-115) Cat No HY-15685

Ripasudil free base (K-115 (free base)) Cat No HY-15685A

RKI-1447 Cat No HY-15755

ROCK inhibitor-2 Cat No HY-119937

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2g

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9843Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Bioactivity ROCK-IN-1 is a potent inhibitor of with an of 12ROCK IC50nM for ROCK2

Bioactivity ROCK2-IN-2 is a selective inhibitor extracted fromROCK2patent US20180093978A1 Compound A-30 has an of lt1IC50μM

Bioactivity SAR407899 is a selective potent and ATP-competitive ROCKinhibitor with an of 135 nM for and s of 36IC50 ROCK-2 KinM and 41 nM for human and rat respectivelyROCK-2

Bioactivity SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an of 135 nM forROCK IC50

and s of 36 nM and 41 nM for human and rat ROCK-2 Ki ROCK-2

respectively

Bioactivity SB-772077B dihydrochloride is an aminofurazan-based Rho inhibitor with s of 56 nM and 6 nM towardkinase( ROCK) IC50

ROCK1 and ROCK2 respevtively [1]

Bioactivity SLx-2119 (KD-025) is a selective inhibitor of with anROCK2 of 105 nMIC50

Bioactivity SR-3677 is a potent and selective inhibitor with anROCK-II of ~3 nMIC50

Bioactivity Thiazovivin is a potent inhibitor which can protectROCKhuman embryonic stem cells

Bioactivity Y-27632 is an ATP-competitive inhibitor of and ROCK-I ROCK-IIwith of 220 nM and 300 nM for and Ki ROCK-I ROCK-II

respectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

Bioactivity Y-27632 dihydrochloride is a cell-permeable ATP-competitiveinhibitor of and with s of 220 and 300 nMROCK-I ROCK-II Kirespectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

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ROCK-IN-1 Cat No HY-U00351

ROCK2-IN-2 Cat No HY-103620

SAR407899 Cat No HY-15687A

SAR407899 hydrochloride Cat No HY-15687

SB-772077B dihydrochloride Cat No HY-108518

SLx-2119 (KD-025) Cat No HY-15307

SR-3677 Cat No HY-13300

Thiazovivin Cat No HY-13257

Y-27632 Cat No HY-10071

Y-27632 dihydrochloride Cat No HY-10583

wwwMedChemExpresscom 143

Purity 9923Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity Y-33075 is a selective inhibitor derived from Y-27632ROCKand is more potent than Y-27632 with an of 36 nMIC50

Bioactivity Y-33075 dihydrochloride is a selective inhibitor with anROCK of 36 nMIC50

Bioactivity ZINC00881524 is a inhibitorROCK

Y-33075 (Y 39983) Cat No HY-10067

Y-33075 dihydrochloride Cat No HY-10069

ZINC00881524 Cat No HY-101244

Sirtuin

Sirtuin (Sir2 proteins) are a class of proteins that possess eithermono-ADP-ribosyltransferase or deacylase activity includingdeacetylase desuccinylase demalonylase demyristoylase anddepalmitoylase activity Sirtuins regulate important biologicalpathways in bacteria archaeaand eukaryotes Sirtuins have beenimplicated in influencing a wide range of cellular processes like agingtranscription apoptosis inflammation and stress resistance as well asenergy efficiency and alertness during low-calorie situations Sirtuinscan also control circadian clocks and mitochondrial biogenesis

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wwwMedChemExpresscom 145

Purity 9891Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9909Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Sirtuin Inhibitors amp Modulators

Bioactivity 3-TYP is a selective inhibitor with an of 16 nMSIRT3 IC50more potent over SIRT1 ( =88 nM) SIRT2 ( =92 nM)IC50 IC50

Bioactivity AGK2 is a selective inhibitor with of 35 μM AGK2SIRT2 IC50can also inhibit and with of 30 and 91 μMSIRT1 SIRT3 IC50respectively

Bioactivity AK-1 is a potent specific and cell-permeable inhibitorSIRT2with an of 125 μMIC50

Bioactivity AK-7 is a selective cell- and brain-permeable inhibitorSIRT2with an of 155 μMIC50

Bioactivity Cambinol is a and inhibitor with values of 56SIRT1 SIRT2 IC50and 59 μM respectively

Bioactivity CAY10602 is a activatorSIRT1

Bioactivity Dihydrocoumarin is a compound found in Melilotus Dihydrocoumarin is a inhibitorofficinalis yeast Sir2p

Dihydrocoumarin also inhibits and withhuman SIRT1 SIRT2s of 208 μM and 295 μM respectively IC50

[1]

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Ginkgolide C is a flavone isolated from leavesGinkgo bilobapossessing multiple biological functions such as decreasingplatelet aggregation and ameliorating Alzheimer disease

Bioactivity Inauhzin is a dual inhibitor and acts as anSirT1IMPDH2activator used in the research of cancerp53

3-TYP Cat No HY-108331

AGK2 Cat No HY-100578

AK-1 Cat No HY-101465

AK-7 Cat No HY-16691

Cambinol Cat No HY-100732

CAY10602 Cat No HY-104073

Dihydrocoumarin (Hydrocoumarin Chroman-2-one) Cat No HY-N1926

Fisetin Cat No HY-N0182

Ginkgolide C (BN-52022 Ginkgolide-C) Cat No HY-N0785

Inauhzin (INZ) Cat No HY-15869

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9876Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity MC3482 is a specific sirtuin5 ( ) inhibitorSIRT5 Bioactivity Nicotinamide is a form of vitamin B3 that plays essentialroles in cell physiology through facilitating NAD+ redoxhomeostasis and providing NAD+ as a substrate to a class ofenzymes that catalyze non-redox reactions Nicotinamide is aninhibitor of SIRT1

Bioactivity OSS_128167 is a selective inhibitor with s of 89SIRT6 IC501578 and 751 μM for and respectivelySIRT6 SIRT1 SIRT2

Bioactivity PROTAC Sirt2 Degrader-1 is a SirReal-based acts as aPROTAC degrader composed of a highly potent andSirt2

isotype-selective inhibitor a linker and a bona fideSirt2cereblon ligand for E3 ubiquitin ligase PROTAC Sirt2Degrader-1 shows an of 025 μM for Sirt2 with no effecthellipIC50

Bioactivity Salermide is an inhibitor of and can cause strongSirt1 Sirt2cancer-specific apoptotic cell death

Bioactivity Selisistat (EX-527) is a potent and selective inhibitorSIRT1with of 98 nMIC50

Bioactivity Selisistat S-enantiomer (EX-527 S-enantiomer) is theS-enantiomer of Selisistat with an of 123 nM for SIRT1IC50Selisistat S-enantiomer is much more potent than SelisistatR-enantiomer

Bioactivity SIRT-IN-1 is a potent inhibitor of with of 15SIRT123 IC s5010 33 μM respectively

Bioactivity SIRT-IN-2 is a potent inhibitor of with of 4SIRT123 IC s504 7 μM respectively

Bioactivity Sirt2-IN-1 (Compound 9) is a ( ) inhibitor withsirtuin 2 Sirt2an of 163 nM IC50

[1]

146 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

MC3482 Cat No HY-112587

Nicotinamide (Niacinamide Nicotinic acid amide Vitamin B3) Cat No HY-B0150

OSS_128167 Cat No HY-107454

PROTAC Sirt2 Degrader-1 Cat No HY-103636

Salermide Cat No HY-101073

Selisistat (EX-527) Cat No HY-15452

Selisistat S-enantiomer (EX-527 (S-enantiomer)) Cat No HY-15452A

SIRT-IN-1 Cat No HY-16615

SIRT-IN-2 Cat No HY-16616

Sirt2-IN-1 Cat No HY-112427

wwwMedChemExpresscom 147

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9939Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9887Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9944Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity SIRT5 inhibitor 1 is a potent Human deacylaseSirtuin 5inhibitor with an of 011 μMIC50

Bioactivity Sirtinol is a inhibitor with s of 48 μM 577 μMsirtuin IC50and 131 μM for ySir2 hSIRT2 and hSIRT2 respectively

Bioactivity Sirtuin modulator 1 is a modulator of a homolog of SIRTl SIRT3with EC of lt 1 μM extracted from patent WO 201007185315A1 Compound No4

Bioactivity SRT 1460 a potent activator with an Sirtuin-1 (SIRT1) EC15value of 29 μM shows good selectivity for activation ofSIRT1 versus SIRT2 and SIRT3 (EC15 gt 300 μM) and is morepotent than Resveratrol and the closest sirtuin homologhellip

Bioactivity SRT 1720 is a selective activator of human with anSIRT1 of 016 μM and shows less potent activities agaiinstEC15

SIRT2 and SIRT3 with EC s of 37 μM and gt 300 μM15respectively

Bioactivity SRT 1720 Hydrochloride is a selective activator of withSIRT1an of 016 μM and shows less potent activities onEC15SIRT2 and SIRT3 with EC s of 37 μM and 300 μM15respectively

Bioactivity SRT 2104 is a first-in-class highly selective andbrain-permeable activator of the NAD dependent deacetylase+

increases Sirt1 protein but shows no effect on Sirt1Sirt1mRNA Used in the research of diabetes mellitus hellip

Bioactivity SRT 2183 is a selective activator with anSirtuin-1 (SIRT1) value of 036 μM SRT 2183 induces growth arrestEC15

[1]

and apoptosis concomitant with deacetylation of STAT3 andNF-κB and reduction of c-Myc protein levels [2]

Bioactivity Tenovin-1 is an inhibitor of and ansirtuin 1 sirtuin 2activator of and may have potential in the management ofp53cancer

Bioactivity Tenovin-6 is an inhibitor of and slightly inhibitsSIRT1 SIRT2 and is also a potent activator of with s ofHDAC8 p53 IC50

21 μM 10 μM and 67 μM for SirT1 SirT2 and SirT3respectively

SIRT5 inhibitor 1 Cat No HY-112634

Sirtinol Cat No HY-13515

Sirtuin modulator 1 Cat No HY-19758A

SRT 1460 Cat No HY-124037

SRT 1720 Cat No HY-10532

SRT 1720 Hydrochloride Cat No HY-15145

SRT 2104 Cat No HY-15262

SRT 2183 Cat No HY-19759

Tenovin-1 Cat No HY-13423

Tenovin-6 Cat No HY-15510

Purity 9855Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Tenovin-6 Hydrochloride is an inhibitor of and SIRT1 SIRT2slightly inhibits and is also a potent activator ofHDAC8

with s of 21 μM 10 μM and 67 μM for SirT1 SirT2p53 IC50and SirT3 respectively

Bioactivity Thiomyristoyl is a potent and specific inhibitor with anSIRT2 of 28 nMIC50

Bioactivity UBCS039 is the first synthetic specific Sirtuin 6 (SIRT6)activator inducing autophagy in human tumor cells with an

of 38 μM EC50[1]

148 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Tenovin-6 Hydrochloride Cat No HY-15510B

Thiomyristoyl Cat No HY-101278

UBCS039 Cat No HY-115453

wwwMedChemExpresscom 149

SRPKSerine-arginine protein kinases

SRPKs is a critical enzyme family that regulates splicing activity in thecell The first serine-arginine (SR) protein kinase identified is SRPK1which is isolated from mitotic cells and it is described tophosphorylate SR proteins and to promote their release from nuclearspeckles during the G2M phase of the cell cycle SRPK1 is theprototype of the SRPK family which also includes the twohomologous SRPK2 and SRPK3 proteins SRPKs are characterized by abipartite catalytic domain separated by a unique spacer sequence andare mainly localized in the cytoplasm of mammalian cellsSRPKs can translocate into the nucleus of cells under severalconditions such as during the G2M phase of the cell cycle or after

osmotic stress or as a consequence of activation of the epidermal growth factor (EGF) signal transduction pathway

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9917Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

SRPK Inhibitors amp Modulators

Bioactivity SPHINX31 is a potent and selective inhibitor of with an ofserinearginine-rich protein kinase 1 (SRPK1) IC50

59 nM SPHINX31 inhibits phosphorylation ofserinearginine-rich splicing factor 1 (SRSF1) SPHINX31 is apotential topical therapeutic for neovascular eye diseasehellip

Bioactivity SRPIN340 is an ATP-competitive serine-arginine-rich proteinkinase ( ) inhibitor with a of 089 μM for SRPK1SRPK Ki

Bioactivity SRPKIN-1 is a covalent and irreversible inhibitorSRPK12with s of 356 and 98 nM respectively Anti-angiogenesisIC50

effect [1]

150 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SPHINX31 Cat No HY-117661

SRPIN340 (SRPK inhibitor) Cat No HY-13949

SRPKIN-1 Cat No HY-116856

wwwMedChemExpresscom 151

Telomerase

Telomerase is a ribonucleoprotein that is an enzyme that adds DNAsequence repeats (TTAGGG in all vertebrates) to the 3 end of DNAstrands in the telomere regions which are found at the ends ofeukaryotic chromosomes This region of repeated nucleotide calledtelomeres contains noncoding DNA and hinders the loss of importantDNA from chromosome ends As a result every time the chromosomeis copied only 100ndash200 nucleotides are lost which causes no damageto the organisms DNA Telomerase is a reverse transcriptase thatcarries its own RNA molecule which is used as a template when itelongates telomeres which are shortened after each replication cycleTelomerase a eukaryotic ribonucleoprotein (RNP) complex contains

both an essential RNA and a protein reverse transcriptase subunit By reverse transcription the telomerase RNPmaintains telomere length stability in almost all cancer cells

Purity 980Clinical Data No Development ReportedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Telomerase Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity BIBR 1532 is a potent selective and non-competitive inhibitor with of 100 nM intelomerase IC50

a cell-free assay

Bioactivity Telomerase-IN-1 is a inhibitor with an ofTelomerase IC50019 μM

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

152 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

BIBR 1532 Cat No HY-17353

Telomerase-IN-1 Cat No HY-U00268

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

wwwMedChemExpresscom 153

TOPKT-LAK cell-originated protein kinase

TOPK (T-lymphokine-activated killer cellndashoriginated protein kinasealso known as PBK or PDZ-binding kinase) is a SerThr protein kinasethat is highly expressed in many types of human cancer includingbreast and lung cancers TOPK is included in the ldquoconsensus stemnessranking signaturerdquo gene list that is up-regulated in cancer stemcell-enriched tumors and is associated with poor prognosis inmultiple types of cancerTOPKPBK is an oncogenic kinase upregulated in most humancancers TOPK is important for mitotic cell division and thatphosphorylation by Cdk1 is needed for its activationTOPK a member of the MEK36-related MAPKK family is expressed in

a wide range of proliferating cells and tissues including cancer cells and testis TOPK negatively regulates the activityof p38α by phosphorylating the p38α-specific phosphatase MKP1 and enhancing the stability of MKP1 The MAPKphosphatase MKP1 an archetypal member of the MKP family plays a pivotal role in the deactivation of p38 through adephosphorylation reaction

Purity 9563Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

TOPK Inhibitors amp Modulators

Bioactivity HI-TOPK-032 is a potent and specific inhibitorTOPK Bioactivity OTS-964 is a potent T-lymphokine-activated killer inhibitor ( =28cell-originated protein kinase (TOPK) IC50

nM) which inhibits TOPK kinase activity with high affinityand selectivity

Bioactivity OTS514 is a highly potent inhibitor which inhibits TOPKTOPKkinase activity with a median inhibitory concentration ( )IC50value of 26 nM

154 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

HI-TOPK-032 Cat No HY-101550

OTS-964 Cat No HY-12467

OTS514 Cat No HY-18621

wwwMedChemExpresscom 155

Topoisomerase

Topoisomerases are enzymes that regulate the overwinding orunderwinding of DNA The winding problem of DNA arises due to theintertwined nature of its double-helical structure Topoisomerases areisomerase enzymes that act on the topology of DNA Type Itopoisomerase cuts one strand of a DNA double helix relaxationoccurs and then the cut strand is reannealed Type I topoisomerasesare subdivided into two subclasses type IA topoisomerases whichshare many structural and mechanistic features with the type IItopoisomerases and type IB topoisomerases which utilize acontrolled rotary mechanism Type II topoisomerase cuts both strandsof one DNA double helix pass another unbroken DNA helix through

it and then reanneal the cut strands This class is also split into two subclasses type IIA and type IIB topoisomeraseswhich possess similar structure and mechanisms

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 1 mg 5 mg

Purity 980Clinical Data LaunchedSize 1 mg 5 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9243Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 9808Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9889Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Topoisomerase Inhibitors amp Modulators

Bioactivity 9-Aminocamptothecin is a inhibitor withtopoisomerase Ipotent anticancer activity

Bioactivity Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) afluorescent molecule and the first described non-peptidicinhibitor showing discrete specificity for the CTRL(chymotrypsin-like) activity of the 20S proteasome [1]

Aclacinomycin A hydrochloride is also a dual inhibitor ofhellip

Bioactivity Aldoxorubicin (INNO-206) is an albumin-binding prodrug ofdoxorubicin which is released from albumin under acidicconditions Aldoxorubicin (INNO-206) has potent antitumoractivities in various cancer cell lines and in murine tumormodels

Bioactivity Amonafide is a inhibitor and DNAtopoisomerase IIintercalator that induces apoptotic signaling by blocking thebinding of Topo II to DNA

Bioactivity Amrubicin (SM-5887) is a DNA inhibitortopoisomerase IIused for the research of cancer

Bioactivity Amrubicin (hydrochloride) (SM-5887 (hydrochloride)) is a DNA inhibitor used for the research of cancertopoisomerase II

Bioactivity Amsacrine (m-AMSA) is an inhibitor of andtopoisomerase IIacts as an antineoplastic agent which can intercalates intothe DNA of tumor cells

Bioactivity Amsacrine hydrochloride (mAMSA hydrochloride) is an inhibitorof and acts as an antineoplastic agenttopoisomerase IIwhich can intercalates into the DNA of tumor cells

Bioactivity Banoxantrone D12 (AQ4N D12) is the deuterium labeledbanoxantrone Banoxantrone is a novel bioreductive agent thatcan be reduced to a stable DNA-affinic compound AQ4 which isa potent inhibitortopoisomerase II

Bioactivity Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) isthe deuterium labeled banoxantrone dihydrochlorideBanoxantrone is a novel bioreductive agent that can be reducedto a stable DNA-affinic compound AQ4 which is a potent

inhibitortopoisomerase II

156 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

9-amino-CPT (9-amino-20(S)-camptothecin) Cat No HY-100309

Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) Cat No HY-N2306A

Aldoxorubicin (INNO-206 DOXO-EMCH) Cat No HY-16261

Amonafide (AS1413) Cat No HY-10982

Amrubicin (SM-5887 AMR) Cat No HY-B0067

Amrubicin hydrochloride (SM-5887 (hydrochloride) AMR (hydrochloride)) Cat No HY-B0067A

Amsacrine (m-AMSA acridinyl anisidide) Cat No HY-13551

Amsacrine hydrochloride (m-AMSA hydrochloride acridinyl anisidide hydrochloride) Cat No HY-13551A

Banoxantrone D12 (AQ4N D12) Cat No HY-13562S

Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) Cat No HY-13562AS

wwwMedChemExpresscom 157

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity 9826Clinical Data Phase 4Size 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9635Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg

Purity 9818Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9880Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg

Bioactivity Banoxantrone dihydrochloride is a novel bioreductive agentthat can be reduced to a stable DNA-affinic compound AQ4which is a potent inhibitortopoisomerase II

Bioactivity Belotecan hydrochloride (CKD-602 hydrochloride) a inhibitor is a synthetic and water-solubleTopoisomerase I

camptothecin derivative

Bioactivity Berberine chloride is an alkaloid isolated from the Chineseherbal medicine Huanglian as an Berberine chlorideantibioticinduces reactive oxygen species ( ) generation andROSinhibits Antineoplastic propertiesDNA topoisomerase

[1]

Bioactivity Berberine chloride hydrate is an alkaloid isolated from theChinese herbal medicine Huanglian as an Berberineantibioticchloride hydrate induces reactive oxygen species ( )ROSgeneration and inhibits AntineoplasticDNA topoisomeraseproperties [1]

Bioactivity Betulinic acid is a natural pentacyclic triterpenoid acts asa eukaryotic inhibitor with an of 5topoisomerase I IC50μM and possesses anti-HIV anti-malarial anti-inflammatoryand anti-tumor properties

Bioactivity Bisantrene is a highly effective antitumor drug targetseukaryotic type II topoisomerases

Bioactivity Campathecin is a potent DNA enzyme topoisomerase Iinhibitor with an of 679 nMIC50

Bioactivity Daun02 is a prodrug of the inhibitortopoisomeraseDaunorubicin

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Banoxantrone dihydrochloride (AQ4N dihydrochloride) Cat No HY-13562A

Belotecan hydrochloride (CKD-602) Cat No HY-13566A

Berberine chloride (Natural Yellow 18 (chloride)) Cat No HY-18258

Berberine chloride hydrate (Natural Yellow 18 (chloride hydrate)) Cat No HY-17577

Betulinic acid (Lupatic acid Betulic acid) Cat No HY-10529

Bisantrene (CL216942) Cat No HY-100875

Campathecin (Camptothecin (S)-(+)-Camptothecin CPT) Cat No HY-16560

Daun02 Cat No HY-13061

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9965Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9888Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9839Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9947Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Doxorubicin is a cytotoxic anthracycline antibiotic for thetreatment of multiple cancers The possible mechanisms bywhich doxorubicin acts in the cancer cell are intercalationinto DNA and disruption of -mediated DNAtopoisomerase-IIrepair

Bioactivity Doxorubicin hydrochloride is a cytotoxic anthracyclineantibiotic for the treatment of multiple cancers The possiblemechanisms by which doxorubicin acts in the cancer cell areintercalation into DNA and disruption of

-mediated DNA repairtopoisomerase-II

Bioactivity Dxd is a potent inhibitor with an ofDNA topoisomerase I IC50031 μM used as a conjugated drug of HER2-targeting ADC(DS-8201a)

Bioactivity Edotecarin is a potent inhibitor of that cantopoisomerase Iinduces single-strand DNA cleavage with of 50 nMIC50

Bioactivity Ellipticine (NSC 71795) is a potent antineoplastic agentinhibits activitiesDNA topoisomerase II

Bioactivity Ellipticine (NSC 71795) hydrochloride is a potentantineoplastic agent inhibits DNA topoisomerase IIactivities

Bioactivity Epirubicin is a semisynthetic L-arabino derivative ofdoxorubicin and an antineoplastic agent by inhibiting

Topoisomerase

Bioactivity Epirubicin (hydrochloride) is a semisynthetic L-arabinoderivative of doxorubicin and an antineoplastic agent byinhibiting Topoisomerase

Bioactivity Etoposide (VP-16 VP-16-213) a chemotherapy medication usedfor the treatments of a number of types of cancer inhibits

by forming a complex with topoisomerase II andDNA synthesisDNA Etoposide arrests cell cycle in G2 and induces apoptoshellip

Bioactivity Exatecan is a water soluble inhibitor withtopoisomerase Ian of 22 μM (0975 μgmL) and can be used in cancerIC50research

158 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Doxorubicin (Hydroxydaunorubicin) Cat No HY-15142A

Doxorubicin hydrochloride (Hydroxydaunorubicin (hydrochloride)) Cat No HY-15142

Dxd (Exatecan derivative for ADC) Cat No HY-13631D

Edotecarin (J 107088 PF 804950) Cat No HY-13618

Ellipticine (NSC 71795) Cat No HY-15753

Ellipticine hydrochloride (NSC 71795 (hydrochloride)) Cat No HY-15753A

Epirubicin Cat No HY-13624

Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride) Cat No HY-13624A

Etoposide (VP-16 VP-16-213) Cat No HY-13629

Exatecan (DX-8951) Cat No HY-13631

wwwMedChemExpresscom 159

Purity 9830Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9803Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9912Clinical Data Phase 3Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg 500 mg

Bioactivity Exatecan Mesylate is a water soluble topoisomerase Iinhibitor with an of 22 μM (0975 μgmL) and can beIC50used in cancer research

Bioactivity Flumequine (R-802) is a quinolone antibiotic and acts as a inhibitor with an of 15 μM (392topoisomerase II IC50

μgmL)

Bioactivity Genz-644282 is a non-camptothecin inhibitortopoisomerase Iused for cancer research

Bioactivity Idarubicin hydrochloride is an anthracycline antileukemicdrug It inhibits the interfering with thetopoisomerase IIreplication of DNA and RNA transcription

Bioactivity Indotecan (LMP-400) is a potent topoisomerase 1(Top1)inhibitor with values of 300 1200 560 nM for P388IC50HCT116 MCF-7 cell lines respectively

Bioactivity Intoplicine is a and inhibitorDNA topoisomerase I II

Bioactivity Irinotecan is a water soluble inhibitortopoisomerase Ipreventing religation of the DNA strand by binding totopoisomerase I-DNA complex

Bioactivity Irinotecan hydrochloride is a water soluble topoisomerase Iinhibitor mainly used to treat colon cancer and rectal cancer

Bioactivity Irinotecan hydrochloride trihydrate is a water soluble inhibitor with antitumor activitytopoisomerase I

Bioactivity Karenitecin (Cositecan) is a inhibitor withtopoisomerase Ipotent anti-cancer activity

Exatecan Mesylate (DX8951f) Cat No HY-13631A

Flumequine (R-802) Cat No HY-B0526

Genz-644282 Cat No HY-16228

Idarubicin hydrochloride (4-Demethoxydaunorubicin hydrochloride) Cat No HY-17381

Indotecan (LMP-400 NSC-724998) Cat No HY-18351

Intoplicine Cat No HY-101647

Irinotecan ((+)-Irinotecan CPT-11) Cat No HY-16562

Irinotecan hydrochloride (CPT-11 hydrochloride Camptothecin 11 hydrochloride) Cat No HY-16562A

Irinotecan hydrochloride trihydrate Cat No HY-16568

Karenitecin (Cositecan BNP 1350) Cat No HY-14812

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9690Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9902Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9702Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg

Bioactivity LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I inhibitor with antitumor activity (Top1) [1]

Bioactivity LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNAintercalator and inhibitor withTopoisomerase I (Top1)antitumor activity [1]

Bioactivity MC-DOXHZN is an albumin-binding prodrug of Doxorubicin withacid-sensitive properties [1]

Bioactivity MC-DOXHZN hydrochloride is an albumin-binding prodrug ofDoxorubicin with acid-sensitive properties [1]

Bioactivity Mitoxantrone is a inhibitor also inhibitstopoisomerase IIprotein kinase C ( ) activity with an of 85 μMPKC IC50

Bioactivity Mitoxantrone dihydrochloride is a topoisomerase IIinhibitor also inhibits protein kinase C ( ) activityPKCwith an of 85 μMIC50

Bioactivity Namitecan is a potent inhibitor withtopoisomerase Iantitumor property

Bioactivity Pirarubicin is an anthracycline antibiotics acts as a inhibitor and is a widely used fortopoisomerase II

treatment of various cancers in particular solid tumors

Bioactivity Pirarubicin Hydrochloride is an anthracycline antibioticsacts as a inhibitor and is a widely usedtopoisomerase IIfor treatment of various cancers in particular solid tumors

Bioactivity Pixantrone is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

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LMP744 (MJ-III65 NSC706744) Cat No HY-U00248

LMP744 hydrochloride (MJ-III65 hydrochloride NSC706744 hydrochloride) Cat No HY-U00248A

MC-DOXHZN (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat No HY-16261A

MC-DOXHZN hydrochloride (Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat No HY-16261B

Mitoxantrone (mitozantrone) Cat No HY-13502

Mitoxantrone dihydrochloride (mitozantrone dihydrochloride) Cat No HY-13502A

Namitecan (ST-1968) Cat No HY-14821

Pirarubicin (THP) Cat No HY-13725

Pirarubicin Hydrochloride (THP Hydrochloride) Cat No HY-13725A

Pixantrone (BBR 2778) Cat No HY-13727

wwwMedChemExpresscom 161

Purity 9920Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 100 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 50 mg 100 mg 200 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9960Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Pixantrone dimaleate is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

Bioactivity Podocarpusflavone A is a DNA topoisomerase I inhibitor havemoderated anti-proliferative activity induce cell apoptosis inMCF-7 is developing anti-tumor drugs target DNAtopoisomerase I In vitro podocarpusflavone-A show significantinhibitions against DLD KB MCF-7 HEp-2 tumor cell lineshellip

Bioactivity SN-38 (NK012) is an active metabolite of the Topoisomerase Iinhibitor Irinotecan SN-38 (NK012) inhibits and DNA RNA

with s of 0077 and 13 μM respectivelysynthesis IC50

Bioactivity SW044248 is a non-canonical inhibitor andtopoisomerase Iselectively toxic for certain non-small cell lung cancer(NSCLC) cell lines

Bioactivity TAS-103 is a dual inhibitor of DNA usedtopoisomerase IIIfor cancer research

Bioactivity TAS-103 dihydrochloride is a dual inhibitor of DNA used for cancer researchtopoisomerase III

Bioactivity Teniposide is a podophyllotoxin derivative acts as a inhibitor and used as a chemotherapeutictopoisomerase II

agent

Bioactivity Top1 inhibitor 1 (compound 28) is a potent human inhibitor with an value of 29topoisomerase I (Top1) IC50

nM [1]

Bioactivity Topotecan (SKF 104864A NSC 609669) is a Topoisomerase Iinhibitor The values of Topotecan at 24 h are 273plusmn025IC50μM of U251 cells 295plusmn023 μM of U87 cells 546plusmn041 μM ofGSCs-U251 and 595plusmn024 μM of GSCs-U87

Bioactivity Topotecan Hydrochloride (SKF 104864A Hydrochloride NSC 609669Hydrochloride) is a inhibitor with potentTopoisomerase Iantineoplastic activities

Pixantrone dimaleate (BBR 2778 dimaleate) Cat No HY-13727A

Podocarpusflavone A Cat No HY-N2198

SN-38 (NK012) Cat No HY-13704

SW044248 Cat No HY-19637

TAS-103 (BMS-247615) Cat No HY-13758

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) Cat No HY-13758A

Teniposide (VM26) Cat No HY-13761

Top1 inhibitor 1 Cat No HY-126142

Topotecan (SKF 104864A NSC 609669) Cat No HY-13768

Topotecan Hydrochloride (SKF 104864A (Hydrochloride) NSC 609669 (Hydrochloride)) Cat No HY-13768A

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Bioactivity Voreloxin is a first-in-class inhibitortopoisomerase IIthat intercalates DNA and induces site-selective DNA DSB G2arrest and apoptosis

Bioactivity Voreloxin Hydrochloride is a first-in-class topoisomerase IIinhibitor that intercalates DNA and induces site-selective DNADSB G2 arrest and apoptosis

Bioactivity β-Lapachone is a naturally occurring O-naphthoquinone acts asa inhibitor and induces apoptosis bytopoisomerase Iinhibiting cell cycle progression

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Voreloxin (SNS-595 Vosaroxin AG 7352) Cat No HY-10534

Voreloxin Hydrochloride (SNS-595 Hydrochloride Vosaroxin

Hydrochloride AG 7352 Hydrochloride) Cat No HY-16518

β-Lapachone (ARQ-501 NSC-26326) Cat No HY-13555

wwwMedChemExpresscom 163

Wee1

Wee1 is a nuclear kinase belonging to the SerThr family of proteinkinases in the fission yeast ( )Schizosaccharomyces pombe S pombeWee1 has amolecular mass of 96 kDa and it is a key regulator of cellcycle progression Wee1 influences cell size by inhibiting the entryinto mitosis through inhibiting Cdk1 Wee1 has homologues in manyother organisms including mammals Wee1 inhibits Cdk1 byphosphorylating it on two different sites Tyr15 and Thr14 Cdk1 iscrucial for the cyclin-dependent passage of the various cell cyclecheckpoints At least three checkpoints exist for which the inhibitionof Cdk1 by Wee1 is important G M checkpoint Cell size checkpoint2DNA damage checkpoint Wee1 is shown to phosphorylate histone

H2B at tyrosine 37 residue which regulates global expression of histones

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Wee1 Inhibitors amp Modulators

Bioactivity Adavosertib (AZD-1775 MK-1775) is a potent inhibitorWee1with an of 52 nMIC50

Bioactivity PD0166285 is a inhibitor and a weak inhibitorWEE1 Myt1with s of 24 and 72 nM respectivelyIC50

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Adavosertib (AZD1775 MK-1775) Cat No HY-10993

PD0166285 Cat No HY-13925

Page 4: Cell Cycle/DNA Damage - MedchemExpress.com · 2019. 7. 2. · G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition,

Antifolate

Antifolates are compounds that antagonise the actions of folic acid(vitamin B9) Folic acids primary function in the body is as a cofactorto various methyltransferases involved in serine methioninethymidine and purine biosynthesis Consequently antifolates inhibitcell division DNARNA synthesis and repair and protein synthesisSome such as Proguanil Pyrimethamine and Trimethoprim selectivelyinhibit folates actions in microbial organisms such as bacteriaprotozoa and fungi The majority of antifolates work by inhibitingdihydrofolate reductase (DHFR) Many are primarily DHFR inhibitorsbut Raltitrexed is an inhibitor of thymidylate synthase andPemetrexed inhibits both and a third enzyme Antifolates act

specifically during DNA and RNA synthesis and thus are cytotoxic during the S-phase of the cell cycle Thus they havea greater toxic effect on rapidly dividing cells

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Purity 9517Clinical Data LaunchedSize 10 mg 50 mg

Purity 9524Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg 1 g 2 g

Purity 9973Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9973Clinical Data LaunchedSize 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Antifolate Inhibitors amp Modulators

Bioactivity Calcium N5-methyltetrahydrofolate(NSC173328) is the calciumsalt of levomefolic acid which has been proposed fortreatment of cardiovascular disease and advanced cancers suchas breast and colorectal cancers

Bioactivity Cycloguanil D6 is the deuterium labeled Cycloguanil which isa dihydrofolate reductase inhibitor

Bioactivity Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanilwhich is a dihydrofolate reductase inhibitor

Bioactivity Diaveridine (EGIS-5645) is a ( )dihydrofolate reductase DHFRinhibitor with a of 115 nM for the wild type DHFR and alsoKian antibacterial agent

Bioactivity EC0489 a conjugate of folic acid and desacetyl vinblastinehydrazide is a high-affinity ligand for the folate receptor(FR) Refractory or metastatic Tumor Small molecule-drug[1]

conjugate (SMDC) [2]

Bioactivity Folinic acid is an adjuvant used in cancer chemotherapyinvolving the drug methotrexate Target Antifolate Folinicacid is a 5-formyl derivative of tetrahydrofolic acid It isreadily converted to other reduced folic acid derivatives(eg tetrahydrofolate) and thus has vitamin activity thathellip

Bioactivity Leucovorin Calcium is a reduced folic acid IC50 Value 30 μMfor zcSHMT and70 μM for zmSHMT [2] Target Antifolate invitro Increasing concentrations of leucovorin (N5-CHO-THF)inhibit both zcSHMT and hcSHMT activities substantially yetto a lesser extent than zmSHMT The IC50 of leucovorin ishellip

Bioactivity Folinic Acid is a reduced folic acid which is used incombination with other chemotherapy drugs Target Folateanalog Approved 2008 Folinic acid (calcium salt pentahydrate)is the calcium salt form of folinic acid which is one of theforms of folate found naturally in foods Folate deficiency ishellip

Bioactivity Levoleucovorin calcium is the calcium salt of Levoleucovorinwhich is the enantiomerically active form of folinic acidIC50 value Target Levoleucovorin is used to treat or preventtoxic effects of methotrexate in people who have receivedmethotrexate to treat bone cancer Levoleucovorin is also usedhellip

Bioactivity Levomefolate is an artificial form of folate IC50 ValueTarget Antifolate The calcium salt ofL-5-methyltetrahydrofolic acid which belongs to the group offolate vitamins (Vitamin B9 Folacin) It is a coenzymatedform of folic acid and a more bioavailable alternative inhellip

Calcium N5-methyltetrahydrofolate (NSC173328) Cat No HY-17557

Cycloguanil D6 (Chlorguanide triazine D6) Cat No HY-12784S

Cycloguanil D6 Nitrate (Chlorguanide triazine D6 Nitrate) Cat No HY-12784S1

Diaveridine (EGIS-5645) Cat No HY-B1902

EC0489 Cat No HY-114306

Folinic acid (leucovorin) Cat No HY-17556

Folinic acid Calcium (Leucovorin Calcium Calcium Folinate) Cat No HY-13664

Folinic acid calcium salt pentahydrate (Leucovorin calcium salt pentahydrate) Cat No HY-B0080

Levoleucovorin Calcium (Calcium levofolinate CL307782) Cat No HY-13667

Levomefolate calcium Cat No HY-17383

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9923Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg

Purity 9977Clinical Data LaunchedSize 10mM x 1mL in Water

50 mg 100 mg 200 mg

Purity 9930Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity LY 254155 an antifolate inhibits and binds tohGARFT with s of 21plusmn02 and 17plusmn01 nM respectivelymFBP Ki

Bioactivity LY309887 is a potent inhibitor of glycinamide ribonucleotideformyltransferase ( ) with a of 65 nM and hasGARFT Kiantitumor activity

Bioactivity Methotrexate is a antagonist with median of 78 nMfolate IC50in assayin vitro

Bioactivity Pemetrexed is a novel the values of theantifolate Kipentaglutamate of LY231514 are 13 72 and 65 nM forinhibits thymidylate synthase ( ) dihydrofolate reductaseTS( ) and glycinamide ribonucleotide formyltransferase (DHFR

) respectivelyGARFT

Bioactivity Pemetrexed disodium is a novel that inhibits theantifolatefolatedependent enzymes thymidylate synthase dihydrofolate

and reductase glycinamide ribonucleotide with s of 13 72 and 65 nMformyltransferase Ki

respectively

Bioactivity Pemetrexed disodium hemipenta hydrate is a novel antifolatethe values of the pentaglutamate of LY231514 are 13 72Kiand 65 nM for inhibits thymidylate synthase ( )TSdihydrofolate reductase ( ) and glycinamideDHFRribonucleotide formyltransferase ( ) respectivelyGARFT

Bioactivity Pralatrexate(Folotyn) is an antifolate and structurally afolate analog Its IC50 is lt 300 nM in some cell linesIC50 Value lt 300 nM Target Antifolate Pralatrexate is anantifolate (a folate analogue metabolic inhibitor) designed toaccumulate preferentially in cancer cells Based onhellip

Bioactivity Pyrimethamine(RP4753) is a medication used for protozoalinfections interferes with tetrahydrofolic acid synthesisfrom folic acid by inhibiting the enzyme dihydrofolatereductase (DHFR) IC50 Value 154 nM (Plasmodium falciparum)[1] Target DHFR antifolate in vitro Three susceptibilityhellip

Bioactivity Trimethoprim is a bacteriostatic antibiotic used mainly in theprophylaxis and treatment of urinary tract infections

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LY 254155 Cat No HY-14523

LY309887 Cat No HY-10818

Methotrexate (Amethopterin CL14377 WR19039) Cat No HY-14519

Pemetrexed (LY231514) Cat No HY-10820

Pemetrexed disodium (LY231514 disodium) Cat No HY-10820A

Pemetrexed disodium hemipenta hydrate (LY231514 (disodium hemipenta hydrate)) Cat No HY-13781

Pralatrexate Cat No HY-10446

Pyrimethamine (Pirimecidan Pirimetamin RP 4753) Cat No HY-18062

Trimethoprim Cat No HY-B0510

wwwMedChemExpresscom 7

APCAnaphase promoting complex

APC (Anaphase-Promoting Complex) is an E3 ubiquitin ligase thatmarks target cell cycle proteins for degradation by the 26Sproteasome The APCC is a large complex of 11ndash13 subunit proteinsincluding a cullin (Apc2) and RING (Apc11) subunit much like SCF TheAPCCs main function is to trigger the transition from metaphase toanaphase by tagging specific proteins for degradation The twoproteins of most importance that get degraded in this process assubstrates of the APCC are securin and S and M cyclins Securinreleases separase a protease after being degraded which in turntriggers the cleavage of cohesin the protein complex that binds sisterchromatids together During metaphase sister chromatids are linked

by intact cohesin complexes When securin undergoes ubiquitination by the APCC and releases separase whichdegrades cohesin sister chromatids become free to move to opposite poles for anaphase The APCC also targets themitotic cyclins for degradation resulting in the inactivation of M-CdK (mitotic cyclin-dependent kinase) complexespromoting exit from mitosis and cytokinesis

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9911Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

APC Inhibitors amp Modulators

Bioactivity TAME is a inhibitor and can be also utilizedserine proteaseas a substrate for the serine proteases trypsin plasmin andthrombin TAME is an inhibitor of[1] [2] [3]

which binds to the hellipanaphase-promoting complex (APC)

Bioactivity TAME hydrochloride is a inhibitor and can beserine proteasealso utilized as a substrate for the serine proteases trypsinplasmin and thrombin TAME hydrochloride is an[1] [2] [3]

inhibitor of which bihellipanaphase-promoting complex (APC)

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TAME Cat No HY-13255

TAME hydrochloride Cat No HY-13255A

wwwMedChemExpresscom 9

ATMATRAtaxia telangiectasia mutatedATM and RAD3 related

ATMATR are members of the PI3 family of serine-threonine kinasesand function as essential links between the sensors and effectors ofthe DNA damage response The roles of ATM and ATR partiallyoverlap and are cooperative however they are also known to playdistinct roles in protecting the cell from DNA damage ATM is mostlyresponsible for sending signals from DSBs (double-strand breaks)induced by ionizing radiation while the closely related ATR respondsto UV damage or stalled replication forks ATM and ATR are known tophosphorylate common as well as specific substrates to activatecheckpoint signaling The G1 S and G2 cell cycle checkpoints areprimarily regulated by the ATM (ataxia telangiectasia mutated) and

ATR (ATM and Rad3-related) protein kinases

Purity 9976Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9904Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9960Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

ATMATR Inhibitors amp Modulators

Bioactivity ATM Inhibitor-1 is a highly potent selective and orallyactive inhibitor with an of 07 nM shows weakATM IC50activity against mTOR (IC 21 μM) DNAPK (IC 28 μM)50 50PI3Kα (IC 38 μM) PI3Kβ (IC 103 μM) PI3Kγ hellip50 50

Bioactivity ATR inhibitor 1 is a inhibitor extracted from patentATRWO2015187451A1 compound I-l has a value below 1 microΜ Ki

[1]

Bioactivity AZ20 is a potent and selective inhibitor of with an ATR IC50of 5 nM and has 8-fold selectivity against (IC =38mTOR 50nM)

Bioactivity AZ32 is an orally bioavailable and blood-brainbarrier-penetrating inhibitor with an of lt62ATM IC50nM for ATM enzyme and an of 031 μM for ATM in cellIC50

Bioactivity AZD0156 is an oral potent and selective inhibitor withATMan of 058 nMIC50

Bioactivity AZD1390 is an inhibitorATM

Bioactivity BAY-1895344 is a potent orally available and selective ATRinhibitor with of 7 nM Anti-tumor activity IC50

[1]Bioactivity BAY-1895344 hydrochloride is a potent orally available and

selective inhibitor with of 7 nM Anti-tumorATR IC50

activity [1]

Bioactivity Berzosertib (VE-822) is an inhibitor with a value ofATR Kiless than 02 nM It also inhibits with a of 34 nMATM Ki

Bioactivity Ceralasertib (AZD6738) is a potent inhibitor of kinaseATRwith an of 1 nMIC50

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ATM Inhibitor-1 Cat No HY-112614

ATR inhibitor 1 Cat No HY-111451

AZ20 Cat No HY-15557

AZ32 Cat No HY-112305

AZD0156 Cat No HY-100016

AZD1390 Cat No HY-109566

BAY-1895344 Cat No HY-101566

BAY-1895344 hydrochloride Cat No HY-101566A

Berzosertib (VE-822 VX-970) Cat No HY-13902

Ceralasertib (AZD6738) Cat No HY-19323

wwwMedChemExpresscom 11

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9947Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9988Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9840Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity CGK733 is a potent inhibitor used for the researchATMATRof cancer

Bioactivity CP-466722 is a rapidly reversible inhibitor of with anATM of 41 μM and has no effects on PI3K or closely relatedIC50

PI3K-like protein kinase (PIKK) family members

Bioactivity ETP-46464 is an effective and inhibitor withmTOR ATRs of 06 and 14 nM respectivelyIC50

Bioactivity KU 59403 is a potent inhibitor with an of 3 nMATM IC50

Bioactivity KU-55933 is a potent inhibitor with an and ofATM IC50 Ki129 and 22 nM respectively and is highly selective for ATMas compared to DNA-PK PI3KPI4K ATR and mTOR

Bioactivity KU-60019 is an improved kinase-specific inhibitor withATM of 63 nMIC50

Bioactivity VE-821 is a potent ATP-competitive inhibitor of with ATR Ki of 13 nM26 nMIC50

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

CGK733 Cat No HY-15520

CP-466722 Cat No HY-11002

ETP-46464 Cat No HY-15521

KU 59403 Cat No HY-18650

KU-55933 Cat No HY-12016

KU-60019 Cat No HY-12061

VE-821 Cat No HY-14731

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

Aurora Kinase

Aurora kinases are serinethreonine kinases that are essential for cellproliferation Aurora kinase helps the dividing cell dispense its geneticmaterials to its daughter cells More specifically Aurora kinases play acrucial role in cellular division by controlling chromatid segregationDefects in this segregation can cause genetic instability a conditionwhich is highly associated with tumorigenesis Three Aurora kinaseshave been identified in mammalian cells to date Aurora A Aurora BAurora C Besides being implicated as mitotic regulators these threekinases have generated significant interest in the cancer research fielddue to their elevated expression profiles in many human cancers Thehuman Aurora kinases present a similar domain organization with a

N-terminal domain of 39 to 129 residues in length a protein kinase domain and a short C-terminal domain containing15 to 20 residues The N-terminal domain of three proteins share low sequence conservation which determinesselectivity during protein-protein interactions

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Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9895Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9874Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Aurora Kinase Inhibitors amp Modulators

Bioactivity Alisertib (MLN 8237) is an oral active and selective Aurora A inhibitor with an of 12 nMkinase IC50

Bioactivity AMG 900 is a potent and highly selective kinasespan-Aurorainhibitor with of 5 nM 4 nM and 1 nM for IC50 Aurora A B

and respectivelyC

Bioactivity AT9283 is a multitargeted kinase inhibitor which potentlyinhibits ( =12 nM 11 nM)aurora kinase AB JAK23 IC50

Bioactivity Aurora A inhibitor I is a potent and highly selective Aurora inhibitor with with an of 34 nMA IC50

Bioactivity Aurora B inhibitor 1 is an (Aurora-1) inhibitorAurora Bextracted from patent WO2007059299A1 compound 1-3 has a Kivalue of lt0010 uM

Bioactivity Aurora inhibitor 1 is a potent inhibitor with an Aurora IC50of le 4 nM and le13 nM for and kinaseAurora A Aurora Brespectively [1]

Bioactivity AZD1152 is a pro-drug of Barasertib-hQPA which is a highlyselective inhibitor with of 037 nM in aAurora B IC50cell-free assay

Bioactivity AZD1152-HQPA is a highly selective Aurora inhibitor with an of 037 nM in aB IC50

cell-free assay and shows 3700-fold selectivity for Aurora Bover Aurora A

Bioactivity BI-847325 is an ATP competitive dual inhibitor of andMEKaurora kinases ( ) with values of 4 and 15 nM forAK IC50human MEK2 and AK-C respectively

Bioactivity CCT 137690 is a potent and orally available kinaseaurorainhibitor with s of 15 25 and 19 nM for aurora A B andIC50C respectively

Alisertib (MLN 8237) Cat No HY-10971

AMG 900 Cat No HY-13253

AT9283 Cat No HY-50514

Aurora A inhibitor I Cat No HY-70061

Aurora B inhibitor 1 Cat No HY-U00304

Aurora inhibitor 1 Cat No HY-111506

AZD1152 (Barasertib) Cat No HY-10127

Barasertib-HQPA (AZD2811 INH-34 AZD1152-HQPA) Cat No HY-10126

BI-847325 Cat No HY-18955

CCT 137690 Cat No HY-10804

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 1 mg 5 mg 10 mg 20 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9859Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9923Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9944Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data Phase 1Size 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 950Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity CCT129202 is an kinase inhibitor with s of 42aurora IC50198 and 227 nM for aurora A B and C respectively

Bioactivity CCT241736 is a potent and orally bioavailable dual andFLT3 inhibitor which inhibits Aurora kinasesAurora kinase

(Aurora-A 75 nM 38 nM Aurora-B 48 nM)Kd IC50 KdFLT3 kinase ( 62 nM) and FLT3 mutants includhellipKd

Bioactivity CYC-116 is a potent and inhibitor withaurora A aurora Bs of 8 and 9 nM respectivelyKi

Bioactivity Danusertib is a pyrrolo-pyrazole and inhibitoraurora kinasewith of 13 79 and 61 nM for Aurora A B and CIC50respectively

Bioactivity ENMD-2076 is a multi-targeted kinase inhibitor with s ofIC50186 14 582 159 927 708 564 nM for Aurora A Flt3

KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src PDGFRαrespectively

Bioactivity ENMD-2076 Tartrate is a multi-targeted kinase inhibitor withs of 186 14 582 159 927 708 564 nM for IC50 Aurora

A Flt3 KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src respectivelyPDGFRα

Bioactivity GSK-1070916 is a potent and selective ATP-competitiveinhibitor of and with s of 038 andaurora B aurora C Ki15 nM respectively and is gt250- fold selective overAurora A

Bioactivity Hesperadin is an ATP-competitive inhibitor of aurora Bkinase with an of 250 nMIC50

Bioactivity Ilorasertib (ABT-348) is an ATP-competitive multitargetedkinase inhibitor with s for inhibiting binding Aurora B (7IC50nM) C (1 nM) and A (120 nM) and also inhibits RET tyrosinekinase PDGFRβ and Flt1 with s of 7 nM 3 nM and 32 nMIC50

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

14 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CCT129202 Cat No HY-12049

CCT241736 Cat No HY-18161

CYC-116 Cat No HY-10558

Danusertib (PHA-739358) Cat No HY-10179

ENMD-2076 Cat No HY-10987A

ENMD-2076 Tartrate Cat No HY-10987

GSK-1070916 (GSK-1070916A) Cat No HY-70044

Hesperadin Cat No HY-12054

Ilorasertib (ABT-348) Cat No HY-16018

JNJ-7706621 Cat No HY-10329

wwwMedChemExpresscom 15

Purity 9820Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9928Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9911Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity KW-2449 is a multi-targeted kinase inhibitor of FLT3 ABL and with s of 66 14 4 and 48 nMABLT315I Aurora kinase IC50

respectively

Bioactivity LY3295668 is a potent orally active and highly specific inhibitor with values of 08 nM and 1038Aurora-A kinase Ki

nM for AurA and AurB respectively

Bioactivity MK-5108 is a highly potent and specific inhibitor of Aurora A with an value of 0064 nMkinase IC50

Bioactivity MK-8745 is an kinase inhibitor with an of 06aurora A IC50nM

Bioactivity MLN8054 is a potent selective and orally available aurora Akinase inhibitor with an of 4 nMIC50

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity PF-03814735 is a potent orally available and reversible and inhibitor with s of 08 and 05aurora A aurora B IC50

nM respectively

Bioactivity PHA-680632 is an kinase inhibitor with s of 27aurora IC50135 and 120 nM for aurora A B and C respectively

Bioactivity Reversine is a novel class of ATP-competitive Aurora kinaseinhibitor with s of 400 500 and 400 nM for IC50 Aurora A

and respectivelyAurora B Aurora C

Bioactivity SCH-1473759 is an inhibitor with s of 4 and 13 nMaurora IC50for aurora A and B respectively

KW-2449 Cat No HY-10339

LY3295668 (AK-01) Cat No HY-114258

MK-5108 (VX-689) Cat No HY-13252

MK-8745 Cat No HY-13819

MLN8054 Cat No HY-10180

NU6140 Cat No HY-107419

PF-03814735 Cat No HY-14574

PHA-680632 Cat No HY-10178

Reversine Cat No HY-14711

SCH-1473759 Cat No HY-10482

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg

Purity 9980Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity SCH-1473759 hydrochloride is an inhibitor with saurora IC50of 4 and 13 nM for aurora A and B respectively

Bioactivity SNS-314 is a potent and selective kinase inhibitoraurorawith s of 9 31 and 6 nM for aurora A B and CIC50respectively

Bioactivity TAK-632 is a potent inhibitor with of 14 24pan-RAF IC50

and 83 nM for respectivelyCRAF BRAFV600E BRAFWT

Bioactivity TAK-901 is a multi-targeted inhibitor with s of 21aurora IC50and 15 nM for aurora A and B respectively

Bioactivity Tozasertib (VX 680 MK-0457) is an inhibitor of Aurora ABC with s of 06 18 46 nM respectivelykinases Ki

Bioactivity XL228 is a multi-targeted tyrosine kinase inhibitor with sIC50of 5 31 16 61 2 nM for Bcr-Abl Aurora A IGF-1R Srcand respectivelyLyn

Bioactivity ZM-447439 is an kinase inhibitor with s of 110 andaurora IC50130 nM for aurora A and B respectively

16 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SCH-1473759 hydrochloride Cat No HY-10483

SNS-314 (SNS-314 Mesylate) Cat No HY-12003

TAK-632 Cat No HY-15767

TAK-901 Cat No HY-12201

Tozasertib (VX 680 MK-0457) Cat No HY-10161

XL228 Cat No HY-15749

ZM-447439 Cat No HY-10128

wwwMedChemExpresscom 17

Casein Kinase

Casein Kinases (CKs) are serinethreonine-selective enzymes thatfunction as regulators of signal transduction pathways in mosteukaryotic cell types

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9992Clinical Data Phase 2Size 1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Casein Kinase Inhibitors amp Modulators

Bioactivity Casein Kinase II Inhibitor IV is a small-molecule inducer ofepidermal keratinocyte differentiation

Bioactivity Casein Kinase II Inhibitor IV Hydrochloride is asmall-molecule inducer of epidermal keratinocytedifferentiation

Bioactivity CK1-IN-1 is a inhibitor extracted fromcasein kinase 1 (CK1)patent WO2015119579A1 compound 1c has s of 15 nM 16 nMIC50

73 nM for CK1δ and CK1ε p38σ MAPK respectively [1]

Bioactivity D4476 is a potent selective and cell-permeable inhibitor ofcasein kinase 1( ) with an value of 03 μM CK1 IC50 in vitro

Bioactivity DMAT is a potent and specific inhibitor with an CK2 IC50value of 130 nM

Bioactivity Ellagic acid is a natural antioxidant and acts as a potentand ATP-competitive inhibitor with an of 40 nM andCK2 IC50a of 20 nMKi

Bioactivity Emodin is a broad-spectrum anticancer agent Emodin inhibits II (CKII) activity with of 2 μMcasein kinase IC50

Bioactivity IC261 is a selective ATP-competitive inhibitor withCK1s of 1 μM 1 μM 16 μM for and Ckiα1IC50 Ckiδ Ckiε

respectively

Bioactivity LH846 is a selective inhibitor of with an of 290 nMCKIδ IC50and less potently inhibits CKIα and CKIε with s of 25 μMIC50and 13 μM respectively

Bioactivity Longdaysin is a and CK1α CK1δ extracellular inhibitor with s of  56signal-regulated kinase 2 (ERK2) IC50

microM 88 microM and 52 microM respectively [1] [2]

18 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Casein Kinase II Inhibitor IV Cat No HY-111378

Casein Kinase II Inhibitor IV Hydrochloride Cat No HY-111378A

CK1-IN-1 Cat No HY-111820

D4476 (Casein Kinase I Inhibitor) Cat No HY-10324

DMAT (Casein kinase II Inhibitor CK2 Inhibitor) Cat No HY-15535

Ellagic acid Cat No HY-B0183

Emodin (Frangula emodin) Cat No HY-14393

IC261 Cat No HY-12774

LH846 Cat No HY-15704

Longdaysin Cat No HY-18285

wwwMedChemExpresscom 19

Purity 9701Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9827Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Bioactivity NCC007 is a dual and inhibitorcasein kinase Iα (CKIα) δ (CKIδ)with s of 18 and 36 μM respectively and can be used inIC50

research of modulating mammalian circadian rhythms [1]

Bioactivity PF-4800567 is a potent and selective inhibitor of caseinkinase 1ϵ ( ) with an of 32 nM which is greaterCK1ϵ IC50than 20-fold selectivity over CK1δ ( 711 nM)IC50

Bioactivity PF-670462 is a potent and selective inhibitor of casein kinase with s of 77 nM and 14 nM( and )CK1ε CK1δ IC50

respectively

Bioactivity Silmitasertib (CX-4945) is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity Silmitasertib sodium salt is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity SR-3029 is a potent and ATP competitive and CK1δ CK1εinhibitor with s of 44 nM and 260 nM respectively andIC50

s of 97 nM for both kinasesKi

Bioactivity TA-01 is a potent and inhibitor with sCK1 p38 MAPK IC50of 64 nM 68 nM 67 nM for CK1ε CK1δ and p38 MAPKrespectively

Bioactivity TBB is a cell-permeable and ATP-competitive inhibitorCK2with an of 015 μM for rat liver CK2IC50

Bioactivity TTP 22 is a potent inhibitor with an of 100 nM andCK2 IC50a of 40 nMKi

NCC007 Cat No HY-128677

PF-4800567 Cat No HY-12470

PF-670462 Cat No HY-15490

Silmitasertib (CX-4945) Cat No HY-50855

Silmitasertib sodium salt (CX-4945 (sodium salt)) Cat No HY-50855B

SR-3029 Cat No HY-100011

TA-01 Cat No HY-100114

TBB (NSC 231634 Casein Kinase II Inhibitor I) Cat No HY-14394

TTP 22 Cat No HY-15479

CDKCyclin dependent kinase

CDKs (Cyclin-dependent kinases) are serine-threonine kinases firstdiscovered for their role in regulating the cell cycle They are alsoinvolved in regulating transcription mRNA processing and thedifferentiation of nerve cells CDKs are relatively small proteins withmolecular weights ranging from 34 to 40 kDa and contain little morethan the kinase domain In fact yeast cells can proliferate normallywhen their CDK gene has been replaced with the homologous humangene By definition a CDK binds a regulatory protein called a cyclinWithout cyclin CDK has little kinase activity only the cyclin-CDKcomplex is an active kinaseThere are around 20 Cyclin-dependent kinases (CDK1-20) known till

date CDK1 4 and 5 are involved in cell cycle and CDK 7 8 9 and 11 are associated with transcriptionCDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational Mostknowledge of CDK structure and function is based on CDKs of (Cdc2) (CDC28) and vertebratesS pombe S cerevisia(CDC2 and CDK2) The four major mechanisms of CDK regulation are cyclin binding CAK phosphorylation regulatoryinhibitory phosphorylation and binding of CDK inhibitory subunits (CKIs)

20 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 21

Purity 9815Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9969Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9973Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

CDK Inhibitors amp Modulators

Bioactivity (+)-BAY-1251152 is a inhibitor extracted from patent WOCDK92014076091 A1 example 1

Bioactivity (-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation(-) BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity (plusmn)-BAY-1251152 is a racemic mixture of BAY-1251152BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity 5-Iodo-indirubin-3-monoxime is a potent GSK-3β CDK5P25and inhibitor competing with ATP for binding toCDK1cyclin Bthe catalytic site of the kinase with s of 9 20 and 25IC50

nM respectively [1]

Bioactivity Abemaciclib (LY2835219) is a selective inhibitor withCDK46 values of 2 nM and 10 nM for CDK4 and CDK6 respectivelyIC50

Bioactivity Abemaciclib Metabolites M2 is a metabolite of abemaciclibacts as a potent and inhibitor with s in theCDK4 CDK6 IC50

range of 1-3 nM Anti-cancer activity [1]

Bioactivity Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is aselective inhibitor with s of 2 nM and 10 nM forCDK46 IC50CDK4 and CDK6 respectively

Bioactivity AMG 925 is a potent selective and orally available FLT3 dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMCDK4 IC50

respectively

Bioactivity AMG 925 HCl is a potent selective and orally available dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMFLT3 CDK4 IC50

respectively

Bioactivity AT7519 as a potent inhibitor of with s of 210 47CDKs IC50100 13 170 and lt10 nM for CDK1 CDK2 CDK4 to CDK6 andCDK9 respectively

(+)-BAY-1251152 Cat No HY-103019

(-)-BAY-1251152 Cat No HY-103019B

(plusmn)-BAY-1251152 Cat No HY-103019A

5-Iodo-indirubin-3-monoxime Cat No HY-111930

Abemaciclib (LY2835219) Cat No HY-16297A

Abemaciclib Metabolites M2 Cat No HY-128669

Abemaciclib methanesulfonate (LY2835219 (methanesulfonate)) Cat No HY-16297

AMG 925 Cat No HY-15889

AMG 925 HCl Cat No HY-15889A

AT7519 Cat No HY-50940

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 1Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9999Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9700Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9848Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9816Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity AT7519 Hydrochloride is a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity AT7519 trifluoroacetate as a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity Atuveciclib (BAY-1143572) is a potent and highly selectiveoral inhibitor Atuveciclib (BAY-1143572)PTEFb CDK9inhibits with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib Racemate (BAY-1143572 Racemate) is the racematemixture of Atuveciclib Atuveciclib is a potent and highlyselective oral inhibitor which supressesP-TEFb CDK9

with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is apotent and selective inhibitor which inhibits CDK9 CDK9

with an of 16 nMCycT1 IC50

Bioactivity AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 82nM AUZ 454 (K03861) inhibits CDK2 activity by competing withbinding of activating cyclins

Bioactivity AZD-5438 is a potent inhibitor of with of 16CDK129 IC50nM6 nM20 nM in cell-free assays AZD-5438 shows lessinhibition activity against GSK3β CDK5 and CDK6

Bioactivity AZD4573 is a inhibitor with an of lt3 nMCDK9 IC50extracted from patent US 20160376287 A1 example 14

Bioactivity BGG463 is a inhibitorCDK2 Bioactivity BI-1347 is a potent inhibitor extracted from patentCDK8WO2017202719A1 product I-003 has an of 11 nM IC50

[1]

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AT7519 Hydrochloride Cat No HY-50943

AT7519 trifluoroacetate Cat No HY-50940A

Atuveciclib (BAY-1143572) Cat No HY-12871B

Atuveciclib Racemate (BAY-1143572 Racemate) Cat No HY-12871

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) Cat No HY-12871C

AUZ 454 (K03861) Cat No HY-15004

AZD-5438 Cat No HY-10012

AZD4573 Cat No HY-112088

BGG463 Cat No HY-100600

BI-1347 Cat No HY-120350

wwwMedChemExpresscom 23

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9754Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9747Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity BMS-265246 is a potent and selective CDK12 inhibitor forCDK1cyclin B and CDK2cyclin E with IC50 of 6 nM and 9 nMrespectively

Bioactivity BS-181 is a highly selective inhibitor with an ofCDK7 IC5021 nM showing 40-fold selective over CDK1 2 4 5 6 or 9

Bioactivity BS-181 hydrochloride is a highly selective inhibitorCDK7with of 21 nM and gt 40-fold selective for CDK7 thanIC50CDK1 2 4 5 6 or 9

Bioactivity BSJ-03-123 is a potent and novel -selective small-moleculeCDK6degrader

Bioactivity Ca channel agonist 1 is an agonist of 2+ N-type Ca channel2+

and an inhibitor of with s of 1423 μM and 334Cdk2 EC50μM respectively and is used as a potential treatment formotor nerve terminal dysfunction

Bioactivity CC-671 is a dual ( )TTK protein kinase CDC2-like kinase CLK2inhibitor with s of 0005 and 0006 μM for TTK and CLK2IC50respectively

Bioactivity CCT-251921 is a potent selective and orally bioavailable inhibitor with an of 23 nMCDK8 IC50

Bioactivity CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 oflt8 nM extracted from reference 1 example 4 IC50 Valuelt8 nM [1] Target CDK9 In vitro In vivo

Bioactivity CDK46-IN-2 is a potent and inhibitor extractedCDK4 CDK6from patent US20180000819A1 Compound 1 has s of 27 andIC50

16 nM for CDK4 and CDK6 respectively [1]

Bioactivity CDK461 Inhibitor is a inhibitor with s of 3 andCDK46 IC501 nM respectively

BMS-265246 Cat No HY-15275

BS-181 Cat No HY-13266

BS-181 hydrochloride Cat No HY-13266A

BSJ-03-123 Cat No HY-111556

Ca2+ channel agonist 1 Cat No HY-41076

CC-671 Cat No HY-108709

CCT-251921 Cat No HY-19984

CDK-IN-2 (CDK inhibitor II) Cat No HY-13033

CDK46-IN-2 Cat No HY-114339

CDK461 Inhibitor Cat No HY-112280

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9548Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CDK8-IN-1 is a potent and selective inhibitor with anCDK8 of 3 nMIC50

Bioactivity CDK8-IN-3 is an inhibitor of extracted from patentCDK8WO2016041618A1 compound example 17

Bioactivity CDK8-IN-4 is an inhibitor of extracted from patentCDK8WO2014090692A1 compound example 16 with an of 02 nMIC50

Bioactivity CDK819-IN-1 is a potent selective and oral bioavailable dual inhibitor with s of 046 nM 099 nM andCDK819 IC50

270 nM for CDK8 CDK19 and CDK9 respectively

Bioactivity CDK9 Antagonist-1 (compounds 11c) is a potent and selective degrader based on PROTAC with an of 17 μM in MCF-7CDK9 IC50

cell lines Natural product Wogonin binds ubiquitin E3 ligasecereblon (CRBN) via a linker to form PROTAC [1]

Bioactivity CDK9-IN-1 is a novel selective inhibitor for theCDK9treatment of HIV infection with an of 39 nM forIC50CDK9CycT1 extracted from reference compound 87

Bioactivity CDK9-IN-2 is a special cyclin-dependent kinase 9 ( )CDK9inhibitor extracted from patent WO2012131594A1 compoundCDKI(8) has an of 5 nM and 7 nM in H929 multipleIC50myeloma(MM) cell line (72 hours) and A2058 skin cell line (72hours) respectively

Bioactivity CDK9-IN-8 is a highly effective and selective inhibitorCDK9with an of 12 nMIC50

Bioactivity CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM showsselective toxicity to CLL cells(LD50=80 nM) versus normal Bcell and normal CD34+ cell(LD50gt20 uM) IC50 value 4 nM80nM(KiLD50) [1] Target CDK9 inhibitor in vitro CDKI-73 wascytotoxic to all of the CLL samples tested (n = 38) with ahellip

Bioactivity CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 () inhibitor with an IC of 2 nMCLK1 50

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CDK8-IN-1 Cat No HY-103492

CDK8-IN-3 Cat No HY-111463

CDK8-IN-4 Cat No HY-111465

CDK819-IN-1 Cat No HY-111427

CDK9 Antagonist-1 Cat No HY-112811

CDK9-IN-1 Cat No HY-13231

CDK9-IN-2 Cat No HY-16462

CDK9-IN-8 Cat No HY-102039

CDKI-73 Cat No HY-12445

CLK1-IN-1 Cat No HY-103082

wwwMedChemExpresscom 25

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9900Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9973Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9998Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CMPD 7 is a potent and selective inhibitor with an CDK12 IC50of 491 nM in enzymatic assay

Bioactivity CT7001 hydrochloride is a selective inhibitor withCDK7s of 41 nM and 578 nM for andIC50 CDK7CycHMAT1

respectivelyCDK2cycE1

Bioactivity Cucurbitacin E is a natural compound which from the climbingstem of Cucurbitacin E significantlyCucumic melo Lsuppresses the activity of the complexcyclin B1 CDC2

Bioactivity CVT-313 is a potent selective reversible andATP-competitive inhibitor of with of 05 μMCDK2 IC50

Bioactivity CYC065 is a second-generation orally availableATP-competitive inhibitor of kinasesCDK2 CDK 9

Bioactivity Dinaciclib is a potent inhibitor of with s of 1 1CDK IC503 and 4 nM for and respectivelyCDK2 CDK5 CDK1 CDK9

Bioactivity EHT 5372 is a strong inhibitor of family kinases withDYRKrsquos of 022 028 nM for DYRK1A and DYRK1B respectivelyIC s50

Bioactivity Flavopiridol is a broad spectrum and competitive inhibitor of inhibiting CDK1 CDK2 CDK4 with s of 30 170 100CDKs IC50

nM respectively

Bioactivity Flavopiridol Hydrochloride is a broad inhibitor of CDKcompeting with ATP to inhibit CDKs including CDK1 CDK2 CDK4with s of 30 170 100 nM respectivelyIC50

Bioactivity FMF-04-159-2 is a covalent inhibitor FMF-04-159-2CDK14inhibits CDK14 and CDK2 with s of 396 nM and 256 nM inIC50

NanoBRET assay respectively [1]

CMPD 7 Cat No HY-112261

CT7001 hydrochloride (ICEC0942 hydrochloride) Cat No HY-103712A

Cucurbitacin E (α-Elaterin α-Elaterine) Cat No HY-N0417

CVT-313 (Cdk2 Inhibitor III) Cat No HY-15339

CYC065 Cat No HY-101212

Dinaciclib (SCH 727965) Cat No HY-10492

EHT 5372 Cat No HY-111380

Flavopiridol (L868275 HMR-1275 Alvocidib) Cat No HY-10005

Flavopiridol Hydrochloride (HL 275 NSC 649890 MDL 107826A

FLAVOPIRIDOL HCL Alvocidib Hydrochloride) Cat No HY-10006

FMF-04-159-2 Cat No HY-127104

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9204Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 251 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9841Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity FN-1501 is a potent inhibitor of and with s ofFLT3 CDK IC50247 085 196 and 028 nM for CDK2cyclin A CDK4cyclinD1 CDK6cyclin D1 and FLT3 respectively FN-1501 hasanticancer activity

Bioactivity GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO) is apotent selective reversible and ATP-competitive inhibitor of

and complex with s of 5 nM320GSK-3αβ CDK1-cyclinB IC50nM80nM for (GSK-3αβ)CDK1CDK5 respectively

Bioactivity GSK3186899 is an inhibitor of cdc-2-related kinase 12 () with an of 14 μM for in anCRK12 EC50 L donovani

intra-macrophage assay

Bioactivity IIIM-290 is a potent and oral inhibitor with s of 90CDK IC50and 94 nM for CDK2A and CDK9T1

Bioactivity Indirubin-3-monoxime-5-sulphonic acid is a potent andselective inhibitor of and with s ofCDK1 CDK5 GSK-3β IC50

5 nM 7 nM and 80 nM respectively [1]

Bioactivity Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK)inhibitor with values of 55 nM 35 nM 150 nM 300 nMIC50and 65 nM for CDK1cyclin B CDK2cyclin A CDK2cyclin ECDK4cyclin D1 and CDK5p35 respectively [1]

Bioactivity JH-XI-10-02 is a potent and selective degrader of withCDK8an of 159 nM based on JH-XI-10-02 causesIC50 PROTAC

proteasomal degradation does not affect CDK8 mRNA levelsJH-XI-10-02 shows no effect on CDK19 [1]

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

Bioactivity JSH-150 is a highly selective and potent inhibitor withCDK9an IC of 1 nM50

Bioactivity Kenpaullone is a potent inhibitor of andCDK1cyclin B with s of 04 μM and 23 nM and also inhibitsGSK-3β IC50

CDK2cyclin A CDK2cyclin E and CDK5p25 with s of 068IC50μM 75 μM 085 μM respectively

26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

FN-1501 Cat No HY-111361

GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO MLS 2052) Cat No HY-10580

GSK3186899 (DDD-853651) Cat No HY-112622

IIIM-290 Cat No HY-111356

Indirubin-3-monoxime-5-sulphonic acid Cat No HY-111931

Indirubin-5-sulfonate Cat No HY-111932

JH-XI-10-02 Cat No HY-111518

JNJ-7706621 Cat No HY-10329

JSH-150 Cat No HY-X0150

Kenpaullone (9-Bromopaullone NSC-664704) Cat No HY-12302

wwwMedChemExpresscom 27

Purity 9861Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9847Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Bioactivity KH-CB19 is a potent and highly specific inhibitor of theCDC2-like kinase isoforms 1 and 4 (CLK1CLK4) IC50 value 20nM (CLK1) [1] Target CLK14 inhibitor in vitro KH-CB19showed potent inhibition of CLK1 with an IC50 of 20 nM andfor the pure isomer KH-CB19 almost 100-fold selectivityhellip

Bioactivity LDC000067 is a highly specific inhibitor with an CDK9 IC50value of 44plusmn10 nM in vitro

Bioactivity LDC4297 is a potent and selective inhibitor with an CDK7 IC50of 013 nM

Bioactivity Lerociclib (G1T38) is a potent and selective inhibitor of with of 1 nM 2 nM for CDK4CyclinD1 andCDK46 IC s50

CDK6CyclinD3 respectively

Bioactivity Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potentand selective inhibitor of with of 1 nMCDK4 CDK6 IC s50and 2 nM for and respectivelyCDK4 CyclinD1 CDK6 CyclinD3

Bioactivity LY2857785 is a type I reversible and competitive ATP kinaseinhibitor against ( 11 nM) and other transcriptionCDK9 IC50kinases ( 16 nM) and ( 246 nM)CDK8 IC50 CDK7 IC50

Bioactivity LY3177833 is an and inhibitor extracted fromCDC7 pMCM2patent US 20140275131and patent WO 2014143601 A1 compoundexample 4 has values of 33 nM and 290 nM respectivelyIC50

Bioactivity MBQ-167 is a dual inhibitor with of 103 nMRacCdc42 IC s50for Rac 123 and 78 nM for Cdc42 in MDA-MB-231 cellsrespectively

Bioactivity MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin inhibitor with an of 5 nM at least 22-fold moreT1 IC50

selective for CDK9 over other CDKs MC180295 also inhibitsGSK-3α and GSK-3β MC180295 ((rel)-MC180295) has pothellip

Bioactivity Milciclib (PHA-848125) is a potent dual inhibitor of andCDK with s of 45 150Tropomyosin receptor kinase (TRK) IC50

160 363 398 nM and 53 nM for cyclin ACDK2 cyclin HCDK7cyclin D1CDK4 cyclin ECDK2 cyclin BCDK1 and TRKArespectively

KH-CB19 Cat No HY-12828

LDC000067 (LDC067) Cat No HY-15878

LDC4297 Cat No HY-12653

Lerociclib (G1T38) Cat No HY-112272

Lerociclib dihydrochloride (G1T38 dihydrochloride) Cat No HY-112272A

LY2857785 Cat No HY-12293

LY3177833 Cat No HY-100023

MBQ-167 Cat No HY-112842

MC180295 ((rel)-MC180295) Cat No HY-119940

Milciclib (PHA-848125) Cat No HY-10424

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9703Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9851Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Bioactivity ML167 is a highly selective Cdc2-like kinase 4 ( )Clk4inhibitor with of 136 nM gt10-fold selectivity forIC50closely related kinases Clk1 Clk2 Clk3 and Dyrk1A1B

Bioactivity MSC2530818 is a potent selective and orally available CDK8inhibitor with an of 26 nM for CDK8IC50

Bioactivity NG 52 (Compound 52 ) is a potent cell-permeable reversibleselective and ATP-compatible inhibitor of the cellcycle-regulating kinase Cdc28p (IC50 = 7 μM) and the relatedPho85p kinase (IC50 = 2 μM)

Bioactivity Nimbolide is a triterpene derived from the leaves and flowersof neem ( L) Nimbolide induces apoptosisAzadirachta indicathrough inactivation of Nimbolide inhibits NF-κB CDK4

kinase activity Nimbolide suppresses the NF-κB WntCDK6PI3K-Akt MAPK and JAK-STAT signaling pathways [1]

Bioactivity NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and26 μM for CDK2 and CDK1 IC50 value 17μM (CDK2) 26μM (CDK1)Target CDK in vitro NU2058 is a competitive inhibitor ofCDK2 with respect to ATP (Ki value CDK2 12 3 μM) that bindsin the ATP binding pocket in a different orientation fromhellip

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity NU6300 is the first covalent ATP-competitive CDK2 inhibitorIC50 value Target CDK2 in vitro NU6300 is a covalent CDK2inhibitor that illustrates the potential of using vinylsulfones to mediate irreversible inhibition NU6300 blocks theinhibitor binding site The effect was time dependent andhellip

Bioactivity NVP-2 is a inhibitor with an of 05 nMCDK9 IC50

Bioactivity NVP-LCQ195 (AT9311 LCQ195) is a small molecule heterocyclicinhibitor of CDK1 CDK2 CDK3 and CDK5 with IC50 of 1-42 nM

Bioactivity ON-013100 an antineoplastic drug acts a mitotic inhibitorthat could inhibit expressionCyclin D1

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ML167 (CID44968231 NCGC00188654) Cat No HY-15951

MSC2530818 Cat No HY-101611

NG 52 (Compound 52) Cat No HY-15154

Nimbolide Cat No HY-116035

NU2058 (O6-(Cyclohexylmethyl)guanine) Cat No HY-19316

NU6140 Cat No HY-107419

NU6300 Cat No HY-18930

NVP-2 Cat No HY-12214A

NVP-LCQ195 (LCQ-195 AT9311) Cat No HY-15241

ON-013100 Cat No HY-112822

wwwMedChemExpresscom 29

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9996Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity ON123300 is a potent inhibitor of CDK4 with an IC50 of 38nM with little inhibitory activity against CDKs 125 and 8

Bioactivity Palbociclib (PD 0332991) is a selective and CDK4 CDK6inhibitor with s of 11 and 16 nM respectivelyIC50Palbociclib is a drug for the treatment of ER-positive andHER2-negative breast cancer

Bioactivity Palbociclib hydrochloride is a highly selective CDK46inhibitor with s of 11 nM and 16 nM respectivelyIC50

Bioactivity Palbociclib isethionate is a highly selective inhibitorof with s of 11 nM16 nMCDK46 IC50respectively

Bioactivity PF-06873600 is a selective and orally bioavailable inhibitorof cyclin-dependent kinase with values of 009 nM(CDK) Ki013 nM and 016 nM for CDK2 CDK4 and CDK6 respectivelyPF-06873600 has potential antineoplastic activity [1] [2]

Bioactivity PHA-767491 is a dual inhibitor with s of 10 nMCdc7Cdk9 IC50and 34 nM respectively

Bioactivity PHA-767491 hydrochloride is a dual inhibitor withCdc7Cdk9s of 10 nM and 34 nM respectivelyIC50

Bioactivity PHA-793887 is a potent ATP-competitive inhibitor canCDKinhibit Cdk2 Cdk1 Cdk4 and Cdk9 with s of 8 nM 60 nMIC5062 nM and 138 nM respectively and also inhibits glycogensynthase kinase 3β with an of 79 nMIC50

Bioactivity PROTAC CDK9 Degrader-1 is a selective degraderCDK9 Bioactivity Purvalanol A is a potent inhibitor which inhibitsCDKcdc2-cyclin B cdk2-cyclin A cdk2-cyclin E cdk4-cyclin D1and cdk5-p35 with s of 4 70 35 850 75 nMIC50resepctively

ON123300 Cat No HY-12624

Palbociclib (PD 0332991) Cat No HY-50767

Palbociclib hydrochloride (PD 0332991 hydrochloride) Cat No HY-50767A

Palbociclib isethionate (PD 0332991 isethionate) Cat No HY-A0065

PF-06873600 Cat No HY-114177

PHA-767491 (CAY10572) Cat No HY-13461

PHA-767491 hydrochloride (CAY-10572 hydrochloride) Cat No HY-13461A

PHA-793887 Cat No HY-11001

PROTAC CDK9 Degrader-1 Cat No HY-103628

Purvalanol A (NG-60) Cat No HY-18299A

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9900Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9983Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitorwith IC50 values of 6 6 9 gt 10000 and 6 nM forcdc2cyclin B cdk2cyclin A cdk2cyclin E cdk4cyclin D1and cdk5-p35 respectively

Bioactivity R547 is a potent ATP-competitive inhibitor of CDK124 with Kiof 2 nM3 nM1 nM

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity Ribociclib (LEE011) is a highly specific inhibitorCDK46with s of 10 nM and 39 nM respectivelyIC50

Bioactivity Ribociclib hydrochloride (LEE011 hydrochloride) is a highlyspecific inhibitor with values of 10 nM and 39CDK46 IC50nM respectively and is over 1000-fold less potent againstthe cyclin BCDK1 complex

Bioactivity Ribociclib succinate (LEE011 succinate) is a highly specific inhibitor with values of 10 nM and 39 nMCDK46 IC50

respectively and is over 1000-fold less potent against thecyclin BCDK1 complex

Bioactivity Ribociclib succinate hydrate (LEE011 succinate hydrate) is ahighly specific inhibitor with values of 10 nMCDK46 IC50and 39 nM respectively and is over 1000-fold less potentagainst the cyclin BCDK1 complex

Bioactivity Riviciclib (P276-00 free base) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib shows antituhellip[1] [2]

Bioactivity Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib hydrochlorhellip[1] [2]

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Purvalanol B (NG 95) Cat No HY-18299

R547 Cat No HY-10014

RGB-286638 Cat No HY-15504

RGB-286638 free base Cat No HY-15504A

Ribociclib (LEE011) Cat No HY-15777

Ribociclib hydrochloride (LEE011 (hydrochloride)) Cat No HY-15777A

Ribociclib succinate (LEE011 (succinate)) Cat No HY-15777B

Ribociclib succinate hydrate (LEE011 (succinate hydrate)) Cat No HY-15777C

Riviciclib (P276-00 (free base)) Cat No HY-16559A

Riviciclib hydrochloride (P276-00) Cat No HY-16559

wwwMedChemExpresscom 31

Purity 9850Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9907Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9677Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ro-3306 is a potent and selective inhibitor of with sCDK1 Kiof 20 nM 35 nM and 340 nM for CDK1 CDK1cyclin B1 andCDK2cyclin E respectively

Bioactivity Roniciclib is an orally bioavailable pan-cyclin dependentkinase inhibitor with of 5-25 nM for CDK1 CDK2(CDK) IC s50CDK3 CDK4 CDK7 and CDK9

Bioactivity SB1317 is a potent inhibitor of and forCDK2 JAK2 FLT3the treatment of cancer with of 13 73 and 56 nM forIC50CDK2 JAK2 and FLT3 respectively

Bioactivity SEL120-34A is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A HCl is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A monohydrochloride is an ATP-competitive andselective inhibitor inhibits kinase activities ofCDK8CDK8CycC and CDK19CycC complexes with s of 44 nM andIC50104 nM respectively with a of 3 nM for CDhellipKd

Bioactivity Seliciclib (Roscovitine) is a potent and selective CDKsinhibitor with s of 02 μM 065 μM and 07 μM for IC50 CDK5

and respectivelyCdc2 CDK2

Bioactivity Senexin A is a inhibitor with an of 280 nMCDK8 IC50

Bioactivity Simurosertib (TAK-931) is a selective cycle 7 kinase(CDC7)inhibitor with an lt03 nMIC50

Bioactivity SNS-032 (BMS-387032) is a selective inhibitor of CDK2 and with s of 38 nM 62 nM and 4CDK7 CDK9 IC50

nM respectively

Ro-3306 Cat No HY-12529

Roniciclib (BAY 1000394) Cat No HY-13914

SB1317 (TG02) Cat No HY-15166

SEL120-34A Cat No HY-111388

SEL120-34A HCl Cat No HY-111388B

SEL120-34A monohydrochloride Cat No HY-111388A

Seliciclib (Roscovitine CYC202 R-roscovitine) Cat No HY-30237

Senexin A Cat No HY-15681

Simurosertib (TAK-931) Cat No HY-100888

SNS-032 (BMS-387032) Cat No HY-10008

Purity 9846Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9796Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9882Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity SU9516 is a potent inhibitor with an of 22 nM andCDK2 IC50also shows inhibitory effects on CDK1 and CDK4 with s ofIC5040 200 nM respectively

Bioactivity SY-1365 is a highly selective covalent inhibitor of CDK7SY-1365 possesses therapeutic potential in both hematologicaland solid tumors [1]

Bioactivity T025 is an orally available and highly potent Cdc2-like kinase inhibitor with s of 48 0096 65 and 061 nM(CLK) Kd

for CLK1 CLK2 CLK3 and CLK4 respectively

Bioactivity THAL-SNS-032 is a selective degrader PROTAC consistingCDK9of a CDK-binding SNS-032 ligand linked to a thalidomidederivative that binds the E3 ubiquitin ligase Cereblon (CRBN)

[1]

Bioactivity THZ1 is a selective and potent covalent inhibitor withCDK7an of 32 nMIC50

Bioactivity THZ1 Hydrochloride is a selective and potent inhibitorCDK7with an of 32 nMIC50

Bioactivity THZ1-R is a non-cysteine reactive analog of THZ1 whichdisplays diminished activity for inhibition THZ1-RCDK7binds to with a of 142 nMCDK7 Kd

Bioactivity THZ2 is a potent and selective inhibitor with an ofCDK7 IC50139 nM

Bioactivity THZ531 is a covalent inhibitor of both and withCDK12 CDK13s of 158 nM and 69 nM respectivelyIC50

Bioactivity Trilaciclib is a inhibitor with s of 1 nM and 4 nMCDK46 IC50for CDK4 and CDK6 respectively

32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SU9516 Cat No HY-18629

SY-1365 Cat No HY-128587

T025 Cat No HY-112296

THAL-SNS-032 Cat No HY-123937

THZ1 Cat No HY-80013

THZ1 Hydrochloride Cat No HY-80013A

THZ1-R Cat No HY-19988

THZ2 Cat No HY-12280

THZ531 Cat No HY-103618

Trilaciclib (G1T28) Cat No HY-101467

wwwMedChemExpresscom 33

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Trilaciclib hydrochloride is a inhibitor with s ofCDK46 IC501 nM and 4 nM for CDK4 and CDK6 respectively

Bioactivity Voruciclib hydrochloride is a clinical stage oral CDK9inhibitor Voruciclib hydrochloride represses expression ofMCL-1 in multiple models of diffuse large B-cell lymphoma(DLBCL) [1]

Bioactivity Wogonin is a naturally occurring mono-flavonoid can inhibitthe activity of and and exhibitsCDK8 Wntanti-inflammatory and anti-tumor effects

Bioactivity XL413 is a potent selective and ATP competitive inhibitor of with an of 34 nM and also shows potent effectCdc7 IC50

with s of 215 42 nM on CK2 PIM1 respectively and anIC50 of 118 nM on pMCMEC50

Bioactivity XL413 hydrochloride is a potent selective and ATP competitiveinhibitor of with an of 34 nM and also showsCdc7 IC50potent effect with s of 215 42 nM on CK2 PIM1IC50respectively and an of 118 nM on pMCMEC50

Trilaciclib hydrochloride (G1T28 hydrochloride) Cat No HY-101467A

Voruciclib hydrochloride Cat No HY-12422A

Wogonin Cat No HY-N0400

XL413 Cat No HY-15260

XL413 hydrochloride Cat No HY-15260A

Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) are protein kinases that are involved in cellcycle control Two checkpoint kinase subtypes have been identifiedChk1 and Chk2 Chk1 is a central component of genome surveillancepathways and is a key regulator of the cell cycle and cell survivalChk1 is required for the initiation of DNA damage checkpoints andhas recently been shown to play a role in the normal (unperturbed)cell cycle Chk1 impacts various stages of the cell cycle including the Sphase G2M transition and M phase In addition to mediating cellcycle checkpoints Chk1 also contributes to DNA repair processesgene transcription embryo development cellular responses to HIVinfection and somatic cell viability Chk2 is a protein kinase that is

activated in response to DNA damage and is involved in cell cycle arrest In response to DNA damage and replicationblocks cell cycle progression is halted through the control of cell cycle regulators The protein encoded by this gene isa cell cycle checkpoint regulator and putative tumor suppressor

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wwwMedChemExpresscom 35

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9877Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9990Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Checkpoint Kinase (Chk) Inhibitors amp Modulators

Bioactivity AZD-7762 is a potent ATP-competitive checkpoint kinase ( )Chkinhibitor in with an of 5 nM for Chk1IC50

Bioactivity BML-277 is a selective checkpoint kinase 2 ( ) inhibitorChk2with an of 15 nMIC50

Bioactivity CCT241533 is a potent and selective ATP competitive inhibitorof with an of 3 nM and of 116 nMCHK2 IC50 Ki

Bioactivity CCT241533 hydrochloride is a potent and selective CHK2inhibitor with an of 3 nM and a of 116 nMIC50 Ki

Bioactivity CCT244747 is a potent orally bioavailable and highlyselective inhibitor with an of 77 nM CCT244747CHK1 IC50also abrogates G2 checkpoint with an of 29 nMIC50

Bioactivity CCT245737 is a orally active and seletive inhibitorChk1with an of 13 nMIC50

Bioactivity CHIR-124 is a potent and selective inhibitor with Chk1 IC50of 03 nM and also potently targets and withPDGFR FLT3

s of 66 nM and 58 nMIC50

Bioactivity CHK-IN-1 is an inhibitor of and withCHK1 CHK2anti-proliferative activities

Bioactivity CHK1 inhibitor is an inhibitor of CHK1 Bioactivity CHK1-IN-2 is a checkpoint kinase 1 inhibitor with an(CHK1) of 6 nMIC50

AZD-7762 Cat No HY-10992

BML-277 (Chk2 Inhibitor II) Cat No HY-13946

CCT241533 Cat No HY-14715

CCT241533 hydrochloride Cat No HY-14715B

CCT244747 Cat No HY-18175

CCT245737 Cat No HY-18958

CHIR-124 Cat No HY-13263

CHK-IN-1 Cat No HY-U00345

CHK1 inhibitor Cat No HY-104022

CHK1-IN-2 Cat No HY-111369

Purity 9965Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9791Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity CHK1-IN-3 is a inhibitor with anCheckpoint Kinase 1 (CHK1) of 04 nM IC50

[1]Bioactivity GDC-0575 (ARRY-575 RG7741) is a highly-selective oral

small-molecule inhibitor with an of 12nMChk1 IC50

Bioactivity GDC-0575 dihydrochloride is an orally bioavailable CHK1inhibitor with an of 12 nM and has antitumor activityIC50

Bioactivity PF 477736 is a potent selective ATP-competitive inhibitor of with a of 049 nM 100-fold selectivity versus Chk1 Ki Chk2

( 47 nM)Ki

Bioactivity Prexasertib (LY2606368) is a potent selective andATP-competitive inhibitor with ancheckpoint kinase 1 (Chk1)

and a of lt1 nM and 09 nM respectivelyIC50 Ki

Bioactivity Prexasertib dihydrochloride (LY2606368 dihydrochloride) is apotent and selective ATP competitive inhibitor of the Chk1protein kinase with s of lt1 nM and 8 nM for CHK1 andIC50CHK2 respectively and a of 09 nM against purified CHK1Ki

Bioactivity Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is apotent selective ATP competitive and inhibitorCHK1 CHK2with a of 09 nM for CHK1 and s of lt1 nM 8 nM forKi IC50CHK1 and CHK2 respectively Prexasertib Mesylate Hydrateinhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2hellip

Bioactivity Rabusertib (LY2603618) is a potent and selective inhibitor of with an of 7 nMChk1 IC50

Bioactivity SCH900776 is a potent selective and oral inhibitor ofcheckpoint kinase1 ( ) with an of 3 nM It shows 50-Chk1 IC50and 500-fold selectivity over CDK2 andChk2 respectively

36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CHK1-IN-3 Cat No HY-128601

GDC-0575 (ARRY-575 RG7741) Cat No HY-112167

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride RG7741 dihydrochloride) Cat No HY-112167A

PF 477736 (PF 00477736) Cat No HY-10032

Prexasertib (LY2606368) Cat No HY-18174

Prexasertib dihydrochloride (LY2606368 (dihydrochloride)) Cat No HY-18174A

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate LY2940930) Cat No HY-18174B

Rabusertib (LY2603618 IC-83) Cat No HY-14720

SCH900776 (MK-8776) Cat No HY-15532

wwwMedChemExpresscom 37

CRISPRCas9

CRISPRCas9 (Clustered Regularly-Interspaced Short PalindromicRepeatsCas9) is a bacterial immune system that has been adaptedfor genome editing in mammalian cells Cas9 is a programmablenuclease that generates double-stranded breaks (DSB) in DNAdictated by binding of a ~20 nucleotide recombinant ldquoguide RNArdquo(gRNA) to the target site DSBrsquos produced by Cas9 are most oftenrepaired through the cellrsquos error-prone non-homologous end joining(NHEJ) pathway resulting in small insertions or deletions (indels) Thevast majority of indels shift the reading frame introducing apremature stop codon or resulting in nonsense mediated decay ofthe mRNA-effectively ldquoknocking outrdquo a gene

The CRISPRCas9 system has substantially advanced efforts in specific gene editing and has been successfully appliedto modify the episomal genomes of human and other organisms The CRISPRCas9 system utilizes a prokaryoticRNA-guided programmable nuclease that can make a double-strand DNA break (DSB) at a specific site under theguidance of a leading RNA This DSB process depends on the co-expression of two basic components a guide RNA(gRNA) and Cas9 nuclease Making a specific DSB can trigger DNA repair via either error-prone non-homologous endjoining (NHEJ) or homology-directed repair (HDR) In the presence of the CRISPRCas9 system the NHEJ inhibitorSCR7 is proven to increase the efficiency of Cas9-mediated HDR by at least by 7-fold in mammalian cells Genomeediting via CRISPRCas9 has become an efficient and reliable way to make precise targeted changes to the genome ofliving cells

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

CRISPRCas9 Inhibitors amp Modulators

Bioactivity Brefeldin A is a specific inhibitor of whichprotein traffickingblocks the protein transport from the endoplasmic reticulum tothe Golgi complex

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity L755507 is a potent selective agonist of with an β -AR3 IC50of 35 nM

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity Zidovudine is a nucleoside reverse transcriptase inhibitor () widely used to treat HIV infection Zidovudine increasesNRTI

CRISPRCas9-mediated editing frequency

38 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Brefeldin A (BFA Cyanein Decumbin) Cat No HY-16592

KU-57788 (NU7441) Cat No HY-11006

L755507 Cat No HY-19334

Nocodazole (Oncodazole R17934) Cat No HY-13520

RS-1 Cat No HY-19793

SCR7 Cat No HY-12742

Zidovudine (Azidothymidine AZT ZDV) Cat No HY-17413

wwwMedChemExpresscom 39

DeubiquitinaseDUBs

Deubiquitinases (DUBs) are a large group of proteases that cleaveubiquitin from proteins and other molecules Ubiquitin is attached toproteins in order to regulate the degradation of proteins via theproteasome and lysosome coordinate thecellular localisation ofproteins activate and inactivate proteins and modulateprotein-protein interactions DUBs can reverse these effects bycleaving the peptide or isopeptide bond between ubiquitin and itssubstrate protein In humans there are nearly 100 DUB genes whichcan be classified into two main classes cysteine proteases andmetalloproteases The cysteine proteases comprise ubiquitin-specificproteases (USPs) ubiquitin C-terminal hydrolases (UCHs)

Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU) The metalloprotease groupcontains only the Jab1Mov34Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases DUBs play several roles inthe ubiquitin pathway One of the best characterised functions of DUBs is the removal of monoubiqutin andpolyubiquitin chainsfrom proteins

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9940Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9892Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9893Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Deubiquitinase Inhibitors amp Modulators

Bioactivity 6-Thioguanine (Thioguanine) is an anti-leukemia andimmunosuppressant agent acts as an inhibitor of SARS and MERScoronavirus papain-like proteases ( ) and also potentlyPLprosinhibits activity with s of 25 μM and 40 μM forUSP2 IC50Plpros and recombinant human USP2 respectively

Bioactivity b-AP15 is a specific inhibitor of the enzymesdeubiquitinating and UCHL5 Usp14

Bioactivity BAY 11-7082 is a inhibitor which decreases NF-κB byNF-κBinhibiting TNF-α-induced phosphorylation of IκB-α BAY 11-7082inhibits ubiquitin-specific protease and withUSP7 USP21

s of 019 μM and 096 μM respectivelyIC50

Bioactivity C527 is a is a pan inhibitor with a highDUB enzymepotency for the complex ( =088 μM)USP1UAF1 IC50

Bioactivity Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB)inhibitor directly inhibiting DUB activity of USP9x USP5USP14 and UCH37 Degrasyn has been shown to downregulate theantiapoptotic proteins and Bcr-Abl JAK2

Bioactivity DUBs-IN-1 is an active inhibitor of ubiquitin-specific with an of 024 μM for USP8proteases (USPs) IC50

Bioactivity DUBs-IN-2 is a potent inhibitor with an ofdeubiquitinase IC50028 μM for USP8

Bioactivity DUBs-IN-3 is a potent enzyme inhibitordeubiquitinase (USP)extracted from reference compound 22c with an of 056 μMIC50for USP8

Bioactivity EOAI3402143 is a ( ) inhibitor whichdeubiquitinase DUBinhibits dose-dependently inhibits and Usp9x Usp24 Usp5

Bioactivity FT671 is a potent non-covalent and selective inhibitorUSP7with an of 52 nM and binds to the USP7 catalytic domainIC50with a of 65 nMKd

40 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

6-Thioguanine (Thioguanine2-Amino-6-purinethiol) Cat No HY-13765

b-AP15 (NSC 687852) Cat No HY-13989

BAY 11-7082 (BAY 11-7821) Cat No HY-13453

C527 Cat No HY-12988

Degrasyn (WP1130) Cat No HY-13264

DUBs-IN-1 Cat No HY-50736

DUBs-IN-2 Cat No HY-50737A

DUBs-IN-3 Cat No HY-50737

EOAI3402143 Cat No HY-111408

FT671 Cat No HY-107985

wwwMedChemExpresscom 41

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9773Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9684Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity FT827 is a selective and covalent ubiquitin-specific protease7 ( ) inhibitor with an of 52 nMUSP7 IC50

Bioactivity GNE-6640 is a selective and non-covalent inhibitor ofubiquitin epecific peptidase 7 with values of(USP7) IC50075 μM 043 μM 203 μM and 023 μM for full length USP7USP7 catalytic domain full length USP43 and Ub-MDM2respectively

Bioactivity GNE-6776 is a selective inhibitorUSP7 Bioactivity HBX 19818 is a specific inhibitor of ubiquitin-specific with an of 281 μMprotease 7 (USP7) IC50

Bioactivity IU1 is a special inhibitor with of 4-5 μMUsp14 IC50 Bioactivity IU1-47 is a potent inhibitor with an of 06 μMUSP14 IC50

IU1-47 induces tau elimination in cultured neurons [1]

Bioactivity LDN-57444 is a reversible competitive and site-directedinhibitor of withubiquitin C-terminal hydrolase L1 (UCH-L1)an of 088 μM and a of 040 μM LDN-57444 alsoIC50 Kisuppresses UCH-L3 activity with an of 25 μMIC50

Bioactivity MF-094 is a potent and selective inhibitor with an USP30 IC50of 120 nM

Bioactivity ML-323 is a reversible potent inhibitor with USP1-UAF1 IC50of 76 nM in a Ub-Rho assay The measured inhibition constantsof ML-323 for the free enzyme ( ) is 68 nMKi

Bioactivity ML364 is an inhibitor of ubiquitin specific peptidase 2 and can be used for the research of breast cancer(USP2)

extracted from patent WO 2016134026 A1 compound Figure 10G

FT827 Cat No HY-111350

GNE-6640 Cat No HY-112937

GNE-6776 Cat No HY-107986

HBX 19818 Cat No HY-17540

IU1 Cat No HY-13817

IU1-47 Cat No HY-122243

LDN-57444 Cat No HY-18637

MF-094 Cat No HY-112438

ML-323 Cat No HY-17543

ML364 Cat No HY-100900

Purity 9800Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9737Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9843Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NSC632839 is a nonselective isopeptidase inhibitor whichinhibits and with s of 45plusmn4 μMUSP2 USP7 SENP2 EC5037plusmn1 μM and 98plusmn18 μM respectively

Bioactivity P 22077 is a cell-permeable ubiquitin-specific protease 7 inhibitor with an of 801 μM It also inhibits(USP7) EC50

USP47 with an of 874 μMEC50

Bioactivity P005091 is a selective and potent inhibitor of with anubiquitin-specific protease 7 (USP7)

of 42 μMEC50

Bioactivity PR-619 is a broad-range inhibitor with of 393DUB EC5049 686 72 and 861 μM for USP4 USP8 USP7 USP2and respectivelyUSP5

Bioactivity SJB2-043 is an inhibitor of the native complex withUSP1UAF1 of 544 nMIC50

Bioactivity SJB3-019A is a potent and novel inhibitor 5 times moreUSP1potent than SJB2-043 in promoting ID1 degradation andcytoxicity in K562 cells with of 00781 μMIC50

Bioactivity USP7-IN-1 is a selective and reversible inhibitor of with an of 77 μMubiquitin-specific protease 7 (USP7) IC50

and can be used for the research of cancer

Bioactivity USP7-IN-3 (Compound 5) is a potent and selective allostericubiquitin-specific protease 7 ( ) inhibitor USP7 [1]

Bioactivity USP7USP47 inhibitor is a selective ubiquitin-specific protease inhibitor with s of 042 μM and 10747 (USP7USP47) EC50

μM respectively

Bioactivity VLX1570 is a competitive inhibitor of proteasomedeubiquitinases ( ) with an of approximate 10 μMDUBs IC50

42 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NSC632839 Cat No HY-100708

P 22077 Cat No HY-13865

P005091 (P5091) Cat No HY-15667

PR-619 Cat No HY-13814

SJB2-043 Cat No HY-15757

SJB3-019A Cat No HY-80012

USP7-IN-1 Cat No HY-16709

USP7-IN-3 Cat No HY-112128

USP7USP47 inhibitor Cat No HY-13487

VLX1570 Cat No HY-12471

wwwMedChemExpresscom 43

DNA AlkylatorCrosslinker

DNA alkylatorcrosslinker is a molecule that alkylates DNA or cancross link with DNA DNA alkylatorcrosslinker can have mutagenicpharmaceutical or other effects Alkylation is the transfer of an alkylgroup from one molecule to another The alkyl group may betransferred as an alkyl carbocation a free radical a carbanion or acarbene Alkylating agents are widely used in chemistry because thealkyl group is probably the most common group encountered inorganic molecules Selective alkylation or adding parts to the chainwith the desired functional groups is used especially if there is nocommonly available biological precursor Alkylation with only onecarbon is termed methylation In medicine alkylation of DNA is used

in chemotherapy to damage the DNA of cancer cells Alkylation is accomplished with the class of drugs calledalkylating antineoplastic agents Crosslinking of DNA occurs when various exogenous or endogenous agents reactwith two different positions in the DNA This can either occur in the same strand (intrastrand crosslink) or in theopposite strands of the DNA (interstrand crosslink) Crosslinks also occur between DNA and protein DNA replicationis blocked by crosslinks which causes replication arrest and cell death if the crosslink is not repaired The RAD51family plays a role in repair

Purity 990Clinical Data LaunchedSize 100 mg 500 mg

Purity 9879Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9844Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9961Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

DNA AlkylatorCrosslinker Inhibitors amp Modulators

Bioactivity Altretamine is an antineoplastic agentalkylating Bioactivity Altretamine hydrochloride is an antineoplasticalkylatingagent

Bioactivity Bendamustine D4 is the deuterium labeled BendamustineBendamustine is a agent that causes DNADNA cross-linkingbreaks with alkylating and antimetabolite properties

Bioactivity Bendamustine hydrochloride is a agent thatDNA cross-linkingcauses DNA breaks with alkylating and antimetaboliteproperties

Bioactivity Busulfan is a potent with selective immunosuppressivealkylatoreffect on bone marrow

Bioactivity Calicheamicin is a cytotoxic agent that causes double-strandDNA breaks

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity Carmustine is an antitumor chemotherapeutic agent which worksby akylating DNA and RNA

Bioactivity Chlorambucil is an agent with antitumor activityalkylating Bioactivity Cisplatin is a antineoplastic chemotherapy drug which works bycross-linking with and causing DNA damage in cancerDNAcells

44 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Altretamine (ENT-50852 RB-1515 WR-95704) Cat No HY-B0181

Altretamine hydrochloride (ENT-50852 hydrochloride RB-1515

hydrochloride WR-95704 hydrochloride) Cat No HY-B0181A

Bendamustine D4 (SDX-105 D4) Cat No HY-13567S

Bendamustine hydrochloride (SDX-105 EP-3101) Cat No HY-B0077

Busulfan Cat No HY-B0245

Calicheamicin (Calicheamicin γ1) Cat No HY-19609

Carboplatin (NSC 241240) Cat No HY-17393

Carmustine Cat No HY-13585

Chlorambucil (CB-1348 WR-139013) Cat No HY-13593

Cisplatin (CDDP cis-Diaminodichloroplatinum) Cat No HY-17394

wwwMedChemExpresscom 45

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 980Clinical Data LaunchedSize 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Bioactivity Cyclophosphamide is a synthetic agent chemicallyalkylatingrelated to the nitrogen mustards with antineoplastic andimmunosuppressive activities

Bioactivity Cyclophosphamide hydrate is a synthetic agentalkylatingchemically related to the nitrogen mustards withantineoplastic and immunosuppressive activities

Bioactivity Fotemustine is a agent with antitumor activityDNA-alkylating Bioactivity Ifosfamide is an chemotherapeutic agent withalkylatingactivity against a wide range of tumors

Bioactivity Lomustine (CCNU) is a agent with antitumorDNA alkylatingactivity

Bioactivity Melphalan is an effective agent with potentDNA alkylatingantitumor activity

Bioactivity Methylnitronitrosoguanidine (MNNG) is an agent withalkylatingtoxic and mutagenic effects [1]

Bioactivity Miriplatin is a chemotherapy agent which belongs to the classof agentsalkylating

Bioactivity Miriplatin hydrate is a chemotherapy agent which belongs tothe class of agentsalkylating

Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Cyclophosphamide Cat No HY-17420

Cyclophosphamide hydrate (Cyclophosphamide monohydrate) Cat No HY-17420A

Fotemustine (S10036) Cat No HY-B0733

Ifosfamide Cat No HY-17419

Lomustine (CCNU NSC 79037) Cat No HY-13669

Melphalan (L-PAM) Cat No HY-17575

Methylnitronitrosoguanidine (MNNG) Cat No HY-128612

Miriplatin (SM-11355) Cat No HY-16325A

Miriplatin hydrate (SM-11355 (hydrate)) Cat No HY-16325

Mitomycin C (Ametycine) Cat No HY-13316

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9926Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9986Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Oxaliplatin is a inhibitor It causes DNADNA synthesiscrosslinking damage prevents DNA replication andtranscription and causes cell death

Bioactivity Palifosfamide is a novel DNA alkylator and the activemetabolite of ifosfamide with antitumor activity

Bioactivity Procarbazine Hydrochloride is an agent withalkylatinganticancer activity

Bioactivity RITA is an inhibitor of binds top53-HDM-2 interactionp53dN with a of 15 nM and also induces Kd DNA-DNA

cross-links

Bioactivity Satraplatin is an agent with potent antitumoralkylatingeffect

Bioactivity SJG-136 is a agent with an of 45 nMDNA cross-linking XL50for pBR322 DNA SJG-136 has potent antitumor activity

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity Temozolomide (NSC 362856 CCRG 81045) is an oral DNA agent used to treat some brain cancersalkylating

Bioactivity Thio-TEPA is a agent with antitumor activityDNA alkylating Bioactivity Treosulfan (NSC 39069Treosulphan) is an agent withalkylatingactivity in ovarian cancer and other solid tumor types

46 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Oxaliplatin Cat No HY-17371

Palifosfamide (Isophosphoramide mustard IPM ZIO-201) Cat No HY-14798

Procarbazine Hydrochloride Cat No HY-13733

RITA (NSC 652287) Cat No HY-13424

Satraplatin (BMS182751 BMY45594 JM216) Cat No HY-17576

SJG-136 (NSC-694501) Cat No HY-14573

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

Temozolomide (NSC 362856 CCRG 81045 TMZ) Cat No HY-17364

Thio-TEPA Cat No HY-17574

Treosulfan (NSC 39069 Treosulphan) Cat No HY-16503

wwwMedChemExpresscom 47

Purity 980Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Uramustine is an oral agent effective in thealkylatingtreatment of lymphosarcoma chronic lymphatic leukaemia andthrombocythemia

Bioactivity VAL-083 is an agent that creates N7 methylation onalkylatingDNA with antitumor activity

Uramustine (Uracil mustard) Cat No HY-13544

VAL-083 (Dianhydrodulcitol Dianhydrogalactitol) Cat No HY-16513

DNA-PKDNA-dependent protein kinase

DNA-PKcs (DNA-dependent protein kinase catalytic subunit) is anenzyme that in humans is encoded by the PRKDC gene DNA-PKcsbelongs to the phosphatidylinositol 3-kinase-related kinase proteinfamily DNA-PKcs is the catalytic subunit of a nuclear DNA-dependentserinethreonine protein kinase called DNA-PK The secondcomponent is the autoimmune antigen Ku On its own DNA-PKcs isinactive and relies on Ku to direct it to DNA ends and trigger itskinase activity DNA-PKcs is required for the non-homologous endjoining (NHEJ) pathway of DNA repair Many proteins have beenidentified as substrates for the kinase activity of DNA-PKAutophosphorylation of DNA-PKcs appears to play a key role in NHEJ

and is thought to induce a conformational change that allows end processing enzymes to access the ends of thedouble-strand break DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNAdamage checkpoint

48 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 49

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9943Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9722Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9664Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9239Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

DNA-PK Inhibitors amp Modulators

Bioactivity (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer ofNedisertib with an in the range of 7-30 nM for IC50 DNA-PK

[1]

Bioactivity AZD-7648 is a potent and selective inhibitorDNA-PKAnti-tumor activity [1]

Bioactivity CC-115 is a potent and dual and kinaseDNA-PK mTORinhibitor with s of 13 nM and 21 nM respectively CC-115IC50blocks both and signalingmTORC1 mTORC2

Bioactivity CC-115 hydrochloride is a potent and dual and DNA-PK mTORkinase inhibitor with s of 13 nM and 21 nM respectivelyIC50CC-115 blocks both and signalingmTORC1 mTORC2

Bioactivity Compound 401 is a synthetic inhibitor of ( = 028DNA-PK IC50μM) that also targets mTOR but not PI3K in vitro

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity LTURM34 is a specific inhibitor with an of 0034DNA-PK IC50μM

Bioactivity LY3023414 potently and selectively inhibits class I PI3Kisoforms and with s of 607 nM 776DNA-PK mTORC12 IC50nM 38 nM 238 nM 424 nM and 165 nM for PI3Kα PI3KβPI3Kδ PI3Kγ DNA-PK and mTOR respectively LY3023414potently inhibits at low nanomolarhellipmTORC1 2

Bioactivity Nedisertib (M3814) is a potent and selective inhibitor of ( ) with an of lt3DNA-dependent Protein Kinase DNA-PK IC50

nM

Bioactivity NU 7026 is a novel specific inhibitor with ofDNA-PK IC50023plusmn001 μM also inhibits with of 13plusmn3 μMPI3K IC50

(R)-Nedisertib ((R)-M3814) Cat No HY-101570A

AZD-7648 Cat No HY-111783

CC-115 Cat No HY-16962

CC-115 hydrochloride Cat No HY-16962A

Compound 401 Cat No HY-19341

KU-57788 (NU7441) Cat No HY-11006

LTURM34 Cat No HY-101667

LY3023414 Cat No HY-12513

Nedisertib (M3814) Cat No HY-101570

NU 7026 (DNA-PK Inhibitor II LY293646) Cat No HY-15719

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9937Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9145Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity PI-103 is a potent and inhibitor with s of 8PI3K mTOR IC50nM 88 nM 48 nM 150 nM 20 nM and 83 nM for p110α p110β

and PI-103 also inhibitsp110δ p110γ mTORC1 mTORC2 with an of 2 nMDNA-PK IC50

Bioactivity PI-103 Hydrochloride is a dual and inhibitor withPI3K mTORs of 8 nM 88 nM 48 nM 150 nM 20 nM and 83 nM forIC50

and p110α p110β p110δ p110γ mTORC1 mTORC2PI-103 also inhibits with an of 2 nMDNA-PK IC50

Bioactivity PIK-75 is a and inhibitor which inhibits DNA-PKDNA-PK PI3K and p110γ with s of 2 58 and 76 nM respectivelyp110α IC50

PIK-75 inhibits p110α gt200-fold more potently than p110β(IC =13 μM)50

Bioactivity PIK-90 is a and inhibitor which inhibits DNA-PK PI3K p110α and with s of 11 18 and 13 nMp110γ DNA-PK IC50

respectively

Bioactivity Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib apotent inhibitor with an of lt3 nM DNA-PK IC50

[1]Bioactivity SF2523 is a highly selective and potent inhibitor of withPI3K

s of 34 nM 158 nM 9 nM 241 nM and 280 nM for IC50 PI3Kα

BRD4 and mTOR respectivelyPI3Kγ DNA-PK

Bioactivity STL127705 (Compound L) is a Ku 7080 heterodimer proteininhibitor inhibits Ku7080-DNA interaction with an ofIC5035 μM STL127705 also inhibits Ku-dependent activation ofDNA-PKCS kinase ( 25 μM) IC50

[1]

Bioactivity Torin 2 is an inhibitor with of 025 nM formTOR EC50inhibiting cellular mTOR activity and exhibits 800-foldselectivity over PI3K (EC 200 nM) Torin 2 also inhibits50

with an of 05 nM in the cell free assay TorihellipDNA-PK IC50

Bioactivity VX-984 is a potent inhibitorDNA-PK Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

50 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

PI-103 Cat No HY-10115

PI-103 Hydrochloride Cat No HY-10115A

PIK-75 (PIK-75 Hydrochloride) Cat No HY-13281

PIK-90 Cat No HY-12030

Rac-Nedisertib (Rac-M3814) Cat No HY-101570B

SF2523 Cat No HY-101146

STL127705 Cat No HY-122727

Torin 2 Cat No HY-13002

VX-984 (M9831) Cat No HY-19939S

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

wwwMedChemExpresscom 51

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity YU238259 is an inhibitor of homology-dependent DNA repair () used for cancer researchHDR

YU238259 Cat No HY-19977

DNARNA Synthesis

RNA synthesis which is also called DNA transcription is a highlyselective process Transcription by RNA polymerase II extends beyondRNA synthesis towards a more active role in mRNA maturationsurveillance and export to the cytoplasmSingle-strand breaks are repaired by DNA ligase using thecomplementary strand of the double helix as a template with DNAligase creating the final phosphodiester bond to fully repair theDNADNA ligases discriminate against substrates containing RNAstrands or mismatched base pairs at positions near the ends of thenickedDNA Bleomycin (BLM) exerts its genotoxicity by generatingfree radicals whichattack C-4prime in the deoxyribose backbone of DNA

leading to opening of the ribose ring and strand breakage it is an S-independentradiomimetic agent that causesdouble-strand breaks in DNAFirst strand cDNA is synthesized using random hexamer primers and M-MuLV Reverse Transcriptase (RNase H)Second strand cDNA synthesis is subsequently performed using DNA Polymerase I and RNase H The remainingoverhangs are converted into blunt ends using exonucleasepolymerase activity After adenylation of the 3prime ends ofDNA fragments NEBNext Adaptor with hairpin loop structure is ligated to prepare the samples for hybridization Cellcycle and DNA replication are the top two pathways regulated by BET bromodomain inhibition Cycloheximide blocksthe translation of mRNA to protein

52 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 53

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 1 mg 2 mg 5 mg

Purity 9876Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9989Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 9968Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

25 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

DNARNA Synthesis Inhibitors amp Modulators

Bioactivity 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is amodified nucleoside 2-(Methylamino)-1H-purin-6(7H)-one is anendogenous methylated nucleoside found in human fluids

Bioactivity 374-Trihydroxyflavone isolated from Rhus javanica var is a flavonoid with DNA strand-scission activityroxburghiana

[1]

Bioactivity 5-Methoxyflavone belonged to Flavonoid family is a DNApolymerase-beta inhibitor and neuroprotective agent againstbeta-amyloid toxicity possess central nervous system (CNS)depressant effect mediated through the ionotropic GABA Areceptors

Bioactivity 6-Thio-2-Deoxyguanosine is a nucleoside analogue that can beincorporated into de novo-synthesized telomeres by telomerase

Bioactivity Acelarin (NUC-1031) is a ProTide transformation andenhancement of the widely-used nucleoside analoguegemcitabine

Bioactivity Actinomycin D inhibits with an of 042 μMDNA repair IC50

Bioactivity Adenine is a purine derivative and a nucleobase with a varietyof roles in biochemistry Target Nucleosideantimetaboliteanalog Adenine is a nucleobase with a varietyof roles in biochemistry including cellular respiration inthe form of both the energy-rich adenosine triphosphate (ATP)hellip

Bioactivity alpha-Amanitin is the principal toxin of several deadlypoisonous mushrooms exerting its toxic function by inhibiting

RNA-polymerase II

Bioactivity Anisomycin is a potent inhibitor whichprotein synthesisinterferes with protein and by inhibitingDNA synthesispeptidyl transferase or the 80S ribosome system Anisomycin isa JNK activator which increases phospho-JNK

Bioactivity Beaucage reagent is found to be potent in causing DNAcleavage

2-(Methylamino)-1H-purin-6(7H)-one (N2-methylguanine) Cat No HY-101412

374-Trihydroxyflavone (5-Deoxykampferol) Cat No HY-111806

5-Methoxyflavone Cat No HY-107790

6-Thio-2-Deoxyguanosine (6-thio-dG β-TGdR) Cat No HY-18762

Acelarin (NUC-1031) Cat No HY-100885

Actinomycin D (Dactinomycin Actinomycin IV) Cat No HY-17559

Adenine (6-Aminopurine Vitamin B4) Cat No HY-B0152

alpha-Amanitin (α-Amanitin α-Amatoxin) Cat No HY-19610

Anisomycin (Flagecidin Wuningmeisu C) Cat No HY-18982

Beaucage reagent Cat No HY-100951

Purity 9847Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity 9804Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9896Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Bioactivity Bleomycin sulfate is a inhibitor with potentDNA synthesisantitumor activity

Bioactivity BMH-21 is a small molecule DNA intercalator that bindsribosomal DNA and inhibits RNA polymerase I (Pol I)transcription does not cause phosphorylation of H2AX

Bioactivity Branaplam (LMI070) is a highly potent selective and orallyactive small molecule modulatorSMN2 splicing

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity CeMMEC1 is an inhibitor of and also has high affinityBRD4for with an of 09 μM for TAF1 and a of 18TAF1 IC50 KdμM for TAF1 (2)

Bioactivity CeMMEC13 is a potent inhibitor of bromodomain withTAF1 (2)an of 21 μMIC50

Bioactivity Chebulinic acid is a potent natural inhibitor of Mtuberculosis DNA gyrase also can inhibit SMAD-3phosphorylation inhibit H+ K+-ATPase activity

Bioactivity COH29 is a potent ribonucleotide reductase ( ) inhibitorRNRwith anticancer activity COH29 inhibits α and β subunit ofRNR with s of 16 μMIC50

Bioactivity CX-5461 is a potent and oral inhibitor ItrRNA synthesisinhibits RNA polymerase I-driven transcription of rRNA with

s of 142 113 and 54 nM in HCT-116 A375 and MIA PaCa-2IC50cells respectively

54 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Bleomycin sulfate Cat No HY-17565

BMH-21 Cat No HY-12484

Branaplam (LMI070 NVS-SM1) Cat No HY-19620

Capecitabine Cat No HY-B0016

Carboplatin (NSC 241240) Cat No HY-17393

CeMMEC1 Cat No HY-111445

CeMMEC13 Cat No HY-101088

Chebulinic acid Cat No HY-N2033

COH29 (RNR Inhibitor COH29) Cat No HY-19931

CX-5461 Cat No HY-13323

wwwMedChemExpresscom 55

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9872Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9963Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9945Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg

Bioactivity CX-5461 dihydrochloride is a potent and orally bioavailableinhibitor of Pol I-mediated with s of 142rRNA synthesis IC50nM in HCT-116 113 nM in A375 and 54 nM in MIA PaCa-2 cellsand shows little or no effect on Pol II ( ge25 μM)IC50

Bioactivity Cycloheximide (Naramycin A) is an eukaryote protein synthesisinhibitor with s of 5325 nM and 2880 nM for proteinIC50synthesis and RNA synthesis respectivelyin vivo

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Datelliptium chloride is a DNA-intercalating agent derivedfrom ellipticine with anti-tumor activities

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Didox (NSC-324360) is a synthetic (ribonucleotide reductase) inhibitorRR

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

CX-5461 dihydrochloride Cat No HY-13323A

Cycloheximide (Naramycin A Actidione CHX) Cat No HY-12320

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Datelliptium chloride Cat No HY-U00337

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Didox (NSC-324360) Cat No HY-19387

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Bioactivity Folic acid(Vitamin M Vitamin B9) is a B vitamin is necessaryfor the production and maintenance of new cells for DNAsynthesis and RNA synthesis

Bioactivity GC7 Sulfate is a ( ) inhibitordeoxyhypusine synthase DHPS

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity GNE-371 is a potent and selective chemical probe for thesecond bromodomains of human transcription-initiation-factor

subunit 1 and transcription-initiation-factor TFIID TFIIDsubunit 1-like with an of 10 nM for TAF1(2)IC50

Bioactivity Guanine is one of the fundamental components of nucleic acids( and ) Guanine is a purine derivative consistingDNA RNAof a fused pyrimidine-imidazole ring system with conjugateddouble bonds

Bioactivity Halofuginone (RU-19110) is a less-toxic form of Febrifuginewhich is isolated from the plant Dichroa febrifuga [1]

Halofuginone inhibits in anprolyl-tRNA synthetaseATP-dependent manner with a of 183 nM HalofuginhellipKi

[2]

Bioactivity Halofuginone hydrobromide (RU-19110 hydrobromide) is aless-toxic form of Febrifugine which is isolated from theplant Halofuginone inhibits Dichroa febrifuga [1] prolyl-tRNA

in an ATP-dependent manner with a of 183hellipsynthetase Ki

Bioactivity Hydroxyurea is a cell apoptosis inducer that inhibit DNAsynthesis through inhibition of ribonucleotide reductase

Bioactivity L189 is a novel human DNA ligase inhibitor inhibitshLigIIIIIV with IC50 of 595 μM

56 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Folic acid (Vitamin B9 Vitamin M) Cat No HY-16637

GC7 Sulfate Cat No HY-108314A

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

GNE-371 Cat No HY-112803

Guanine Cat No HY-Y1055

Halofuginone (RU-19110) Cat No HY-N1584

Halofuginone hydrobromide (RU-19110 (hydrobromide)) Cat No HY-N1584A

Hydroxyurea (Hydroxycarbamide) Cat No HY-B0313

L189 Cat No HY-15588

wwwMedChemExpresscom 57

Purity 990Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9839Clinical Data No Development ReportedSize 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9977Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9988Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity L67 is a novel competitive human DNA ligase inhibitorinhibits DNA ligases I and III with IC50 of 10 μM and 10 μM

Bioactivity Madrasin is a potent and cell penetrant splicing inhibitorthat interferes with the early stages of spliceosome assemblyMadrasin is cytotoxic at higher concentrations although atlower concentrations it induces cell cycle arrest promotes aspecific reorganization of subnuclear protein localizationhellip

Bioactivity MB-7133 is a inhibitorDNA synthesis Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Bioactivity ML216(CID-49852229) is a potent inhibitor of the DNA unwindingactivity of BLM helicase showing similar IC50s of 30 and097 μM for full length BLM and BLM636ndash1298 respectively IC50value 30097 uM(Full length636ndash1298 BLM) Target BLMhelicase inhibitor ML216 shows cell-based activity and canhellip

Bioactivity Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNAdamage agent

Bioactivity NITD008 is a potent and selective inhibitor whichflavivirusecan inhibit with an ofDengue Virus Type 2 (DENV-2) EC50064 μM

Bioactivity Oxolinic acid is a potent inhibitor of DNA gyrase and DNAsynthesis lead to DNA cleavage when extracted chromosomes areincubated with sodium dodecyl sulfate

Bioactivity Phen-DC3 is a (G4) specific ligand which canG-quadruplexinhibit and helicases with s of 65plusmn6 and 50plusmn10FANCJ DinG IC50nM respectively

Bioactivity Plicamycin is a selective specificity protein 1 ( )Sp1inhibitor Plicamycin inhibits the growth of various cancersby decreasing Sp1 protein

L67 (DNA Ligase Inhibitor) Cat No HY-15586

Madrasin (DDD00107587) Cat No HY-100236

MB-7133 Cat No HY-16311

Mitomycin C (Ametycine) Cat No HY-13316

ML216 (CID-49852229) Cat No HY-12342

Nedaplatin (NSC 375101D) Cat No HY-13700

NITD008 (7-Deaza-2-C-acetylene-adenosine) Cat No HY-12957

Oxolinic acid Cat No HY-B1002

Phen-DC3 Cat No HY-15594

Plicamycin (Mithramycin A) Cat No HY-A0122

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9762Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9931Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Quarfloxin (CX 3543) a fluoroquinolone derivative withantineoplastic activity targets and inhibits RNA pol Iactivity with IC values in the nanomolar range in50neuroblastoma cells Quarfloxin disrupts the interactionbetween the nucleolin protein and a G-quadruplex DNA structurehellip

Bioactivity RG7800 a small molecule splicing modifier to enterSMN2human clinical trials to treat spinal muscular atrophy

Bioactivity RG7800 hydrochloride is an orally active splicingSMN2modulator with s of 23 nM and 87 nM for EC15x SMN2

splicing and RG7800 hydrochloride has theSMN proteinpotential to treat spinal muscular atrophy

Bioactivity Risdiplam (RG7916 RO7034067) is an orally administeredcentrally and peripherally distributed pre-mRNASMN2splicing modifier that increases survival motor neuron (SMN)protein levels

Bioactivity Saccharin 1-methylimidazole is an activator for DNARNASynthesis

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity SMN-C3 is an orally active splicing modulator and hasSMN2the potential to treat spinal muscular atrophy (SMA)

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 valueof 08 nM less potent for MTH2 NUDT5 NUDT12 NUDT14 andNUDT16

Bioactivity TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) withan IC50 value of 08 nM less potent for MTH2 NUDT5 NUDT12NUDT14 and NUDT16

58 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Quarfloxin (CX 3543) Cat No HY-14776

RG7800 (RO6885247) Cat No HY-101792

RG7800 hydrochloride (RO6885247 hydrochloride) Cat No HY-101792A

Risdiplam (RG7916 RO7034067) Cat No HY-109101

Saccharin 1-methylimidazole Cat No HY-112060

SCR7 Cat No HY-12742

SMN-C3 Cat No HY-112633

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

TH287 Cat No HY-16965

TH287 hydrochloride Cat No HY-16965A

wwwMedChemExpresscom 59

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9920Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 25 mg 50 mg 100 mg

Bioactivity TH588 is first-in-class nudix hydrolase family inhibitor thatpotently and selectively engage and inhibit the (MTH1

= 5 nM)IC50

Bioactivity TH588 hydrochloride is first-in-class nudix hydrolase familyinhibitor that potently and selectively engage and inhibit the

( = 5 nM)MTH1 IC50

Bioactivity Thiarabine (OSI-7836) shows potent anti-tumor activity andinhibition of synthesisDNA

Bioactivity Triapine is a novel inhibitor of the M2 subunit of ( ) and is a potentribonucleotide reductase RR

radiosensitizer

Bioactivity Triciribine is a inhibitor also inhibits DNA synthesis Aktand with of 130 nM and 002-046 μMHIV-12 IC50respectively

Bioactivity YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding tothe oncogenic transciption factor EWS-FLI1 YK-4-279 inhibitsEwings sarcoma family tumor (ESFT) cell growth YK-4-279induces apoptosis

Bioactivity Zoliflodacin (ETX0914AZD0914) is a novelspiropyrimidinetrione bacterial DNA gyrasetopoisomeraseinhibitor Zoliflodacin has potent antibacterialin vitroactivity against Gram-positive and Gram-negative organismsincluding with the of 025 μgmLS aureus MIC90

TH588 Cat No HY-12814

TH588 hydrochloride Cat No HY-12814A

Thiarabine (OSI-7836) Cat No HY-16496

Triapine (3-AP PAN-811 OCX191 NSC663249) Cat No HY-10082

Triciribine (API-2 NSC 154020 TCN) Cat No HY-15457

YK-4-279 Cat No HY-14507

Zoliflodacin (ETX0914 AZD0914) Cat No HY-17647

Eukaryotic Initiation Factor (eIF)

Eukaryotic initiation factors (eIFs) are proteins involved in theinitiation phase of eukaryotic translation These proteins help stabilizethe formation of the functional ribosome around the start codon andalso provide regulatory mechanisms in translation initiationEukaryotic initiation factor 2B (eIF2B) is a guaninenucleotide-exchange factor which mediates the exchange of GDP(bound to initiation factor eIF2) for GTP thus regenerating the active[eIF2GTP] complex that is required for peptide-chain initiation Theactivity of eIF2B is a key control point for eukaryotic protein synthesisand is altered in response to viral infection hormones nutrientsgrowth factors and certain stresses

Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis oncapped mRNAs in the cytoplasm Eukaryotic initiation factor (elF) 4A functions as a subunit of the initiation factorcomplex elF4F which mediates the binding of mRNA to the ribosome

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Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 2 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Eukaryotic Initiation Factor (eIF) Inhibitors amp Modulators

Bioactivity 4E1RCat is an inhibitor of cap-dependent translation andinhibits interaction with an an of 4 μMeIF4EeIF4GI IC50

Bioactivity 4E2RCat is an inhibitor of interaction with an eIF4E-eIF4G IC50of 135 μM

Bioactivity 4EGI-1 is an inhibitor of interaction with a eIF4EeIF4G Kdof 25 μM against eIF4E binding

Bioactivity Briciclib is a water soluble derivative of ON 013100 and hasthe potential in targeting for solid cancerseIF4E

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic inhibitor with an of 110initiation factor 4A-3 (eIF4A3) IC50

nM

Bioactivity Episilvestrol is a derivative of silvestrol isolated from thefruits and twigs of and is a specificAglaia silvestris

-targeting translation inhibitor with antitumor activityeIF4A

Bioactivity GCN2iB is an ATP-competitive inhibitor of aserinethreonine-protein kinase general control

with an of 24 nMnonderepressible 2 (GCN2) IC50

Bioactivity SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1and disrupts the eIF4F complex

Bioactivity Silvestrol is a eukaryotic translation initiation factor 4A () inhibitor isolated from the fruits and twigs of eIF4A Aglaia

foveolata

4E1RCat Cat No HY-14427

4E2RCat Cat No HY-100733

4EGI-1 Cat No HY-19831

Briciclib (ON 014185) Cat No HY-16366

CCT020312 Cat No HY-119240

eIF4A3-IN-2 Cat No HY-101785

Episilvestrol Cat No HY-15359

GCN2iB Cat No HY-112654

SBI-0640756 (SBI-756) Cat No HY-19560

Silvestrol ((-)-Silvestrol) Cat No HY-13251

G-quadruplex

G-quadruplexes (G-tetrads or G4-DNA) are nucleic acid sequencesthat are rich in guanine and are capable of forming a four-strandedstructure Four guanine bases can associate through Hoogsteenhydrogen bonding to form a square planar structure called a guaninetetrad and two or more guanine tetrads can stack on top of eachother to form a G-quadruplex The quadruplex structure is furtherstabilized by the presence of a cation especially potassium which sitsin a central channel between each pair of tetradsThey can be formedof DNA RNA LNA and PNA and may be intramolecular bimolecularor tetramolecular Depending on the direction of the strands or partsof a strand that form the tetrads structures may be described as

parallel or antiparallel

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Purity 980Clinical Data No Development ReportedSize 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity 9680Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

G-quadruplex Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity APTO-253 is an inducer of andKruppel-like factor 4 (KLF4)also stabilizes with anti-proliferative activityGquadruplex

Bioactivity Phen-DC3 Trifluoromethanesulfonate is a (G4)G-quadruplexspecific ligand which can inhibit and helicasesFANCJ DinGwith s of 65plusmn6 and 50plusmn10 nM respectivelyIC50

Bioactivity Pyridostatin is a stabilizer with a of 490G-quadruplexe KdnM

Bioactivity Pyridostatin hydrochloride is a stabilizer withG-quadruplexea of 490 nMKd

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

APTO-253 (LOR-253 LT-253) Cat No HY-16291

Phen-DC3 Trifluoromethanesulfonate (Phen-DC3 Triflate) Cat No HY-15594A

Pyridostatin (RR82) Cat No HY-15176

Pyridostatin hydrochloride (RR-82 hydrochloride) Cat No HY-15176A

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

Haspin Kinase

Haspin is a protein kinase that regulates chromosome and spindlefunction during mitosis and meiosis Haspin expression is detected infetal liver skin kidney small intestine and in all proliferating cellsHaspin phosphorylates H3 thr3 (H3T3ph) in human cell lines anddepletion of Haspin by RNA interference reveals that Haspin isrequired for H3 thr3 phosphorylation in mitotic cells Phosphorylationof H3T3ph by Haspin is necessary for chromosomal passengercomplex (CPC) accumulation at centromeres H3T3ph then positionsthe CPC at centromeres to regulate selected targets of Aurora Bduring mitosis

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Purity 9956Clinical Data No Development ReportedSize 5 mg

Purity 9812Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Haspin Kinase Inhibitors amp Modulators

Bioactivity CHR-6494 is a potent inhibitor of inhibiting histonehaspinH3T3 phosphorylation with an of 2 nMIC50

Bioactivity LDN-192960 is a potent ( Haspin Haploid Germ Cell-Specific) inhibitor with an of 0010 microMNuclear Protein Kinase IC50

CHR-6494 Cat No HY-15217

LDN-192960 Cat No HY-13455

HDACHistone deacetylases

HDAC (Histone deacetylases) are a class of enzymes that removeacetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid onahistone allowing the histones to wrap the DNA more tightly This isimportant because DNA is wrapped around histones and DNAexpression is regulated by acetylation and de-acetylation Its action isopposite to that of histone acetyltransferase HDAC proteins are nowalso called lysine deacetylases (KDAC) to describe their functionrather than their target which also includes non-histone proteinsTogether with the acetylpolyamine amidohydrolases and the acetoinutilization proteins the histone deacetylases form an ancient proteinsuperfamily known as the histone deacetylase superfamily

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Purity 9600Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9971 Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9896Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

HDAC Inhibitors amp Modulators

Bioactivity Abexinostat (CRA 024781) is a novel pan- inhibitorHDACmostly targeting HDAC1 with of 7 nMKi

Bioactivity ACY-1083 is a selective and brain-penetrating inhibitorHDAC6with an of 3 nM and is 260-fold more selective for HDAC6IC50than all other classes of HDAC isoforms ACY-1083 effectivelyreverses chemotherapy-induced peripheral neuropathy [1]

Bioactivity ACY-738 is a potent selective and orally-bioavailable HDAC6inhibitor with an of 17 nM ACY-738 also inhibitsIC50HDAC1 HDAC2 and HDAC3 with s of 94 128 and 218 nMIC50

Bioactivity ACY-775 is a potent and selective inhibitor of the of histonedeacetylase 6 ( ) with an of 75nMHDAC6 IC50

Bioactivity ACY-957 is a selective inhibitor of and withHDAC1 HDAC2s of 7 nM 18 nM and 1300 nM against HDAC123IC50

respectively and shows no inhibition on HDAC456789

Bioactivity AES-135 is a potent inhibitor inhibits HDAC HDAC3 HDAC6 with s of 654 190 and 636 nM respectivelyHDAC11 IC50

Anti-tumor activity [1]

Bioactivity Belinostat is a potent inhibitor with an of 27 nMHDAC IC50in HeLa cell extracts

Bioactivity Benzenebutyric acid is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity BG45 is an HDAC class I inhibitor with selectivity for HDAC3(IC50 = 289 nM) It inhibits HDAC1 HDAC2 and HDAC6 withgreatly reduced potency (IC50s = 2 22 and gt20 μMrespectively) IC50 value 289 nM (HDAC3) 2 μM (HDAC1) 22μM (HDAC2) gt20 μM (HDAC6) Target HDAC At concentrationshellip

Bioactivity BML-210 is a novel HDAC inhibitor and its mechanism of actionhas not been characterized IC50 value 5 μM[1] Target HDAC4In vitro Cell cycle analysis indicated that HeLa celltreatment with 20 and 30 μM concentration of BML-210 increasedthe proportion of cells in G0G1 phase and causedhellip

Abexinostat (CRA 024781 PCI-24781) Cat No HY-10990

ACY-1083 Cat No HY-111791

ACY-738 Cat No HY-19327

ACY-775 Cat No HY-19328

ACY-957 Cat No HY-104008

AES-135 Cat No HY-114483

Belinostat (PXD101 PX105684) Cat No HY-10225

Benzenebutyric acid (4-Phenylbutyric acid) Cat No HY-A0281

BG45 Cat No HY-18712

BML-210 Cat No HY-19350

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9875Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9906Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BRD 4354 is a moderately potent inhibitor of andHDAC5 with of 085 and 188 μM respectivelyHDAC9 IC s50

Bioactivity BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitorof and with of 085 and 188 μMHDAC5 HDAC9 IC s50

respectively [1]

Bioactivity BRD73954 ia a potent and selective HDAC inhibitor with IC50 of36 nM and 120 nM for HDAC6 and HDAC8 respectively

Bioactivity Bufexamac is a class IIB histone deacetylases (HDAC6 andHDAC10) inhibitor used as an anti-inflammatory agent

Bioactivity CAY10603 (BML-281) is a potent and selective inhibitorHDAC6with an of 2 pM CAY10603 (BML-281) also inhibits HDAC1IC50HDAC2 HDAC3 HDAC8 HDAC10 with s of 271 252 042IC506851 907 nM

Bioactivity CHDI-390576 a potent cell permeable and CNS penetrant class inhibitor with s of 54 nMIIa histonedeacetylase (HDAC) IC50

60 nM 31 nM 50 nM for class IIa HDAC4 HDAC5 HDAC7 HDAC9respectively shows gt500-fold selectivity over class IHDACs (1 2 3) and ~150-fold selectivity over HDAC8 and thehellip

Bioactivity Citarinostat is a HDAC6 specific inhibitor with IC50 of 4 nMand 76 nM for HDAC6 and HDAC3 respectively IC50 value 4 nM(HDAC6) 76 nM (HDAC3) Target HDAC The detailed informationplease refer to WO2015061684A1 and 2015054197A1

Bioactivity CM-675 is a dual and phosphodiesterase 5 (PDE5) class I histone-selective inhibitor with values of 114 nMdeacetylases IC50

and 673 nM for PDE5 and HDAC1 respectively CM-675 haspotential to treat Alzheimerrsquos disease [1]

Bioactivity Corin is a dual inhibitor of histone lysine specificdemethylase and histone deacetylase with a(LSD1) (HDAC)

of 110 nM for LSD1 and an IC of 147 nM forK (inact)i 50HDAC1

Bioactivity CRA-026440 is a potent broad-spectrum inhibitor The HDAC Kivalues against recombinant HDAC isoenzymes HDAC1 HDAC2

and are 4 14 11 15 7 andHDAC3 HDAC6 HDAC8 HDAC1020 nM respectively

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BRD 4354 Cat No HY-112719

BRD 4354 ditrifluoroacetate Cat No HY-112719B

BRD73954 Cat No HY-18700

Bufexamac (Bufexamic acid) Cat No HY-B0494

CAY10603 (BML-281) Cat No HY-18613

CHDI-390576 Cat No HY-119939

Citarinostat (ACY241) Cat No HY-15994

CM-675 Cat No HY-114303

Corin Cat No HY-111048

CRA-026440 Cat No HY-19754

wwwMedChemExpresscom 69

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in Ethanol

2 mg 5 mg 10 mg 50 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9809Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9959Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity CUDC-101 is a potent inhibitor of and withHDAC EGFR HER2s of 44 24 and 157 nM respectivelyIC50

Bioactivity Dacinostat is a potent inhibitor with an of 32 nMHDAC IC50Dacinostat also inhibits with an of 9 nM and usedHDAC1 IC50in cancer research

Bioactivity Domatinostat (4SC-202 free base) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Domatinostat tosylate (4SC-202) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Droxinostat(NS41080) is a selective inhibitor of HDAC3 HDAC6and HDAC8 with IC50 of 169 247 and 146 μM respectivelygt 8-fold selective against HDAC3 and no inhibition toHDAC1 2 4 5 7 9 and 10 IC50 Value 169 μM(HDAC3) 247μM(HDAC6) 146 μM(HDAC8) Target HDAC368 in vitrohellip

Bioactivity EDO-S101 is a pan inhibitor inhibits HDAC1 HDAC2 andHDACHDAC3 with values of 9 9 and 25 nM respectivelyIC50

Bioactivity Entinostat is an oral and selective class I inhibitorHDACwith s of 243 nM 453 nM and 248 nM for IC50 HDAC1 HDAC2

and respectivelyHDAC3

Bioactivity Fimepinostat (CUDC-907) potently inhibits class I s as wellPI3Kas classes I and II enzymes with an of 195439 nMHDAC IC50and 17501828 nM for PI3KαPI3KβPI3Kδ andHDAC1HDAC2HDAC3HDAC10 respectively

Bioactivity FT895 is a potent and selective inhibitor with an HDAC11 IC50

of 3 nM [1]

Bioactivity Givinostat (ITF-2357) is a inhibitor with an of 198HDAC IC50and 157 nM for and respectivelyHDAC1 HDAC3

CUDC-101 Cat No HY-10223

Dacinostat (NVP-LAQ824 LAQ824) Cat No HY-13606

Domatinostat (4SC-202 (free base)) Cat No HY-16012A

Domatinostat tosylate (4SC-202) Cat No HY-16012

Droxinostat (NS 41080) Cat No HY-13267

EDO-S101 (Tinostamustine) Cat No HY-101780

Entinostat (MS-275 SNDX-275) Cat No HY-12163

Fimepinostat (CUDC-907) Cat No HY-13522

FT895 Cat No HY-112285

Givinostat (ITF-2357) Cat No HY-14842

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9849Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9609Clinical Data LaunchedSize 2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Bioactivity Givinostat hydrochloride (ITF-2357 hydrochloride) is a HDACinhibitor with an of 198 and 157 nM for andIC50 HDAC1

respectivelyHDAC3

Bioactivity Givinostat hydrochloride monohydrate (ITF-2357 hydrochloridemonohydrate) is a inhibitor with an of 198 and 157HDAC IC50nM for and respectivelyHDAC1 HDAC3

Bioactivity HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2008040934 A1

Bioactivity HDAC-IN-4 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2007045844 A1 20070426

Bioactivity HDAC-IN-5 is a histone deacetylase inhibitor(HDAC) Bioactivity HDAC-IN-7 (Chidamide impurity) is an impurity of ChidamideChidamide is a potent and orally bioavailable HDAC enzymesclass I (HDAC123) and class IIb (HDAC10) inhibitor

Bioactivity HDAC6-IN-1 is a potent and selective inhibitor for withHDAC6an of 17 nM and shows 25-fold and 200-fold selectivityIC50relative to ( =422 nM) and ( =3398 nM)HDAC1 IC50 HDAC8 IC50respectively

Bioactivity HDAC8-IN-1 is a inhibitor with an of 272 nMHDAC8 IC50

Bioactivity HDACsmTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs)and targetmammalian target of Rapamycin (mTOR)inhibitor for treating hematologic malignancies with ofIC s50019 nM 18 nM 12 nM and gt500 nM for HDAC1 HDAC6 mTORand PI3Kα respectively HDACsmTOR Inhibitor 1 stimulateshellip

Bioactivity HPOB is a highly potent and selective inhibitor of histonedeacetylase 6 (HDAC6) with IC50 of 56 nM gt30 fold lesspotent against other HDACs target HDAC6 [1] IC 50 56nM [1]In vitro HPOB causes growth inhibition of normal andtransformed cells but does not induce cell death HPOBhellip

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Givinostat hydrochloride (ITF-2357 hydrochloride) Cat No HY-14842A

Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) Cat No HY-14842B

HDAC-IN-3 Cat No HY-19772

HDAC-IN-4 (CXD101) Cat No HY-100748

HDAC-IN-5 Cat No HY-18362

HDAC-IN-7 (Chidamide impurity) Cat No HY-13592

HDAC6-IN-1 Cat No HY-18947

HDAC8-IN-1 Cat No HY-111342

HDACsmTOR Inhibitor 1 Cat No HY-114414

HPOB Cat No HY-19747

wwwMedChemExpresscom 71

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg 100 mg

Bioactivity IDO1 and HDAC1 Inhibitor (Compound 10) is a dual andIDO1 inhibitor with s of 690 nM and 665 nMHDAC1 IC50

respectively [1]

Bioactivity ITSA-1 is membrane permeable and specifically suppresses TSAinhibition of HDAC (histone deacetylase) but not other HDACinhibitors

Bioactivity J22352 is a PROTAC (proteolysis-targeting chimeras)-like andhighly selective inhibitor with an value of 47HDAC6 IC50nM J22352 promotes HDAC6 degradation and induces anticancereffects by inhibiting autophagy and eliciting the antitumorimmune response in glioblastoma cancers and leading to thehellip

Bioactivity JAKHDAC-IN-1 is a potent dual inhibitor exhibitsJAK2HDACantiproliferative and proapoptotic activities in severalhematological cell lines JAKHDAC-IN-1 shows s of 4 and 2IC50

nM for JAK2 and HDAC respectively [1]

Bioactivity LMK-235 is a potent and selective inhibitor inhibitsHDAC45HDAC5 HDAC4 HDAC6 HDAC1 HDAC2 HDAC11 and HDAC8 with

s of 422 nM 119 nM 557 nM 320 nM 881 nM 852 nM andIC501278 nM respectively and is used in cancer research

Bioactivity M344 (D 237) is an inhibitor of ( =100histone deacetylase IC50nM) and an inducer of terminal cell fifferentiation

Bioactivity MC1568 is a selective class II (IIa) histone deacetylas () inhibitor used for cancer researchHDAC II

Bioactivity Mocetinostat (MGCD0103) is a potent orally active andisotype-selective inhibitor with s ofHDAC (Class IIV) IC50015 029 166 and 059 μM for andHDAC1 HDAC2 HDAC3

respectively Mocetinostat shows no inhibition onHDAC11HDAC4 HDAC5 HDAC6 HDAC7 or HDAC8

Bioactivity Nanatinostat (CHR-3996) is a potent class I selective andorally active inhibitor with anhistone deacetylase (HDAC)

of 8 nM IC50[1]

Bioactivity Nexturastat A is a potent and selective HDAC6 inhibitor withIC50 of 5 nM no inhibition on other HDAC forms

IDO1 and HDAC1 Inhibitor Cat No HY-112147

ITSA-1 Cat No HY-100508

J22352 Cat No HY-126147

JAKHDAC-IN-1 Cat No HY-126141

LMK-235 Cat No HY-18998

M344 (D 237 MS 344) Cat No HY-13506

MC1568 Cat No HY-16914

Mocetinostat (MGCD0103) Cat No HY-12164

Nanatinostat (CHR-3996) Cat No HY-13432

Nexturastat A Cat No HY-16699

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9907Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9867Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9797Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NKL 22 is a HDAC inhibitor The value of IC 50 is 78 uM NKL 22increase frataxin protein concentrations NKL 22 inhibitorsincrease FXN mRNA in FRDA lymphocytes HDAC inhibitors actdirectly on FXN [1]

Bioactivity Oxamflatin (Metacept-3) is a potent inhibitor with anHDAC of 157 nMIC50

Bioactivity Panobinostat is a non-selective histone deacetylase ( )HDACinhibitor

Bioactivity PCI-34051 is a potent and selective inhibitor with HDAC8 IC50of 10 nM with gt200-fold selectivity over the other HDACisoforms

Bioactivity PI3KHDAC-IN-1 is a potent dual inhibitor of PI3KHDACpotently inhibits PI3Kδ and HDAC1 with s of 81 nM and 14IC50

nM respectively [1]

Bioactivity Pimelic diphenylamide 106 is a slow tight-binding inhibitorof class I HDAC (HDAC 1 2 and 3 with IC50 values of 150 nM 760nM and 370 nM respectively) demonstrating no activityagainst class II HDACs

Bioactivity Pracinostat is a potent inhibitorhistone deacetylase (HDAC)with s of 40-140 nM used for cancer researchIC50

Bioactivity PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDACPTACH exerts potent growth inhibition against various humancancer cells with EC50 values ranging from 1 to 10 μM

Bioactivity Quisinostat (JNJ-26481585) is an orally available potent inhibitor with an of 011 nM for HDAC1HDAC IC50

Bioactivity Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of which is under developmenthistone deacetylase enzymes (HDAC)

for the treatment of cutaneous T-cell lymphoma [1]

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NKL 22 Cat No HY-100384

Oxamflatin (Metacept-3) Cat No HY-102033

Panobinostat (LBH589 NVP-LBH589) Cat No HY-10224

PCI-34051 Cat No HY-15224

PI3KHDAC-IN-1 Cat No HY-128582

Pimelic Diphenylamide 106 (RGFA-8 TC-H 106 Histone Deacetylase Inhibitor VII) Cat No HY-19348

Pracinostat (SB939) Cat No HY-13322

PTACH (NCH-51) Cat No HY-12954

Quisinostat (JNJ-26481585) Cat No HY-15433

Remetinostat (SHP-141) Cat No HY-100365

wwwMedChemExpresscom 73

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9970Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Bioactivity Resminostat is a potent inhibitor of andHDAC1 HDAC3 with mean values of 425 501 718 nMHDAC6 IC50

respectively and shows less potent activities against HDAC8with an of 877 nMIC50

Bioactivity Resminostat hydrochloride is a potent inhibitor of HDAC1 and with mean values of 425 501 718HDAC3 HDAC6 IC50

nM respectively and shows less potent activities againstHDAC8 with an of 877 nMIC50

Bioactivity RG2833 is a brain-penetrant inhibitor with of 60 nMHDAC IC50and 50 nM for HDAC1 and HDAC3 respectively

Bioactivity RGFP966 is a highly selective inhibitor with an ofHDAC3 IC5080 nM and shows no inhibition to other HDACs at concentrationsup to 15 μM

Bioactivity Ricolinostat (ACY-1215) is a potent and selective HDAC6inhibitor with an of 5 nM ACY-1215 also inhibitsIC50

and with s of 58 48 and 51 nMHDAC1 HDAC2 HDAC3 IC50respectively

Bioactivity Romidepsin is a potent and inhibitor with sHDAC1 HDAC2 IC50of 36 and 47 nM respectively

Bioactivity RTS-V5 is a dual inhibitor with s ofHDACproteasome IC5069 18 15 027 053 μM for HDAC1 HDAC2 HDAC3 HDAC6HDAC8 respectively

Bioactivity Santacruzamate A (CAY-10683) is a potent and selective HDAC2inhibitor with an of 119 pM IC50

[1]

Bioactivity Scriptaid is a potent inhibitorhistone deacetylase (HDAC)used in cancer research

Bioactivity Sinapinic acid (Sinapic acid) is a phenolic compound isolatedfrom Jack Rhizome acts as anHydnophytum formicaruminhibitor of with an of 227 mM and alsoHDAC IC50

[1]

inhibits activity Sinapinic acid posssess pothellipACE-I [2]

Resminostat (RAS2410 4SC-201) Cat No HY-14718

Resminostat hydrochloride (RAS2410 hydrochloride 4SC-201 hydrochloride) Cat No HY-14718A

RG2833 (RGFP109) Cat No HY-16425

RGFP966 Cat No HY-13909

Ricolinostat (ACY-1215 Rocilinostat) Cat No HY-16026

Romidepsin (FK 228 FR 901228 NSC 630176) Cat No HY-15149

RTS-V5 Cat No HY-112908

Santacruzamate A (CAY-10683) Cat No HY-N0931

Scriptaid (Scriptide GCK1026) Cat No HY-15489

Sinapinic acid (Sinapic acid) Cat No HY-W009732

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg

Purity 9800Clinical Data Phase 3Size 10mM x 1mL in Water

1 g 5 g 500 g

Bioactivity Butyric acid is a inhibitor withhistone deacetylase (HDAC)anti-tumor effects in several cancers

Bioactivity Sodium phenylbutyrate is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity SR-4370 is an inhibitor of with s of 013 μM 058HDAC IC50μM 0006 μM 23 μM and 34 μM for HDAC1 HDAC2 HDAC3HDAC8 and HDAC6 respectively

Bioactivity ST8154AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity ST8155AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity Sulforaphane is an isothiocyanate present naturally in widelyconsumed vegetables has shown anticancer and cardioprotectiveactivities

Bioactivity SW-100 a selective inhibitorhistone deacetylase 6 (HDAC6)with an of 23 nM shows at least 1000-fold selectivityIC50for HDAC6 relative to all other HDAC isozymes SW-100 displaysa significantly improved ability to cross hellip

Bioactivity Tacedinaline (N-acetyldinaline) is an inhibitor of the histonedeacetylase ( ) with s of 09 09 12 μM forHDAC IC50recombinant HDAC 1 2 and 3 respectively

Bioactivity Tasquinimod is an oral antiangiogenic agent in clinical trialsfor the treatment of castration-resistant prostate cancerTasquinimod binds to the regulatory Zn binding domain of2+

with of 10-30 nMHDAC4 Kd

Bioactivity TH34 an inhibitor with s of 46 μM 19HDAC6 8 10 IC50μM and 77 μM respectively shows high selectivity overHDAC123 [1]

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Sodium Butyrate (Butanoic acid sodium salt) Cat No HY-B0350A

Sodium phenylbutyrate (Sodium 4-phenylbutyrate TriButyrate) Cat No HY-15654

SR-4370 Cat No HY-111400

ST8154AA1 Cat No HY-112805

ST8155AA1 Cat No HY-112806

Sulforaphane Cat No HY-13755

SW-100 Cat No HY-115475

Tacedinaline (N-acetyldinaline CI-994 Goe-5549) Cat No HY-50934

Tasquinimod (ABR-215050) Cat No HY-10528

TH34 Cat No HY-111818

wwwMedChemExpresscom 75

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g 25 g

Purity 9867Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g 25 g

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9887Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TMP195 is a selective class IIa histone deacetylase ( )HDACinhibitor with s of 59 60 26 15 nM for HDAC4 HDAC5KiHDAC7 and HDAC9 respectively

Bioactivity TMP269 is a novel and selective class IIa histone deacetylase inhibitor with s of 157 nM 97 nM 43 nM and 23 nM(HDAC) IC50

for HDAC4 HDAC5 HDAC7 and HDAC9 respectively

Bioactivity Trichostatin A is a potent and specific inhibitor of HDAC with an value of 18 nM for HDACclass III IC50

Bioactivity Tubacin is a potent and selective inhibitor of with anHDAC6 value of 4 nM and approximately 350-fold selectivity overIC50

HDAC1

Bioactivity Tubastatin A (Hydrochloride) is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tubastatin-A is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tucidinostat is a potent and orally bioavailable enzymesHDACclass I ( ) and class IIb ( ) inhibitor withHDAC123 HDAC10

s of 95 160 67 and 78 nM less active on HDAC8 andIC50HDAC11 ( s 733 nM 432 nM respectively) and showshellipIC50

Bioactivity UF010 is a potent and selective HDAC inhibitor with IC50 ~006μM 01 μM 05 μM and 15 μM for HDACs 3 2 1 and 8respectively It has gt 6-fold selectivity over other HDACsIC50 value 006 μM (HDAC3) 01 μM (HDAC2) 05 μM (HDAC1)15 μM(HDAC 8) Target HDAC in vitro UF010 is a competitivehellip

Bioactivity Valproic acid is an inhibitor with in the range ofHDAC IC5005 and 2 mM also inhibits ( 400 μM) andHDAC1 IC50induces proteasomal degradation of Valproic acidHDAC2sodium salt is used in the treatment of epilepsy bipohellip

Bioactivity Valproic acid sodium salt is an anticonvulsants used to treatepilepsy bipolar disorder and migraines Valproic acidinhibits with an of 04 mMhistone deacetylase 1 (HDAC1) IC50

TMP195 Cat No HY-18361

TMP269 Cat No HY-18360

Trichostatin A (TSA) Cat No HY-15144

Tubacin Cat No HY-13428

Tubastatin A Hydrochloride (Tubastatin A HCl TSA HCl) Cat No HY-13271

Tubastatin-A Cat No HY-13271A

Tucidinostat (Chidamide HBI-8000 CS 055) Cat No HY-109015

UF010 Cat No HY-18976

Valproic acid (VPA 2-Propylpentanoic Acid) Cat No HY-10585

Valproic acid sodium salt (Sodium Valproate) Cat No HY-10585A

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

250 mg 500 mg 1 g 5 g

Bioactivity Vorinostat is a potent and orally available inhibitor of and andHDAC1 HDAC2 HDAC3 (Class I) HDAC7 (Class II)

with values of 10 nM and 20 nM forHDAC11 (Class IV ) ID50HDAC1 and HDAC3 respectively

Bioactivity WT-161 is a potent and selective inhibitor with an HDAC6 IC50of 040 nM

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Vorinostat (SAHA) Cat No HY-10221

WT-161 Cat No HY-100871

wwwMedChemExpresscom 77

HSPHeat shock proteins

HSP (Heat shock proteins) are a group of proteins induced by heatshock the most prominent members of this group are a class offunctionally related proteins involved in the folding and unfolding ofother proteins HSP expression is increased when cells are exposed toelevated temperatures or other stress This increase in expression istranscriptionally regulated The dramatic upregulation of the heatshock proteins is a key part of the heat shock response and is inducedprimarily by heat shock factor (HSF) HSPs are found in virtually allliving organisms from bacteria to humans Heat shock proteinsappear to serve a significant cardiovascular role Hsp90 Hsp84Hsp70 Hsp27 Hsp20 and alpha B crystallin all have been reported as

having roles in the cardiovasculature

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 g

Purity 9997Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9932Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 1 mg

HSP Inhibitors amp Modulators

Bioactivity Alvespimycin is a potent inhibitor of binding to Hsp90Hsp90with an of 62 plusmn 29 nMEC50

Bioactivity Alvespimycin hydrochloride is a potent inhibitor of Hsp90binding to Hsp90 with of 62plusmn29 nMEC50

Bioactivity Apoptozole is an inhibitor of the ATPase domain of andHsc70 with s of 021 and 014 μM respectively and canHsp70 Kd

induce apoptosis

Bioactivity Arimoclomol maleate (BRX-220) is a co-inducer of heat shockproteins ( )HSP

Bioactivity BIIB021 is an orally available fully synthetic inhibitor of with and of 17 nM and 38 nM respectivelyHSP90 Ki EC50

Bioactivity Bimoclomol is a coinducer used forheat shock protein (HSP)treatment of cardiovascular diseases

Bioactivity CCT251236 is an orally available pirin ligand from a heatshock transcription factor 1 (hsf1) phenotypic screen with an

of 19 nM for inhibition of HSF1-mediated IC50 HSP72

induction

Bioactivity Col003 is a potent inhibitor of competitively binds toHsp47the collagen binding site on Hsp47 ( 18 μM) andIC50inhibits collagen secretion by destabilizing the collagentriple helix [1]

Bioactivity Debio 0932 is an orally active inhibitor with s ofHSP90 IC50100 and 103 nM for HSP90α and HSP90β respectively

Bioactivity Ethoxyquin is an antioxidant which has been used in animalfeed for many years and also an inhibitor of heat shock

( )protein 90 Hsp90

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Alvespimycin (17-DMAG NSC 707545) Cat No HY-10389

Alvespimycin hydrochloride (17-DMAG hydrochloride KOS-1022 BMS 826476) Cat No HY-12024

Apoptozole (Apoptosis Activator VII) Cat No HY-15098

Arimoclomol maleate (BRX-220) Cat No HY-106443A

BIIB021 (CNF2024) Cat No HY-10212

Bimoclomol Cat No HY-U00398

CCT251236 Cat No HY-101026

Col003 Cat No HY-124817

Debio 0932 (CUDC-305) Cat No HY-13469

Ethoxyquin Cat No HY-B1425

wwwMedChemExpresscom 79

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9994Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Bioactivity Feretoside a phenolic compound extracted from the barks of E is a which act as cytoprotectiveulmoides HSP inducer

agent

Bioactivity Ganetespib is a heat shock protein 90 ( ) inhibitorHSP90which exhibits potent cytotoxicity in a wide variety ofhematological and solid tumor cell lines

Bioactivity Geldanamycin is a inhibitor with antimicrobial activityHsp90against many Gram-positive and some Gram-negative bacteria

Bioactivity Grp94 Inhibitor-1 is a potent selective inhibitor withGrp94an value of 2 nM and over 1000-fold selectivity to Grp94IC50

against Hsp90α [1]

Bioactivity HA15 a molecule that targets specifically BiP GRP78 HSPA5inhibits the ATPase activity of BiP HA15 strongly increasesBiP protein expression in A375 melanoma cells [1]

Bioactivity HSF1A is a cell-permeable activator of heat shocktranscription factor 1 ( )HSF1

Bioactivity HSP70-IN-1 is a heat shock protein ( ) inhibitor inhibitsHSPthe growth of Kasumi-1 cells with an of 23 μMIC50

Bioactivity JG-98 is an allosteric heat shock protein 70 (Hsp70)inhibitor with anti-cancer activities which disrupts Hsp70

and affects signalinginteraction with a co-chaperone Bag3pathways important for cancer development [1] [2] [3]

Bioactivity KNK437 is a inhibitor and inhibits the induction ofHSPHSP105 HSP70 and HSP40

Bioactivity KRIBB11 is an inhibitor of withHeat shock factor 1 (HSF1) of 12 μMIC50

Feretoside Cat No HY-N6249

Ganetespib (STA-9090) Cat No HY-15205

Geldanamycin Cat No HY-15230

Grp94 Inhibitor-1 Cat No HY-112910

HA15 Cat No HY-100437

HSF1A Cat No HY-103000

HSP70-IN-1 Cat No HY-12622

JG-98 Cat No HY-117282

KNK437 (Heat Shock Protein Inhibitor I) Cat No HY-100110

KRIBB11 Cat No HY-100872

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 100 mg

Purity 9569Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9914Clinical Data Phase 2Size 5 mg 10 mg 25 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity KU-32 is a novel novobiocin-based inhibitor that canHsp90protect against neuronal cell death

Bioactivity KW-2478 is an inhibitor of with an of 38 nMHsp90α IC50and has antitumor activity against various human hematologicaltumor cells

Bioactivity Luminespib (NVP-AUY922) is a potent inhibitor withHSP90s of 78 and 21 nM for HSP90α and HSP90β respectivelyIC50

Bioactivity MKT-077 is a rhodacyanine dye and also a heat shock protein 70( ) inhibitor which exhibits significant antitumorHsp70activity

Bioactivity NVP-HSP990 is a potent and selective inhibitor withHsp90 values of 06 08 and 85 nM for Hsp90α Hsp90β andIC50

Grp94 respectively

Bioactivity Onalespib (AT13387) is a potent inhibitor of with aHsp90 of 071 nMKd

Bioactivity p5 Ligand for Dnak and DnaJ is a nonapeptide whichcorresponds to the main binding site for the 23-residue partof the presequence of mitochondrial aspartateaminotransferase p5 Ligand for Dnak and DnaJ is ahigh-affinity ligand for DnaK and DnaJ [1]

Bioactivity Pifithrin-μ is an inhibitor of and with antitumorp53 HSP70and neuroprotective activity

Bioactivity PU-WS13 is a selective inhibitor with an ofGrp94 EC50022 μM

Bioactivity Retaspimycin is a potent and water-soluble inhibitor of with s of 119 nM for both Hsp90 and Grp9Hsp90 EC50

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KU-32 Cat No HY-108248

KW-2478 Cat No HY-13468

Luminespib (NVP-AUY922 AUY922 VER-52296) Cat No HY-10215

MKT-077 (FJ-776) Cat No HY-15096

NVP-HSP990 (HSP-990) Cat No HY-15190

Onalespib (AT13387) Cat No HY-14463

p5 Ligand for Dnak and DnaJ Cat No HY-P1887

Pifithrin-μ (PFTμ 2-Phenylethynesulfonamide) Cat No HY-10940

PU-WS13 Cat No HY-18680

Retaspimycin Cat No HY-15263

wwwMedChemExpresscom 81

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9740Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9982Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9903Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Retaspimycin Hydrochloride is a potent and water-solubleinhibitor of with s of 119 nM for both Hsp90 andHsp90 EC50Grp9

Bioactivity Shepherdin (79-87) is amino acids 79 to 87 fragment ofShepherdin Shepherdin is a peptidomimetic antagonist of thecomplex between Hsp90 and Survivin Anticancer activity [1]

Bioactivity SNX-5422 Mesylate (PF-04929113 Mesylate) a prodrug ofSNX-2112 is an orally active inhibitor with a ofHsp90 Kd41 nM and also induces Her-2 degradation with an ofIC5037nM

Bioactivity Tanespimycin (17-AAG) is a potent inhibitor with anHSP90 of 5 nM having a 100-fold higher binding affinity forIC50

tumour cell derived HSP90 than normal cell derived HSP90

Bioactivity TAS-116 is an oral bioavailable ATP-competitive highlyspecific inhibitor ( s of 347 nM and 213HSP90αHSP90β KinM respectively) without inhibiting other HSP90 familyproteins such as GRP94 TAS-116 demonstrates less ocuhellip[1]

Bioactivity Teprenone is a anti-ulcer drug and works as an inducer ofheat shock proteins ( )HSPs

Bioactivity TRC051384 is a heat shock protein 70 ( ) inducerHSP70 Bioactivity VER-155008 is an inhibitor of with s of 05 μMHsp70 IC5026 μM and 26 μM for Hsc70 and Grp7 respectivelyHsp70and with a of 03 μM for Kd Hsp70

Bioactivity VER-49009 is a inhibitor with an of 25 nM and aHsp90 IC50 of 78 nMKd

Bioactivity VER-50589 is a inhibitor with an of 21 nM and aHsp90 IC50 of 45 nMKd

Retaspimycin Hydrochloride (IPI-504) Cat No HY-10210

Shepherdin 79-87 Cat No HY-P1750

SNX-5422 Mesylate (PF-04929113 (Mesylate)) Cat No HY-10213A

Tanespimycin (17-AAG NSC 330507 CP 127374) Cat No HY-10211

TAS-116 Cat No HY-15785

Teprenone (Geranylgeranylacetone) Cat No HY-B0779

TRC051384 Cat No HY-101712

VER-155008 Cat No HY-10941

VER-49009 (CCT 129397) Cat No HY-15986

VER-50589 Cat No HY-15984

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9924Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity VER-82576 (NVP-BEP800) is a potent orally available andselective inhibitor with an of 58 nM for Hsp90βHsp90 IC50VER-82576 also slightly blocks Grp94 and Trap-1 with s ofIC5041 and 55 μM respectively

Bioactivity XL888 is a heat shock protein-90 ( ) inhibitor with anHSP90 of 24 nMIC50

Bioactivity YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathwayagainst glioblastoma directly binding to heat shock protein

with an of 820 nM on NFAT nuclear90 (HSP90) IC50translocation YZ129-induced GBM cell-cycle arrest at the G2Mphase promotes apoptosis and inhibited tumor cellhellip

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VER-82576 (NVP-BEP800) Cat No HY-10942

XL888 Cat No HY-13313

YZ129 Cat No HY-114413

wwwMedChemExpresscom 83

IRE1Inositol requiring enzyme 1

The serinethreonine-protein kinaseendoribonucleaseinositol-requiring enzyme 1 (IRE1) is an enzyme that in humans isencoded by the gene IRE1 is an endoplasmic reticulum (ER)ERN1transmembrane sensor that activates UPR to maintain ER and cellularfunction While mammalian IRE1 promotes cell survive it can initiateapoptosis via decay of anti-apoptotic microRNAsIRE1 activation is initiated by homotypic interactions of thestress-sensing lumenal domain favoring transautophosphorylation ofthe kinase-extension nuclease (KEN) domain on the cytoplasmic sideof the ER membraneIRE1XBP-1 has been shown to regulate a variety of genes in various

cell types in response to ER stress mostly related to ER function and the secretory pathway although the target genesvary depending on the cell type and nature of the stress stimuli

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9875Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg

IRE1 Inhibitors amp Modulators

Bioactivity 36-DMAD hydrochloride is a inhibitor of the pathwayIRE1α-XBP1of the unfolded protein response

Bioactivity 4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor ofIRE1α

Bioactivity 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1αinhibitor with an of 008 μM extracted from patent WOIC502008154484 A1 IRE-lα inhibitor compound 3-5

Bioactivity APY29 is an allosteric modulator of which inhibits IRE1αIRE1αautophosphorylation with of 280 nM and activates IRE1αIC50RNase activity

Bioactivity B I09 is an RNase inhibitor with an of 1230 nMIRE-1 IC50 Bioactivity GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1alpha ( ) which can inhibit and IRE1α IRE1α kinase activity RNase

with s of 20 and 200 nM respectivelyactivity IC50

Bioactivity GSK2850163 hydrochloride is a novel inhibitor ofinositol-requiring enzyme-1 alpha ( ) which can inhibitIRE1α

and with s of 20 andIRE1α kinase activity RNase activity IC50200 nM respectively

Bioactivity KIRA6 allosterically inhibits activity withIRE1α RNase kinasean of 06 microMIC50

Bioactivity Kira8 is a mono-selective inhibitor that allostericallyIRE1αattenuates with an of 59 nM IRE1α RNase activity IC50

[1]Bioactivity MKC3946 is a potent and soluble inhibitor used forIRE1α

cancer research

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36-DMAD hydrochloride Cat No HY-U00460

4μ8C (IRE1 Inhibitor III) Cat No HY-19707

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) Cat No HY-107371

APY29 Cat No HY-17537

B I09 Cat No HY-107400

GSK2850163 Cat No HY-U00459

GSK2850163 hydrochloride Cat No HY-U00459B

KIRA6 Cat No HY-19708

Kira8 Cat No HY-114368

MKC3946 Cat No HY-19710

wwwMedChemExpresscom 85

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity MKC8866 is an inhibitor with an of less thanIRE1 RNase IC5001 μM for IRE1α RNase

Bioactivity MKC9989 is a ( ) inhibitor and alsoHydroxy aryl aldehydes HAAinhibits with an of 023 to 44 μMIRE1α IC50

Bioactivity STF-083010 is an inhibitor STF-083010 inhibits Ire1Ire1endonuclease activity without affecting its kinase activityafter endoplasmic reticulum stress

MKC8866 Cat No HY-104040

MKC9989 Cat No HY-12399

STF-083010 Cat No HY-15845

Kinesin

Kinesin is a protein belonging to a class of motor proteins found ineukaryotic cells Kinesins move along microtubule filaments and arepowered by the hydrolysis of ATP (thus kinesins are ATPases) Theactive movement of kinesins supports several cellular functionsincluding mitosis meiosis and transport of cellular cargo Mostkinesins walk towards the plus end of a microtubule entailstransporting cargo from the centre of the cell towards the peripheryKinesins were discovered as microtubule (MT)-based anterogradeintracellular transport motors The founding member of thissuperfamily the genomes of mammals encode more than 40 kinesinproteins organized into at least 14 families named kinesin-1 through

kinesin-14

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wwwMedChemExpresscom 87

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9871Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9973Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Kinesin Inhibitors amp Modulators

Bioactivity (R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of ARRY-520(R)-Filanesib ((R)-ARRY-520) is a synthetic kinesin spindle

inhibitor with of 6 nMprotein (KSP) IC50

Bioactivity AZ82 is a selective kinesin-like protein KIFC1 (HSETKIFC1)inhibitor with a of 43 nM and an of 300 nM for KIFC1Ki IC50

Bioactivity CW-069 is an allosteric inhibitor of microtubule motor with an of 75 μMprotein HSET IC50

Bioactivity Dimethylenastron is a potent inhibitor with ankinesin Eg5 of 200 nMIC50

Bioactivity Eg5 Inhibitor V trans-24 is a potent and specific kinesin Eg5inhibitor with an of 065 μM and can be used in theIC50research of cancer

Bioactivity EMD534085 is a potent and selective inhibitor of the mitotic with an of 8 nMkinesin-5 IC50

Bioactivity Filanesib (ARRY-520) is a synthetic kinesin spindle protein inhibitor with of 6 nM(KSP) IC50

Bioactivity Ispinesib is a specific inhibitor of kinesin spindle protein with a of 17 nM(KSP) Ki app

Bioactivity K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5with an of 13 μMIC50

Bioactivity Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member and is used for the research of cellular15 (Kif15)

proliferative diseases

(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A

AZ82 Cat No HY-12241

CW-069 Cat No HY-15857

Dimethylenastron Cat No HY-19944

Eg5 Inhibitor V trans-24 Cat No HY-112915

EMD534085 Cat No HY-15000

Filanesib (ARRY-520) Cat No HY-15187

Ispinesib (SB-715992) Cat No HY-50759

K858 Racemic Cat No HY-19966

Kif15-IN-1 Cat No HY-15948

Purity 9731Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9705Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg

Purity 9959Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9651Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Kif15-IN-2 is an inhibitor of the mitotic and iskinesin Kif15used for the research of cellular proliferative diseases

Bioactivity Litronesib is a selective mitosis-specific kinesin Eg5inhibitor with antitumor activity

Bioactivity Litronesib (Racemate) is the racemate of litronesibLitronesib is a selective allosteric inhibitor of kinesin

Eg5

Bioactivity Monastrol is a potent and cell-permeable inhibitor of themitotic with an value of 14 μMkinesin Eg5 IC50

Bioactivity Paprotrain is a cell-permeable inhibitor of the kinesin inhibits the ATPase activity of MKLP-2 with an MKLP-2 IC50

of 135 μM and a of 336 μM and shows a moderate inhibitionKiactivity on with an of 55 μMDYRK1A IC50

Bioactivity PF-2771 is a potent and selective centromere protein E inhibitor inhibiting CENP-E motor activity with an(CENP-E)

of 161 nM PF-2771 is used as an anticancer agentIC50

Bioactivity SB-743921 is a potent inhibitor of the mitotic kinesin KSP with a of 01 nM(Eg5) Ki

88 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Kif15-IN-2 Cat No HY-15949

Litronesib (LY-2523355 KF-89617) Cat No HY-14846

Litronesib Racemate (LY-2523355 Racemate KF-89617 Racemate) Cat No HY-14846A

Monastrol ((plusmn)-Monastrol) Cat No HY-101071A

Paprotrain Cat No HY-101298

PF-2771 Cat No HY-19530

SB-743921 Cat No HY-12069

wwwMedChemExpresscom 89

LIM Kinase (LIMK)LIMKs

LIM kinases (LIMKs) are important cell cytoskeleton regulators thatplay a prominent role in cancer manifestation and neuronal diseasesThe LIMK family consists of two homologues LIMK1 and LIMK2which differ from one another in expression profile intercellularlocalization and function The main substrate of LIMK is cofilin amember of the actin-depolymerizing factor (ADF) protein familyWhen phosphorylated by LIMK cofilin is inactive LIMKs play acontributory role in several neurodevelopmental disorders and incancer growth and metastasisLIM domain kinases (LIMK1 and 2) are substrate for Cdc42Rac-PAKand modulate actin dynamics by phosphorylating cofilin at serine-3

This modification inactivates cofilinrsquos actin severing and depolymerizing activity LIMKs also translocate into thenucleus and regulate cell cycle progression LIMKs are potential therapeutic targets for NF2 and other merlin-deficienttumors

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

LIM Kinase (LIMK) Inhibitors amp Modulators

Bioactivity BMS-3 is a potent inhibitor with s of 5 nM and 6LIMK IC50nM for and respectivelyLIMK1 LIMK2

Bioactivity BMS-5 (LIMKi 3) is a potent inhibitor with s of 7LIMK IC50nM and 8 nM for and respectivelyLIMK1 LIMK2

Bioactivity R-10015 a broad-spectrum antiviral compound for HIVinfection acts as a potent and selective inhibitor of LIM

and binds to the ATP-binding pocketdomain kinase (LIMK)with an of 38 nM for human LIMK1 IC50

[1]

Bioactivity T56-LIMKi is a selective inhibitor of inhibits theLIMK2growth of Panc-1 cells with an of 352 μMIC50

90 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

BMS-3 Cat No HY-18304

BMS-5 (LIMKi 3) Cat No HY-18305

R-10015 Cat No HY-120097

T56-LIMKi (T5601640) Cat No HY-19352

wwwMedChemExpresscom 91

MicrotubuleTubulin

Microtubules are a component of the cytoskeleton found throughoutthe cytoplasm These tubular polymers of tubulin can grow as long as50 micrometres with an average length of 25 microm and are highlydynamic The outer diameter of a microtubule is about 24 nm whilethe inner diameter is about 12 nm Microtubules are found ineukaryotic cells and are formed by the polymerization of a dimer oftwo globular proteins alpha and beta tubulin Tubulin is one ofseveral members of a small family of globular proteins The tubulinsuperfamily includes five distinct families the alpha- beta- gamma-delta- and epsilon-tubulins and a sixth family which is present only inkinetoplastid protozoa The most common members of the tubulin

family are α-tubulin and β-tubulin the proteins that make up microtubules Microtubules are very important in anumber of cellular processes They are involved in maintaining the structure of the cell

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9987Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9920Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9982Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

MicrotubuleTubulin Inhibitors amp Modulators

Bioactivity 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivativewith improved pharmacological features and higher watersolubility IC50 value Target Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cyclearrest and apoptosis as measured by flow cytometry DNAhellip

Bioactivity 10-Oxo Docetaxel (Docetaxel Impurity) is a novel taxoid havingremarkable anti-tumor properties and a Docetaxel intermediate

Bioactivity 2-Methoxyestradiol is an inhibitor and angiogenesis apoptosisinducer with potent antineoplastic activity2-Methoxyestradiol also destablize microtubules

Bioactivity 4-Demethylepipodophyllotoxin(4-DMEP) is a key intermediatecompound for the preparation of podophyllotoxin-typeanti-cancer drugs a potent inhibitor of microtubule assembly

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity ofdocetaxel detected by high performance liquid chromatography(HPLC)

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity C 7-Epitaxotere)is a impurity of docetaxel

Bioactivity 7-epi-Taxol is an active metabolite of taxol with activitycomparable to that of taxol against cell replicationpromoting bundle formation and againstmicrotubulemicrotubule depolymerization

Bioactivity 7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel)derivative Paclitaxel binds to tubulin and inhibits thedisassembly of microtubules

Bioactivity ABT-751(E 7010) is a novel bioavailable tubulin-binding andantimitotic sulfonamide agent with IC50 of about 15 and 34μM in neuroblastoma and non-neuroblastoma cell linesrespectively IC50 Value 15 μM(neuroblastoma) 34μM(non-neuroblastoma) Target MicrotubuleTubulin in vitrohellip

Bioactivity Amphethinile is an agent The affinity constantanti-tubulinfor the association ( ) of Amphethinile with tubulin isKa13 μM

92 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol

10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584

10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674

2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033

4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435

7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675

7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676

7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227

7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574

ABT-751 (E7010) Cat No HY-13270

Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190

wwwMedChemExpresscom 93

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9903Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9949Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9751Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ansamitocin P-3 is a inhibitor Ansamitocin P-3microtubuleis a macrocyclic antitumor antibiotic

Bioactivity Auristatin E is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAE analog and cytotoxin inAntibody-drug conjugates

Bioactivity Auristatin F is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAF analog and cytotoxin inAntibody-drug conjugates

Bioactivity BNC105 is a tubulin polymerization inhibitor with potentantiproliferative and tumor vascular disrupting properties

Bioactivity BTB-1 is a potent selective and reversible mitotic motorprotein inhibitor with an of 169 μMKif18A IC50

Bioactivity Cabazitaxel is a semi-synthetic derivative of the naturaltaxoid 10-deacetylbaccatin III with potential antineoplasticactivity

Bioactivity CCB02 is a selective inhibitor bindingCPAP-tubulin interactionto tubulin and competing for the CPAP binding site ofβ-tubulin with an of 689 nM and shows potent anti-tumorIC50activity CCB02 shows no inhibition on the cell cycle- andcentrosome-related kinases or the phosphorylation status ofhellip

Bioactivity Cephalomannine is a taxol derivative with antitumorantiproliferative properties

Bioactivity Cevipabulin (TTI-237) is an oral microtubule-active antitumorcompound and inhibits the binding of [ H] vinblastine to3

tubulin with an of 18-40 nM for cytotoxicity in humanIC50

tumor cell line [1] [2]

Bioactivity Cevipabulin fumarate (TTI-237 fumarate) is an oralmicrotubule-active antitumor compound and inhibits thebinding of [ H] vinblastine to tubulin with an of3 IC50

18-40 nM for cytotoxicity in human tumor cell line [1] [2]

Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739

Auristatin E Cat No HY-15582

Auristatin F Cat No HY-15583

BNC105 Cat No HY-16114

BTB-1 Cat No HY-101770

Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459

CCB02 Cat No HY-114302

Cephalomannine Cat No HY-77554

Cevipabulin (TTI-237) Cat No HY-14949

Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C

Purity 9828Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9956Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9831Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Bioactivity Colchicine is a inhibitor and a tubulin microtubuledisrupting agent Colchicine inhibits microtubulepolymerization with an of 3 nMIC50

Bioactivity Combretastatin A4 is a -targeting agent thatmicrotubulebinds with of 04 μMβ-tubulin Kd

Bioactivity Crolibulin is a small molecule tubulin polymerizationinhibitor

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate IC50 Value NATarget tubulin ADCs For comparison purposes the ADC A1-mc-MMAD andor A1 -vc-MMAD were used The linker payloadmc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) washellip

Bioactivity D-64131 is a novel inhibitor of Tubulin polymerization thatcompetitively binds with [(3)H]colchicine to αβ-Tubulin

Bioactivity D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule

Bioactivity D8-MMAE is a deuterated labeled MMAE a potent mitoticinhibitor

Bioactivity D8-MMAF is a deuterated form of MMAF which is a disrupting agentmicrotubule

Bioactivity D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a disrupting agentmicrotubule

Bioactivity DM4 is is an agent that inhibit cell division DM4antitubulincan be used in the preparation of antibody drug conjugate

94 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Colchicine Cat No HY-16569

Combretastatin A4 (CRC 87-09) Cat No HY-N2146

Crolibulin (EPC2407) Cat No HY-13603

Cys-mcMMAD Cat No HY-15750

D-64131 Cat No HY-15482

D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8

Monomethyl Dolastatin 10 D8) Cat No HY-15581S

D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A

D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S

D8-MMAF hydrochloride Cat No HY-15579AS

DM4 Cat No HY-12454

wwwMedChemExpresscom 95

Purity 9897Clinical Data LaunchedSize 500u g 1 mg

Purity gt98Clinical Data LaunchedSize 1 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Purity 9988Clinical Data Phase 3Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9555Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9983Clinical Data Phase 2Size 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg

Bioactivity Docetaxel is an antineoplastic drug by inhibiting depolymerization and attenuating of themicrotubule

effects of and gene expressionbcl-2 bcl-xL

Bioactivity Docetaxel Trihydrate is a semi-synthetic taxane analogue actsas a stabilizermicrotubule

Bioactivity Angiotensin II human is a vasoconstrictor that acts on the and the receptorAT1 AT2

Bioactivity ELR510444 is a novel microtubule disruptor inhibitsMDA-MB-231 cell proliferation with IC50 of 309 nM not asubstrate for the P-glycoprotein drug transporter and retainsactivity in βIII-tubulin-overexpressing cell lines

Bioactivity Entasobulin is a polymerization inhibitor withβ-tubulinpotential anticancer activity

Bioactivity Epothilone A is a competitive inhibitor of the binding of [H] paclitaxel to polymers with a of 06-14 μM3 tubulin Ki

Bioactivity Epothilone B is a stabilizer with a ofmicrotubule Ki071μM It acts by binding to the αβ-tubulin heterodimersubunit which causes decreasing of αβ-tubulin dissociation

Bioactivity Epothilone D (KOS 862) is a potent stabilizermicrotubule

Bioactivity Eribulin (E7389) is a targeting agent that ismicrotubuleused in the treatment of metastatic breast cancer Eribulin(E7389) inhibits the proliferation of cancer cells by bindingmicrotubule proteins and microtubules

Bioactivity Eribulin mesylate (E7389 mesylate) is a microtubuletargeting agent that is used in the treatment of metastaticbreast cancer Eribulin mesylate (E7389 mesylate) inhibits theproliferation of cancer cells by binding microtubule proteinsand microtubules

Docetaxel (RP-56976) Cat No HY-B0011

Docetaxel Trihydrate (RP-56976 (Trihydrate)) Cat No HY-B0011A

Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580

ELR510444 Cat No HY-16191

Entasobulin Cat No HY-16777

Epothilone A (Epo A) Cat No HY-13503

Epothilone B (EPO 906 Patupilone) Cat No HY-17029

Epothilone D (KOS 862) Cat No HY-15278

Eribulin (B1939 E7389 ER-086526) Cat No HY-13442

Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A

Purity 9874Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9723Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9947Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9801Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Bioactivity Estramustine phosphate sodium is an antimicrotubulechemotherapy agent arrests prostate cancer cells in the G2Mphase of the cell cycle

Bioactivity Fosbretabulin disodium(CA 4DP CA 4P) is a microtubuledestabilizing drug a type of vascular-targeting agent a drugdesigned to damage the vasculature (blood vessels) of cancertumors causing central necrosis IC50 Value 4 nM [1] Targetmicrotubule in vitro Cytotoxic IC(50) values of CA-4 in humanhellip

Bioactivity Ixabepilone is an orally bioavailable inhibitor which binds to tubulin andmicrotubule

promotes tubulin polymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of the cell cycle andinduces tumor cell apoptosis

Bioactivity Lexibulin(CYT-997) is a potent tubulin polymerisationinhibitor with IC50 of 10-100 nM in cancer cell lines withpotent cytotoxic and vascular disrupting activity in vitro andin vivo

Bioactivity Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM in cancer celllines with potent cytotoxic and vascular disrupting activityin vitro and in vivo

Bioactivity Maytansinol inhibits microtubule assembly and inducesmicrotubule disassembly in vitro Target MicrotubuleTubulinin vitro Maytansinol disrupts the mitotic spindle andprevents mitotic exit in Drosophila Maytansinol reduces thegrowth andor survival of HCT116 cells in a dose-dependenthellip

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate Mc-MMAD is aprotective group (maleimidocaproyl) -conjugated MMAD IC50Value Target tubulin ADCs For comparison purposes the ADCA1 -mc-MMAD andor A1 -vc-MMAD were used The linkerpayloadhellip

Bioactivity Mc-MMAE is a protective group (maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE) which is a potent tubulininhibitor is a toxin payload in antibody drug conjugate (

)ADC

Bioactivity Mc-MMAF is a protective group-conjugated MMAF MMAF is a morepotent drug than Monomethyl auristatin E (MMAE) but ischarged and relatively membrane-impermeable is a potenttubulin inhibitor is a toxin payload in antibody drugconjugate Target MMAF is a new auristatin derivative with ahellip

Bioactivity Mertansine (DM1) is a inhibitor and is anmicrotubulinantibody-conjugatable maytansinoid that is developed toovercome systemic toxicity associated with maytansine and toenhance tumor-specific delivery Mertansine can be attached toa monoclonal antibody with a linker to create an antibody-drughellip

96 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Estramustine phosphate sodium Cat No HY-13627

Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449

Ixabepilone (Azaepothilone B BMS 247550 BMS 247550-1) Cat No HY-10222

Lexibulin (CYT-997) Cat No HY-10498

Lexibulin dihydrochloride (CYT-997 dihydrochloride) Cat No HY-10498A

Maytansinol (Ansamitocin P-0) Cat No HY-19474

Mc-MMAD Cat No HY-15740

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741

McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578

Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792

wwwMedChemExpresscom 97

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9957Clinical Data Phase 3Size 10mM x 1mL in Water

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 4Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity Microtubule inhibitor 1 is an antitumor agent with inhibitory activity with anmicrotubule polymerization

value of 9-16 nM in cancer cells IC50[1]

Bioactivity MMAD is a potent inhibitor is a toxin payload intubulinantibody drug conjugates ( )ADCs

Bioactivity MMAF (Monomethylauristatin F) is an antitubulin agent thatinhibit cell division inhibits H3397 cell growth with an IC50of 105 nM

Bioactivity MMAF hydrochloride is an antitubulin agent that inhibit celldivision inhibits H3397 cell growth with an of 105 nMIC50

Bioactivity Monomethyl auristatin E (MMAE SGD-1010) is a syntheticderivative of dolastatin 10 and functions as a potent

inhibitor by inhibiting tubulin polymerizationmitoticMMAE is widely used as a cytotoxic component of antibody-drug

to treat several different cancer typesconjugates (ADCs)

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity Ombrabulin (AVE8062) is a derivative of CA-4 phosphate whichis known to exhibit antivascular effects through selectivedisruption of the cytoskeleton of endothelial cellstubulin

Bioactivity Ombrabulin hydrochloride is a derivative of CA-4 phosphatewhich is known to exhibit antivascular effects throughselective disruption of the cytoskeleton of endothelialtubulincells

Bioactivity OSIP-486823 is a novel -interfering agent withmicrotubuledistinct biological effects on both protein kinase G (PKG) andmicrotubules

Bioactivity Paclitaxel (Taxol) a naturally occurring antineoplasticagent stabilizes resulting intubulin polymerizationarrest at the G2M phase of the cell cycle and apoptotic celldeath [1] [2]

Microtubule inhibitor 1 Cat No HY-114313

MMAD (Demethyldolastatin 10 Monomethylauristatin D

Monomethyl Dolastatin 10) Cat No HY-15581

MMAF (Monomethylauristatin F) Cat No HY-15579

MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat No HY-15579A

Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162

Nocodazole (Oncodazole R17934) Cat No HY-13520

Ombrabulin (AVE8062 AC7700) Cat No HY-14797

Ombrabulin hydrochloride (AVE8062 (hydrochloride) AC7700 (hydrochloride)) Cat No HY-18256

OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004

Paclitaxel (Taxol) Cat No HY-B0015

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9979Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9344Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9968Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Bioactivity Parbendazole is a potent inhibitor of assemblymicrotubuledestabilizes tubulin with an of 879nM and exhibitsEC50a broad-spectrum anthelmintic activity

Bioactivity PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX) compound acts asa -depolymerizing agent and an apoptotic agentmicrotubule

Bioactivity PE859 is a potent inhibitor of both and aggregationtau Aβwith values of 066 and 12 μM respectivelyIC50

Bioactivity PF-06380101 is a novel cytotoxic Dolastatin 10 analogue withexcellent potencies in tumor cell proliferation assays anddifferential ADME properties when compared to other syntheticauristatin analogues that are used in the preparation of ADCsIC50 value ~02 nM(GI50 in BT474 MDA-MB-361-DYT2 and N87hellip

Bioactivity Plinabulin (NPI-2358) is a vascular disrupting agents (VDA)against tubulin-depolymerizing with IC50 of 98~18 nM in tumorcells IC50 Value 98~18 nM Target MicrotubuleTubulin invitro NPI-2358 binds to the colchicine-binding site oftubulin and has potent inhibitory to human tumor cell lineshellip

Bioactivity Podofilox (Podophyllotoxin) is a potent inhibitor ofmicrotubule assembly and DNA topoisomerase II

Bioactivity Rosabulin is a potent inhibitor withmicrotubuleanti-cancer activities

Bioactivity Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10derivative and inhibitor of polymerizationtubulin

Bioactivity SSE15206 is a polymerization inhibitor (GI microtubule 50= 197 nM in HCT116 cells) that overcomes multidrug resistanceCauses aberrant mitosis resulting in G2M arrest due toincomplete spindle formation in cancer cells [1]

Bioactivity Taltobulin (HTI-286 SPA-110) is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibitedproliferation of all three hepatic tumor cell lines (mean IC50= 2 nmolL +- 1 nmolL) in vitro Interestingly no decreasehellip

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Parbendazole (SKF 29044) Cat No HY-115364

PBOX 6 Cat No HY-U00446

PE859 Cat No HY-12662

PF-06380101 Cat No HY-12522

Plinabulin (NPI-2358) Cat No HY-14444

Podofilox (Podophyllotoxin) Cat No HY-15552

Rosabulin (STA 5312) Cat No HY-14934

Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672

SSE15206 Cat No HY-111425

Taltobulin (HTI-286 SPA-110) Cat No HY-15584

wwwMedChemExpresscom 99

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9624Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9996Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Taltobulin hydrochloride is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibits proliferationof all three hepatic tumor cell lines (mean IC50 = 2 nmolL+- 1 nmolL) Interestingly no decrease in viable primaryhellip

Bioactivity Taltobulin trifluoroacetate (HTI-286 SPA-110) is an analogueof Hemiasterlin potent tubulin inhibitor ADCs cytotoxinIC50 value Target tubulin in vitro HTI-286 significantlyinhibited proliferation of all three hepatic tumor cell lines(mean IC50 = 2 nmolL +- 1 nmolL) in vitro Interestinglyhellip

Bioactivity Tasidotin hydrochloride is a peptide analog of the antimitoticdepsipeptide dolastatin 15 as an inhibitor of microtubuleassembly and microtubule dynamics

Bioactivity Tirbanibulin (KX2-391) is an inhibitor of that targetsSrcthe peptide substrate site of Src with of 9-60 nM inGI50cancer cell lines

Bioactivity Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) isan inhibitor of that targets the peptide substrate siteSrcof Src with of 9-60 nM in cancer cell linesGI50

Bioactivity Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitorof that targets the peptide substrate site of Src withSrc

of 9-60 nM in cancer cell linesGI50

Bioactivity Triclabendazole(CGA89317) is a benzimidazole it binds totubulin impairing intracellular transport mechanisms andinterferes with protein synthesis Target MicrotubuleTubulinTriclabendazole treatment produces percentage decreases of thefluke egg output by 153 43 and 366 respectively inhellip

Bioactivity Tubulin inhibitor 1 is a inhibitor occupying thetubulincolchicine binding site inhibits tubulin polymerizationTubulin inhibitor 1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase and inducescellular apoptosis [1]

Bioactivity Tubulysin A(TubA) is a myxobacterial product that can functionas an antiangiogenic agent in many in vitro assaysanti-microtubule anti-mitotic an apoptosis induceranticancer anti-angiogenic and antiproliferative IC50value Target microtubule Tubulysin A is a novel antibiotichellip

Bioactivity Valecobulin (CKD516) a valine prodrug of (S516) and avascular disrupting agent (VDA) is a potent beta-tubulin

inhibitor with marked antitumor activitypolymerizationagainst murine and human solid tumors [1] [2]

Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A

Tasidotin hydrochloride (ILX651) Cat No HY-13760

Tirbanibulin (KX2-391 KX-01) Cat No HY-10340

Tirbanibulin dihydrochloride (KX2-391 (dihydrochloride) KX-01 (dihydrochloride)) Cat No HY-10340A

Tirbanibulin Mesylate (KX2-391 (Mesylate) KX01 (Mesylate)) Cat No HY-10340B

Triclabendazole (CGA89317) Cat No HY-B0621

Tubulin inhibitor 1 Cat No HY-112607

Tubulysin A (TubA) Cat No HY-15995

Valecobulin (CKD-516) Cat No HY-13598

Purity 9958Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9914Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data LaunchedSize 10 mg 50 mg 100 mg 200 mg

Purity 9987Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9989Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Bioactivity Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulininhibitor (MMAD) Vc-MMAD is an antibody drug conjugate IC50Valu NA Target tubulin ADCs Monomethyl auristatin D(MMAD) a potent tubulin inhibitor is a toxin payload andantibody drug conjugate For comparison purposes the ADC A1hellip

Bioactivity VcMMAE is a with potentdrug-linker conjugate for ADCantitumor activity by using the anti-mitotic agent monomethylauristatin E (MMAE) linked via the lysosomally cleavabledipeptide valine-citrulline (vc)

Bioactivity Vinblastine sulfate is a cytotoxic alkaloid used againstvarious cancer types Vinblastine sulfate inhibits theformation of microtubule and suppresses nAChR with an ofIC5089 μM

Bioactivity Vincristine sulfate is an antitumor vinca alkaloid whichinhibits formation in mitotic spindlemicrotubuleresulting in an arrest of dividing cells at the metaphasestage It binds to with a of 85 nMmicrotubule Ki

Bioactivity Vinflunine is a new vinca alkaloid uniquely fluorinated withthe properties of mitotic-arresting and tubulin-interactingactivity

Bioactivity Vinflunine Tartrat is a new vinca alkaloid uniquelyfluorinated with the properties of mitotic-arresting andtubulin-interacting activity Target MicrotubuleTubulin Themajor effects of Vinflunine on dynamic instability are aslowing of the microtubule growth rate an increase in growthhellip

Bioactivity Vinorelbine is an anti-mitotic agent which inhibits theproliferation of Hela cells with IC of 125 nM50

Bioactivity Vinorelbine (ditartrate) is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC of 12550nM

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Vc-MMAD Cat No HY-15742

VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575

Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780

Vincristine sulfate (Leurocristine sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488

Vinflunine Cat No HY-B0628

Vinflunine Tartrate Cat No HY-B0628A

Vinorelbine (KW-2307 base) Cat No HY-12053

Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A

wwwMedChemExpresscom 101

Mps1Monopolar spindle 1

Monopolar spindle 1 (Mps1) also known as TTK is a serine threoninekinase which ensures proper biorientation of sister chromatids on themitotic spindle by the activation of the spindle assembly checkpoint(SAC) Mps1 has been shown to function as the key kinase thatactivates the spindle assembly checkpoint (SAC) to secure properdistribution of chromosomes to daughter cellsMps1 is a dual specificity protein kinase that is essential for thebipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomesare properly attached Mps1 is expressed at high levels during mitosisand is abundantly expressed in cancer cells Disruption of Mps1

function induces aneuploidy and cell death

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Mps1 Inhibitors amp Modulators

Bioactivity AZ3146 is a reasonably potent and selective inhibitorMps1with of 35 nM for Mps1 IC50

CatBioactivity BAY 1217389 is a potent and selective inhibitor of the

monopolar spindle 1 ( ) kinase with an value lessMPS1 IC50than 10 nM

Bioactivity BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1)checkpoint with an of 2 nMIC50

Bioactivity CCT251455 is a potent and selective mitotic kinase monopolarspindle 1 ( ) inhibitor with an of 3 nMMPS1 IC50

Bioactivity CFI-402257 is a highly selective and orally bioavailable inhibitor with an of 17 nM for TTK in vitroTTKMps1 IC50

CFI-402257 has anti-cancer activity [1]

Bioactivity CFI-402257 hydrochloride is a highly selective and orallybioavailable inhibitor with an of 17 nM forTTKMps1 IC50TTK in vitro CFI-402257 hydrochloride has anti-canceractivity [1]

Bioactivity Empesertib (BAY 1161909) is a potent inhibitor withMps1an of lt 1 nMIC50

Bioactivity MPI-0479605 is a potent and selective ATP-competitiveinhibitor of with an of 18 nMMps1 IC50

Bioactivity Mps1-IN-1 is a potent selective and ATP-competitive Mps1kinase inhibitor with an and a of 367 nM and 27 nMIC50 Kd

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

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AZ3146 Cat No HY-14710

BAY1217389 Cat No HY-12859

BOS-172722 Cat No HY-112162

CCT251455 Cat No HY-12603

CFI-402257 Cat No HY-101340

CFI-402257 hydrochloride Cat No HY-101340A

Empesertib (BAY 1161909) Cat No HY-12858

MPI-0479605 Cat No HY-12660

Mps1-IN-1 Cat No HY-13298

Mps1-IN-2 Cat No HY-13994

wwwMedChemExpresscom 103

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-3 is a potent and selective kinase inhibitorMPS1with an of 50 nMIC50

Bioactivity NMS-P715 is a selective ATP-competitive inhibitor of MPS1with an of 182 nMIC50

Bioactivity NMS-P715 analog is an inhibitor of with an of 84MPS1 IC50nM

Mps1-IN-3 Cat No HY-12401

NMS-P715 Cat No HY-12382

NMS-P715 analog Cat No HY-14712

Nucleoside AntimetaboliteAnalog

Nucleoside analogues are molecules that act like nucleosides in DNAsynthesis They include a range of antiviral products used to preventviral replication in infected cells Nucleoside analogues can be usedagainst hepatitis B virus hepatitis C virus herpes simplex and HIVOnce they are phosphorylated they work as antimetabolites by beingsimilar enough to nucleotidesto be incorporated into growing DNAstrands Less selective nucleoside analogues are used aschemotherapy agents to treat cancer eg gemcitabine and 5-FUAntimetabolite is a chemical that inhibits the use of a metabolitewhich is another chemical that is part of normal metabolism Suchsubstances are often similar in structure to the metabolite that they

interfere with such as the antifolates that interfere with the use of folic acid The presence of antimetabolites can havetoxic effects on cells such as halting cell growth and cell division so these compounds are used as chemotherapy forcancer

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wwwMedChemExpresscom 105

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Nucleoside AntimetaboliteAnalog Inhibitors amp Modulators

Bioactivity 1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is abicyclic nucleoside

Bioactivity 1-Methylcytosine is a methylated form of the DNA base cytosineand used as a nucleobase of hachimoji DNA in which it pairswith Isoguanine [1] [2]

Bioactivity 1-Methylinosine is a modified nucleotide found at position 37in tRNA 3 to the anticodon of eukaryotic tRNA [1]

Bioactivity 2-Deoxypseudoisocytidine is a nucleoside analogue

Bioactivity 2rsquo-O4rsquo-C-Methyleneuridine (Compound 15a) is a bicyclicnucleoside

Bioactivity 3-Azido-3-deoxy-5-fluorocytidine (Compound 12) is a cytidinederivative

Bioactivity 3-Azido-3-deoxy-beta-L-uridine (Compound 25) is a nucleosidederivative

Bioactivity 3-Methylcytidine a urinary nucleoside can be used as abiomarker of four different types of cancer lung cancergastric cancer colon cancer and breast cancer [1]

Bioactivity 5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methyluridine is a derivative of LNA-type nucleoside

Bioactivity 5-Aza-7-deazaguanine is a substrate for wild-type (WT) E coli and its Ser90Ala mutant in thepurine nucleoside phosphorylase

synthesis of base-modified nucleosides [1]

1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine Cat No HY-111638

1-Methylcytosine Cat No HY-W006395

1-Methylinosine (N1-Methylinosine) Cat No HY-113139

2-Deoxypseudoisocytidine Cat No HY-101968

2rsquo-O4rsquo-C-Methyleneuridine Cat No HY-111639

3-Azido-3-deoxy-5-fluorocytidine Cat No HY-111641

3-Azido-3-deoxy-beta-L-uridine Cat No HY-111642

3-Methylcytidine Cat No HY-111645

5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methylurid

ine

Cat No HY-111807

5-Aza-7-deazaguanine Cat No HY-111627

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9874Clinical Data Phase 4Size 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 960Clinical Data LaunchedSize 50 mg 100 mg 500 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in Water

50 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Bioactivity 5-Azacytidine is a nucleoside analogue of cytidine thatspecifically inhibits DNA methylation by trapping DNA

methyltransferases

Bioactivity 5-BrdU is a nucleoside analog that competes with thymidine forincorporation into DNA 5-BrdU is commonly used in thedetection of proliferating cells

Bioactivity 5-Fluorouracil is a potent antitumor agent that affectspyrimidine synthesis by inhibiting thymidylate synthetasethus depleting intracellular dTTP pools

Bioactivity 6-Amino-5-nitropyridin-2-one is a pyridine base and used as anucleobase of hachimoji DNA in which it pairs with5-aza-7-deazaguanine [1]

Bioactivity 6-Mercaptopurine is a purine analogue which acts as anantagonist of the and has been widely usedendogenous purinesas antileukemic agent and immunosuppressive drug

Bioactivity 6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MPhydrate) is a purine analogue which acts as an antagonist ofthe and has been widely used asendogenous purinesantileukemic agent and immunosuppressive drug

Bioactivity 6-O-Methyl Guanosine is a modified nucleoside 6-O-Methyl[1]

Guanosine (6-methylguanosine) inhibit colony-forming abilityin a malignant xeroderma pigmentosum cell line [2]

Bioactivity 7-Methylguanosine is a novel cNIIIB nucleotidase inhibitorwith IC value of 878 plusmn 75 microM50

Bioactivity 8-Azaguanine is a purine analogue which shows antineoplasticactivity

Bioactivity Adenosine is a nucleoside composed of a molecule of adenineattached to a ribose sugar molecule (ribofuranose) moiety viaa β-N9-glycosidic bond Target Nucleosideantimetaboliteanalog Adenosine plays an important role inbiochemical processes such as energy transfer mdash as adenosinehellip

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5-Azacytidine (Ladakamycin 5-AzaC Azacitidine) Cat No HY-10586

5-BrdU (BUdR BRDU) Cat No HY-15910

5-Fluorouracil (5-FU) Cat No HY-90006

6-Amino-5-nitropyridin-2-one Cat No HY-50071

6-Mercaptopurine (Mercaptopurine 6-MP) Cat No HY-13677

6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MP hydrate) Cat No HY-13677A

6-O-Methyl Guanosine Cat No HY-111648

7-Methylguanosine Cat No HY-122524

8-Azaguanine Cat No HY-B1468

Adenosine (Adenine riboside D-Adenosine) Cat No HY-B0228

wwwMedChemExpresscom 107

Purity 9818Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 1 g

Purity 9897Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carmofur is a derivative of fluorouracil an antimetaboliteused as an antineoplastic agent

Bioactivity Clofarabine(Clolar Clofarex) inhibits the enzymaticactivities of ribonucleotide reductase (IC50 = 65 nM) and DNApolymerase IC50 Value 65 nM Target in vitro Clofarabine isa second generation purine nucleoside analog withantineoplastic activity It is phosphorylated intracellularlyhellip

Bioactivity CNDAC is a major metabolite of oral drug sapacitabine and anucleoside analog

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Cytidine is a nucleoside molecule that is formed when cytosineis attached to a ribose ring cytidine is a component of RNATarget Nucleoside antimetaboliteanalog Cytidine is anucleoside molecule that is formed when cytosine is attachedto a ribose ring (also known as a ribofuranose) via ahellip

Bioactivity Dacarbazine(DTIC-Dome DTIC) is an antineoplastic agent Ithas significant activity against melanomas Target Nucleosideantimetaboliteanalog Approved May 1975 Dacarbazine (DTIC) isthe only single-agent approved by the Food and DrugAdministration for treating metastatic melanoma With DTIC ashellip

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Deoxypseudouridine is a nucleotide analog

Capecitabine Cat No HY-B0016

Carmofur (HCFU) Cat No HY-B0182

Clofarabine Cat No HY-A0005

CNDAC Cat No HY-16445A

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Cytidine (Cytosine β-D-riboside Cytosine-1-β-D-ribofuranoside) Cat No HY-B0158

Dacarbazine (Imidazole Carboxamide) Cat No HY-B0078

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Deoxypseudouridine Cat No HY-101970

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in Water

1000u g 2500u g 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 2500u g 5 mg 10 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 50 mg

Bioactivity DMTr-LNA-5MeU-3-CED-phosphoramidite is a nucleoside derivative[1]

Bioactivity Doxifluridine is a thymidine phosphorylase activator forPC9-DPE2 cells with IC50 of 062 μM

Bioactivity Ethynylcytidine is a new nucleoside antimetabolite Bioactivity Floxuridine (5-fluorodeoxyuridine) is an oncology drug thatbelongs to the class known as antimetabolites with an GI50 of51 μM for the inhibition of PEPT1 IC50 value TargetNucleoside antimetaboliteanalog Floxuridine (Fludara) is aprodrug of floxuridine and an oncology agent with an GI50 ofhellip

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

Bioactivity Fludarabine (phosphate) is an analogue of adenosine anddeoxyadenosine which is able to compete with dATP forincorporation into DNA and inhibit DNA synthesis

Bioactivity Forodesine(BCX-1777 freebase Immucillin-H) is an orallybioavailable PNP inhibitor with picomolar potency inducesapoptosis mainly in T cells

Bioactivity Forodesine hydrochloride is a potent and oral purine nucleoside inhibitor with s ranging from 048 tophosphorylase (PNP) IC50

157 nM

Bioactivity Fosteabine is an oral and prodrug analogue of cytarabine whichis resistant to deoxycytidine deaminase

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

108 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

DMTr-LNA-5MeU-3-CED-phosphoramidite Cat No HY-111531

Doxifluridine (Ro 21-9738 5-Fluoro-5-deoxyuridine 5-DFUR) Cat No HY-B0021

Ethynylcytidine (ECyD TAS-106 3-C-Ethynylcytidine) Cat No HY-16200

Floxuridine (5-Fluorouracil 2-deoxyriboside) Cat No HY-B0097

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Fludarabine phosphate (NSC 118218 (phosphate)) Cat No HY-B0028

Forodesine (BCX-1777 freebase Immucillin-H) Cat No HY-16210

Forodesine hydrochloride (BCX-1777 Immucillin-H hydrochloride) Cat No HY-16209

Fosteabine (Cytarabine ocfosfate YNK 01) Cat No HY-106349

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

wwwMedChemExpresscom 109

Purity 9575Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 9971Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9829Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Gemcitabine elaidate(CP-4126 CO-101) is a lipophilicunsaturated fatty acid ester derivative of gemcitabine (dFdC)an antimetabolite deoxynucleoside analogue with potentialantineoplastic activity IC50 value Target Gemcitabineanalog Upon hydrolysis intracellularly by esterases thehellip

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity Isocytosine is a non-natural nucleobase and an isomer ofcytosine It is used in combination with Isoguanine in studiesof unnatural nucleic acid analogues of the normal base pairsin DNA and used as a nucleobase of hachimoji RNA [1] [2]

Bioactivity Isoguanine is a purine base that is an isomer of guanine Abuilding block in organic synthesis

Bioactivity LY2334737 is an orally available prodrug of gemcitabine whichis a nucleoside analog used as chemotherapy

Bioactivity N2-methylguanosine is a modified nucleoside that occurs atseveral specific locations in many tRNAs

Bioactivity N6N6-Dimethyladenosine is a modified ribonucleosidepreviously found in rRNA and also exhibits in mycobacteriumbovis Bacille Calmette-Gueacuterin tRNA [1]

Bioactivity N6-Etheno 2-deoxyadenosine is a reactive oxygen species(ROS)reactive nitrogen species (RNS)-induced DNA oxidationproduct used as a biomarker to evaluate chronic inflammationand lipid peroxidation in animal or human tissues [1]

Bioactivity Nelarabine (Arranon 506U78) is a purine nucleoside analog andDNA synthesis inhibitor with IC50 from 0067-215 μM in tumorcells Nelarabine is a chemotherapy drug used in T-cell acutelymphoblastic leukemia

Bioactivity Orotic acid (OA) is an intermediate in pyrimidine metabolismIC50 Value Target Nucleoside antimetaboliteanalog in vitroOA increases cell proliferation and decreases apoptosis inserum-starved SK-Hep1 hepatocellular carcinoma cells whichmay ascribe to the inhibition of AMP-activated protein kinasehellip

Gemcitabine elaidate (CP-4126 CO-101 Gemcitabine 5-elaidate) Cat No HY-13538

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

Isocytosine Cat No HY-W002272

Isoguanine Cat No HY-124143

LY2334737 Cat No HY-13672

N2-Methylguanosine Cat No HY-111647

N6N6-Dimethyladenosine Cat No HY-101984

N6-Etheno 2-deoxyadenosine Cat No HY-111646

Nelarabine (506U78 GW 506U78 Nelzarabine) Cat No HY-13701

Orotic acid (6-Carboxyuracil Vitamin B13) Cat No HY-N0157

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9972Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9783Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9887Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9745Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity Pseudothymidine is a C-nucleoside analog of thymidine Bioactivity Raltitrexed is an antimetabolite drug used in chemotherapyacting by inhibiting thymidylate synthase

Bioactivity RX-3117(TV-1360 Fluorocyclopentenylcytosine) is novel acytidine analog shows anticancer activity in several cancercell lines including gemcitabine-resistant variants

Bioactivity Sapacitabine is an orally available prodrugnucleoside analogthat is structurally related to cytarabine

Bioactivity Tegafur (FT 207 NSC 148958) is a chemotherapeutic 5-FUprodrug used in the treatment of cancers is a component oftegafur-uracil

Bioactivity Tipiracil is a thymidine phosphorylase ( ) inhibitorTPase

Bioactivity Tipiracil (hydrochloride) is a thymidine phosphorylaseinhibitor (TPI) used for cancer research

Bioactivity Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT)is an irreversible inhibitor andthymidylate synthasethereby suppresses Trifluridine is an antiviralDNA synthesisdrug for infectionherpes simplex virus (HSV)

Bioactivity Trifluridine-tipiracil hydrochloride mixture (TAS-102) is anovel oral combination drug that consists of an antineoplasticthymidine-based nucleoside analog trifluorothymidine and apotent inhibitor tipiracil in athymidine phosphorylase105 molar ratio

Bioactivity Vidarabine (Ara-A) an antiviral drug which is active againstherpes simplex and varicella zoster viruses

110 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Pseudothymidine (5-Methyl-2-Deoxypseudouridin) Cat No HY-101969

Raltitrexed (ZD1694 D1694 ICI-D1694) Cat No HY-10821

RX-3117 (TV-1360 fluorocyclopentenylcytosine) Cat No HY-15228

Sapacitabine (CS682 CYC682) Cat No HY-16445

Tegafur (FT 207NSC 148958) Cat No HY-17400

Tipiracil Cat No HY-A0063A

Tipiracil hydrochloride Cat No HY-A0063

Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT) Cat No HY-A0061

Trifluridinetipiracil hydrochloride mixture (TAS-102) Cat No HY-16478

Vidarabine (Ara-A Adenine Arabinoside

9-β-D-Arabinofuranosyladenine) Cat No HY-B0277

wwwMedChemExpresscom 111

p97VCPCdc48

p97 an abundant hexameric ATPase of the AAA family is involved inhomotypic membrane fusion It is thought to disassemble SNAREcomplexes formed during the process of membrane fusion Twostructures have been reported a crystal structure of the N-terminaland D1 ATPase domains of murine p97 at 29 A resolution and acryoelectron microscopy structure of full-length rat p97 at 18 Aresolution Together these structures show that the D1 and D2hexamers pack in a tail-to-tail arrangement and that the N domain isflexible A comparison with NSF D2 (ATP complex) reveals possibleconformational changes induced by ATP hydrolysis

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9765Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

p97 Inhibitors amp Modulators

Bioactivity CB-5083 is a potent selective and orally bioavailable p97inhibitor with an value of 11 nMIC50

Bioactivity DBeQ is a selective potent reversible and ATP-competitive inhibitor with an value of 15 μM and 16 μM forp97 IC50

p97(wt) and p97(C522A) respectively DBeQ also inhibits Vps4with an of 115 μMIC50

Bioactivity ML240 is a potent inhibitor inhibiting p97 ATPase withp97 value of 100 nMIC50

Bioactivity ML241 hydrochloride is a potent inhibitor inhibiting p97p97ATPase with value of 100 nMIC50

Bioactivity NMS-859 is a potent covalent inhibitor withVCP (p97)s of 037 and 036 μM for wild-type VCP in the presence ofIC50

60 μM and 1 mM ATP in cells respectively

Bioactivity NMS-873 is a potent selective allosteric inhibitorVCPp97with value of 30 nMIC50

112 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CB-5083 Cat No HY-12861

DBeQ (JRF 12) Cat No HY-15945

ML240 Cat No HY-19795

ML241 hydrochloride Cat No HY-19797A

NMS-859 Cat No HY-15714

NMS-873 Cat No HY-15713

wwwMedChemExpresscom 113

PAKp21 activated kinases

PAKs (p21-activated kinases) are key regulators of actin dynamics cellproliferation and cell survival PAKs are SerThr kinases that areclassified into two groups on the basis of their structural andfunctional features group I (PAK1ndash3) and group II (PAK4ndash6) Group IPAKs have an auto-inhibitory domain (also called an inhibitory switchdomain) and a kinase domain (catalytic domain CD) and are activatedby the binding of the active (that is GTP-bound) forms of RhoGTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPasesBecause the deregulation of PAKs is closely associated with varioushuman diseasessmall-molecule inhibitors of these kinases have great

potential as therapeutic agents In addition these compounds can also be used as powerful tools in studies aimed atunderstanding the PAK signaling pathwayPAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actinremodelling and their ability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role intumor cell invasion and metastasis The current evidence suggests the involvement of PAKs in motility cell survivalanchorage-independent growth angiogenesis invasion migration and regulation of cell cycle and mitosisConsequently PAKs have also been implicated in a number of pathological conditions including cancer

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9902Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 1 g 5 g

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

PAK Inhibitors amp Modulators

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Fingolimod is a ( ) antagonistsphingosine 1-phosphate S1Pwith of 0033 nM in K562 and NK cells Fingolimod also isIC50a activatorpak1

Bioactivity Fingolimod hydrochloride is a ( )sphingosine 1-phosphate S1Pantagonist with an of 0033 nM in K562 and NK cellsIC50Fingolimod hydrochloride also is a activatorpak1

Bioactivity FRAX1036 is a inhibitor with s of 233 nM 724 nM andPAK Ki24 μM for PAK1 PAK2 and PAK4 respectively

Bioactivity FRAX486 is a p21-activated kinase ( ) inhibitor with sPAK IC50of 14 33 and 39 nM for PAK1 PAK2 and PAK3 respectively

Bioactivity FRAX597 is a potent group I p21-activated Kinases ( s)PAKinhibitor with of 8 13 and 19 nM for and IC50 PAK1 2 3

Bioactivity G-5555 is a potent p21-activated kinase 1 ( ) inhibitorPAK1with s of 37 nM and 11 nM for PAK1 and PAK2 respectivelyKi

Bioactivity G-5555 hydrochloride is a potent and selective p21-activatedkinase 1 ( ) inhibitor with a of 37 nMPAK1 Ki

Bioactivity IPA-3 is a selective non-ATP competitive inhibitor withPAK1 of 25 μM and shows no inhibition to group II PAKs (PAKsIC50

4-6)

Bioactivity NVS-PAK1-1 is a potent and selective allosteric PAK1inhibitor with an of 5 nMIC50

114 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Fingolimod (FTY720 free base) Cat No HY-11063

Fingolimod hydrochloride (FTY720) Cat No HY-12005

FRAX1036 Cat No HY-19538

FRAX486 Cat No HY-15542B

FRAX597 Cat No HY-15542A

G-5555 Cat No HY-19635

G-5555 hydrochloride Cat No HY-19635A

IPA-3 Cat No HY-15663

NVS-PAK1-1 Cat No HY-100519

wwwMedChemExpresscom 115

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity PAK-IN-1 is a inhibitor that displays group IIPAKselectivity PAK-IN-1 inhibits PAK4 PAK5 and PAK6 with sIC50of 75 36 126 nM respectively

Bioactivity PF-3758309 is an inhbitor of with of 13 nM forPAK IC50PAK4

PAK-IN-1 Cat No HY-12632

PF-3758309 Cat No HY-13007

PARPpoly ADP ribose polymerase

PARP is a family of proteins involved in a number of cellular processesinvolving mainly DNA repair and programmed cell death The PARPfamily comprises 17 members They have all very different structuresand functions in the cell PARP1 PARP2 VPARP (PARP4) Tankyrase-1and -2 (PARP-5a or TNKS and PARP-5b or TNKS2) have a confirmedPARP activity Others include PARP3 PARP6 TIPARP (or PARP7)PARP8 PARP9 PARP10 PARP11 PARP12 PARP14 PARP15 andPARP16 PARP is found in the cellrsquos nucleus The main role is to detectand signal single-strand DNA breaks (SSB) to the enzymaticmachinery involved in the SSB repair

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wwwMedChemExpresscom 117

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9839Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in Water

200 mg 500 mg

PARP Inhibitors amp Modulators

Bioactivity 3-Aminobenzamide is a potent inhibitor of with of appr 50 nM in CHO cellsPARP IC50

and acts as a mediator of oxidant-induced myocyte dysfunctionduring reperfusion

Bioactivity A-966492 is a novel and potent inhibitor of and with of 1 nM andPARP1 PARP2 Ki

15 nM respectively

Bioactivity AG14361 is a potent inhibitor with a of lt 5 nMPARP-1 Kiand in permeabilized SW620 and intact SW620 cells the sIC50are 29 nM and 14 nM respectively

Bioactivity AZ6102 is a potent dual and inhibitor withTNKS1 TNKS2s of 3 nM and 1 nM respectively and alao has 100-foldIC50

selectivity against other PARP family enzymes with s ofIC5020 μM 05 μM and gt3 μM for PARP1 PARP2 and PARhellip

Bioactivity AZD-2461 is a potent inhibitor with s of 5 nM 2 nMPARP IC50and 200 nM for PARP1 PARP2 and PARP3 respectively

Bioactivity BGP-15 is a inhibitor with an and a of 120 andPARP IC50 Ki57 μM respectively

Bioactivity BRCA1-IN-1 is a novel small-molecule-like inhibitorBRCA1with and of 053 μM and 071 μM respecrivelyIC50 Ki

Bioactivity Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolatedfrom traditional Chinese herb WT WangCorydalis yanhusuoDehydrocorydaline regulates protein expression of Bax Bcl-2activates and inactivates caspase-7 caspase-8 PARP

Bioactivity E7449 is a potent and inhibitor and alsoPARP1 PARP2inhibits and with s of 20 10 50 andTNKS1 TNKS2 IC5050 nM for PARP1 PARP2 TNKS1 and TNKS2 respectively using

P-NAD as substrate32 +

Bioactivity G007-LK is a potent and selective inhibitor of andTNKS1 with s of 46 nM and 25 nM respectivelyTNKS2 IC50

3-Aminobenzamide (PARP-IN-1) Cat No HY-12022

A-966492 Cat No HY-10614

AG14361 Cat No HY-12032

AZ6102 Cat No HY-12975

AZD-2461 Cat No HY-13536

BGP-15 Cat No HY-100828

BRCA1-IN-1 Cat No HY-100863

Dehydrocorydaline (13-Methylpalmatine) Cat No HY-N0674

E7449 Cat No HY-12418

G007-LK Cat No HY-12438

Purity 9952Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Bioactivity GeA-69 is a selective highly cell permeable allostericinhibitor of poly-adenosine-diphosphate-ribose polymerase 14

targeting macrodomain 2 with a of 21 microM (PARP14) Kd[1]

Bioactivity Iniparib (BSI-201) is an irreversible inhibitor of PARP1used in the research of triple negative breast cancer

Bioactivity JW 55 is a potent and selective signaling pathwayβ-catenininhibitor which functions via inhibition of the PARP domainof tankyrase 1 and tankyrase 2 (TNKS12) JW 55 decreasesauto-PARsylation of TNKS12 in vitro with s of 19 μM andIC50830 nM respectively

Bioactivity K-756 is a direct and selective ( ) inhibitortankyrase TNKSwhich inhibits the ADP-ribosylation activity of andTNKS1

with s of 31 and 36 nM respectivelyTNKS2 IC50

Bioactivity ME0328 is a potent and selective inhibitor withARTD3 PARP3an of 089plusmn028 μMIC50

Bioactivity MN-64 is a potent inhibitor with s of 6 nMtankyrase 1 IC5072 nM 191 μM and 394 μM for TNKS2 ARTD1 andTNKS1ARTD2 respectively

Bioactivity Niraparib (MK-4827) is a highly potent and PARP1 PARP2inhibitor with s of 38 and 21 nM respectivelyIC50

Bioactivity Niraparib hydrochloride (MK-4827 hydrochloride) is anexcellent and inhibitor with of 38 and 21PARP1 PARP2 IC50nM respectively

Bioactivity Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent inhibitor with of 24 nMPARP1 IC50

Bioactivity Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1and inhibitor with an of 38 and 21 nMPARP2 IC50respectively

118 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

GeA-69 Cat No HY-108708

Iniparib (BSI-201 NSC-746045 IND-71677) Cat No HY-12015

JW 55 Cat No HY-13968

K-756 Cat No HY-U00422

ME0328 Cat No HY-100225

MN-64 Cat No HY-19351

Niraparib (MK-4827) Cat No HY-10619

Niraparib hydrochloride (MK-4827 (hydrochloride)) Cat No HY-10619A

Niraparib R-enantiomer (MK 4827 (R-enantiomer)) Cat No HY-10619D

Niraparib tosylate (MK-4827 (tosylate)) Cat No HY-10619B

wwwMedChemExpresscom 119

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg

Purity 9768Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2 g

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NMS-P118 is a potent orally available and highly selective Inhibitor for cancer therapyPARP-1

Bioactivity NMS-P515 is a potent and stereospecific inhibitorPARP-1with an of 27 nM in hela cells Anti-tumor activity IC50

[1]

Bioactivity NVP-TNKS656 is a highly potent selective and orally active inhibitor with of 6 nM and is gt 300 foldTNKS2 IC50

selectivity against and PARP1 PARP2

Bioactivity Olaparib (AZD2281KU0059436) is a potent and oral PARPinhibitor with s of 5 and 1 nM for and IC50 PARP1 PARP2

respectively

Bioactivity Pamiparib is a inhibitor which can be used for thePARPtreatment of various cancers including the solid tumorextracted from patent WO 2013097225 A1

Bioactivity PARP-2-IN-1 is a potent and selective inhibitor withPARP-2an of 115 nMIC50

Bioactivity PJ34 is a potent specific inhibitor of with ofPARPl 2 IC50110 nM and 86 nM respectively

Bioactivity PJ34 hydrochloride is an inhibitor of with of 110PARPl12 IC50nM and 86 nM respectively

Bioactivity PROTAC PARP1 degrader is a degrader based on thePARP1 technology It induces significant PARP1 cleavage andPROTAC

programmed cell death PROTAC PARP1 degrader at 10 μM at 24 hinhibits MDA-MB-231 cell line with an of 612 μMIC50

Bioactivity RK-287107 is a potent and specific inhibitor withtankyrases of 143 and 106 nM for and IC50 tankyrase-1 tankyrase-2

respectively RK-287107 blocks colorectal cancer cell growth[1]

NMS-P118 Cat No HY-18954

NMS-P515 Cat No HY-128599

NVP-TNKS656 (TNKS656) Cat No HY-13990

Olaparib (AZD2281 KU0059436) Cat No HY-10162

Pamiparib (BGB-290) Cat No HY-104044

PARP-2-IN-1 Cat No HY-102035

PJ34 Cat No HY-13688A

PJ34 hydrochloride Cat No HY-13688

PROTAC PARP1 degrader Cat No HY-114324

RK-287107 Cat No HY-123892

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9962Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9888Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9508Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9983Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9989Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9981Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity Rucaparib (AG014699) is an inhibitor of with of 14 nM for PARP1 in aPARP Ki

cell-free assay and also shows binding affinity to eightother PARP domains

Bioactivity Rucaparib Camsylate is an inhibitor of with a of 14PARP KinM for PARP1 and also shows binding affinity to eight otherPARP domains

Bioactivity Rucaparib phosphate (AG-014699 phosphate) is a potent and oral inhibitor with a of 14 nM for PARP1 in cell-freePARP Ki

assay also showing binding affinity to eight other PARPdomains

Bioactivity Talazoparib (BMN-673) is a highly potent inhibitorPARP12with s of 12 nM and 087 nM respectivelyKi

Bioactivity Talazoparib 8R9S (BMN-673 8R9S) is an enantiomer ofTalazoparib less active than Talazoparib on the inhibition of

with an of 144 nMPARP1 IC50

Bioactivity Talazoparib tosylate (BMN 673ts) is a novel potent and orallyavailable inhibitor with an of 057 nM forPARP12 IC50PARP1

Bioactivity UPF 1069 is a inhibitor with s of 8 and 03 μM forPARP IC50PARP-1 and PARP-2 respectively

Bioactivity Veliparib is a potent inhibitor inhibiting andPARP PARP1 with s of 52 and 29 nM respectivelyPARP2 Ki

Bioactivity Veliparib (dihydrochloride) is a potent inhibitor of and with s of 52PARP1 PARP2 Ki

nM and 29 nM in cell-free assays respectively

Bioactivity WD2000-012547 is a selective poly(ADP-ribose)-polymerase(PARP-1) inhibitor with a pK of 8221i

120 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Rucaparib (AG014699 PF-01367338) Cat No HY-10617A

Rucaparib Camsylate Cat No HY-102003

Rucaparib phosphate (AG-014699 phosphate PF-01367338 phosphate) Cat No HY-10617

Talazoparib (BMN-673 LT-673) Cat No HY-16106

Talazoparib 8R9S (BMN-673 (8R9S) (8R9S)-LT-673) Cat No HY-16106A

Talazoparib tosylate (BMN 673ts) Cat No HY-108413

UPF 1069 Cat No HY-14478

Veliparib (ABT-888) Cat No HY-10129

Veliparib dihydrochloride (ABT-888 dihydrochloride) Cat No HY-10130

WD2000-012547 Cat No HY-U00223

wwwMedChemExpresscom 121

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity XAV-939 is a inhibitor and an indirecttankyrase (TNKS)inhibitor of with s of 5 and 2Wntβ-catenin signaling IC50nM for TNKS1 and TNKS2 respectively

XAV-939 Cat No HY-15147

PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinase

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) isactivated in response to a variety of endoplasmic reticulum stressesimplicated in numerous disease states PERK is implicated intumorigenesis and cancer cell survival GSK2606414 is an orallyavailable potent and selective PERK inhibitor GSK2606414 inhibitsPERK activation in cells and inhibits the growth of a human tumorxenograft in mice PERK activation is independent of the largeincrease in unfolded nascent proteins within the ER followingtransient global brain ischemia

122 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 123

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

PERK Inhibitors amp Modulators

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity GSK2606414 is a cell-permeable and orally available proteinkinase R-like endoplasmic reticulum (ER) kinase (PERK)inhibitor with an of 04 nMIC50

Bioactivity GSK2656157 is a selective and ATP-competitive inhibitor ofprotein kinase R (PKR)-like endoplasmic reticulum kinase (

) with an of 09 nMPERK IC50

Bioactivity ISRIB (trans-isomer) is a potent inhibitor of with anPERK of 5 nMIC50

CCT020312 Cat No HY-119240

GSK2606414 Cat No HY-18072

GSK2656157 Cat No HY-13820

ISRIB trans-isomer Cat No HY-12495

Polo-like Kinase (PLK)

Polo-like Kinases (PLKs) are important regulators of the cell cycle Plksare involved in the formation of and the changes in the mitoticspindle and in the activation of CDKcyclin complexes duringM-phase of the cell cyclePolo-like kinases (Plks) are a family ofconserved serinethreonine kinases involved in the regulation of cellcycle progression through G2 and mitosis Mammalian polo-likekinases include Plk1 (Xenopus Plx1) Plk2Snk (Xenopus Plx2)Plk3PrkFnK (Xenopus Plx3) Plk4Sak and Plk5 Plk1 is involved in theregulation of key steps during cell division DNA damage repairpathways apoptosis and the progression of the cell cycle Plk3 is amultifunctional stress response protein that responses to signals

induced by DNA damage andor mitotic spindle disruption

124 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 125

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9982Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9897Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9857Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Polo-like Kinase (PLK) Inhibitors amp Modulators

Bioactivity BI 2536 is a dual and inhibitor with s of 083PLK1 BRD4 IC50

and 25 nM respectively BI-2536 suppresses IFNB[1]

(encoding IFN-β) gene transcription [4]

Bioactivity Centrinone (LCR-263) is a selective and reversible inhibitorof polo-like kinase 4 ( ) with a of 016 nMPlK4 Ki

Bioactivity Centrinone-B (LCR-323) is a potent and highly selective PLK4inhibitor with a of 059 nMKi

Bioactivity CFI-400945 free base is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity CFI-400945 fumarate is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity GSK461364 is a selective reversible and ATP-competitive inhibitor with a value of 22 nMPolo-like kinase 1 (PLK1) Ki

Bioactivity GW843682X is a selective ATP-competitive inhibitor of PLK1and with s of 22 nM and 91 nM respectively andPLK3 IC50is also gt100-fold selective against 30 other kinases

Bioactivity HMN-214 an orally bioavailable prodrug of HMN-176 is aninhibitor of polo-like kinase-1 ( ) with antitumorplk1activity

Bioactivity LFM-A13 is a potent inhibitor inhibitsBTK JAK2 PLKrecombinant BTK Plx1 and PLK3 with s of 25 μM 10 μM andIC5061 μM LFM-A13 shows no effects on JAK1 and JAK3 Src familykinase HCK EGFR and IRK

Bioactivity MLN0905 is a potent inhibitor with an of 2 nMPLK1 IC50

BI 2536 Cat No HY-50698

Centrinone (LCR-263) Cat No HY-18682

Centrinone-B (LCR-323) Cat No HY-18683

CFI-400945 free base Cat No HY-12300

CFI-400945 fumarate Cat No HY-12300B

GSK461364 (GSK461364A) Cat No HY-50877

GW843682X (GW843682) Cat No HY-11003

HMN-214 (IVX-214) Cat No HY-12045

LFM-A13 Cat No HY-18009

MLN0905 (PLK1 Inhibitor) Cat No HY-15155

Purity 9759Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9949Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9809Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9626Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9970Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

Bioactivity NMS-1286937 is a potent selective and orally available PLK1inhibitor with an of 2 nMIC50

Bioactivity Poloxime a hydrolysis product of poloxin is anon-ATP-competitive inhibitor with moderate Plk1Plk1inhibitory activity

Bioactivity Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1)inhibitor that targets the polo-box domain with an ofIC50appr 48 μM

Bioactivity Rigosertib (ON-01910) is a multi-kinase inhibitor and aselective anti-cancer agent which induces apoptosis byinhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib is a selective andhellip[1] [2]

Bioactivity Rigosertib sodium (ON-01910 sodium) is a multi-kinaseinhibitor and a selective anti-cancer agent which inducesapoptosis by inhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib sodium is a selective andhellip[1] [2]

Bioactivity Ro3280 is a potent highly selective inhibitor of withPLK1an and a of 3 nM and 009 nM respectively andIC50 Kdnearly has no effect on PLK2 and PLK3

Bioactivity SBE13 is a potent and selective inhibitor with an ofPlk1 IC50200 pM SBE13 poorly inhibits Plk2 (IC gt66 μM) or Plk350(IC =875 nM)50

Bioactivity SBE13 Hydrochloride is a potent and selective inhibitorPlk1with an of 200 pM SBE13 Hydrochloride poorly inhibitsIC50Plk2 (IC gt66 μM) or Plk3 (IC =875 nM)50 50

Bioactivity TAK-960 is an orally available selective inhibitor of with an of 08 nM at 10 μMpolo-like kinase 1 (PLK1) IC50

ATP TAK-960 also shows inhibitory activities against PLK2and with s of 169 and 502 nM respectivelyPLK3 IC50

126 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Mps1-IN-2 Cat No HY-13994

NMS-1286937 (NMS-P937) Cat No HY-15828

Poloxime Cat No HY-77195

Poloxin Cat No HY-12134

Rigosertib (ON-01910) Cat No HY-12037A

Rigosertib sodium (ON-01910 sodium) Cat No HY-12037

Ro3280 Cat No HY-15161

SBE13 Cat No HY-15158A

SBE13 Hydrochloride Cat No HY-15158

TAK-960 Cat No HY-15160

wwwMedChemExpresscom 127

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9955Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TAK-960 dihydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 dihydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TAK-960 hydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 hydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TC-S 7005 is a inhibitor with s ofPolo-like kinases (Plks) IC504 nM 24 nM and 214 nM for Plk2 Plk3 and Plk1 respectively

[1]

Bioactivity Volasertib is a highly potent Polo-like kinase 1 (PLK1)inhibitor with an of 087 nM as well as the two closelyIC50related kinases and with s of 5 and 56 nMPLK2 PLK3 IC50respectively

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

TAK-960 dihydrochloride Cat No HY-15160B

TAK-960 hydrochloride Cat No HY-15160A

TC-S 7005 Cat No HY-108597

Volasertib (BI 6727) Cat No HY-12137

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

PPARPeroxisome proliferator-activated receptors

PPARs (Peroxisome proliferator-activated receptors) areligand-activated transcription factors of nuclear hormone receptorsuperfamily comprising of the following three subtypes PPARαPPARγ and PPARβδ PPARs play essential roles in the regulation ofcellular differentiation development and metabolism (carbohydratelipid protein) and tumorigenesis of higher organisms All PPARsheterodimerize with the retinoid X receptor (RXR) and bind to specificregions on the DNA of target genes Activation of PPAR-α reducestriglyceride level and is involved in regulation of energy homeostasisActivation of PPAR-γ enhances glucose metabolism whereasactivation of PPAR-βδ enhances fatty acids metabolism

128 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 129

Purity 9905Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9921Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 980Clinical Data Phase 4Size 50 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg

Purity gt98Clinical Data Phase 2Size 1 mg

Purity 9900Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

PPAR Inhibitors amp Modulators

Bioactivity 4-O-Methyl honokiol is a natural neolignan isolated from acts as a agonist and inhibtisMagnolia officinalis PPARγ

activity used for cancer and inflammation researchNF-κB

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Adelmidrol exerts important anti-inflammatory effects that arepartly dependent on Adelmidrol reduces PPARγ NF-κBtranslocation and expressionCOX-2

Bioactivity Aleglitazar(R1439 RO-0728804) is a new dual PPAR-αγ agonistwith IC50 of 28 nM46 nM

Bioactivity Arhalofenate (MBX 102) is a selective partial agonist ofperoxisome proliferator-activated receptor used for(PPAR)-γthe treatment of type 2 diabetes

Bioactivity Astaxanthin a red dietary carotenoid isolated from is an inhibitor of and aHaematococcus pluvialis PPARγ

potent antioxidant with antiproliferative neuroprotective andanti-inflammatory activity Astaxanthin has potential in[1]

the treatment of various diseases such as cancers andhellip

Bioactivity Astragalus polysaccharide are active components of thepolysaccharides extract of Astragulus attenuatesTNF-α-induced insulin resistance by suppressing miR-721 andactivating and in 3T3-L1 adipocytesPPAR-γ PI3KAkt

Bioactivity AVE-8134 is a potent agonist with values of 100PPARα EC50and 3000 nM for human and rodent PPARα receptor respectively

Bioactivity Balaglitazone is a selective partial agonist with anPPARγ of 1351 μM for human EC50 PPARγ

Bioactivity Bezafibrate is an agonist of with s of 50 μM 60PPAR EC50μM 20 μM for and and 90 μMhuman PPARα PPARγ PPARδ55 μM 110 μM for and murine PPARα PPARγ PPARδrespectively Bezafibrate is used as an hypolipidemic agent

4-O-Methyl honokiol Cat No HY-U00450

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Adelmidrol Cat No HY-B1026

Aleglitazar (R1439 RO0728804) Cat No HY-14728

Arhalofenate (MBX 102 JNJ 39659100) Cat No HY-14831

Astaxanthin Cat No HY-B2163

Astragalus polysaccharide (Astragalus Polysacharin) Cat No HY-N0937

AVE-8134 Cat No HY-U00014

Balaglitazone (DRF 2593 NN 2344) Cat No HY-16086

Bezafibrate (BM15075) Cat No HY-B0637

Purity 9877Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data Phase 4Size 10mM x 1mL in DMSO

500 mg 1 g 5 g 10 g

Purity 9959Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9981Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BMS-687453 is a potent and selective agonist with anPPARα and of 10 nM and 260 nM for human and 4100EC50 IC50 PPARα

nM and gt15000 nM for PPARγ in PPAR-GAL4 transactivationassays

Bioactivity CDDO-Im (CDDO-imidazolide) is an activator of and Nrf2 PPARwith s of 232 and 344 nM for PPARα and PPARγKi

Bioactivity Chiglitazar is a dual agonist with of 12PPARαγ EC s50008 17 μM for PPARα PPARγ and PPARδ respectively

Bioactivity Choline Fenofibrate (ABT-335) is the choline salt offenofibric acid under clinical development as a combinationtherapy with rosuvastatin for the management of dyslipidemia

Bioactivity Ciprofibrate is a peroxisome proliferator-activated receptoragonist

Bioactivity Ciprofibrate D6 is deuterium labeled Ciprofibrate which is aperoxisome proliferator-activated receptor agonist

Bioactivity Clofibrate is an agonist of with s of 50 μM 500PPAR EC50μM for murine PPARα and PPARγ and 55 μM 500 μM for humanPPARα and PPARγ respectively

Bioactivity Daidzein is a soy isoflavone which acts as a activatorPPAR

Bioactivity DG172 dihydrochloride is a selective antagonist withPPARβδan of 27 nMIC50

Bioactivity Elafibranor is a agonist with s of 45 and 175PPARαδ EC50nM respectively

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BMS-687453 Cat No HY-10678

CDDO-Im (RTA-403 TP-235 CDDO-Imidazolide) Cat No HY-15725

Chiglitazar Cat No HY-106266

Choline Fenofibrate (ABT-335) Cat No HY-14739

Ciprofibrate (Win35833) Cat No HY-B0664

Ciprofibrate D6 Cat No HY-B0664S

Clofibrate Cat No HY-B0287

Daidzein Cat No HY-N0019

DG172 dihydrochloride Cat No HY-19737A

Elafibranor (GFT505) Cat No HY-16737

wwwMedChemExpresscom 131

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Ertiprotafib is an inhibitor of PTP1B IkB kinase β (IKK-β)and a dual agonist with an of 16 μMPPARα and PPARβ IC50for PTP1B 400 nM for IKK-β an of ~1 μM forEC50PPARαPPARβ

Bioactivity Eupatilin a lipophilic flavonoid isolated from Artemisiaspecies is a agonist and possesses anti-apoptoticPPARαanti-oxidative and anti-inflammatory activities

Bioactivity Fenofibrate is a agonist with an of 30 μMPPARα EC50 Bioactivity Fenofibric acid an active metabolite of fenofibrate is a activitor with s of 224 microM 147 microM and 106 microMPPAR EC50

for PPARα PPARγ and PPARδ respectively Fenofibric acid alsoinhibits enzyme activity with an of 48 nMCOX-2 IC50

Bioactivity FH535 is an inhibitor of and withWntβ-catenin PPARanti-tumor activities

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Fonadelpar is a agonist used in the research ofPPARδneuroparalytic keratopathy

Bioactivity Gemfibrozil is an activator of used as aPPAR-αlipid-lowering drug Gemfibrozil is also a nonselectiveinhibitor of several isoforms with values forP450 KiCYP2C9 2C19 2C8 and 1A2 of 58 24 69 and 82 μMrespectively

Bioactivity Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2Sanchinoside Rh1) is isolated from the root of Panax GinsengGinsenoside Rh1 inhibits the expression of PPAR-γ TNF-α

and IL-6 IL-1β

Bioactivity Glabridin is a natural isoflavan from bindsGlycyrrhiza glabrato and activates with an of 6115 nM GlabridinPPARγ EC50exhibits antioxidant anti-bacterial anti-nephriticanti-diabetic anti-fungal antitumor anti-inflammatoryantiosteoporotic cardiovascular protective neuroprotectivehellip

Ertiprotafib (PTP 112) Cat No HY-19383

Eupatilin Cat No HY-N0783

Fenofibrate Cat No HY-17356

Fenofibric acid (FNF acid) Cat No HY-B0760

FH535 Cat No HY-15721

Fisetin Cat No HY-N0182

Fonadelpar (NPS-005 SJP-0035) Cat No HY-17633

Gemfibrozil (CI-719) Cat No HY-B0258

Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2 Sanchinoside Rh1) Cat No HY-N0604

Glabridin Cat No HY-N0393

Purity 9875Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9727Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9667Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity GSK0660 is a potent antagonist of and withPPARβ PPARδs of 155 nM for both isoformsIC50

Bioactivity GSK376501A is a selective peroxisome proliferator-activatedreceptor gamma ( ) modulator for the treatment of type 2PPARγdiabetes mellitus

Bioactivity GSK3787 is a selective and irreversible peroxisomeproliferator-activated receptor δ ( ) antagonist withPPARδ

of 66pIC50

Bioactivity GW 501516 is a agonist with an of 11 nMPPARδ EC50

Bioactivity GW 6471 is a potent antagonistPPARα Bioactivity GW0742 is a potent and agonist with an ofPPARβ PPARδ IC501 nM for human in binding assay and s of 1 nMPPARδ EC5011 μM and 2 μM for human PPARα and PPARγPPARδrespectively

Bioactivity GW1929 is a potent agonist with a of 884 forPPAR-γ pKihuman and s of 856 and 827 for human PPAR-γ pEC50 PPAR-γ

and murine respectivelyPPAR-γ

Bioactivity GW7647 is a potent agonist with s of 6 nM 11PPARα EC50μM and 62 μM for human PPARα PPARγ and PPARδ respectively

Bioactivity GW9662 is a potent and selective antagonist with anPPARγ of 33 nM showing 10 and 1000-fold selectivity overIC50

PPARα and PPARδ respectively

Bioactivity Icariin is a flavonol glycoside Icariin inhibits andPDE5 activities with s of 432 nM and 7350 μMPDE4 IC50

respectively Icariin also is a activatorPPARα

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GSK0660 Cat No HY-12377

GSK376501A Cat No HY-101746

GSK3787 Cat No HY-15577

GW 501516 (GW 1516 GSK-516) Cat No HY-10838

GW 6471 Cat No HY-15372

GW0742 (GW610742) Cat No HY-13928

GW1929 Cat No HY-15655

GW7647 Cat No HY-13861

GW9662 Cat No HY-16578

Icariin (Ieariline) Cat No HY-N0014

wwwMedChemExpresscom 133

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9889Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9921Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 2Size 5 mg

Purity 9942Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Bioactivity Imiglitazar (TAK559) is a potent and dual human andPPARα agonist with values of 67 and 31 nMPPARγ1 EC50

Bioactivity Indeglitazar is an orally available peroxisomeproliferator-activated receptor ( ) pan-agonist for allPPARthree PPAR subtypes alpha (α) delta (δ) and gamma (γ)

Bioactivity Inolitazone a novel high-affinity agonist that isPPARγdependent upon PPARγ for its biological activity with ofIC5008 nM for growth inhibition

Bioactivity Inolitazone dihydrochloride is a novel high-affinity PPARγagonist that is dependent upon PPARγ for its biologicalactivity with of 08 nM for growth inhibitionIC50

Bioactivity KD3010 is a potent orally active and selective PPARδagonist

Bioactivity L-165041 is a cell permeable agonist with s of 6 nMPPARδ Kiand appr 730 nM for PPARδ and PPARγ respectively and inducesadipocyte differentiation in NIH-PPARδ cells

Bioactivity Lanifibranor is a pan peroxisome proliferator-activated ( ) agonist with s of 15 087 and 021receptor PPAR EC50

μM for human and respectivelyPPARα PPARσ PPARγ

Bioactivity LJ570 is a dual agonist with s of 105PPARα PPARγ EC50

and 012 μM respectively [1]

Bioactivity MA-0204 is a potent highly selective and orally availableperoxisome proliferator activated receptor δ ( )PPARδmodulator with s of 04 nM 79 nM and 10 nM for humanEC50mouse and rat PPARδ respectively Potential treatment hellip

Bioactivity Magnolol a natural lignan isolated from the stem bark of is a dual agonist of both andMagnolia officinalis RXRα

with values of 104 microM and 177 microMPPARγ EC50respectively

Imiglitazar (TAK-559) Cat No HY-101649

Indeglitazar (PPM 204) Cat No HY-14817

Inolitazone (Efatutazone CS-7017 RS5444) Cat No HY-14792

Inolitazone dihydrochloride (Efatutazone (dihydrochloride)

CS-7017 (dihydrochloride) RS5444 (dihydrochloride)) Cat No HY-14792B

KD-3010 Cat No HY-111068

L-165041 Cat No HY-20019

Lanifibranor (IVA337) Cat No HY-104049

LJ570 Cat No HY-111775

MA-0204 Cat No HY-114739

Magnolol Cat No HY-N0163

Purity 9639Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9918Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in Ethanol

10 mg

Purity gt98Clinical DataSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9872Clinical Data Phase 1Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Bioactivity Naringenin is the predominant flavanone in grapefruitdisplays strong anti-inflammatory and antioxidant activities

Bioactivity Naveglitazar racemate is the racemate of NaveglitazarNaveglitazar is a nonthiozolidinedione peroxisomeproliferator-activated receptor ( ) α-γ dual γ-dominantPPARagonist that has shown glucose-lowering potential in animalmodels and in the clinic

Bioactivity NXT629 is a potent selective and competitive PPAR-αantagonist with an of 77 nM for human PPARα shows highIC50selectivity over other nuclear hormone receptor such asPPARδ PPARγ ERβ GR and TRβ s are 60 15 152 3hellipIC50

Bioactivity Oleoylethanolamide is a high affinity endogenous PPAR-αagonist which plays an important role in the treatment ofobesity and arteriosclerosis

Bioactivity Palmitelaidic acid is the trans isomer of palmitoleic acidPalmitoleic acid is one of the most abundant fatty acids inserum and tissue

Bioactivity Peliglitazar racemate is the racemate of PeliglitazarPeliglitazar is a novel dual αγ PPAR activator

Bioactivity Pemafibrate is a highly selective agonist with anPPARα of 1 nMEC50

Bioactivity Pemafibrate racemate is the racemate of pemafibrate andactivates activity with s of 1 nM gt10 μM andPPARα EC5017 μM for h-PPARα h-PPARγ and h-PPARδ respectively

Bioactivity Pioglitazone is a potent and selective agonist withPPARγhigh affinity binding to the PPARγ ligand-binding domain with

of 093 and 099 μM for human and mouse PPARγEC50respectively

Bioactivity Pioglitazone hydrochloride is a potent and selective PPARγagonist with s of 093 and 099 μM for human and mouseEC50PPARγ respectively

134 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Naringenin Cat No HY-N0100

Naveglitazar racemate Cat No HY-U00036

NXT629 Cat No HY-114263

Oleoylethanolamide (N-(2-Hydroxyethyl)oleamide

N-Oleoyl-2-aminoethanol N-Oleoylethanolamide hellip) Cat No HY-107542

Palmitelaidic Acid (9-trans-Hexadecenoic acid trans-Palmitoleic acid) Cat No HY-N2341

Peliglitazar racemate (BMS 426707-01 racemate) Cat No HY-101738A

Pemafibrate ((R)-K-13675) Cat No HY-17618

Pemafibrate racemate (K13675 (racemate)) Cat No HY-17618A

Pioglitazone (U 72107) Cat No HY-13956

Pioglitazone hydrochloride (U 72107A AD 4833) Cat No HY-14601

wwwMedChemExpresscom 135

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9836Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 250 mg

Bioactivity Pirinixic acid (Wy-14643) is a potent agonist of withPPARαs of 063 μM 32 μM for murine and PPARγ and 50EC50 PPARα

μM 60 μM 35 μM for human PPARγ and PPARδPPARαrespectively

Bioactivity PPAR agonist 1 is an agonist of and usedPPAR α PPAR γfor reducing blood glucose lipid levels lowering cholesteroland reducing body weight

Bioactivity PPARα-MO-1 is a potent modulator extracted from patentPPARαWO2004110982A1 formula I

Bioactivity PPARδ agonist is a agonist extracted from patentPPARδUS20180071304 compound example 10

Bioactivity Pparδ agonist 1 is a agonist with an of 506PPAR-δ EC50nM used in the research of PPAR-delta related diseases suchas mitochondrial diseases muscular diseases vasculardiseases demyelinating diseases and metabolic diseases

Bioactivity Pparδ agonist 2 is a agonist extracted from patent WOPPARδ2016057656 A1

Bioactivity Raspberry ketone is a major aromatic compound of redraspberry widely used as a fragrance in cosmetics and as aflavoring agent in foodstuff also shows agonisticPPAR-αactivity

Bioactivity Retinoic acid is a metabolite of vitamin A that playsimportant roles in cell growth differentiation andorganogenesis Retinoic acid is a natural agonist of RARnuclear receptors with s of 14 nM for RARαβγ RetinhellipIC50

Bioactivity RG-12525 is a a specific competitive and orally effectiveantagonist of the and peptidoleukotrienes LTC4 LTD4 LTE4inhibiting LTC4- LTD4- and LTE4-inducd guinea pig parenchymalstrips contractions with s of 26 nM 25 nM and 7 nMIC50respectively RG-12525 is also a peroxisomehellip

Bioactivity Rosiglitazone (BRL49653) is a selective agonist withPPARγs of 30 nM 100 nM and 60 nM for andEC50 PPARγ1 PPARγ2

respectivelyPPARγ

Pirinixic acid (Wy-14643) Cat No HY-16995

PPAR agonist 1 Cat No HY-U00340

PPARα-MO-1 Cat No HY-U00068

Pparδ agonist Cat No HY-112597

Pparδ agonist 1 Cat No HY-107901

Pparδ agonist 2 Cat No HY-100120

Raspberry ketone (Frambione 4-(4-Hydroxyphenyl)-2-butanone) Cat No HY-N1426

Retinoic acid (ATRA Tretinoin Vitamin A acid all-trans-Retinoic acid) Cat No HY-14649

RG-12525 (NID 525) Cat No HY-101676

Rosiglitazone (BRL49653) Cat No HY-17386

Purity 9953Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9852Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9885Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9803Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9925Clinical Data LaunchedSize 100 mg 500 mg

Bioactivity Rosiglitazone maleate is a potent and selective activator of with s of 30 nM 100 nM and 60 nM for PPARγ EC50 PPARγ1

and respectively and a of appr 40 nMPPARγ2 PPARγ Kdfor Rosiglitazone maleate is also an modulator of PPARγ hellip

Bioactivity Saroglitazar is a novel peroxisome proliferator-activatedreceptor ( ) agonist with predominant PPARα and moderatePPARPPARγ activity with values of 065 pM and 3 nM in HepG2EC50cells respectively

Bioactivity Saroglitazar magnesium is a novel peroxisomeproliferator-activated receptor ( ) agonist withPPARpredominant PPARα and moderate PPARγ activity with EC50values of 065 pM and 3 nM in HepG2 cells respectively

Bioactivity Seladelpar is an orally active potent (50 effectconcentration 2 nM) and specific agonistEC50 PPAR-δ

Bioactivity Seladelpar sodium salt (MBX-8025) is an orally active potentand specific agonist with an of 2 nM showingPPARδ EC50more than 750-fold and 2500-fold selectivity over the PPARαand PPARγ receptors respectively

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

Bioactivity Troglitazone is a agonist with s of 550 nM andPPARγ EC50780 nM for human and murinePPARγ receptor respectively

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Rosiglitazone maleate (BRL 49653C) Cat No HY-14600

Saroglitazar Cat No HY-19937

Saroglitazar Magnesium Cat No HY-19937A

Seladelpar (MBX-8025) Cat No HY-19522

Seladelpar sodium salt (MBX-8025 sodium salt RWJ-800025 sodium salt) Cat No HY-19522A

T0070907 Cat No HY-13202

Troglitazone (CS-045) Cat No HY-50935

wwwMedChemExpresscom 137

RAD51

RAD51 protein family assist in repair of DNA double strand breaksRAD51 family members are homologous to the bacterial RecA andyeast Rad51 In humans RAD51 is a 339-amino acid protein that playsa major role in homologous recombination of DNA during doublestrand break repair RAD51 is involved in the search for homologyand strand pairing stages of the process RAD51 can interact with thessDNA-binding protein RPA BRCA2 PALB2 and RAD52 Recentstudies using fluorescent labeled Rad5 has indicated that Rad51fragments elongate via multiple nucleation events followed bygrowth with the total fragment terminating when it reaches about 2μm in length

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

500 mg

RAD51 Inhibitors amp Modulators

Bioactivity Harmine is a natural dual-specificity tyrosinephosphorylation-regulated kinase ( ) inhibitor with(DYRK)anticancer and anti-inflammatory activities

Bioactivity IBR2 is a specific inhibitorRAD51

Bioactivity RAD51 Inhibitor B02 (B02) is an inhibitor of human withRAD51an of 274 μMIC50

Bioactivity RAD51-IN-2 (compound example 67A) is a inhibitorRAD51extracted from patent WO2019051465A1 [1]

Bioactivity RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM Bioactivity RI-2 is a reversible inhibitor with an of 4417RAD51 IC50μM and specifically inhibits homologous recombination repairin human cells

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

138 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Harmine (Telepathine) Cat No HY-N0737A

IBR2 Cat No HY-103710

RAD51 Inhibitor B02 (B02) Cat No HY-101462

RAD51-IN-2 Cat No HY-111887

RI-1 Cat No HY-15317

RI-2 Cat No HY-16904

RS-1 Cat No HY-19793

T0070907 Cat No HY-13202

wwwMedChemExpresscom 139

ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROK

ROCK (Rho-associated protein kinase) is a kinase belonging to theAGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopusinvertebrates and chicken Human ROCK1 has a molecular mass of158 kDa and is a major downstream effector of the small GTPaseRhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces thekinase activity of ROCKs by an autoinhibitory intramolecular fold ifRhoA-GTP is not present ROCK plays a role in a wide range ofdifferent cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators

of the cytoskeleton

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9954Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

ROCK Inhibitors amp Modulators

Bioactivity AT13148 is an orally active and ATP-competitive multi- AGC inhibitor with s of 38 nM402 nM50 nM 8 nM 3 nMkinase IC50

and 6 nM4 nM for Akt123 p70S6K PKA and ROCKIIIrespectively

Bioactivity Azaindole 1 is an orally active and ATP-competitive ROCKinhibitor with s of 06 and 11nM for human andIC50 ROCK-1

respectivelyROCK-2

Bioactivity BDP5290 is a potent inhibitor of both and withROCK MRCKs of 5 nM 50 nM 10 nM and 100 nM for IC50 ROCK1 ROCK2

and respectivelyMRCKα MRCKβ

Bioactivity Chroman 1 is a highly potent inhibitor with an ofROCK2 IC501 nM

Bioactivity Fasudil (HA-1077 AT877) a potent inhibitor of with aROCK of 033 μM for ROCK1 which is also a potent Ki Ca channel2+

antagonist and vasodilator

Bioactivity Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877Hydrochloride) a potent inhibitor of with a of 033ROCK Ki

μM for ROCK1 which is also a potent antagonistCa channel2+

and vasodilator

Bioactivity GSK180736A is a G protein-coupled receptor kinase 2 ( )GRK2inhibitor with an of 077 μMIC50

Bioactivity GSK269962A is a potent inhibitor with s of 16 and 4ROCK IC50nM for recombinant human and respectivelyROCK1 ROCK2

Bioactivity GSK429286A is a selective inhibitor of with an ROCK1 IC50value of 14 nM

Bioactivity H-1152 is a membrane-permeable and selective inhibitorROCKwith a value of 16 nM and an value of 12 nM forKi IC50

ROCK2

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AT13148 Cat No HY-16071

Azaindole 1 (TC-S 7001) Cat No HY-10319

BDP5290 Cat No HY-12437

Chroman 1 Cat No HY-15392

Fasudil (HA-1077 AT877) Cat No HY-10341A

Fasudil Hydrochloride (HA-1077 (Hydrochloride) AT-877 (Hydrochloride)) Cat No HY-10341

GSK180736A Cat No HY-18990

GSK269962A (GSK 269962) Cat No HY-15556

GSK429286A Cat No HY-11000

H-1152 Cat No HY-15720

wwwMedChemExpresscom 141

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9726Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical DataSize 10 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9929Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9940Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9813Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity H-1152 dihydrochloride is a membrane-permeable and selective inhibitor with a value of 16 nM and an valueROCK Ki IC50

of 12 nM for ROCK2

Bioactivity Hydroxyfasudil is a inhibitor with s of 073 andROCK IC50072 μM for and respectivelyROCK1 ROCK2

Bioactivity Hydroxyfasudil hydrochloride is a inhibitor with sROCK IC50of 073 and 072 μM for and respectivelyROCK1 ROCK2

Bioactivity LX7101 is a potent inhibitor of and with LIMK ROCK2 IC50values of 24 16 and 10 nM for LIMK1 LIMK2 and ROCK2respectively also inhibits with an less than 1 nMPKA IC50

Bioactivity Narciclasine is a plant growth modulator Narciclasinemodulates the RhoRho kinaseLIM kinasecofilin signalingpathway greatly increasing GTPase RhoA activity as well asinducing actin stress fiber formation in a RhoA-dependentmanner

Bioactivity Pentanoic acid a short-chain fatty acid is a product ofbacterial metabolism and are associated with allergic skindisorders Pentanoic acid activates signaling pathwayROCK

Bioactivity Ripasudil (K-115) is a specific inhibitor of with sROCK IC50of 19 and 51 nM for and respectivelyROCK2 ROCK1

Bioactivity Ripasudil free base (K-115 free base) is a specific inhibitorof with s of 19 and 51 nM for and ROCK IC50 ROCK2 ROCK1

respectively

Bioactivity RKI-1447 is a potent small molecule inhibitor of andROCK1 with values of 145 nM and 62 nM respectivelyROCK2 IC50

Bioactivity ROCK inhibitor-2 is a selective dual and ROCK1 ROCK2inhibitor with s of 17 nM and 2 nM respectively IC50

[1]

H-1152 dihydrochloride Cat No HY-15720A

Hydroxyfasudil (HA-1100) Cat No HY-13911

Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100

hydrochloride HA1100 hydrochloride) Cat No HY-13911A

LX7101 Cat No HY-12659

Narciclasine (Lycoricidinol) Cat No HY-16563

Pentanoic acid Cat No HY-N6056

Ripasudil (K-115) Cat No HY-15685

Ripasudil free base (K-115 (free base)) Cat No HY-15685A

RKI-1447 Cat No HY-15755

ROCK inhibitor-2 Cat No HY-119937

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2g

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9843Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Bioactivity ROCK-IN-1 is a potent inhibitor of with an of 12ROCK IC50nM for ROCK2

Bioactivity ROCK2-IN-2 is a selective inhibitor extracted fromROCK2patent US20180093978A1 Compound A-30 has an of lt1IC50μM

Bioactivity SAR407899 is a selective potent and ATP-competitive ROCKinhibitor with an of 135 nM for and s of 36IC50 ROCK-2 KinM and 41 nM for human and rat respectivelyROCK-2

Bioactivity SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an of 135 nM forROCK IC50

and s of 36 nM and 41 nM for human and rat ROCK-2 Ki ROCK-2

respectively

Bioactivity SB-772077B dihydrochloride is an aminofurazan-based Rho inhibitor with s of 56 nM and 6 nM towardkinase( ROCK) IC50

ROCK1 and ROCK2 respevtively [1]

Bioactivity SLx-2119 (KD-025) is a selective inhibitor of with anROCK2 of 105 nMIC50

Bioactivity SR-3677 is a potent and selective inhibitor with anROCK-II of ~3 nMIC50

Bioactivity Thiazovivin is a potent inhibitor which can protectROCKhuman embryonic stem cells

Bioactivity Y-27632 is an ATP-competitive inhibitor of and ROCK-I ROCK-IIwith of 220 nM and 300 nM for and Ki ROCK-I ROCK-II

respectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

Bioactivity Y-27632 dihydrochloride is a cell-permeable ATP-competitiveinhibitor of and with s of 220 and 300 nMROCK-I ROCK-II Kirespectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

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ROCK-IN-1 Cat No HY-U00351

ROCK2-IN-2 Cat No HY-103620

SAR407899 Cat No HY-15687A

SAR407899 hydrochloride Cat No HY-15687

SB-772077B dihydrochloride Cat No HY-108518

SLx-2119 (KD-025) Cat No HY-15307

SR-3677 Cat No HY-13300

Thiazovivin Cat No HY-13257

Y-27632 Cat No HY-10071

Y-27632 dihydrochloride Cat No HY-10583

wwwMedChemExpresscom 143

Purity 9923Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity Y-33075 is a selective inhibitor derived from Y-27632ROCKand is more potent than Y-27632 with an of 36 nMIC50

Bioactivity Y-33075 dihydrochloride is a selective inhibitor with anROCK of 36 nMIC50

Bioactivity ZINC00881524 is a inhibitorROCK

Y-33075 (Y 39983) Cat No HY-10067

Y-33075 dihydrochloride Cat No HY-10069

ZINC00881524 Cat No HY-101244

Sirtuin

Sirtuin (Sir2 proteins) are a class of proteins that possess eithermono-ADP-ribosyltransferase or deacylase activity includingdeacetylase desuccinylase demalonylase demyristoylase anddepalmitoylase activity Sirtuins regulate important biologicalpathways in bacteria archaeaand eukaryotes Sirtuins have beenimplicated in influencing a wide range of cellular processes like agingtranscription apoptosis inflammation and stress resistance as well asenergy efficiency and alertness during low-calorie situations Sirtuinscan also control circadian clocks and mitochondrial biogenesis

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wwwMedChemExpresscom 145

Purity 9891Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9909Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Sirtuin Inhibitors amp Modulators

Bioactivity 3-TYP is a selective inhibitor with an of 16 nMSIRT3 IC50more potent over SIRT1 ( =88 nM) SIRT2 ( =92 nM)IC50 IC50

Bioactivity AGK2 is a selective inhibitor with of 35 μM AGK2SIRT2 IC50can also inhibit and with of 30 and 91 μMSIRT1 SIRT3 IC50respectively

Bioactivity AK-1 is a potent specific and cell-permeable inhibitorSIRT2with an of 125 μMIC50

Bioactivity AK-7 is a selective cell- and brain-permeable inhibitorSIRT2with an of 155 μMIC50

Bioactivity Cambinol is a and inhibitor with values of 56SIRT1 SIRT2 IC50and 59 μM respectively

Bioactivity CAY10602 is a activatorSIRT1

Bioactivity Dihydrocoumarin is a compound found in Melilotus Dihydrocoumarin is a inhibitorofficinalis yeast Sir2p

Dihydrocoumarin also inhibits and withhuman SIRT1 SIRT2s of 208 μM and 295 μM respectively IC50

[1]

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Ginkgolide C is a flavone isolated from leavesGinkgo bilobapossessing multiple biological functions such as decreasingplatelet aggregation and ameliorating Alzheimer disease

Bioactivity Inauhzin is a dual inhibitor and acts as anSirT1IMPDH2activator used in the research of cancerp53

3-TYP Cat No HY-108331

AGK2 Cat No HY-100578

AK-1 Cat No HY-101465

AK-7 Cat No HY-16691

Cambinol Cat No HY-100732

CAY10602 Cat No HY-104073

Dihydrocoumarin (Hydrocoumarin Chroman-2-one) Cat No HY-N1926

Fisetin Cat No HY-N0182

Ginkgolide C (BN-52022 Ginkgolide-C) Cat No HY-N0785

Inauhzin (INZ) Cat No HY-15869

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9876Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity MC3482 is a specific sirtuin5 ( ) inhibitorSIRT5 Bioactivity Nicotinamide is a form of vitamin B3 that plays essentialroles in cell physiology through facilitating NAD+ redoxhomeostasis and providing NAD+ as a substrate to a class ofenzymes that catalyze non-redox reactions Nicotinamide is aninhibitor of SIRT1

Bioactivity OSS_128167 is a selective inhibitor with s of 89SIRT6 IC501578 and 751 μM for and respectivelySIRT6 SIRT1 SIRT2

Bioactivity PROTAC Sirt2 Degrader-1 is a SirReal-based acts as aPROTAC degrader composed of a highly potent andSirt2

isotype-selective inhibitor a linker and a bona fideSirt2cereblon ligand for E3 ubiquitin ligase PROTAC Sirt2Degrader-1 shows an of 025 μM for Sirt2 with no effecthellipIC50

Bioactivity Salermide is an inhibitor of and can cause strongSirt1 Sirt2cancer-specific apoptotic cell death

Bioactivity Selisistat (EX-527) is a potent and selective inhibitorSIRT1with of 98 nMIC50

Bioactivity Selisistat S-enantiomer (EX-527 S-enantiomer) is theS-enantiomer of Selisistat with an of 123 nM for SIRT1IC50Selisistat S-enantiomer is much more potent than SelisistatR-enantiomer

Bioactivity SIRT-IN-1 is a potent inhibitor of with of 15SIRT123 IC s5010 33 μM respectively

Bioactivity SIRT-IN-2 is a potent inhibitor of with of 4SIRT123 IC s504 7 μM respectively

Bioactivity Sirt2-IN-1 (Compound 9) is a ( ) inhibitor withsirtuin 2 Sirt2an of 163 nM IC50

[1]

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MC3482 Cat No HY-112587

Nicotinamide (Niacinamide Nicotinic acid amide Vitamin B3) Cat No HY-B0150

OSS_128167 Cat No HY-107454

PROTAC Sirt2 Degrader-1 Cat No HY-103636

Salermide Cat No HY-101073

Selisistat (EX-527) Cat No HY-15452

Selisistat S-enantiomer (EX-527 (S-enantiomer)) Cat No HY-15452A

SIRT-IN-1 Cat No HY-16615

SIRT-IN-2 Cat No HY-16616

Sirt2-IN-1 Cat No HY-112427

wwwMedChemExpresscom 147

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9939Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9887Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9944Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity SIRT5 inhibitor 1 is a potent Human deacylaseSirtuin 5inhibitor with an of 011 μMIC50

Bioactivity Sirtinol is a inhibitor with s of 48 μM 577 μMsirtuin IC50and 131 μM for ySir2 hSIRT2 and hSIRT2 respectively

Bioactivity Sirtuin modulator 1 is a modulator of a homolog of SIRTl SIRT3with EC of lt 1 μM extracted from patent WO 201007185315A1 Compound No4

Bioactivity SRT 1460 a potent activator with an Sirtuin-1 (SIRT1) EC15value of 29 μM shows good selectivity for activation ofSIRT1 versus SIRT2 and SIRT3 (EC15 gt 300 μM) and is morepotent than Resveratrol and the closest sirtuin homologhellip

Bioactivity SRT 1720 is a selective activator of human with anSIRT1 of 016 μM and shows less potent activities agaiinstEC15

SIRT2 and SIRT3 with EC s of 37 μM and gt 300 μM15respectively

Bioactivity SRT 1720 Hydrochloride is a selective activator of withSIRT1an of 016 μM and shows less potent activities onEC15SIRT2 and SIRT3 with EC s of 37 μM and 300 μM15respectively

Bioactivity SRT 2104 is a first-in-class highly selective andbrain-permeable activator of the NAD dependent deacetylase+

increases Sirt1 protein but shows no effect on Sirt1Sirt1mRNA Used in the research of diabetes mellitus hellip

Bioactivity SRT 2183 is a selective activator with anSirtuin-1 (SIRT1) value of 036 μM SRT 2183 induces growth arrestEC15

[1]

and apoptosis concomitant with deacetylation of STAT3 andNF-κB and reduction of c-Myc protein levels [2]

Bioactivity Tenovin-1 is an inhibitor of and ansirtuin 1 sirtuin 2activator of and may have potential in the management ofp53cancer

Bioactivity Tenovin-6 is an inhibitor of and slightly inhibitsSIRT1 SIRT2 and is also a potent activator of with s ofHDAC8 p53 IC50

21 μM 10 μM and 67 μM for SirT1 SirT2 and SirT3respectively

SIRT5 inhibitor 1 Cat No HY-112634

Sirtinol Cat No HY-13515

Sirtuin modulator 1 Cat No HY-19758A

SRT 1460 Cat No HY-124037

SRT 1720 Cat No HY-10532

SRT 1720 Hydrochloride Cat No HY-15145

SRT 2104 Cat No HY-15262

SRT 2183 Cat No HY-19759

Tenovin-1 Cat No HY-13423

Tenovin-6 Cat No HY-15510

Purity 9855Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Tenovin-6 Hydrochloride is an inhibitor of and SIRT1 SIRT2slightly inhibits and is also a potent activator ofHDAC8

with s of 21 μM 10 μM and 67 μM for SirT1 SirT2p53 IC50and SirT3 respectively

Bioactivity Thiomyristoyl is a potent and specific inhibitor with anSIRT2 of 28 nMIC50

Bioactivity UBCS039 is the first synthetic specific Sirtuin 6 (SIRT6)activator inducing autophagy in human tumor cells with an

of 38 μM EC50[1]

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Tenovin-6 Hydrochloride Cat No HY-15510B

Thiomyristoyl Cat No HY-101278

UBCS039 Cat No HY-115453

wwwMedChemExpresscom 149

SRPKSerine-arginine protein kinases

SRPKs is a critical enzyme family that regulates splicing activity in thecell The first serine-arginine (SR) protein kinase identified is SRPK1which is isolated from mitotic cells and it is described tophosphorylate SR proteins and to promote their release from nuclearspeckles during the G2M phase of the cell cycle SRPK1 is theprototype of the SRPK family which also includes the twohomologous SRPK2 and SRPK3 proteins SRPKs are characterized by abipartite catalytic domain separated by a unique spacer sequence andare mainly localized in the cytoplasm of mammalian cellsSRPKs can translocate into the nucleus of cells under severalconditions such as during the G2M phase of the cell cycle or after

osmotic stress or as a consequence of activation of the epidermal growth factor (EGF) signal transduction pathway

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9917Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

SRPK Inhibitors amp Modulators

Bioactivity SPHINX31 is a potent and selective inhibitor of with an ofserinearginine-rich protein kinase 1 (SRPK1) IC50

59 nM SPHINX31 inhibits phosphorylation ofserinearginine-rich splicing factor 1 (SRSF1) SPHINX31 is apotential topical therapeutic for neovascular eye diseasehellip

Bioactivity SRPIN340 is an ATP-competitive serine-arginine-rich proteinkinase ( ) inhibitor with a of 089 μM for SRPK1SRPK Ki

Bioactivity SRPKIN-1 is a covalent and irreversible inhibitorSRPK12with s of 356 and 98 nM respectively Anti-angiogenesisIC50

effect [1]

150 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SPHINX31 Cat No HY-117661

SRPIN340 (SRPK inhibitor) Cat No HY-13949

SRPKIN-1 Cat No HY-116856

wwwMedChemExpresscom 151

Telomerase

Telomerase is a ribonucleoprotein that is an enzyme that adds DNAsequence repeats (TTAGGG in all vertebrates) to the 3 end of DNAstrands in the telomere regions which are found at the ends ofeukaryotic chromosomes This region of repeated nucleotide calledtelomeres contains noncoding DNA and hinders the loss of importantDNA from chromosome ends As a result every time the chromosomeis copied only 100ndash200 nucleotides are lost which causes no damageto the organisms DNA Telomerase is a reverse transcriptase thatcarries its own RNA molecule which is used as a template when itelongates telomeres which are shortened after each replication cycleTelomerase a eukaryotic ribonucleoprotein (RNP) complex contains

both an essential RNA and a protein reverse transcriptase subunit By reverse transcription the telomerase RNPmaintains telomere length stability in almost all cancer cells

Purity 980Clinical Data No Development ReportedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Telomerase Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity BIBR 1532 is a potent selective and non-competitive inhibitor with of 100 nM intelomerase IC50

a cell-free assay

Bioactivity Telomerase-IN-1 is a inhibitor with an ofTelomerase IC50019 μM

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

152 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

BIBR 1532 Cat No HY-17353

Telomerase-IN-1 Cat No HY-U00268

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

wwwMedChemExpresscom 153

TOPKT-LAK cell-originated protein kinase

TOPK (T-lymphokine-activated killer cellndashoriginated protein kinasealso known as PBK or PDZ-binding kinase) is a SerThr protein kinasethat is highly expressed in many types of human cancer includingbreast and lung cancers TOPK is included in the ldquoconsensus stemnessranking signaturerdquo gene list that is up-regulated in cancer stemcell-enriched tumors and is associated with poor prognosis inmultiple types of cancerTOPKPBK is an oncogenic kinase upregulated in most humancancers TOPK is important for mitotic cell division and thatphosphorylation by Cdk1 is needed for its activationTOPK a member of the MEK36-related MAPKK family is expressed in

a wide range of proliferating cells and tissues including cancer cells and testis TOPK negatively regulates the activityof p38α by phosphorylating the p38α-specific phosphatase MKP1 and enhancing the stability of MKP1 The MAPKphosphatase MKP1 an archetypal member of the MKP family plays a pivotal role in the deactivation of p38 through adephosphorylation reaction

Purity 9563Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

TOPK Inhibitors amp Modulators

Bioactivity HI-TOPK-032 is a potent and specific inhibitorTOPK Bioactivity OTS-964 is a potent T-lymphokine-activated killer inhibitor ( =28cell-originated protein kinase (TOPK) IC50

nM) which inhibits TOPK kinase activity with high affinityand selectivity

Bioactivity OTS514 is a highly potent inhibitor which inhibits TOPKTOPKkinase activity with a median inhibitory concentration ( )IC50value of 26 nM

154 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

HI-TOPK-032 Cat No HY-101550

OTS-964 Cat No HY-12467

OTS514 Cat No HY-18621

wwwMedChemExpresscom 155

Topoisomerase

Topoisomerases are enzymes that regulate the overwinding orunderwinding of DNA The winding problem of DNA arises due to theintertwined nature of its double-helical structure Topoisomerases areisomerase enzymes that act on the topology of DNA Type Itopoisomerase cuts one strand of a DNA double helix relaxationoccurs and then the cut strand is reannealed Type I topoisomerasesare subdivided into two subclasses type IA topoisomerases whichshare many structural and mechanistic features with the type IItopoisomerases and type IB topoisomerases which utilize acontrolled rotary mechanism Type II topoisomerase cuts both strandsof one DNA double helix pass another unbroken DNA helix through

it and then reanneal the cut strands This class is also split into two subclasses type IIA and type IIB topoisomeraseswhich possess similar structure and mechanisms

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 1 mg 5 mg

Purity 980Clinical Data LaunchedSize 1 mg 5 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9243Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 9808Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9889Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Topoisomerase Inhibitors amp Modulators

Bioactivity 9-Aminocamptothecin is a inhibitor withtopoisomerase Ipotent anticancer activity

Bioactivity Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) afluorescent molecule and the first described non-peptidicinhibitor showing discrete specificity for the CTRL(chymotrypsin-like) activity of the 20S proteasome [1]

Aclacinomycin A hydrochloride is also a dual inhibitor ofhellip

Bioactivity Aldoxorubicin (INNO-206) is an albumin-binding prodrug ofdoxorubicin which is released from albumin under acidicconditions Aldoxorubicin (INNO-206) has potent antitumoractivities in various cancer cell lines and in murine tumormodels

Bioactivity Amonafide is a inhibitor and DNAtopoisomerase IIintercalator that induces apoptotic signaling by blocking thebinding of Topo II to DNA

Bioactivity Amrubicin (SM-5887) is a DNA inhibitortopoisomerase IIused for the research of cancer

Bioactivity Amrubicin (hydrochloride) (SM-5887 (hydrochloride)) is a DNA inhibitor used for the research of cancertopoisomerase II

Bioactivity Amsacrine (m-AMSA) is an inhibitor of andtopoisomerase IIacts as an antineoplastic agent which can intercalates intothe DNA of tumor cells

Bioactivity Amsacrine hydrochloride (mAMSA hydrochloride) is an inhibitorof and acts as an antineoplastic agenttopoisomerase IIwhich can intercalates into the DNA of tumor cells

Bioactivity Banoxantrone D12 (AQ4N D12) is the deuterium labeledbanoxantrone Banoxantrone is a novel bioreductive agent thatcan be reduced to a stable DNA-affinic compound AQ4 which isa potent inhibitortopoisomerase II

Bioactivity Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) isthe deuterium labeled banoxantrone dihydrochlorideBanoxantrone is a novel bioreductive agent that can be reducedto a stable DNA-affinic compound AQ4 which is a potent

inhibitortopoisomerase II

156 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

9-amino-CPT (9-amino-20(S)-camptothecin) Cat No HY-100309

Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) Cat No HY-N2306A

Aldoxorubicin (INNO-206 DOXO-EMCH) Cat No HY-16261

Amonafide (AS1413) Cat No HY-10982

Amrubicin (SM-5887 AMR) Cat No HY-B0067

Amrubicin hydrochloride (SM-5887 (hydrochloride) AMR (hydrochloride)) Cat No HY-B0067A

Amsacrine (m-AMSA acridinyl anisidide) Cat No HY-13551

Amsacrine hydrochloride (m-AMSA hydrochloride acridinyl anisidide hydrochloride) Cat No HY-13551A

Banoxantrone D12 (AQ4N D12) Cat No HY-13562S

Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) Cat No HY-13562AS

wwwMedChemExpresscom 157

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity 9826Clinical Data Phase 4Size 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9635Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg

Purity 9818Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9880Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg

Bioactivity Banoxantrone dihydrochloride is a novel bioreductive agentthat can be reduced to a stable DNA-affinic compound AQ4which is a potent inhibitortopoisomerase II

Bioactivity Belotecan hydrochloride (CKD-602 hydrochloride) a inhibitor is a synthetic and water-solubleTopoisomerase I

camptothecin derivative

Bioactivity Berberine chloride is an alkaloid isolated from the Chineseherbal medicine Huanglian as an Berberine chlorideantibioticinduces reactive oxygen species ( ) generation andROSinhibits Antineoplastic propertiesDNA topoisomerase

[1]

Bioactivity Berberine chloride hydrate is an alkaloid isolated from theChinese herbal medicine Huanglian as an Berberineantibioticchloride hydrate induces reactive oxygen species ( )ROSgeneration and inhibits AntineoplasticDNA topoisomeraseproperties [1]

Bioactivity Betulinic acid is a natural pentacyclic triterpenoid acts asa eukaryotic inhibitor with an of 5topoisomerase I IC50μM and possesses anti-HIV anti-malarial anti-inflammatoryand anti-tumor properties

Bioactivity Bisantrene is a highly effective antitumor drug targetseukaryotic type II topoisomerases

Bioactivity Campathecin is a potent DNA enzyme topoisomerase Iinhibitor with an of 679 nMIC50

Bioactivity Daun02 is a prodrug of the inhibitortopoisomeraseDaunorubicin

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Banoxantrone dihydrochloride (AQ4N dihydrochloride) Cat No HY-13562A

Belotecan hydrochloride (CKD-602) Cat No HY-13566A

Berberine chloride (Natural Yellow 18 (chloride)) Cat No HY-18258

Berberine chloride hydrate (Natural Yellow 18 (chloride hydrate)) Cat No HY-17577

Betulinic acid (Lupatic acid Betulic acid) Cat No HY-10529

Bisantrene (CL216942) Cat No HY-100875

Campathecin (Camptothecin (S)-(+)-Camptothecin CPT) Cat No HY-16560

Daun02 Cat No HY-13061

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9965Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9888Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9839Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9947Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Doxorubicin is a cytotoxic anthracycline antibiotic for thetreatment of multiple cancers The possible mechanisms bywhich doxorubicin acts in the cancer cell are intercalationinto DNA and disruption of -mediated DNAtopoisomerase-IIrepair

Bioactivity Doxorubicin hydrochloride is a cytotoxic anthracyclineantibiotic for the treatment of multiple cancers The possiblemechanisms by which doxorubicin acts in the cancer cell areintercalation into DNA and disruption of

-mediated DNA repairtopoisomerase-II

Bioactivity Dxd is a potent inhibitor with an ofDNA topoisomerase I IC50031 μM used as a conjugated drug of HER2-targeting ADC(DS-8201a)

Bioactivity Edotecarin is a potent inhibitor of that cantopoisomerase Iinduces single-strand DNA cleavage with of 50 nMIC50

Bioactivity Ellipticine (NSC 71795) is a potent antineoplastic agentinhibits activitiesDNA topoisomerase II

Bioactivity Ellipticine (NSC 71795) hydrochloride is a potentantineoplastic agent inhibits DNA topoisomerase IIactivities

Bioactivity Epirubicin is a semisynthetic L-arabino derivative ofdoxorubicin and an antineoplastic agent by inhibiting

Topoisomerase

Bioactivity Epirubicin (hydrochloride) is a semisynthetic L-arabinoderivative of doxorubicin and an antineoplastic agent byinhibiting Topoisomerase

Bioactivity Etoposide (VP-16 VP-16-213) a chemotherapy medication usedfor the treatments of a number of types of cancer inhibits

by forming a complex with topoisomerase II andDNA synthesisDNA Etoposide arrests cell cycle in G2 and induces apoptoshellip

Bioactivity Exatecan is a water soluble inhibitor withtopoisomerase Ian of 22 μM (0975 μgmL) and can be used in cancerIC50research

158 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Doxorubicin (Hydroxydaunorubicin) Cat No HY-15142A

Doxorubicin hydrochloride (Hydroxydaunorubicin (hydrochloride)) Cat No HY-15142

Dxd (Exatecan derivative for ADC) Cat No HY-13631D

Edotecarin (J 107088 PF 804950) Cat No HY-13618

Ellipticine (NSC 71795) Cat No HY-15753

Ellipticine hydrochloride (NSC 71795 (hydrochloride)) Cat No HY-15753A

Epirubicin Cat No HY-13624

Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride) Cat No HY-13624A

Etoposide (VP-16 VP-16-213) Cat No HY-13629

Exatecan (DX-8951) Cat No HY-13631

wwwMedChemExpresscom 159

Purity 9830Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9803Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9912Clinical Data Phase 3Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg 500 mg

Bioactivity Exatecan Mesylate is a water soluble topoisomerase Iinhibitor with an of 22 μM (0975 μgmL) and can beIC50used in cancer research

Bioactivity Flumequine (R-802) is a quinolone antibiotic and acts as a inhibitor with an of 15 μM (392topoisomerase II IC50

μgmL)

Bioactivity Genz-644282 is a non-camptothecin inhibitortopoisomerase Iused for cancer research

Bioactivity Idarubicin hydrochloride is an anthracycline antileukemicdrug It inhibits the interfering with thetopoisomerase IIreplication of DNA and RNA transcription

Bioactivity Indotecan (LMP-400) is a potent topoisomerase 1(Top1)inhibitor with values of 300 1200 560 nM for P388IC50HCT116 MCF-7 cell lines respectively

Bioactivity Intoplicine is a and inhibitorDNA topoisomerase I II

Bioactivity Irinotecan is a water soluble inhibitortopoisomerase Ipreventing religation of the DNA strand by binding totopoisomerase I-DNA complex

Bioactivity Irinotecan hydrochloride is a water soluble topoisomerase Iinhibitor mainly used to treat colon cancer and rectal cancer

Bioactivity Irinotecan hydrochloride trihydrate is a water soluble inhibitor with antitumor activitytopoisomerase I

Bioactivity Karenitecin (Cositecan) is a inhibitor withtopoisomerase Ipotent anti-cancer activity

Exatecan Mesylate (DX8951f) Cat No HY-13631A

Flumequine (R-802) Cat No HY-B0526

Genz-644282 Cat No HY-16228

Idarubicin hydrochloride (4-Demethoxydaunorubicin hydrochloride) Cat No HY-17381

Indotecan (LMP-400 NSC-724998) Cat No HY-18351

Intoplicine Cat No HY-101647

Irinotecan ((+)-Irinotecan CPT-11) Cat No HY-16562

Irinotecan hydrochloride (CPT-11 hydrochloride Camptothecin 11 hydrochloride) Cat No HY-16562A

Irinotecan hydrochloride trihydrate Cat No HY-16568

Karenitecin (Cositecan BNP 1350) Cat No HY-14812

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9690Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9902Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9702Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg

Bioactivity LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I inhibitor with antitumor activity (Top1) [1]

Bioactivity LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNAintercalator and inhibitor withTopoisomerase I (Top1)antitumor activity [1]

Bioactivity MC-DOXHZN is an albumin-binding prodrug of Doxorubicin withacid-sensitive properties [1]

Bioactivity MC-DOXHZN hydrochloride is an albumin-binding prodrug ofDoxorubicin with acid-sensitive properties [1]

Bioactivity Mitoxantrone is a inhibitor also inhibitstopoisomerase IIprotein kinase C ( ) activity with an of 85 μMPKC IC50

Bioactivity Mitoxantrone dihydrochloride is a topoisomerase IIinhibitor also inhibits protein kinase C ( ) activityPKCwith an of 85 μMIC50

Bioactivity Namitecan is a potent inhibitor withtopoisomerase Iantitumor property

Bioactivity Pirarubicin is an anthracycline antibiotics acts as a inhibitor and is a widely used fortopoisomerase II

treatment of various cancers in particular solid tumors

Bioactivity Pirarubicin Hydrochloride is an anthracycline antibioticsacts as a inhibitor and is a widely usedtopoisomerase IIfor treatment of various cancers in particular solid tumors

Bioactivity Pixantrone is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

160 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

LMP744 (MJ-III65 NSC706744) Cat No HY-U00248

LMP744 hydrochloride (MJ-III65 hydrochloride NSC706744 hydrochloride) Cat No HY-U00248A

MC-DOXHZN (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat No HY-16261A

MC-DOXHZN hydrochloride (Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat No HY-16261B

Mitoxantrone (mitozantrone) Cat No HY-13502

Mitoxantrone dihydrochloride (mitozantrone dihydrochloride) Cat No HY-13502A

Namitecan (ST-1968) Cat No HY-14821

Pirarubicin (THP) Cat No HY-13725

Pirarubicin Hydrochloride (THP Hydrochloride) Cat No HY-13725A

Pixantrone (BBR 2778) Cat No HY-13727

wwwMedChemExpresscom 161

Purity 9920Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 100 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 50 mg 100 mg 200 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9960Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Pixantrone dimaleate is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

Bioactivity Podocarpusflavone A is a DNA topoisomerase I inhibitor havemoderated anti-proliferative activity induce cell apoptosis inMCF-7 is developing anti-tumor drugs target DNAtopoisomerase I In vitro podocarpusflavone-A show significantinhibitions against DLD KB MCF-7 HEp-2 tumor cell lineshellip

Bioactivity SN-38 (NK012) is an active metabolite of the Topoisomerase Iinhibitor Irinotecan SN-38 (NK012) inhibits and DNA RNA

with s of 0077 and 13 μM respectivelysynthesis IC50

Bioactivity SW044248 is a non-canonical inhibitor andtopoisomerase Iselectively toxic for certain non-small cell lung cancer(NSCLC) cell lines

Bioactivity TAS-103 is a dual inhibitor of DNA usedtopoisomerase IIIfor cancer research

Bioactivity TAS-103 dihydrochloride is a dual inhibitor of DNA used for cancer researchtopoisomerase III

Bioactivity Teniposide is a podophyllotoxin derivative acts as a inhibitor and used as a chemotherapeutictopoisomerase II

agent

Bioactivity Top1 inhibitor 1 (compound 28) is a potent human inhibitor with an value of 29topoisomerase I (Top1) IC50

nM [1]

Bioactivity Topotecan (SKF 104864A NSC 609669) is a Topoisomerase Iinhibitor The values of Topotecan at 24 h are 273plusmn025IC50μM of U251 cells 295plusmn023 μM of U87 cells 546plusmn041 μM ofGSCs-U251 and 595plusmn024 μM of GSCs-U87

Bioactivity Topotecan Hydrochloride (SKF 104864A Hydrochloride NSC 609669Hydrochloride) is a inhibitor with potentTopoisomerase Iantineoplastic activities

Pixantrone dimaleate (BBR 2778 dimaleate) Cat No HY-13727A

Podocarpusflavone A Cat No HY-N2198

SN-38 (NK012) Cat No HY-13704

SW044248 Cat No HY-19637

TAS-103 (BMS-247615) Cat No HY-13758

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) Cat No HY-13758A

Teniposide (VM26) Cat No HY-13761

Top1 inhibitor 1 Cat No HY-126142

Topotecan (SKF 104864A NSC 609669) Cat No HY-13768

Topotecan Hydrochloride (SKF 104864A (Hydrochloride) NSC 609669 (Hydrochloride)) Cat No HY-13768A

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Bioactivity Voreloxin is a first-in-class inhibitortopoisomerase IIthat intercalates DNA and induces site-selective DNA DSB G2arrest and apoptosis

Bioactivity Voreloxin Hydrochloride is a first-in-class topoisomerase IIinhibitor that intercalates DNA and induces site-selective DNADSB G2 arrest and apoptosis

Bioactivity β-Lapachone is a naturally occurring O-naphthoquinone acts asa inhibitor and induces apoptosis bytopoisomerase Iinhibiting cell cycle progression

162 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Voreloxin (SNS-595 Vosaroxin AG 7352) Cat No HY-10534

Voreloxin Hydrochloride (SNS-595 Hydrochloride Vosaroxin

Hydrochloride AG 7352 Hydrochloride) Cat No HY-16518

β-Lapachone (ARQ-501 NSC-26326) Cat No HY-13555

wwwMedChemExpresscom 163

Wee1

Wee1 is a nuclear kinase belonging to the SerThr family of proteinkinases in the fission yeast ( )Schizosaccharomyces pombe S pombeWee1 has amolecular mass of 96 kDa and it is a key regulator of cellcycle progression Wee1 influences cell size by inhibiting the entryinto mitosis through inhibiting Cdk1 Wee1 has homologues in manyother organisms including mammals Wee1 inhibits Cdk1 byphosphorylating it on two different sites Tyr15 and Thr14 Cdk1 iscrucial for the cyclin-dependent passage of the various cell cyclecheckpoints At least three checkpoints exist for which the inhibitionof Cdk1 by Wee1 is important G M checkpoint Cell size checkpoint2DNA damage checkpoint Wee1 is shown to phosphorylate histone

H2B at tyrosine 37 residue which regulates global expression of histones

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Wee1 Inhibitors amp Modulators

Bioactivity Adavosertib (AZD-1775 MK-1775) is a potent inhibitorWee1with an of 52 nMIC50

Bioactivity PD0166285 is a inhibitor and a weak inhibitorWEE1 Myt1with s of 24 and 72 nM respectivelyIC50

164 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Adavosertib (AZD1775 MK-1775) Cat No HY-10993

PD0166285 Cat No HY-13925

Page 5: Cell Cycle/DNA Damage - MedchemExpress.com · 2019. 7. 2. · G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition,

wwwMedChemExpresscom 5

Purity 9517Clinical Data LaunchedSize 10 mg 50 mg

Purity 9524Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg 1 g 2 g

Purity 9973Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9973Clinical Data LaunchedSize 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Antifolate Inhibitors amp Modulators

Bioactivity Calcium N5-methyltetrahydrofolate(NSC173328) is the calciumsalt of levomefolic acid which has been proposed fortreatment of cardiovascular disease and advanced cancers suchas breast and colorectal cancers

Bioactivity Cycloguanil D6 is the deuterium labeled Cycloguanil which isa dihydrofolate reductase inhibitor

Bioactivity Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanilwhich is a dihydrofolate reductase inhibitor

Bioactivity Diaveridine (EGIS-5645) is a ( )dihydrofolate reductase DHFRinhibitor with a of 115 nM for the wild type DHFR and alsoKian antibacterial agent

Bioactivity EC0489 a conjugate of folic acid and desacetyl vinblastinehydrazide is a high-affinity ligand for the folate receptor(FR) Refractory or metastatic Tumor Small molecule-drug[1]

conjugate (SMDC) [2]

Bioactivity Folinic acid is an adjuvant used in cancer chemotherapyinvolving the drug methotrexate Target Antifolate Folinicacid is a 5-formyl derivative of tetrahydrofolic acid It isreadily converted to other reduced folic acid derivatives(eg tetrahydrofolate) and thus has vitamin activity thathellip

Bioactivity Leucovorin Calcium is a reduced folic acid IC50 Value 30 μMfor zcSHMT and70 μM for zmSHMT [2] Target Antifolate invitro Increasing concentrations of leucovorin (N5-CHO-THF)inhibit both zcSHMT and hcSHMT activities substantially yetto a lesser extent than zmSHMT The IC50 of leucovorin ishellip

Bioactivity Folinic Acid is a reduced folic acid which is used incombination with other chemotherapy drugs Target Folateanalog Approved 2008 Folinic acid (calcium salt pentahydrate)is the calcium salt form of folinic acid which is one of theforms of folate found naturally in foods Folate deficiency ishellip

Bioactivity Levoleucovorin calcium is the calcium salt of Levoleucovorinwhich is the enantiomerically active form of folinic acidIC50 value Target Levoleucovorin is used to treat or preventtoxic effects of methotrexate in people who have receivedmethotrexate to treat bone cancer Levoleucovorin is also usedhellip

Bioactivity Levomefolate is an artificial form of folate IC50 ValueTarget Antifolate The calcium salt ofL-5-methyltetrahydrofolic acid which belongs to the group offolate vitamins (Vitamin B9 Folacin) It is a coenzymatedform of folic acid and a more bioavailable alternative inhellip

Calcium N5-methyltetrahydrofolate (NSC173328) Cat No HY-17557

Cycloguanil D6 (Chlorguanide triazine D6) Cat No HY-12784S

Cycloguanil D6 Nitrate (Chlorguanide triazine D6 Nitrate) Cat No HY-12784S1

Diaveridine (EGIS-5645) Cat No HY-B1902

EC0489 Cat No HY-114306

Folinic acid (leucovorin) Cat No HY-17556

Folinic acid Calcium (Leucovorin Calcium Calcium Folinate) Cat No HY-13664

Folinic acid calcium salt pentahydrate (Leucovorin calcium salt pentahydrate) Cat No HY-B0080

Levoleucovorin Calcium (Calcium levofolinate CL307782) Cat No HY-13667

Levomefolate calcium Cat No HY-17383

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9923Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg

Purity 9977Clinical Data LaunchedSize 10mM x 1mL in Water

50 mg 100 mg 200 mg

Purity 9930Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity LY 254155 an antifolate inhibits and binds tohGARFT with s of 21plusmn02 and 17plusmn01 nM respectivelymFBP Ki

Bioactivity LY309887 is a potent inhibitor of glycinamide ribonucleotideformyltransferase ( ) with a of 65 nM and hasGARFT Kiantitumor activity

Bioactivity Methotrexate is a antagonist with median of 78 nMfolate IC50in assayin vitro

Bioactivity Pemetrexed is a novel the values of theantifolate Kipentaglutamate of LY231514 are 13 72 and 65 nM forinhibits thymidylate synthase ( ) dihydrofolate reductaseTS( ) and glycinamide ribonucleotide formyltransferase (DHFR

) respectivelyGARFT

Bioactivity Pemetrexed disodium is a novel that inhibits theantifolatefolatedependent enzymes thymidylate synthase dihydrofolate

and reductase glycinamide ribonucleotide with s of 13 72 and 65 nMformyltransferase Ki

respectively

Bioactivity Pemetrexed disodium hemipenta hydrate is a novel antifolatethe values of the pentaglutamate of LY231514 are 13 72Kiand 65 nM for inhibits thymidylate synthase ( )TSdihydrofolate reductase ( ) and glycinamideDHFRribonucleotide formyltransferase ( ) respectivelyGARFT

Bioactivity Pralatrexate(Folotyn) is an antifolate and structurally afolate analog Its IC50 is lt 300 nM in some cell linesIC50 Value lt 300 nM Target Antifolate Pralatrexate is anantifolate (a folate analogue metabolic inhibitor) designed toaccumulate preferentially in cancer cells Based onhellip

Bioactivity Pyrimethamine(RP4753) is a medication used for protozoalinfections interferes with tetrahydrofolic acid synthesisfrom folic acid by inhibiting the enzyme dihydrofolatereductase (DHFR) IC50 Value 154 nM (Plasmodium falciparum)[1] Target DHFR antifolate in vitro Three susceptibilityhellip

Bioactivity Trimethoprim is a bacteriostatic antibiotic used mainly in theprophylaxis and treatment of urinary tract infections

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LY 254155 Cat No HY-14523

LY309887 Cat No HY-10818

Methotrexate (Amethopterin CL14377 WR19039) Cat No HY-14519

Pemetrexed (LY231514) Cat No HY-10820

Pemetrexed disodium (LY231514 disodium) Cat No HY-10820A

Pemetrexed disodium hemipenta hydrate (LY231514 (disodium hemipenta hydrate)) Cat No HY-13781

Pralatrexate Cat No HY-10446

Pyrimethamine (Pirimecidan Pirimetamin RP 4753) Cat No HY-18062

Trimethoprim Cat No HY-B0510

wwwMedChemExpresscom 7

APCAnaphase promoting complex

APC (Anaphase-Promoting Complex) is an E3 ubiquitin ligase thatmarks target cell cycle proteins for degradation by the 26Sproteasome The APCC is a large complex of 11ndash13 subunit proteinsincluding a cullin (Apc2) and RING (Apc11) subunit much like SCF TheAPCCs main function is to trigger the transition from metaphase toanaphase by tagging specific proteins for degradation The twoproteins of most importance that get degraded in this process assubstrates of the APCC are securin and S and M cyclins Securinreleases separase a protease after being degraded which in turntriggers the cleavage of cohesin the protein complex that binds sisterchromatids together During metaphase sister chromatids are linked

by intact cohesin complexes When securin undergoes ubiquitination by the APCC and releases separase whichdegrades cohesin sister chromatids become free to move to opposite poles for anaphase The APCC also targets themitotic cyclins for degradation resulting in the inactivation of M-CdK (mitotic cyclin-dependent kinase) complexespromoting exit from mitosis and cytokinesis

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9911Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

APC Inhibitors amp Modulators

Bioactivity TAME is a inhibitor and can be also utilizedserine proteaseas a substrate for the serine proteases trypsin plasmin andthrombin TAME is an inhibitor of[1] [2] [3]

which binds to the hellipanaphase-promoting complex (APC)

Bioactivity TAME hydrochloride is a inhibitor and can beserine proteasealso utilized as a substrate for the serine proteases trypsinplasmin and thrombin TAME hydrochloride is an[1] [2] [3]

inhibitor of which bihellipanaphase-promoting complex (APC)

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TAME Cat No HY-13255

TAME hydrochloride Cat No HY-13255A

wwwMedChemExpresscom 9

ATMATRAtaxia telangiectasia mutatedATM and RAD3 related

ATMATR are members of the PI3 family of serine-threonine kinasesand function as essential links between the sensors and effectors ofthe DNA damage response The roles of ATM and ATR partiallyoverlap and are cooperative however they are also known to playdistinct roles in protecting the cell from DNA damage ATM is mostlyresponsible for sending signals from DSBs (double-strand breaks)induced by ionizing radiation while the closely related ATR respondsto UV damage or stalled replication forks ATM and ATR are known tophosphorylate common as well as specific substrates to activatecheckpoint signaling The G1 S and G2 cell cycle checkpoints areprimarily regulated by the ATM (ataxia telangiectasia mutated) and

ATR (ATM and Rad3-related) protein kinases

Purity 9976Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9904Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9960Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

ATMATR Inhibitors amp Modulators

Bioactivity ATM Inhibitor-1 is a highly potent selective and orallyactive inhibitor with an of 07 nM shows weakATM IC50activity against mTOR (IC 21 μM) DNAPK (IC 28 μM)50 50PI3Kα (IC 38 μM) PI3Kβ (IC 103 μM) PI3Kγ hellip50 50

Bioactivity ATR inhibitor 1 is a inhibitor extracted from patentATRWO2015187451A1 compound I-l has a value below 1 microΜ Ki

[1]

Bioactivity AZ20 is a potent and selective inhibitor of with an ATR IC50of 5 nM and has 8-fold selectivity against (IC =38mTOR 50nM)

Bioactivity AZ32 is an orally bioavailable and blood-brainbarrier-penetrating inhibitor with an of lt62ATM IC50nM for ATM enzyme and an of 031 μM for ATM in cellIC50

Bioactivity AZD0156 is an oral potent and selective inhibitor withATMan of 058 nMIC50

Bioactivity AZD1390 is an inhibitorATM

Bioactivity BAY-1895344 is a potent orally available and selective ATRinhibitor with of 7 nM Anti-tumor activity IC50

[1]Bioactivity BAY-1895344 hydrochloride is a potent orally available and

selective inhibitor with of 7 nM Anti-tumorATR IC50

activity [1]

Bioactivity Berzosertib (VE-822) is an inhibitor with a value ofATR Kiless than 02 nM It also inhibits with a of 34 nMATM Ki

Bioactivity Ceralasertib (AZD6738) is a potent inhibitor of kinaseATRwith an of 1 nMIC50

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ATM Inhibitor-1 Cat No HY-112614

ATR inhibitor 1 Cat No HY-111451

AZ20 Cat No HY-15557

AZ32 Cat No HY-112305

AZD0156 Cat No HY-100016

AZD1390 Cat No HY-109566

BAY-1895344 Cat No HY-101566

BAY-1895344 hydrochloride Cat No HY-101566A

Berzosertib (VE-822 VX-970) Cat No HY-13902

Ceralasertib (AZD6738) Cat No HY-19323

wwwMedChemExpresscom 11

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9947Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9988Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9840Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity CGK733 is a potent inhibitor used for the researchATMATRof cancer

Bioactivity CP-466722 is a rapidly reversible inhibitor of with anATM of 41 μM and has no effects on PI3K or closely relatedIC50

PI3K-like protein kinase (PIKK) family members

Bioactivity ETP-46464 is an effective and inhibitor withmTOR ATRs of 06 and 14 nM respectivelyIC50

Bioactivity KU 59403 is a potent inhibitor with an of 3 nMATM IC50

Bioactivity KU-55933 is a potent inhibitor with an and ofATM IC50 Ki129 and 22 nM respectively and is highly selective for ATMas compared to DNA-PK PI3KPI4K ATR and mTOR

Bioactivity KU-60019 is an improved kinase-specific inhibitor withATM of 63 nMIC50

Bioactivity VE-821 is a potent ATP-competitive inhibitor of with ATR Ki of 13 nM26 nMIC50

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

CGK733 Cat No HY-15520

CP-466722 Cat No HY-11002

ETP-46464 Cat No HY-15521

KU 59403 Cat No HY-18650

KU-55933 Cat No HY-12016

KU-60019 Cat No HY-12061

VE-821 Cat No HY-14731

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

Aurora Kinase

Aurora kinases are serinethreonine kinases that are essential for cellproliferation Aurora kinase helps the dividing cell dispense its geneticmaterials to its daughter cells More specifically Aurora kinases play acrucial role in cellular division by controlling chromatid segregationDefects in this segregation can cause genetic instability a conditionwhich is highly associated with tumorigenesis Three Aurora kinaseshave been identified in mammalian cells to date Aurora A Aurora BAurora C Besides being implicated as mitotic regulators these threekinases have generated significant interest in the cancer research fielddue to their elevated expression profiles in many human cancers Thehuman Aurora kinases present a similar domain organization with a

N-terminal domain of 39 to 129 residues in length a protein kinase domain and a short C-terminal domain containing15 to 20 residues The N-terminal domain of three proteins share low sequence conservation which determinesselectivity during protein-protein interactions

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wwwMedChemExpresscom 13

Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9895Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9874Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Aurora Kinase Inhibitors amp Modulators

Bioactivity Alisertib (MLN 8237) is an oral active and selective Aurora A inhibitor with an of 12 nMkinase IC50

Bioactivity AMG 900 is a potent and highly selective kinasespan-Aurorainhibitor with of 5 nM 4 nM and 1 nM for IC50 Aurora A B

and respectivelyC

Bioactivity AT9283 is a multitargeted kinase inhibitor which potentlyinhibits ( =12 nM 11 nM)aurora kinase AB JAK23 IC50

Bioactivity Aurora A inhibitor I is a potent and highly selective Aurora inhibitor with with an of 34 nMA IC50

Bioactivity Aurora B inhibitor 1 is an (Aurora-1) inhibitorAurora Bextracted from patent WO2007059299A1 compound 1-3 has a Kivalue of lt0010 uM

Bioactivity Aurora inhibitor 1 is a potent inhibitor with an Aurora IC50of le 4 nM and le13 nM for and kinaseAurora A Aurora Brespectively [1]

Bioactivity AZD1152 is a pro-drug of Barasertib-hQPA which is a highlyselective inhibitor with of 037 nM in aAurora B IC50cell-free assay

Bioactivity AZD1152-HQPA is a highly selective Aurora inhibitor with an of 037 nM in aB IC50

cell-free assay and shows 3700-fold selectivity for Aurora Bover Aurora A

Bioactivity BI-847325 is an ATP competitive dual inhibitor of andMEKaurora kinases ( ) with values of 4 and 15 nM forAK IC50human MEK2 and AK-C respectively

Bioactivity CCT 137690 is a potent and orally available kinaseaurorainhibitor with s of 15 25 and 19 nM for aurora A B andIC50C respectively

Alisertib (MLN 8237) Cat No HY-10971

AMG 900 Cat No HY-13253

AT9283 Cat No HY-50514

Aurora A inhibitor I Cat No HY-70061

Aurora B inhibitor 1 Cat No HY-U00304

Aurora inhibitor 1 Cat No HY-111506

AZD1152 (Barasertib) Cat No HY-10127

Barasertib-HQPA (AZD2811 INH-34 AZD1152-HQPA) Cat No HY-10126

BI-847325 Cat No HY-18955

CCT 137690 Cat No HY-10804

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 1 mg 5 mg 10 mg 20 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9859Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9923Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9944Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data Phase 1Size 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 950Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity CCT129202 is an kinase inhibitor with s of 42aurora IC50198 and 227 nM for aurora A B and C respectively

Bioactivity CCT241736 is a potent and orally bioavailable dual andFLT3 inhibitor which inhibits Aurora kinasesAurora kinase

(Aurora-A 75 nM 38 nM Aurora-B 48 nM)Kd IC50 KdFLT3 kinase ( 62 nM) and FLT3 mutants includhellipKd

Bioactivity CYC-116 is a potent and inhibitor withaurora A aurora Bs of 8 and 9 nM respectivelyKi

Bioactivity Danusertib is a pyrrolo-pyrazole and inhibitoraurora kinasewith of 13 79 and 61 nM for Aurora A B and CIC50respectively

Bioactivity ENMD-2076 is a multi-targeted kinase inhibitor with s ofIC50186 14 582 159 927 708 564 nM for Aurora A Flt3

KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src PDGFRαrespectively

Bioactivity ENMD-2076 Tartrate is a multi-targeted kinase inhibitor withs of 186 14 582 159 927 708 564 nM for IC50 Aurora

A Flt3 KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src respectivelyPDGFRα

Bioactivity GSK-1070916 is a potent and selective ATP-competitiveinhibitor of and with s of 038 andaurora B aurora C Ki15 nM respectively and is gt250- fold selective overAurora A

Bioactivity Hesperadin is an ATP-competitive inhibitor of aurora Bkinase with an of 250 nMIC50

Bioactivity Ilorasertib (ABT-348) is an ATP-competitive multitargetedkinase inhibitor with s for inhibiting binding Aurora B (7IC50nM) C (1 nM) and A (120 nM) and also inhibits RET tyrosinekinase PDGFRβ and Flt1 with s of 7 nM 3 nM and 32 nMIC50

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

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CCT129202 Cat No HY-12049

CCT241736 Cat No HY-18161

CYC-116 Cat No HY-10558

Danusertib (PHA-739358) Cat No HY-10179

ENMD-2076 Cat No HY-10987A

ENMD-2076 Tartrate Cat No HY-10987

GSK-1070916 (GSK-1070916A) Cat No HY-70044

Hesperadin Cat No HY-12054

Ilorasertib (ABT-348) Cat No HY-16018

JNJ-7706621 Cat No HY-10329

wwwMedChemExpresscom 15

Purity 9820Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9928Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9911Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity KW-2449 is a multi-targeted kinase inhibitor of FLT3 ABL and with s of 66 14 4 and 48 nMABLT315I Aurora kinase IC50

respectively

Bioactivity LY3295668 is a potent orally active and highly specific inhibitor with values of 08 nM and 1038Aurora-A kinase Ki

nM for AurA and AurB respectively

Bioactivity MK-5108 is a highly potent and specific inhibitor of Aurora A with an value of 0064 nMkinase IC50

Bioactivity MK-8745 is an kinase inhibitor with an of 06aurora A IC50nM

Bioactivity MLN8054 is a potent selective and orally available aurora Akinase inhibitor with an of 4 nMIC50

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity PF-03814735 is a potent orally available and reversible and inhibitor with s of 08 and 05aurora A aurora B IC50

nM respectively

Bioactivity PHA-680632 is an kinase inhibitor with s of 27aurora IC50135 and 120 nM for aurora A B and C respectively

Bioactivity Reversine is a novel class of ATP-competitive Aurora kinaseinhibitor with s of 400 500 and 400 nM for IC50 Aurora A

and respectivelyAurora B Aurora C

Bioactivity SCH-1473759 is an inhibitor with s of 4 and 13 nMaurora IC50for aurora A and B respectively

KW-2449 Cat No HY-10339

LY3295668 (AK-01) Cat No HY-114258

MK-5108 (VX-689) Cat No HY-13252

MK-8745 Cat No HY-13819

MLN8054 Cat No HY-10180

NU6140 Cat No HY-107419

PF-03814735 Cat No HY-14574

PHA-680632 Cat No HY-10178

Reversine Cat No HY-14711

SCH-1473759 Cat No HY-10482

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg

Purity 9980Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity SCH-1473759 hydrochloride is an inhibitor with saurora IC50of 4 and 13 nM for aurora A and B respectively

Bioactivity SNS-314 is a potent and selective kinase inhibitoraurorawith s of 9 31 and 6 nM for aurora A B and CIC50respectively

Bioactivity TAK-632 is a potent inhibitor with of 14 24pan-RAF IC50

and 83 nM for respectivelyCRAF BRAFV600E BRAFWT

Bioactivity TAK-901 is a multi-targeted inhibitor with s of 21aurora IC50and 15 nM for aurora A and B respectively

Bioactivity Tozasertib (VX 680 MK-0457) is an inhibitor of Aurora ABC with s of 06 18 46 nM respectivelykinases Ki

Bioactivity XL228 is a multi-targeted tyrosine kinase inhibitor with sIC50of 5 31 16 61 2 nM for Bcr-Abl Aurora A IGF-1R Srcand respectivelyLyn

Bioactivity ZM-447439 is an kinase inhibitor with s of 110 andaurora IC50130 nM for aurora A and B respectively

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SCH-1473759 hydrochloride Cat No HY-10483

SNS-314 (SNS-314 Mesylate) Cat No HY-12003

TAK-632 Cat No HY-15767

TAK-901 Cat No HY-12201

Tozasertib (VX 680 MK-0457) Cat No HY-10161

XL228 Cat No HY-15749

ZM-447439 Cat No HY-10128

wwwMedChemExpresscom 17

Casein Kinase

Casein Kinases (CKs) are serinethreonine-selective enzymes thatfunction as regulators of signal transduction pathways in mosteukaryotic cell types

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9992Clinical Data Phase 2Size 1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Casein Kinase Inhibitors amp Modulators

Bioactivity Casein Kinase II Inhibitor IV is a small-molecule inducer ofepidermal keratinocyte differentiation

Bioactivity Casein Kinase II Inhibitor IV Hydrochloride is asmall-molecule inducer of epidermal keratinocytedifferentiation

Bioactivity CK1-IN-1 is a inhibitor extracted fromcasein kinase 1 (CK1)patent WO2015119579A1 compound 1c has s of 15 nM 16 nMIC50

73 nM for CK1δ and CK1ε p38σ MAPK respectively [1]

Bioactivity D4476 is a potent selective and cell-permeable inhibitor ofcasein kinase 1( ) with an value of 03 μM CK1 IC50 in vitro

Bioactivity DMAT is a potent and specific inhibitor with an CK2 IC50value of 130 nM

Bioactivity Ellagic acid is a natural antioxidant and acts as a potentand ATP-competitive inhibitor with an of 40 nM andCK2 IC50a of 20 nMKi

Bioactivity Emodin is a broad-spectrum anticancer agent Emodin inhibits II (CKII) activity with of 2 μMcasein kinase IC50

Bioactivity IC261 is a selective ATP-competitive inhibitor withCK1s of 1 μM 1 μM 16 μM for and Ckiα1IC50 Ckiδ Ckiε

respectively

Bioactivity LH846 is a selective inhibitor of with an of 290 nMCKIδ IC50and less potently inhibits CKIα and CKIε with s of 25 μMIC50and 13 μM respectively

Bioactivity Longdaysin is a and CK1α CK1δ extracellular inhibitor with s of  56signal-regulated kinase 2 (ERK2) IC50

microM 88 microM and 52 microM respectively [1] [2]

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Casein Kinase II Inhibitor IV Cat No HY-111378

Casein Kinase II Inhibitor IV Hydrochloride Cat No HY-111378A

CK1-IN-1 Cat No HY-111820

D4476 (Casein Kinase I Inhibitor) Cat No HY-10324

DMAT (Casein kinase II Inhibitor CK2 Inhibitor) Cat No HY-15535

Ellagic acid Cat No HY-B0183

Emodin (Frangula emodin) Cat No HY-14393

IC261 Cat No HY-12774

LH846 Cat No HY-15704

Longdaysin Cat No HY-18285

wwwMedChemExpresscom 19

Purity 9701Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9827Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Bioactivity NCC007 is a dual and inhibitorcasein kinase Iα (CKIα) δ (CKIδ)with s of 18 and 36 μM respectively and can be used inIC50

research of modulating mammalian circadian rhythms [1]

Bioactivity PF-4800567 is a potent and selective inhibitor of caseinkinase 1ϵ ( ) with an of 32 nM which is greaterCK1ϵ IC50than 20-fold selectivity over CK1δ ( 711 nM)IC50

Bioactivity PF-670462 is a potent and selective inhibitor of casein kinase with s of 77 nM and 14 nM( and )CK1ε CK1δ IC50

respectively

Bioactivity Silmitasertib (CX-4945) is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity Silmitasertib sodium salt is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity SR-3029 is a potent and ATP competitive and CK1δ CK1εinhibitor with s of 44 nM and 260 nM respectively andIC50

s of 97 nM for both kinasesKi

Bioactivity TA-01 is a potent and inhibitor with sCK1 p38 MAPK IC50of 64 nM 68 nM 67 nM for CK1ε CK1δ and p38 MAPKrespectively

Bioactivity TBB is a cell-permeable and ATP-competitive inhibitorCK2with an of 015 μM for rat liver CK2IC50

Bioactivity TTP 22 is a potent inhibitor with an of 100 nM andCK2 IC50a of 40 nMKi

NCC007 Cat No HY-128677

PF-4800567 Cat No HY-12470

PF-670462 Cat No HY-15490

Silmitasertib (CX-4945) Cat No HY-50855

Silmitasertib sodium salt (CX-4945 (sodium salt)) Cat No HY-50855B

SR-3029 Cat No HY-100011

TA-01 Cat No HY-100114

TBB (NSC 231634 Casein Kinase II Inhibitor I) Cat No HY-14394

TTP 22 Cat No HY-15479

CDKCyclin dependent kinase

CDKs (Cyclin-dependent kinases) are serine-threonine kinases firstdiscovered for their role in regulating the cell cycle They are alsoinvolved in regulating transcription mRNA processing and thedifferentiation of nerve cells CDKs are relatively small proteins withmolecular weights ranging from 34 to 40 kDa and contain little morethan the kinase domain In fact yeast cells can proliferate normallywhen their CDK gene has been replaced with the homologous humangene By definition a CDK binds a regulatory protein called a cyclinWithout cyclin CDK has little kinase activity only the cyclin-CDKcomplex is an active kinaseThere are around 20 Cyclin-dependent kinases (CDK1-20) known till

date CDK1 4 and 5 are involved in cell cycle and CDK 7 8 9 and 11 are associated with transcriptionCDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational Mostknowledge of CDK structure and function is based on CDKs of (Cdc2) (CDC28) and vertebratesS pombe S cerevisia(CDC2 and CDK2) The four major mechanisms of CDK regulation are cyclin binding CAK phosphorylation regulatoryinhibitory phosphorylation and binding of CDK inhibitory subunits (CKIs)

20 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 21

Purity 9815Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9969Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9973Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

CDK Inhibitors amp Modulators

Bioactivity (+)-BAY-1251152 is a inhibitor extracted from patent WOCDK92014076091 A1 example 1

Bioactivity (-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation(-) BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity (plusmn)-BAY-1251152 is a racemic mixture of BAY-1251152BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity 5-Iodo-indirubin-3-monoxime is a potent GSK-3β CDK5P25and inhibitor competing with ATP for binding toCDK1cyclin Bthe catalytic site of the kinase with s of 9 20 and 25IC50

nM respectively [1]

Bioactivity Abemaciclib (LY2835219) is a selective inhibitor withCDK46 values of 2 nM and 10 nM for CDK4 and CDK6 respectivelyIC50

Bioactivity Abemaciclib Metabolites M2 is a metabolite of abemaciclibacts as a potent and inhibitor with s in theCDK4 CDK6 IC50

range of 1-3 nM Anti-cancer activity [1]

Bioactivity Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is aselective inhibitor with s of 2 nM and 10 nM forCDK46 IC50CDK4 and CDK6 respectively

Bioactivity AMG 925 is a potent selective and orally available FLT3 dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMCDK4 IC50

respectively

Bioactivity AMG 925 HCl is a potent selective and orally available dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMFLT3 CDK4 IC50

respectively

Bioactivity AT7519 as a potent inhibitor of with s of 210 47CDKs IC50100 13 170 and lt10 nM for CDK1 CDK2 CDK4 to CDK6 andCDK9 respectively

(+)-BAY-1251152 Cat No HY-103019

(-)-BAY-1251152 Cat No HY-103019B

(plusmn)-BAY-1251152 Cat No HY-103019A

5-Iodo-indirubin-3-monoxime Cat No HY-111930

Abemaciclib (LY2835219) Cat No HY-16297A

Abemaciclib Metabolites M2 Cat No HY-128669

Abemaciclib methanesulfonate (LY2835219 (methanesulfonate)) Cat No HY-16297

AMG 925 Cat No HY-15889

AMG 925 HCl Cat No HY-15889A

AT7519 Cat No HY-50940

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 1Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9999Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9700Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9848Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9816Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity AT7519 Hydrochloride is a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity AT7519 trifluoroacetate as a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity Atuveciclib (BAY-1143572) is a potent and highly selectiveoral inhibitor Atuveciclib (BAY-1143572)PTEFb CDK9inhibits with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib Racemate (BAY-1143572 Racemate) is the racematemixture of Atuveciclib Atuveciclib is a potent and highlyselective oral inhibitor which supressesP-TEFb CDK9

with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is apotent and selective inhibitor which inhibits CDK9 CDK9

with an of 16 nMCycT1 IC50

Bioactivity AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 82nM AUZ 454 (K03861) inhibits CDK2 activity by competing withbinding of activating cyclins

Bioactivity AZD-5438 is a potent inhibitor of with of 16CDK129 IC50nM6 nM20 nM in cell-free assays AZD-5438 shows lessinhibition activity against GSK3β CDK5 and CDK6

Bioactivity AZD4573 is a inhibitor with an of lt3 nMCDK9 IC50extracted from patent US 20160376287 A1 example 14

Bioactivity BGG463 is a inhibitorCDK2 Bioactivity BI-1347 is a potent inhibitor extracted from patentCDK8WO2017202719A1 product I-003 has an of 11 nM IC50

[1]

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AT7519 Hydrochloride Cat No HY-50943

AT7519 trifluoroacetate Cat No HY-50940A

Atuveciclib (BAY-1143572) Cat No HY-12871B

Atuveciclib Racemate (BAY-1143572 Racemate) Cat No HY-12871

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) Cat No HY-12871C

AUZ 454 (K03861) Cat No HY-15004

AZD-5438 Cat No HY-10012

AZD4573 Cat No HY-112088

BGG463 Cat No HY-100600

BI-1347 Cat No HY-120350

wwwMedChemExpresscom 23

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9754Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9747Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity BMS-265246 is a potent and selective CDK12 inhibitor forCDK1cyclin B and CDK2cyclin E with IC50 of 6 nM and 9 nMrespectively

Bioactivity BS-181 is a highly selective inhibitor with an ofCDK7 IC5021 nM showing 40-fold selective over CDK1 2 4 5 6 or 9

Bioactivity BS-181 hydrochloride is a highly selective inhibitorCDK7with of 21 nM and gt 40-fold selective for CDK7 thanIC50CDK1 2 4 5 6 or 9

Bioactivity BSJ-03-123 is a potent and novel -selective small-moleculeCDK6degrader

Bioactivity Ca channel agonist 1 is an agonist of 2+ N-type Ca channel2+

and an inhibitor of with s of 1423 μM and 334Cdk2 EC50μM respectively and is used as a potential treatment formotor nerve terminal dysfunction

Bioactivity CC-671 is a dual ( )TTK protein kinase CDC2-like kinase CLK2inhibitor with s of 0005 and 0006 μM for TTK and CLK2IC50respectively

Bioactivity CCT-251921 is a potent selective and orally bioavailable inhibitor with an of 23 nMCDK8 IC50

Bioactivity CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 oflt8 nM extracted from reference 1 example 4 IC50 Valuelt8 nM [1] Target CDK9 In vitro In vivo

Bioactivity CDK46-IN-2 is a potent and inhibitor extractedCDK4 CDK6from patent US20180000819A1 Compound 1 has s of 27 andIC50

16 nM for CDK4 and CDK6 respectively [1]

Bioactivity CDK461 Inhibitor is a inhibitor with s of 3 andCDK46 IC501 nM respectively

BMS-265246 Cat No HY-15275

BS-181 Cat No HY-13266

BS-181 hydrochloride Cat No HY-13266A

BSJ-03-123 Cat No HY-111556

Ca2+ channel agonist 1 Cat No HY-41076

CC-671 Cat No HY-108709

CCT-251921 Cat No HY-19984

CDK-IN-2 (CDK inhibitor II) Cat No HY-13033

CDK46-IN-2 Cat No HY-114339

CDK461 Inhibitor Cat No HY-112280

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9548Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CDK8-IN-1 is a potent and selective inhibitor with anCDK8 of 3 nMIC50

Bioactivity CDK8-IN-3 is an inhibitor of extracted from patentCDK8WO2016041618A1 compound example 17

Bioactivity CDK8-IN-4 is an inhibitor of extracted from patentCDK8WO2014090692A1 compound example 16 with an of 02 nMIC50

Bioactivity CDK819-IN-1 is a potent selective and oral bioavailable dual inhibitor with s of 046 nM 099 nM andCDK819 IC50

270 nM for CDK8 CDK19 and CDK9 respectively

Bioactivity CDK9 Antagonist-1 (compounds 11c) is a potent and selective degrader based on PROTAC with an of 17 μM in MCF-7CDK9 IC50

cell lines Natural product Wogonin binds ubiquitin E3 ligasecereblon (CRBN) via a linker to form PROTAC [1]

Bioactivity CDK9-IN-1 is a novel selective inhibitor for theCDK9treatment of HIV infection with an of 39 nM forIC50CDK9CycT1 extracted from reference compound 87

Bioactivity CDK9-IN-2 is a special cyclin-dependent kinase 9 ( )CDK9inhibitor extracted from patent WO2012131594A1 compoundCDKI(8) has an of 5 nM and 7 nM in H929 multipleIC50myeloma(MM) cell line (72 hours) and A2058 skin cell line (72hours) respectively

Bioactivity CDK9-IN-8 is a highly effective and selective inhibitorCDK9with an of 12 nMIC50

Bioactivity CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM showsselective toxicity to CLL cells(LD50=80 nM) versus normal Bcell and normal CD34+ cell(LD50gt20 uM) IC50 value 4 nM80nM(KiLD50) [1] Target CDK9 inhibitor in vitro CDKI-73 wascytotoxic to all of the CLL samples tested (n = 38) with ahellip

Bioactivity CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 () inhibitor with an IC of 2 nMCLK1 50

24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CDK8-IN-1 Cat No HY-103492

CDK8-IN-3 Cat No HY-111463

CDK8-IN-4 Cat No HY-111465

CDK819-IN-1 Cat No HY-111427

CDK9 Antagonist-1 Cat No HY-112811

CDK9-IN-1 Cat No HY-13231

CDK9-IN-2 Cat No HY-16462

CDK9-IN-8 Cat No HY-102039

CDKI-73 Cat No HY-12445

CLK1-IN-1 Cat No HY-103082

wwwMedChemExpresscom 25

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9900Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9973Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9998Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CMPD 7 is a potent and selective inhibitor with an CDK12 IC50of 491 nM in enzymatic assay

Bioactivity CT7001 hydrochloride is a selective inhibitor withCDK7s of 41 nM and 578 nM for andIC50 CDK7CycHMAT1

respectivelyCDK2cycE1

Bioactivity Cucurbitacin E is a natural compound which from the climbingstem of Cucurbitacin E significantlyCucumic melo Lsuppresses the activity of the complexcyclin B1 CDC2

Bioactivity CVT-313 is a potent selective reversible andATP-competitive inhibitor of with of 05 μMCDK2 IC50

Bioactivity CYC065 is a second-generation orally availableATP-competitive inhibitor of kinasesCDK2 CDK 9

Bioactivity Dinaciclib is a potent inhibitor of with s of 1 1CDK IC503 and 4 nM for and respectivelyCDK2 CDK5 CDK1 CDK9

Bioactivity EHT 5372 is a strong inhibitor of family kinases withDYRKrsquos of 022 028 nM for DYRK1A and DYRK1B respectivelyIC s50

Bioactivity Flavopiridol is a broad spectrum and competitive inhibitor of inhibiting CDK1 CDK2 CDK4 with s of 30 170 100CDKs IC50

nM respectively

Bioactivity Flavopiridol Hydrochloride is a broad inhibitor of CDKcompeting with ATP to inhibit CDKs including CDK1 CDK2 CDK4with s of 30 170 100 nM respectivelyIC50

Bioactivity FMF-04-159-2 is a covalent inhibitor FMF-04-159-2CDK14inhibits CDK14 and CDK2 with s of 396 nM and 256 nM inIC50

NanoBRET assay respectively [1]

CMPD 7 Cat No HY-112261

CT7001 hydrochloride (ICEC0942 hydrochloride) Cat No HY-103712A

Cucurbitacin E (α-Elaterin α-Elaterine) Cat No HY-N0417

CVT-313 (Cdk2 Inhibitor III) Cat No HY-15339

CYC065 Cat No HY-101212

Dinaciclib (SCH 727965) Cat No HY-10492

EHT 5372 Cat No HY-111380

Flavopiridol (L868275 HMR-1275 Alvocidib) Cat No HY-10005

Flavopiridol Hydrochloride (HL 275 NSC 649890 MDL 107826A

FLAVOPIRIDOL HCL Alvocidib Hydrochloride) Cat No HY-10006

FMF-04-159-2 Cat No HY-127104

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9204Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 251 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9841Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity FN-1501 is a potent inhibitor of and with s ofFLT3 CDK IC50247 085 196 and 028 nM for CDK2cyclin A CDK4cyclinD1 CDK6cyclin D1 and FLT3 respectively FN-1501 hasanticancer activity

Bioactivity GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO) is apotent selective reversible and ATP-competitive inhibitor of

and complex with s of 5 nM320GSK-3αβ CDK1-cyclinB IC50nM80nM for (GSK-3αβ)CDK1CDK5 respectively

Bioactivity GSK3186899 is an inhibitor of cdc-2-related kinase 12 () with an of 14 μM for in anCRK12 EC50 L donovani

intra-macrophage assay

Bioactivity IIIM-290 is a potent and oral inhibitor with s of 90CDK IC50and 94 nM for CDK2A and CDK9T1

Bioactivity Indirubin-3-monoxime-5-sulphonic acid is a potent andselective inhibitor of and with s ofCDK1 CDK5 GSK-3β IC50

5 nM 7 nM and 80 nM respectively [1]

Bioactivity Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK)inhibitor with values of 55 nM 35 nM 150 nM 300 nMIC50and 65 nM for CDK1cyclin B CDK2cyclin A CDK2cyclin ECDK4cyclin D1 and CDK5p35 respectively [1]

Bioactivity JH-XI-10-02 is a potent and selective degrader of withCDK8an of 159 nM based on JH-XI-10-02 causesIC50 PROTAC

proteasomal degradation does not affect CDK8 mRNA levelsJH-XI-10-02 shows no effect on CDK19 [1]

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

Bioactivity JSH-150 is a highly selective and potent inhibitor withCDK9an IC of 1 nM50

Bioactivity Kenpaullone is a potent inhibitor of andCDK1cyclin B with s of 04 μM and 23 nM and also inhibitsGSK-3β IC50

CDK2cyclin A CDK2cyclin E and CDK5p25 with s of 068IC50μM 75 μM 085 μM respectively

26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

FN-1501 Cat No HY-111361

GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO MLS 2052) Cat No HY-10580

GSK3186899 (DDD-853651) Cat No HY-112622

IIIM-290 Cat No HY-111356

Indirubin-3-monoxime-5-sulphonic acid Cat No HY-111931

Indirubin-5-sulfonate Cat No HY-111932

JH-XI-10-02 Cat No HY-111518

JNJ-7706621 Cat No HY-10329

JSH-150 Cat No HY-X0150

Kenpaullone (9-Bromopaullone NSC-664704) Cat No HY-12302

wwwMedChemExpresscom 27

Purity 9861Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9847Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Bioactivity KH-CB19 is a potent and highly specific inhibitor of theCDC2-like kinase isoforms 1 and 4 (CLK1CLK4) IC50 value 20nM (CLK1) [1] Target CLK14 inhibitor in vitro KH-CB19showed potent inhibition of CLK1 with an IC50 of 20 nM andfor the pure isomer KH-CB19 almost 100-fold selectivityhellip

Bioactivity LDC000067 is a highly specific inhibitor with an CDK9 IC50value of 44plusmn10 nM in vitro

Bioactivity LDC4297 is a potent and selective inhibitor with an CDK7 IC50of 013 nM

Bioactivity Lerociclib (G1T38) is a potent and selective inhibitor of with of 1 nM 2 nM for CDK4CyclinD1 andCDK46 IC s50

CDK6CyclinD3 respectively

Bioactivity Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potentand selective inhibitor of with of 1 nMCDK4 CDK6 IC s50and 2 nM for and respectivelyCDK4 CyclinD1 CDK6 CyclinD3

Bioactivity LY2857785 is a type I reversible and competitive ATP kinaseinhibitor against ( 11 nM) and other transcriptionCDK9 IC50kinases ( 16 nM) and ( 246 nM)CDK8 IC50 CDK7 IC50

Bioactivity LY3177833 is an and inhibitor extracted fromCDC7 pMCM2patent US 20140275131and patent WO 2014143601 A1 compoundexample 4 has values of 33 nM and 290 nM respectivelyIC50

Bioactivity MBQ-167 is a dual inhibitor with of 103 nMRacCdc42 IC s50for Rac 123 and 78 nM for Cdc42 in MDA-MB-231 cellsrespectively

Bioactivity MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin inhibitor with an of 5 nM at least 22-fold moreT1 IC50

selective for CDK9 over other CDKs MC180295 also inhibitsGSK-3α and GSK-3β MC180295 ((rel)-MC180295) has pothellip

Bioactivity Milciclib (PHA-848125) is a potent dual inhibitor of andCDK with s of 45 150Tropomyosin receptor kinase (TRK) IC50

160 363 398 nM and 53 nM for cyclin ACDK2 cyclin HCDK7cyclin D1CDK4 cyclin ECDK2 cyclin BCDK1 and TRKArespectively

KH-CB19 Cat No HY-12828

LDC000067 (LDC067) Cat No HY-15878

LDC4297 Cat No HY-12653

Lerociclib (G1T38) Cat No HY-112272

Lerociclib dihydrochloride (G1T38 dihydrochloride) Cat No HY-112272A

LY2857785 Cat No HY-12293

LY3177833 Cat No HY-100023

MBQ-167 Cat No HY-112842

MC180295 ((rel)-MC180295) Cat No HY-119940

Milciclib (PHA-848125) Cat No HY-10424

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9703Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9851Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Bioactivity ML167 is a highly selective Cdc2-like kinase 4 ( )Clk4inhibitor with of 136 nM gt10-fold selectivity forIC50closely related kinases Clk1 Clk2 Clk3 and Dyrk1A1B

Bioactivity MSC2530818 is a potent selective and orally available CDK8inhibitor with an of 26 nM for CDK8IC50

Bioactivity NG 52 (Compound 52 ) is a potent cell-permeable reversibleselective and ATP-compatible inhibitor of the cellcycle-regulating kinase Cdc28p (IC50 = 7 μM) and the relatedPho85p kinase (IC50 = 2 μM)

Bioactivity Nimbolide is a triterpene derived from the leaves and flowersof neem ( L) Nimbolide induces apoptosisAzadirachta indicathrough inactivation of Nimbolide inhibits NF-κB CDK4

kinase activity Nimbolide suppresses the NF-κB WntCDK6PI3K-Akt MAPK and JAK-STAT signaling pathways [1]

Bioactivity NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and26 μM for CDK2 and CDK1 IC50 value 17μM (CDK2) 26μM (CDK1)Target CDK in vitro NU2058 is a competitive inhibitor ofCDK2 with respect to ATP (Ki value CDK2 12 3 μM) that bindsin the ATP binding pocket in a different orientation fromhellip

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity NU6300 is the first covalent ATP-competitive CDK2 inhibitorIC50 value Target CDK2 in vitro NU6300 is a covalent CDK2inhibitor that illustrates the potential of using vinylsulfones to mediate irreversible inhibition NU6300 blocks theinhibitor binding site The effect was time dependent andhellip

Bioactivity NVP-2 is a inhibitor with an of 05 nMCDK9 IC50

Bioactivity NVP-LCQ195 (AT9311 LCQ195) is a small molecule heterocyclicinhibitor of CDK1 CDK2 CDK3 and CDK5 with IC50 of 1-42 nM

Bioactivity ON-013100 an antineoplastic drug acts a mitotic inhibitorthat could inhibit expressionCyclin D1

28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

ML167 (CID44968231 NCGC00188654) Cat No HY-15951

MSC2530818 Cat No HY-101611

NG 52 (Compound 52) Cat No HY-15154

Nimbolide Cat No HY-116035

NU2058 (O6-(Cyclohexylmethyl)guanine) Cat No HY-19316

NU6140 Cat No HY-107419

NU6300 Cat No HY-18930

NVP-2 Cat No HY-12214A

NVP-LCQ195 (LCQ-195 AT9311) Cat No HY-15241

ON-013100 Cat No HY-112822

wwwMedChemExpresscom 29

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9996Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity ON123300 is a potent inhibitor of CDK4 with an IC50 of 38nM with little inhibitory activity against CDKs 125 and 8

Bioactivity Palbociclib (PD 0332991) is a selective and CDK4 CDK6inhibitor with s of 11 and 16 nM respectivelyIC50Palbociclib is a drug for the treatment of ER-positive andHER2-negative breast cancer

Bioactivity Palbociclib hydrochloride is a highly selective CDK46inhibitor with s of 11 nM and 16 nM respectivelyIC50

Bioactivity Palbociclib isethionate is a highly selective inhibitorof with s of 11 nM16 nMCDK46 IC50respectively

Bioactivity PF-06873600 is a selective and orally bioavailable inhibitorof cyclin-dependent kinase with values of 009 nM(CDK) Ki013 nM and 016 nM for CDK2 CDK4 and CDK6 respectivelyPF-06873600 has potential antineoplastic activity [1] [2]

Bioactivity PHA-767491 is a dual inhibitor with s of 10 nMCdc7Cdk9 IC50and 34 nM respectively

Bioactivity PHA-767491 hydrochloride is a dual inhibitor withCdc7Cdk9s of 10 nM and 34 nM respectivelyIC50

Bioactivity PHA-793887 is a potent ATP-competitive inhibitor canCDKinhibit Cdk2 Cdk1 Cdk4 and Cdk9 with s of 8 nM 60 nMIC5062 nM and 138 nM respectively and also inhibits glycogensynthase kinase 3β with an of 79 nMIC50

Bioactivity PROTAC CDK9 Degrader-1 is a selective degraderCDK9 Bioactivity Purvalanol A is a potent inhibitor which inhibitsCDKcdc2-cyclin B cdk2-cyclin A cdk2-cyclin E cdk4-cyclin D1and cdk5-p35 with s of 4 70 35 850 75 nMIC50resepctively

ON123300 Cat No HY-12624

Palbociclib (PD 0332991) Cat No HY-50767

Palbociclib hydrochloride (PD 0332991 hydrochloride) Cat No HY-50767A

Palbociclib isethionate (PD 0332991 isethionate) Cat No HY-A0065

PF-06873600 Cat No HY-114177

PHA-767491 (CAY10572) Cat No HY-13461

PHA-767491 hydrochloride (CAY-10572 hydrochloride) Cat No HY-13461A

PHA-793887 Cat No HY-11001

PROTAC CDK9 Degrader-1 Cat No HY-103628

Purvalanol A (NG-60) Cat No HY-18299A

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9900Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9983Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitorwith IC50 values of 6 6 9 gt 10000 and 6 nM forcdc2cyclin B cdk2cyclin A cdk2cyclin E cdk4cyclin D1and cdk5-p35 respectively

Bioactivity R547 is a potent ATP-competitive inhibitor of CDK124 with Kiof 2 nM3 nM1 nM

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity Ribociclib (LEE011) is a highly specific inhibitorCDK46with s of 10 nM and 39 nM respectivelyIC50

Bioactivity Ribociclib hydrochloride (LEE011 hydrochloride) is a highlyspecific inhibitor with values of 10 nM and 39CDK46 IC50nM respectively and is over 1000-fold less potent againstthe cyclin BCDK1 complex

Bioactivity Ribociclib succinate (LEE011 succinate) is a highly specific inhibitor with values of 10 nM and 39 nMCDK46 IC50

respectively and is over 1000-fold less potent against thecyclin BCDK1 complex

Bioactivity Ribociclib succinate hydrate (LEE011 succinate hydrate) is ahighly specific inhibitor with values of 10 nMCDK46 IC50and 39 nM respectively and is over 1000-fold less potentagainst the cyclin BCDK1 complex

Bioactivity Riviciclib (P276-00 free base) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib shows antituhellip[1] [2]

Bioactivity Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib hydrochlorhellip[1] [2]

30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Purvalanol B (NG 95) Cat No HY-18299

R547 Cat No HY-10014

RGB-286638 Cat No HY-15504

RGB-286638 free base Cat No HY-15504A

Ribociclib (LEE011) Cat No HY-15777

Ribociclib hydrochloride (LEE011 (hydrochloride)) Cat No HY-15777A

Ribociclib succinate (LEE011 (succinate)) Cat No HY-15777B

Ribociclib succinate hydrate (LEE011 (succinate hydrate)) Cat No HY-15777C

Riviciclib (P276-00 (free base)) Cat No HY-16559A

Riviciclib hydrochloride (P276-00) Cat No HY-16559

wwwMedChemExpresscom 31

Purity 9850Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9907Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9677Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ro-3306 is a potent and selective inhibitor of with sCDK1 Kiof 20 nM 35 nM and 340 nM for CDK1 CDK1cyclin B1 andCDK2cyclin E respectively

Bioactivity Roniciclib is an orally bioavailable pan-cyclin dependentkinase inhibitor with of 5-25 nM for CDK1 CDK2(CDK) IC s50CDK3 CDK4 CDK7 and CDK9

Bioactivity SB1317 is a potent inhibitor of and forCDK2 JAK2 FLT3the treatment of cancer with of 13 73 and 56 nM forIC50CDK2 JAK2 and FLT3 respectively

Bioactivity SEL120-34A is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A HCl is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A monohydrochloride is an ATP-competitive andselective inhibitor inhibits kinase activities ofCDK8CDK8CycC and CDK19CycC complexes with s of 44 nM andIC50104 nM respectively with a of 3 nM for CDhellipKd

Bioactivity Seliciclib (Roscovitine) is a potent and selective CDKsinhibitor with s of 02 μM 065 μM and 07 μM for IC50 CDK5

and respectivelyCdc2 CDK2

Bioactivity Senexin A is a inhibitor with an of 280 nMCDK8 IC50

Bioactivity Simurosertib (TAK-931) is a selective cycle 7 kinase(CDC7)inhibitor with an lt03 nMIC50

Bioactivity SNS-032 (BMS-387032) is a selective inhibitor of CDK2 and with s of 38 nM 62 nM and 4CDK7 CDK9 IC50

nM respectively

Ro-3306 Cat No HY-12529

Roniciclib (BAY 1000394) Cat No HY-13914

SB1317 (TG02) Cat No HY-15166

SEL120-34A Cat No HY-111388

SEL120-34A HCl Cat No HY-111388B

SEL120-34A monohydrochloride Cat No HY-111388A

Seliciclib (Roscovitine CYC202 R-roscovitine) Cat No HY-30237

Senexin A Cat No HY-15681

Simurosertib (TAK-931) Cat No HY-100888

SNS-032 (BMS-387032) Cat No HY-10008

Purity 9846Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9796Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9882Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity SU9516 is a potent inhibitor with an of 22 nM andCDK2 IC50also shows inhibitory effects on CDK1 and CDK4 with s ofIC5040 200 nM respectively

Bioactivity SY-1365 is a highly selective covalent inhibitor of CDK7SY-1365 possesses therapeutic potential in both hematologicaland solid tumors [1]

Bioactivity T025 is an orally available and highly potent Cdc2-like kinase inhibitor with s of 48 0096 65 and 061 nM(CLK) Kd

for CLK1 CLK2 CLK3 and CLK4 respectively

Bioactivity THAL-SNS-032 is a selective degrader PROTAC consistingCDK9of a CDK-binding SNS-032 ligand linked to a thalidomidederivative that binds the E3 ubiquitin ligase Cereblon (CRBN)

[1]

Bioactivity THZ1 is a selective and potent covalent inhibitor withCDK7an of 32 nMIC50

Bioactivity THZ1 Hydrochloride is a selective and potent inhibitorCDK7with an of 32 nMIC50

Bioactivity THZ1-R is a non-cysteine reactive analog of THZ1 whichdisplays diminished activity for inhibition THZ1-RCDK7binds to with a of 142 nMCDK7 Kd

Bioactivity THZ2 is a potent and selective inhibitor with an ofCDK7 IC50139 nM

Bioactivity THZ531 is a covalent inhibitor of both and withCDK12 CDK13s of 158 nM and 69 nM respectivelyIC50

Bioactivity Trilaciclib is a inhibitor with s of 1 nM and 4 nMCDK46 IC50for CDK4 and CDK6 respectively

32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SU9516 Cat No HY-18629

SY-1365 Cat No HY-128587

T025 Cat No HY-112296

THAL-SNS-032 Cat No HY-123937

THZ1 Cat No HY-80013

THZ1 Hydrochloride Cat No HY-80013A

THZ1-R Cat No HY-19988

THZ2 Cat No HY-12280

THZ531 Cat No HY-103618

Trilaciclib (G1T28) Cat No HY-101467

wwwMedChemExpresscom 33

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Trilaciclib hydrochloride is a inhibitor with s ofCDK46 IC501 nM and 4 nM for CDK4 and CDK6 respectively

Bioactivity Voruciclib hydrochloride is a clinical stage oral CDK9inhibitor Voruciclib hydrochloride represses expression ofMCL-1 in multiple models of diffuse large B-cell lymphoma(DLBCL) [1]

Bioactivity Wogonin is a naturally occurring mono-flavonoid can inhibitthe activity of and and exhibitsCDK8 Wntanti-inflammatory and anti-tumor effects

Bioactivity XL413 is a potent selective and ATP competitive inhibitor of with an of 34 nM and also shows potent effectCdc7 IC50

with s of 215 42 nM on CK2 PIM1 respectively and anIC50 of 118 nM on pMCMEC50

Bioactivity XL413 hydrochloride is a potent selective and ATP competitiveinhibitor of with an of 34 nM and also showsCdc7 IC50potent effect with s of 215 42 nM on CK2 PIM1IC50respectively and an of 118 nM on pMCMEC50

Trilaciclib hydrochloride (G1T28 hydrochloride) Cat No HY-101467A

Voruciclib hydrochloride Cat No HY-12422A

Wogonin Cat No HY-N0400

XL413 Cat No HY-15260

XL413 hydrochloride Cat No HY-15260A

Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) are protein kinases that are involved in cellcycle control Two checkpoint kinase subtypes have been identifiedChk1 and Chk2 Chk1 is a central component of genome surveillancepathways and is a key regulator of the cell cycle and cell survivalChk1 is required for the initiation of DNA damage checkpoints andhas recently been shown to play a role in the normal (unperturbed)cell cycle Chk1 impacts various stages of the cell cycle including the Sphase G2M transition and M phase In addition to mediating cellcycle checkpoints Chk1 also contributes to DNA repair processesgene transcription embryo development cellular responses to HIVinfection and somatic cell viability Chk2 is a protein kinase that is

activated in response to DNA damage and is involved in cell cycle arrest In response to DNA damage and replicationblocks cell cycle progression is halted through the control of cell cycle regulators The protein encoded by this gene isa cell cycle checkpoint regulator and putative tumor suppressor

34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 35

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9877Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9990Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Checkpoint Kinase (Chk) Inhibitors amp Modulators

Bioactivity AZD-7762 is a potent ATP-competitive checkpoint kinase ( )Chkinhibitor in with an of 5 nM for Chk1IC50

Bioactivity BML-277 is a selective checkpoint kinase 2 ( ) inhibitorChk2with an of 15 nMIC50

Bioactivity CCT241533 is a potent and selective ATP competitive inhibitorof with an of 3 nM and of 116 nMCHK2 IC50 Ki

Bioactivity CCT241533 hydrochloride is a potent and selective CHK2inhibitor with an of 3 nM and a of 116 nMIC50 Ki

Bioactivity CCT244747 is a potent orally bioavailable and highlyselective inhibitor with an of 77 nM CCT244747CHK1 IC50also abrogates G2 checkpoint with an of 29 nMIC50

Bioactivity CCT245737 is a orally active and seletive inhibitorChk1with an of 13 nMIC50

Bioactivity CHIR-124 is a potent and selective inhibitor with Chk1 IC50of 03 nM and also potently targets and withPDGFR FLT3

s of 66 nM and 58 nMIC50

Bioactivity CHK-IN-1 is an inhibitor of and withCHK1 CHK2anti-proliferative activities

Bioactivity CHK1 inhibitor is an inhibitor of CHK1 Bioactivity CHK1-IN-2 is a checkpoint kinase 1 inhibitor with an(CHK1) of 6 nMIC50

AZD-7762 Cat No HY-10992

BML-277 (Chk2 Inhibitor II) Cat No HY-13946

CCT241533 Cat No HY-14715

CCT241533 hydrochloride Cat No HY-14715B

CCT244747 Cat No HY-18175

CCT245737 Cat No HY-18958

CHIR-124 Cat No HY-13263

CHK-IN-1 Cat No HY-U00345

CHK1 inhibitor Cat No HY-104022

CHK1-IN-2 Cat No HY-111369

Purity 9965Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9791Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity CHK1-IN-3 is a inhibitor with anCheckpoint Kinase 1 (CHK1) of 04 nM IC50

[1]Bioactivity GDC-0575 (ARRY-575 RG7741) is a highly-selective oral

small-molecule inhibitor with an of 12nMChk1 IC50

Bioactivity GDC-0575 dihydrochloride is an orally bioavailable CHK1inhibitor with an of 12 nM and has antitumor activityIC50

Bioactivity PF 477736 is a potent selective ATP-competitive inhibitor of with a of 049 nM 100-fold selectivity versus Chk1 Ki Chk2

( 47 nM)Ki

Bioactivity Prexasertib (LY2606368) is a potent selective andATP-competitive inhibitor with ancheckpoint kinase 1 (Chk1)

and a of lt1 nM and 09 nM respectivelyIC50 Ki

Bioactivity Prexasertib dihydrochloride (LY2606368 dihydrochloride) is apotent and selective ATP competitive inhibitor of the Chk1protein kinase with s of lt1 nM and 8 nM for CHK1 andIC50CHK2 respectively and a of 09 nM against purified CHK1Ki

Bioactivity Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is apotent selective ATP competitive and inhibitorCHK1 CHK2with a of 09 nM for CHK1 and s of lt1 nM 8 nM forKi IC50CHK1 and CHK2 respectively Prexasertib Mesylate Hydrateinhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2hellip

Bioactivity Rabusertib (LY2603618) is a potent and selective inhibitor of with an of 7 nMChk1 IC50

Bioactivity SCH900776 is a potent selective and oral inhibitor ofcheckpoint kinase1 ( ) with an of 3 nM It shows 50-Chk1 IC50and 500-fold selectivity over CDK2 andChk2 respectively

36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CHK1-IN-3 Cat No HY-128601

GDC-0575 (ARRY-575 RG7741) Cat No HY-112167

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride RG7741 dihydrochloride) Cat No HY-112167A

PF 477736 (PF 00477736) Cat No HY-10032

Prexasertib (LY2606368) Cat No HY-18174

Prexasertib dihydrochloride (LY2606368 (dihydrochloride)) Cat No HY-18174A

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate LY2940930) Cat No HY-18174B

Rabusertib (LY2603618 IC-83) Cat No HY-14720

SCH900776 (MK-8776) Cat No HY-15532

wwwMedChemExpresscom 37

CRISPRCas9

CRISPRCas9 (Clustered Regularly-Interspaced Short PalindromicRepeatsCas9) is a bacterial immune system that has been adaptedfor genome editing in mammalian cells Cas9 is a programmablenuclease that generates double-stranded breaks (DSB) in DNAdictated by binding of a ~20 nucleotide recombinant ldquoguide RNArdquo(gRNA) to the target site DSBrsquos produced by Cas9 are most oftenrepaired through the cellrsquos error-prone non-homologous end joining(NHEJ) pathway resulting in small insertions or deletions (indels) Thevast majority of indels shift the reading frame introducing apremature stop codon or resulting in nonsense mediated decay ofthe mRNA-effectively ldquoknocking outrdquo a gene

The CRISPRCas9 system has substantially advanced efforts in specific gene editing and has been successfully appliedto modify the episomal genomes of human and other organisms The CRISPRCas9 system utilizes a prokaryoticRNA-guided programmable nuclease that can make a double-strand DNA break (DSB) at a specific site under theguidance of a leading RNA This DSB process depends on the co-expression of two basic components a guide RNA(gRNA) and Cas9 nuclease Making a specific DSB can trigger DNA repair via either error-prone non-homologous endjoining (NHEJ) or homology-directed repair (HDR) In the presence of the CRISPRCas9 system the NHEJ inhibitorSCR7 is proven to increase the efficiency of Cas9-mediated HDR by at least by 7-fold in mammalian cells Genomeediting via CRISPRCas9 has become an efficient and reliable way to make precise targeted changes to the genome ofliving cells

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

CRISPRCas9 Inhibitors amp Modulators

Bioactivity Brefeldin A is a specific inhibitor of whichprotein traffickingblocks the protein transport from the endoplasmic reticulum tothe Golgi complex

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity L755507 is a potent selective agonist of with an β -AR3 IC50of 35 nM

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity Zidovudine is a nucleoside reverse transcriptase inhibitor () widely used to treat HIV infection Zidovudine increasesNRTI

CRISPRCas9-mediated editing frequency

38 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Brefeldin A (BFA Cyanein Decumbin) Cat No HY-16592

KU-57788 (NU7441) Cat No HY-11006

L755507 Cat No HY-19334

Nocodazole (Oncodazole R17934) Cat No HY-13520

RS-1 Cat No HY-19793

SCR7 Cat No HY-12742

Zidovudine (Azidothymidine AZT ZDV) Cat No HY-17413

wwwMedChemExpresscom 39

DeubiquitinaseDUBs

Deubiquitinases (DUBs) are a large group of proteases that cleaveubiquitin from proteins and other molecules Ubiquitin is attached toproteins in order to regulate the degradation of proteins via theproteasome and lysosome coordinate thecellular localisation ofproteins activate and inactivate proteins and modulateprotein-protein interactions DUBs can reverse these effects bycleaving the peptide or isopeptide bond between ubiquitin and itssubstrate protein In humans there are nearly 100 DUB genes whichcan be classified into two main classes cysteine proteases andmetalloproteases The cysteine proteases comprise ubiquitin-specificproteases (USPs) ubiquitin C-terminal hydrolases (UCHs)

Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU) The metalloprotease groupcontains only the Jab1Mov34Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases DUBs play several roles inthe ubiquitin pathway One of the best characterised functions of DUBs is the removal of monoubiqutin andpolyubiquitin chainsfrom proteins

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9940Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9892Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9893Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Deubiquitinase Inhibitors amp Modulators

Bioactivity 6-Thioguanine (Thioguanine) is an anti-leukemia andimmunosuppressant agent acts as an inhibitor of SARS and MERScoronavirus papain-like proteases ( ) and also potentlyPLprosinhibits activity with s of 25 μM and 40 μM forUSP2 IC50Plpros and recombinant human USP2 respectively

Bioactivity b-AP15 is a specific inhibitor of the enzymesdeubiquitinating and UCHL5 Usp14

Bioactivity BAY 11-7082 is a inhibitor which decreases NF-κB byNF-κBinhibiting TNF-α-induced phosphorylation of IκB-α BAY 11-7082inhibits ubiquitin-specific protease and withUSP7 USP21

s of 019 μM and 096 μM respectivelyIC50

Bioactivity C527 is a is a pan inhibitor with a highDUB enzymepotency for the complex ( =088 μM)USP1UAF1 IC50

Bioactivity Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB)inhibitor directly inhibiting DUB activity of USP9x USP5USP14 and UCH37 Degrasyn has been shown to downregulate theantiapoptotic proteins and Bcr-Abl JAK2

Bioactivity DUBs-IN-1 is an active inhibitor of ubiquitin-specific with an of 024 μM for USP8proteases (USPs) IC50

Bioactivity DUBs-IN-2 is a potent inhibitor with an ofdeubiquitinase IC50028 μM for USP8

Bioactivity DUBs-IN-3 is a potent enzyme inhibitordeubiquitinase (USP)extracted from reference compound 22c with an of 056 μMIC50for USP8

Bioactivity EOAI3402143 is a ( ) inhibitor whichdeubiquitinase DUBinhibits dose-dependently inhibits and Usp9x Usp24 Usp5

Bioactivity FT671 is a potent non-covalent and selective inhibitorUSP7with an of 52 nM and binds to the USP7 catalytic domainIC50with a of 65 nMKd

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6-Thioguanine (Thioguanine2-Amino-6-purinethiol) Cat No HY-13765

b-AP15 (NSC 687852) Cat No HY-13989

BAY 11-7082 (BAY 11-7821) Cat No HY-13453

C527 Cat No HY-12988

Degrasyn (WP1130) Cat No HY-13264

DUBs-IN-1 Cat No HY-50736

DUBs-IN-2 Cat No HY-50737A

DUBs-IN-3 Cat No HY-50737

EOAI3402143 Cat No HY-111408

FT671 Cat No HY-107985

wwwMedChemExpresscom 41

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9773Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9684Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity FT827 is a selective and covalent ubiquitin-specific protease7 ( ) inhibitor with an of 52 nMUSP7 IC50

Bioactivity GNE-6640 is a selective and non-covalent inhibitor ofubiquitin epecific peptidase 7 with values of(USP7) IC50075 μM 043 μM 203 μM and 023 μM for full length USP7USP7 catalytic domain full length USP43 and Ub-MDM2respectively

Bioactivity GNE-6776 is a selective inhibitorUSP7 Bioactivity HBX 19818 is a specific inhibitor of ubiquitin-specific with an of 281 μMprotease 7 (USP7) IC50

Bioactivity IU1 is a special inhibitor with of 4-5 μMUsp14 IC50 Bioactivity IU1-47 is a potent inhibitor with an of 06 μMUSP14 IC50

IU1-47 induces tau elimination in cultured neurons [1]

Bioactivity LDN-57444 is a reversible competitive and site-directedinhibitor of withubiquitin C-terminal hydrolase L1 (UCH-L1)an of 088 μM and a of 040 μM LDN-57444 alsoIC50 Kisuppresses UCH-L3 activity with an of 25 μMIC50

Bioactivity MF-094 is a potent and selective inhibitor with an USP30 IC50of 120 nM

Bioactivity ML-323 is a reversible potent inhibitor with USP1-UAF1 IC50of 76 nM in a Ub-Rho assay The measured inhibition constantsof ML-323 for the free enzyme ( ) is 68 nMKi

Bioactivity ML364 is an inhibitor of ubiquitin specific peptidase 2 and can be used for the research of breast cancer(USP2)

extracted from patent WO 2016134026 A1 compound Figure 10G

FT827 Cat No HY-111350

GNE-6640 Cat No HY-112937

GNE-6776 Cat No HY-107986

HBX 19818 Cat No HY-17540

IU1 Cat No HY-13817

IU1-47 Cat No HY-122243

LDN-57444 Cat No HY-18637

MF-094 Cat No HY-112438

ML-323 Cat No HY-17543

ML364 Cat No HY-100900

Purity 9800Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9737Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9843Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NSC632839 is a nonselective isopeptidase inhibitor whichinhibits and with s of 45plusmn4 μMUSP2 USP7 SENP2 EC5037plusmn1 μM and 98plusmn18 μM respectively

Bioactivity P 22077 is a cell-permeable ubiquitin-specific protease 7 inhibitor with an of 801 μM It also inhibits(USP7) EC50

USP47 with an of 874 μMEC50

Bioactivity P005091 is a selective and potent inhibitor of with anubiquitin-specific protease 7 (USP7)

of 42 μMEC50

Bioactivity PR-619 is a broad-range inhibitor with of 393DUB EC5049 686 72 and 861 μM for USP4 USP8 USP7 USP2and respectivelyUSP5

Bioactivity SJB2-043 is an inhibitor of the native complex withUSP1UAF1 of 544 nMIC50

Bioactivity SJB3-019A is a potent and novel inhibitor 5 times moreUSP1potent than SJB2-043 in promoting ID1 degradation andcytoxicity in K562 cells with of 00781 μMIC50

Bioactivity USP7-IN-1 is a selective and reversible inhibitor of with an of 77 μMubiquitin-specific protease 7 (USP7) IC50

and can be used for the research of cancer

Bioactivity USP7-IN-3 (Compound 5) is a potent and selective allostericubiquitin-specific protease 7 ( ) inhibitor USP7 [1]

Bioactivity USP7USP47 inhibitor is a selective ubiquitin-specific protease inhibitor with s of 042 μM and 10747 (USP7USP47) EC50

μM respectively

Bioactivity VLX1570 is a competitive inhibitor of proteasomedeubiquitinases ( ) with an of approximate 10 μMDUBs IC50

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NSC632839 Cat No HY-100708

P 22077 Cat No HY-13865

P005091 (P5091) Cat No HY-15667

PR-619 Cat No HY-13814

SJB2-043 Cat No HY-15757

SJB3-019A Cat No HY-80012

USP7-IN-1 Cat No HY-16709

USP7-IN-3 Cat No HY-112128

USP7USP47 inhibitor Cat No HY-13487

VLX1570 Cat No HY-12471

wwwMedChemExpresscom 43

DNA AlkylatorCrosslinker

DNA alkylatorcrosslinker is a molecule that alkylates DNA or cancross link with DNA DNA alkylatorcrosslinker can have mutagenicpharmaceutical or other effects Alkylation is the transfer of an alkylgroup from one molecule to another The alkyl group may betransferred as an alkyl carbocation a free radical a carbanion or acarbene Alkylating agents are widely used in chemistry because thealkyl group is probably the most common group encountered inorganic molecules Selective alkylation or adding parts to the chainwith the desired functional groups is used especially if there is nocommonly available biological precursor Alkylation with only onecarbon is termed methylation In medicine alkylation of DNA is used

in chemotherapy to damage the DNA of cancer cells Alkylation is accomplished with the class of drugs calledalkylating antineoplastic agents Crosslinking of DNA occurs when various exogenous or endogenous agents reactwith two different positions in the DNA This can either occur in the same strand (intrastrand crosslink) or in theopposite strands of the DNA (interstrand crosslink) Crosslinks also occur between DNA and protein DNA replicationis blocked by crosslinks which causes replication arrest and cell death if the crosslink is not repaired The RAD51family plays a role in repair

Purity 990Clinical Data LaunchedSize 100 mg 500 mg

Purity 9879Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9844Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9961Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

DNA AlkylatorCrosslinker Inhibitors amp Modulators

Bioactivity Altretamine is an antineoplastic agentalkylating Bioactivity Altretamine hydrochloride is an antineoplasticalkylatingagent

Bioactivity Bendamustine D4 is the deuterium labeled BendamustineBendamustine is a agent that causes DNADNA cross-linkingbreaks with alkylating and antimetabolite properties

Bioactivity Bendamustine hydrochloride is a agent thatDNA cross-linkingcauses DNA breaks with alkylating and antimetaboliteproperties

Bioactivity Busulfan is a potent with selective immunosuppressivealkylatoreffect on bone marrow

Bioactivity Calicheamicin is a cytotoxic agent that causes double-strandDNA breaks

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity Carmustine is an antitumor chemotherapeutic agent which worksby akylating DNA and RNA

Bioactivity Chlorambucil is an agent with antitumor activityalkylating Bioactivity Cisplatin is a antineoplastic chemotherapy drug which works bycross-linking with and causing DNA damage in cancerDNAcells

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Altretamine (ENT-50852 RB-1515 WR-95704) Cat No HY-B0181

Altretamine hydrochloride (ENT-50852 hydrochloride RB-1515

hydrochloride WR-95704 hydrochloride) Cat No HY-B0181A

Bendamustine D4 (SDX-105 D4) Cat No HY-13567S

Bendamustine hydrochloride (SDX-105 EP-3101) Cat No HY-B0077

Busulfan Cat No HY-B0245

Calicheamicin (Calicheamicin γ1) Cat No HY-19609

Carboplatin (NSC 241240) Cat No HY-17393

Carmustine Cat No HY-13585

Chlorambucil (CB-1348 WR-139013) Cat No HY-13593

Cisplatin (CDDP cis-Diaminodichloroplatinum) Cat No HY-17394

wwwMedChemExpresscom 45

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 980Clinical Data LaunchedSize 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Bioactivity Cyclophosphamide is a synthetic agent chemicallyalkylatingrelated to the nitrogen mustards with antineoplastic andimmunosuppressive activities

Bioactivity Cyclophosphamide hydrate is a synthetic agentalkylatingchemically related to the nitrogen mustards withantineoplastic and immunosuppressive activities

Bioactivity Fotemustine is a agent with antitumor activityDNA-alkylating Bioactivity Ifosfamide is an chemotherapeutic agent withalkylatingactivity against a wide range of tumors

Bioactivity Lomustine (CCNU) is a agent with antitumorDNA alkylatingactivity

Bioactivity Melphalan is an effective agent with potentDNA alkylatingantitumor activity

Bioactivity Methylnitronitrosoguanidine (MNNG) is an agent withalkylatingtoxic and mutagenic effects [1]

Bioactivity Miriplatin is a chemotherapy agent which belongs to the classof agentsalkylating

Bioactivity Miriplatin hydrate is a chemotherapy agent which belongs tothe class of agentsalkylating

Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Cyclophosphamide Cat No HY-17420

Cyclophosphamide hydrate (Cyclophosphamide monohydrate) Cat No HY-17420A

Fotemustine (S10036) Cat No HY-B0733

Ifosfamide Cat No HY-17419

Lomustine (CCNU NSC 79037) Cat No HY-13669

Melphalan (L-PAM) Cat No HY-17575

Methylnitronitrosoguanidine (MNNG) Cat No HY-128612

Miriplatin (SM-11355) Cat No HY-16325A

Miriplatin hydrate (SM-11355 (hydrate)) Cat No HY-16325

Mitomycin C (Ametycine) Cat No HY-13316

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9926Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9986Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Oxaliplatin is a inhibitor It causes DNADNA synthesiscrosslinking damage prevents DNA replication andtranscription and causes cell death

Bioactivity Palifosfamide is a novel DNA alkylator and the activemetabolite of ifosfamide with antitumor activity

Bioactivity Procarbazine Hydrochloride is an agent withalkylatinganticancer activity

Bioactivity RITA is an inhibitor of binds top53-HDM-2 interactionp53dN with a of 15 nM and also induces Kd DNA-DNA

cross-links

Bioactivity Satraplatin is an agent with potent antitumoralkylatingeffect

Bioactivity SJG-136 is a agent with an of 45 nMDNA cross-linking XL50for pBR322 DNA SJG-136 has potent antitumor activity

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity Temozolomide (NSC 362856 CCRG 81045) is an oral DNA agent used to treat some brain cancersalkylating

Bioactivity Thio-TEPA is a agent with antitumor activityDNA alkylating Bioactivity Treosulfan (NSC 39069Treosulphan) is an agent withalkylatingactivity in ovarian cancer and other solid tumor types

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Oxaliplatin Cat No HY-17371

Palifosfamide (Isophosphoramide mustard IPM ZIO-201) Cat No HY-14798

Procarbazine Hydrochloride Cat No HY-13733

RITA (NSC 652287) Cat No HY-13424

Satraplatin (BMS182751 BMY45594 JM216) Cat No HY-17576

SJG-136 (NSC-694501) Cat No HY-14573

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

Temozolomide (NSC 362856 CCRG 81045 TMZ) Cat No HY-17364

Thio-TEPA Cat No HY-17574

Treosulfan (NSC 39069 Treosulphan) Cat No HY-16503

wwwMedChemExpresscom 47

Purity 980Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Uramustine is an oral agent effective in thealkylatingtreatment of lymphosarcoma chronic lymphatic leukaemia andthrombocythemia

Bioactivity VAL-083 is an agent that creates N7 methylation onalkylatingDNA with antitumor activity

Uramustine (Uracil mustard) Cat No HY-13544

VAL-083 (Dianhydrodulcitol Dianhydrogalactitol) Cat No HY-16513

DNA-PKDNA-dependent protein kinase

DNA-PKcs (DNA-dependent protein kinase catalytic subunit) is anenzyme that in humans is encoded by the PRKDC gene DNA-PKcsbelongs to the phosphatidylinositol 3-kinase-related kinase proteinfamily DNA-PKcs is the catalytic subunit of a nuclear DNA-dependentserinethreonine protein kinase called DNA-PK The secondcomponent is the autoimmune antigen Ku On its own DNA-PKcs isinactive and relies on Ku to direct it to DNA ends and trigger itskinase activity DNA-PKcs is required for the non-homologous endjoining (NHEJ) pathway of DNA repair Many proteins have beenidentified as substrates for the kinase activity of DNA-PKAutophosphorylation of DNA-PKcs appears to play a key role in NHEJ

and is thought to induce a conformational change that allows end processing enzymes to access the ends of thedouble-strand break DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNAdamage checkpoint

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wwwMedChemExpresscom 49

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9943Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9722Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9664Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9239Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

DNA-PK Inhibitors amp Modulators

Bioactivity (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer ofNedisertib with an in the range of 7-30 nM for IC50 DNA-PK

[1]

Bioactivity AZD-7648 is a potent and selective inhibitorDNA-PKAnti-tumor activity [1]

Bioactivity CC-115 is a potent and dual and kinaseDNA-PK mTORinhibitor with s of 13 nM and 21 nM respectively CC-115IC50blocks both and signalingmTORC1 mTORC2

Bioactivity CC-115 hydrochloride is a potent and dual and DNA-PK mTORkinase inhibitor with s of 13 nM and 21 nM respectivelyIC50CC-115 blocks both and signalingmTORC1 mTORC2

Bioactivity Compound 401 is a synthetic inhibitor of ( = 028DNA-PK IC50μM) that also targets mTOR but not PI3K in vitro

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity LTURM34 is a specific inhibitor with an of 0034DNA-PK IC50μM

Bioactivity LY3023414 potently and selectively inhibits class I PI3Kisoforms and with s of 607 nM 776DNA-PK mTORC12 IC50nM 38 nM 238 nM 424 nM and 165 nM for PI3Kα PI3KβPI3Kδ PI3Kγ DNA-PK and mTOR respectively LY3023414potently inhibits at low nanomolarhellipmTORC1 2

Bioactivity Nedisertib (M3814) is a potent and selective inhibitor of ( ) with an of lt3DNA-dependent Protein Kinase DNA-PK IC50

nM

Bioactivity NU 7026 is a novel specific inhibitor with ofDNA-PK IC50023plusmn001 μM also inhibits with of 13plusmn3 μMPI3K IC50

(R)-Nedisertib ((R)-M3814) Cat No HY-101570A

AZD-7648 Cat No HY-111783

CC-115 Cat No HY-16962

CC-115 hydrochloride Cat No HY-16962A

Compound 401 Cat No HY-19341

KU-57788 (NU7441) Cat No HY-11006

LTURM34 Cat No HY-101667

LY3023414 Cat No HY-12513

Nedisertib (M3814) Cat No HY-101570

NU 7026 (DNA-PK Inhibitor II LY293646) Cat No HY-15719

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9937Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9145Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity PI-103 is a potent and inhibitor with s of 8PI3K mTOR IC50nM 88 nM 48 nM 150 nM 20 nM and 83 nM for p110α p110β

and PI-103 also inhibitsp110δ p110γ mTORC1 mTORC2 with an of 2 nMDNA-PK IC50

Bioactivity PI-103 Hydrochloride is a dual and inhibitor withPI3K mTORs of 8 nM 88 nM 48 nM 150 nM 20 nM and 83 nM forIC50

and p110α p110β p110δ p110γ mTORC1 mTORC2PI-103 also inhibits with an of 2 nMDNA-PK IC50

Bioactivity PIK-75 is a and inhibitor which inhibits DNA-PKDNA-PK PI3K and p110γ with s of 2 58 and 76 nM respectivelyp110α IC50

PIK-75 inhibits p110α gt200-fold more potently than p110β(IC =13 μM)50

Bioactivity PIK-90 is a and inhibitor which inhibits DNA-PK PI3K p110α and with s of 11 18 and 13 nMp110γ DNA-PK IC50

respectively

Bioactivity Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib apotent inhibitor with an of lt3 nM DNA-PK IC50

[1]Bioactivity SF2523 is a highly selective and potent inhibitor of withPI3K

s of 34 nM 158 nM 9 nM 241 nM and 280 nM for IC50 PI3Kα

BRD4 and mTOR respectivelyPI3Kγ DNA-PK

Bioactivity STL127705 (Compound L) is a Ku 7080 heterodimer proteininhibitor inhibits Ku7080-DNA interaction with an ofIC5035 μM STL127705 also inhibits Ku-dependent activation ofDNA-PKCS kinase ( 25 μM) IC50

[1]

Bioactivity Torin 2 is an inhibitor with of 025 nM formTOR EC50inhibiting cellular mTOR activity and exhibits 800-foldselectivity over PI3K (EC 200 nM) Torin 2 also inhibits50

with an of 05 nM in the cell free assay TorihellipDNA-PK IC50

Bioactivity VX-984 is a potent inhibitorDNA-PK Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

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PI-103 Cat No HY-10115

PI-103 Hydrochloride Cat No HY-10115A

PIK-75 (PIK-75 Hydrochloride) Cat No HY-13281

PIK-90 Cat No HY-12030

Rac-Nedisertib (Rac-M3814) Cat No HY-101570B

SF2523 Cat No HY-101146

STL127705 Cat No HY-122727

Torin 2 Cat No HY-13002

VX-984 (M9831) Cat No HY-19939S

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

wwwMedChemExpresscom 51

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity YU238259 is an inhibitor of homology-dependent DNA repair () used for cancer researchHDR

YU238259 Cat No HY-19977

DNARNA Synthesis

RNA synthesis which is also called DNA transcription is a highlyselective process Transcription by RNA polymerase II extends beyondRNA synthesis towards a more active role in mRNA maturationsurveillance and export to the cytoplasmSingle-strand breaks are repaired by DNA ligase using thecomplementary strand of the double helix as a template with DNAligase creating the final phosphodiester bond to fully repair theDNADNA ligases discriminate against substrates containing RNAstrands or mismatched base pairs at positions near the ends of thenickedDNA Bleomycin (BLM) exerts its genotoxicity by generatingfree radicals whichattack C-4prime in the deoxyribose backbone of DNA

leading to opening of the ribose ring and strand breakage it is an S-independentradiomimetic agent that causesdouble-strand breaks in DNAFirst strand cDNA is synthesized using random hexamer primers and M-MuLV Reverse Transcriptase (RNase H)Second strand cDNA synthesis is subsequently performed using DNA Polymerase I and RNase H The remainingoverhangs are converted into blunt ends using exonucleasepolymerase activity After adenylation of the 3prime ends ofDNA fragments NEBNext Adaptor with hairpin loop structure is ligated to prepare the samples for hybridization Cellcycle and DNA replication are the top two pathways regulated by BET bromodomain inhibition Cycloheximide blocksthe translation of mRNA to protein

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wwwMedChemExpresscom 53

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 1 mg 2 mg 5 mg

Purity 9876Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9989Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 9968Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

25 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

DNARNA Synthesis Inhibitors amp Modulators

Bioactivity 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is amodified nucleoside 2-(Methylamino)-1H-purin-6(7H)-one is anendogenous methylated nucleoside found in human fluids

Bioactivity 374-Trihydroxyflavone isolated from Rhus javanica var is a flavonoid with DNA strand-scission activityroxburghiana

[1]

Bioactivity 5-Methoxyflavone belonged to Flavonoid family is a DNApolymerase-beta inhibitor and neuroprotective agent againstbeta-amyloid toxicity possess central nervous system (CNS)depressant effect mediated through the ionotropic GABA Areceptors

Bioactivity 6-Thio-2-Deoxyguanosine is a nucleoside analogue that can beincorporated into de novo-synthesized telomeres by telomerase

Bioactivity Acelarin (NUC-1031) is a ProTide transformation andenhancement of the widely-used nucleoside analoguegemcitabine

Bioactivity Actinomycin D inhibits with an of 042 μMDNA repair IC50

Bioactivity Adenine is a purine derivative and a nucleobase with a varietyof roles in biochemistry Target Nucleosideantimetaboliteanalog Adenine is a nucleobase with a varietyof roles in biochemistry including cellular respiration inthe form of both the energy-rich adenosine triphosphate (ATP)hellip

Bioactivity alpha-Amanitin is the principal toxin of several deadlypoisonous mushrooms exerting its toxic function by inhibiting

RNA-polymerase II

Bioactivity Anisomycin is a potent inhibitor whichprotein synthesisinterferes with protein and by inhibitingDNA synthesispeptidyl transferase or the 80S ribosome system Anisomycin isa JNK activator which increases phospho-JNK

Bioactivity Beaucage reagent is found to be potent in causing DNAcleavage

2-(Methylamino)-1H-purin-6(7H)-one (N2-methylguanine) Cat No HY-101412

374-Trihydroxyflavone (5-Deoxykampferol) Cat No HY-111806

5-Methoxyflavone Cat No HY-107790

6-Thio-2-Deoxyguanosine (6-thio-dG β-TGdR) Cat No HY-18762

Acelarin (NUC-1031) Cat No HY-100885

Actinomycin D (Dactinomycin Actinomycin IV) Cat No HY-17559

Adenine (6-Aminopurine Vitamin B4) Cat No HY-B0152

alpha-Amanitin (α-Amanitin α-Amatoxin) Cat No HY-19610

Anisomycin (Flagecidin Wuningmeisu C) Cat No HY-18982

Beaucage reagent Cat No HY-100951

Purity 9847Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity 9804Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9896Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Bioactivity Bleomycin sulfate is a inhibitor with potentDNA synthesisantitumor activity

Bioactivity BMH-21 is a small molecule DNA intercalator that bindsribosomal DNA and inhibits RNA polymerase I (Pol I)transcription does not cause phosphorylation of H2AX

Bioactivity Branaplam (LMI070) is a highly potent selective and orallyactive small molecule modulatorSMN2 splicing

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity CeMMEC1 is an inhibitor of and also has high affinityBRD4for with an of 09 μM for TAF1 and a of 18TAF1 IC50 KdμM for TAF1 (2)

Bioactivity CeMMEC13 is a potent inhibitor of bromodomain withTAF1 (2)an of 21 μMIC50

Bioactivity Chebulinic acid is a potent natural inhibitor of Mtuberculosis DNA gyrase also can inhibit SMAD-3phosphorylation inhibit H+ K+-ATPase activity

Bioactivity COH29 is a potent ribonucleotide reductase ( ) inhibitorRNRwith anticancer activity COH29 inhibits α and β subunit ofRNR with s of 16 μMIC50

Bioactivity CX-5461 is a potent and oral inhibitor ItrRNA synthesisinhibits RNA polymerase I-driven transcription of rRNA with

s of 142 113 and 54 nM in HCT-116 A375 and MIA PaCa-2IC50cells respectively

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Bleomycin sulfate Cat No HY-17565

BMH-21 Cat No HY-12484

Branaplam (LMI070 NVS-SM1) Cat No HY-19620

Capecitabine Cat No HY-B0016

Carboplatin (NSC 241240) Cat No HY-17393

CeMMEC1 Cat No HY-111445

CeMMEC13 Cat No HY-101088

Chebulinic acid Cat No HY-N2033

COH29 (RNR Inhibitor COH29) Cat No HY-19931

CX-5461 Cat No HY-13323

wwwMedChemExpresscom 55

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9872Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9963Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9945Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg

Bioactivity CX-5461 dihydrochloride is a potent and orally bioavailableinhibitor of Pol I-mediated with s of 142rRNA synthesis IC50nM in HCT-116 113 nM in A375 and 54 nM in MIA PaCa-2 cellsand shows little or no effect on Pol II ( ge25 μM)IC50

Bioactivity Cycloheximide (Naramycin A) is an eukaryote protein synthesisinhibitor with s of 5325 nM and 2880 nM for proteinIC50synthesis and RNA synthesis respectivelyin vivo

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Datelliptium chloride is a DNA-intercalating agent derivedfrom ellipticine with anti-tumor activities

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Didox (NSC-324360) is a synthetic (ribonucleotide reductase) inhibitorRR

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

CX-5461 dihydrochloride Cat No HY-13323A

Cycloheximide (Naramycin A Actidione CHX) Cat No HY-12320

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Datelliptium chloride Cat No HY-U00337

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Didox (NSC-324360) Cat No HY-19387

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Bioactivity Folic acid(Vitamin M Vitamin B9) is a B vitamin is necessaryfor the production and maintenance of new cells for DNAsynthesis and RNA synthesis

Bioactivity GC7 Sulfate is a ( ) inhibitordeoxyhypusine synthase DHPS

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity GNE-371 is a potent and selective chemical probe for thesecond bromodomains of human transcription-initiation-factor

subunit 1 and transcription-initiation-factor TFIID TFIIDsubunit 1-like with an of 10 nM for TAF1(2)IC50

Bioactivity Guanine is one of the fundamental components of nucleic acids( and ) Guanine is a purine derivative consistingDNA RNAof a fused pyrimidine-imidazole ring system with conjugateddouble bonds

Bioactivity Halofuginone (RU-19110) is a less-toxic form of Febrifuginewhich is isolated from the plant Dichroa febrifuga [1]

Halofuginone inhibits in anprolyl-tRNA synthetaseATP-dependent manner with a of 183 nM HalofuginhellipKi

[2]

Bioactivity Halofuginone hydrobromide (RU-19110 hydrobromide) is aless-toxic form of Febrifugine which is isolated from theplant Halofuginone inhibits Dichroa febrifuga [1] prolyl-tRNA

in an ATP-dependent manner with a of 183hellipsynthetase Ki

Bioactivity Hydroxyurea is a cell apoptosis inducer that inhibit DNAsynthesis through inhibition of ribonucleotide reductase

Bioactivity L189 is a novel human DNA ligase inhibitor inhibitshLigIIIIIV with IC50 of 595 μM

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Folic acid (Vitamin B9 Vitamin M) Cat No HY-16637

GC7 Sulfate Cat No HY-108314A

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

GNE-371 Cat No HY-112803

Guanine Cat No HY-Y1055

Halofuginone (RU-19110) Cat No HY-N1584

Halofuginone hydrobromide (RU-19110 (hydrobromide)) Cat No HY-N1584A

Hydroxyurea (Hydroxycarbamide) Cat No HY-B0313

L189 Cat No HY-15588

wwwMedChemExpresscom 57

Purity 990Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9839Clinical Data No Development ReportedSize 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9977Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9988Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity L67 is a novel competitive human DNA ligase inhibitorinhibits DNA ligases I and III with IC50 of 10 μM and 10 μM

Bioactivity Madrasin is a potent and cell penetrant splicing inhibitorthat interferes with the early stages of spliceosome assemblyMadrasin is cytotoxic at higher concentrations although atlower concentrations it induces cell cycle arrest promotes aspecific reorganization of subnuclear protein localizationhellip

Bioactivity MB-7133 is a inhibitorDNA synthesis Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Bioactivity ML216(CID-49852229) is a potent inhibitor of the DNA unwindingactivity of BLM helicase showing similar IC50s of 30 and097 μM for full length BLM and BLM636ndash1298 respectively IC50value 30097 uM(Full length636ndash1298 BLM) Target BLMhelicase inhibitor ML216 shows cell-based activity and canhellip

Bioactivity Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNAdamage agent

Bioactivity NITD008 is a potent and selective inhibitor whichflavivirusecan inhibit with an ofDengue Virus Type 2 (DENV-2) EC50064 μM

Bioactivity Oxolinic acid is a potent inhibitor of DNA gyrase and DNAsynthesis lead to DNA cleavage when extracted chromosomes areincubated with sodium dodecyl sulfate

Bioactivity Phen-DC3 is a (G4) specific ligand which canG-quadruplexinhibit and helicases with s of 65plusmn6 and 50plusmn10FANCJ DinG IC50nM respectively

Bioactivity Plicamycin is a selective specificity protein 1 ( )Sp1inhibitor Plicamycin inhibits the growth of various cancersby decreasing Sp1 protein

L67 (DNA Ligase Inhibitor) Cat No HY-15586

Madrasin (DDD00107587) Cat No HY-100236

MB-7133 Cat No HY-16311

Mitomycin C (Ametycine) Cat No HY-13316

ML216 (CID-49852229) Cat No HY-12342

Nedaplatin (NSC 375101D) Cat No HY-13700

NITD008 (7-Deaza-2-C-acetylene-adenosine) Cat No HY-12957

Oxolinic acid Cat No HY-B1002

Phen-DC3 Cat No HY-15594

Plicamycin (Mithramycin A) Cat No HY-A0122

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9762Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9931Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Quarfloxin (CX 3543) a fluoroquinolone derivative withantineoplastic activity targets and inhibits RNA pol Iactivity with IC values in the nanomolar range in50neuroblastoma cells Quarfloxin disrupts the interactionbetween the nucleolin protein and a G-quadruplex DNA structurehellip

Bioactivity RG7800 a small molecule splicing modifier to enterSMN2human clinical trials to treat spinal muscular atrophy

Bioactivity RG7800 hydrochloride is an orally active splicingSMN2modulator with s of 23 nM and 87 nM for EC15x SMN2

splicing and RG7800 hydrochloride has theSMN proteinpotential to treat spinal muscular atrophy

Bioactivity Risdiplam (RG7916 RO7034067) is an orally administeredcentrally and peripherally distributed pre-mRNASMN2splicing modifier that increases survival motor neuron (SMN)protein levels

Bioactivity Saccharin 1-methylimidazole is an activator for DNARNASynthesis

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity SMN-C3 is an orally active splicing modulator and hasSMN2the potential to treat spinal muscular atrophy (SMA)

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 valueof 08 nM less potent for MTH2 NUDT5 NUDT12 NUDT14 andNUDT16

Bioactivity TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) withan IC50 value of 08 nM less potent for MTH2 NUDT5 NUDT12NUDT14 and NUDT16

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Quarfloxin (CX 3543) Cat No HY-14776

RG7800 (RO6885247) Cat No HY-101792

RG7800 hydrochloride (RO6885247 hydrochloride) Cat No HY-101792A

Risdiplam (RG7916 RO7034067) Cat No HY-109101

Saccharin 1-methylimidazole Cat No HY-112060

SCR7 Cat No HY-12742

SMN-C3 Cat No HY-112633

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

TH287 Cat No HY-16965

TH287 hydrochloride Cat No HY-16965A

wwwMedChemExpresscom 59

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9920Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 25 mg 50 mg 100 mg

Bioactivity TH588 is first-in-class nudix hydrolase family inhibitor thatpotently and selectively engage and inhibit the (MTH1

= 5 nM)IC50

Bioactivity TH588 hydrochloride is first-in-class nudix hydrolase familyinhibitor that potently and selectively engage and inhibit the

( = 5 nM)MTH1 IC50

Bioactivity Thiarabine (OSI-7836) shows potent anti-tumor activity andinhibition of synthesisDNA

Bioactivity Triapine is a novel inhibitor of the M2 subunit of ( ) and is a potentribonucleotide reductase RR

radiosensitizer

Bioactivity Triciribine is a inhibitor also inhibits DNA synthesis Aktand with of 130 nM and 002-046 μMHIV-12 IC50respectively

Bioactivity YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding tothe oncogenic transciption factor EWS-FLI1 YK-4-279 inhibitsEwings sarcoma family tumor (ESFT) cell growth YK-4-279induces apoptosis

Bioactivity Zoliflodacin (ETX0914AZD0914) is a novelspiropyrimidinetrione bacterial DNA gyrasetopoisomeraseinhibitor Zoliflodacin has potent antibacterialin vitroactivity against Gram-positive and Gram-negative organismsincluding with the of 025 μgmLS aureus MIC90

TH588 Cat No HY-12814

TH588 hydrochloride Cat No HY-12814A

Thiarabine (OSI-7836) Cat No HY-16496

Triapine (3-AP PAN-811 OCX191 NSC663249) Cat No HY-10082

Triciribine (API-2 NSC 154020 TCN) Cat No HY-15457

YK-4-279 Cat No HY-14507

Zoliflodacin (ETX0914 AZD0914) Cat No HY-17647

Eukaryotic Initiation Factor (eIF)

Eukaryotic initiation factors (eIFs) are proteins involved in theinitiation phase of eukaryotic translation These proteins help stabilizethe formation of the functional ribosome around the start codon andalso provide regulatory mechanisms in translation initiationEukaryotic initiation factor 2B (eIF2B) is a guaninenucleotide-exchange factor which mediates the exchange of GDP(bound to initiation factor eIF2) for GTP thus regenerating the active[eIF2GTP] complex that is required for peptide-chain initiation Theactivity of eIF2B is a key control point for eukaryotic protein synthesisand is altered in response to viral infection hormones nutrientsgrowth factors and certain stresses

Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis oncapped mRNAs in the cytoplasm Eukaryotic initiation factor (elF) 4A functions as a subunit of the initiation factorcomplex elF4F which mediates the binding of mRNA to the ribosome

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Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 2 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Eukaryotic Initiation Factor (eIF) Inhibitors amp Modulators

Bioactivity 4E1RCat is an inhibitor of cap-dependent translation andinhibits interaction with an an of 4 μMeIF4EeIF4GI IC50

Bioactivity 4E2RCat is an inhibitor of interaction with an eIF4E-eIF4G IC50of 135 μM

Bioactivity 4EGI-1 is an inhibitor of interaction with a eIF4EeIF4G Kdof 25 μM against eIF4E binding

Bioactivity Briciclib is a water soluble derivative of ON 013100 and hasthe potential in targeting for solid cancerseIF4E

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic inhibitor with an of 110initiation factor 4A-3 (eIF4A3) IC50

nM

Bioactivity Episilvestrol is a derivative of silvestrol isolated from thefruits and twigs of and is a specificAglaia silvestris

-targeting translation inhibitor with antitumor activityeIF4A

Bioactivity GCN2iB is an ATP-competitive inhibitor of aserinethreonine-protein kinase general control

with an of 24 nMnonderepressible 2 (GCN2) IC50

Bioactivity SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1and disrupts the eIF4F complex

Bioactivity Silvestrol is a eukaryotic translation initiation factor 4A () inhibitor isolated from the fruits and twigs of eIF4A Aglaia

foveolata

4E1RCat Cat No HY-14427

4E2RCat Cat No HY-100733

4EGI-1 Cat No HY-19831

Briciclib (ON 014185) Cat No HY-16366

CCT020312 Cat No HY-119240

eIF4A3-IN-2 Cat No HY-101785

Episilvestrol Cat No HY-15359

GCN2iB Cat No HY-112654

SBI-0640756 (SBI-756) Cat No HY-19560

Silvestrol ((-)-Silvestrol) Cat No HY-13251

G-quadruplex

G-quadruplexes (G-tetrads or G4-DNA) are nucleic acid sequencesthat are rich in guanine and are capable of forming a four-strandedstructure Four guanine bases can associate through Hoogsteenhydrogen bonding to form a square planar structure called a guaninetetrad and two or more guanine tetrads can stack on top of eachother to form a G-quadruplex The quadruplex structure is furtherstabilized by the presence of a cation especially potassium which sitsin a central channel between each pair of tetradsThey can be formedof DNA RNA LNA and PNA and may be intramolecular bimolecularor tetramolecular Depending on the direction of the strands or partsof a strand that form the tetrads structures may be described as

parallel or antiparallel

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Purity 980Clinical Data No Development ReportedSize 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity 9680Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

G-quadruplex Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity APTO-253 is an inducer of andKruppel-like factor 4 (KLF4)also stabilizes with anti-proliferative activityGquadruplex

Bioactivity Phen-DC3 Trifluoromethanesulfonate is a (G4)G-quadruplexspecific ligand which can inhibit and helicasesFANCJ DinGwith s of 65plusmn6 and 50plusmn10 nM respectivelyIC50

Bioactivity Pyridostatin is a stabilizer with a of 490G-quadruplexe KdnM

Bioactivity Pyridostatin hydrochloride is a stabilizer withG-quadruplexea of 490 nMKd

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

APTO-253 (LOR-253 LT-253) Cat No HY-16291

Phen-DC3 Trifluoromethanesulfonate (Phen-DC3 Triflate) Cat No HY-15594A

Pyridostatin (RR82) Cat No HY-15176

Pyridostatin hydrochloride (RR-82 hydrochloride) Cat No HY-15176A

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

Haspin Kinase

Haspin is a protein kinase that regulates chromosome and spindlefunction during mitosis and meiosis Haspin expression is detected infetal liver skin kidney small intestine and in all proliferating cellsHaspin phosphorylates H3 thr3 (H3T3ph) in human cell lines anddepletion of Haspin by RNA interference reveals that Haspin isrequired for H3 thr3 phosphorylation in mitotic cells Phosphorylationof H3T3ph by Haspin is necessary for chromosomal passengercomplex (CPC) accumulation at centromeres H3T3ph then positionsthe CPC at centromeres to regulate selected targets of Aurora Bduring mitosis

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Purity 9956Clinical Data No Development ReportedSize 5 mg

Purity 9812Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Haspin Kinase Inhibitors amp Modulators

Bioactivity CHR-6494 is a potent inhibitor of inhibiting histonehaspinH3T3 phosphorylation with an of 2 nMIC50

Bioactivity LDN-192960 is a potent ( Haspin Haploid Germ Cell-Specific) inhibitor with an of 0010 microMNuclear Protein Kinase IC50

CHR-6494 Cat No HY-15217

LDN-192960 Cat No HY-13455

HDACHistone deacetylases

HDAC (Histone deacetylases) are a class of enzymes that removeacetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid onahistone allowing the histones to wrap the DNA more tightly This isimportant because DNA is wrapped around histones and DNAexpression is regulated by acetylation and de-acetylation Its action isopposite to that of histone acetyltransferase HDAC proteins are nowalso called lysine deacetylases (KDAC) to describe their functionrather than their target which also includes non-histone proteinsTogether with the acetylpolyamine amidohydrolases and the acetoinutilization proteins the histone deacetylases form an ancient proteinsuperfamily known as the histone deacetylase superfamily

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Purity 9600Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9971 Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9896Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

HDAC Inhibitors amp Modulators

Bioactivity Abexinostat (CRA 024781) is a novel pan- inhibitorHDACmostly targeting HDAC1 with of 7 nMKi

Bioactivity ACY-1083 is a selective and brain-penetrating inhibitorHDAC6with an of 3 nM and is 260-fold more selective for HDAC6IC50than all other classes of HDAC isoforms ACY-1083 effectivelyreverses chemotherapy-induced peripheral neuropathy [1]

Bioactivity ACY-738 is a potent selective and orally-bioavailable HDAC6inhibitor with an of 17 nM ACY-738 also inhibitsIC50HDAC1 HDAC2 and HDAC3 with s of 94 128 and 218 nMIC50

Bioactivity ACY-775 is a potent and selective inhibitor of the of histonedeacetylase 6 ( ) with an of 75nMHDAC6 IC50

Bioactivity ACY-957 is a selective inhibitor of and withHDAC1 HDAC2s of 7 nM 18 nM and 1300 nM against HDAC123IC50

respectively and shows no inhibition on HDAC456789

Bioactivity AES-135 is a potent inhibitor inhibits HDAC HDAC3 HDAC6 with s of 654 190 and 636 nM respectivelyHDAC11 IC50

Anti-tumor activity [1]

Bioactivity Belinostat is a potent inhibitor with an of 27 nMHDAC IC50in HeLa cell extracts

Bioactivity Benzenebutyric acid is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity BG45 is an HDAC class I inhibitor with selectivity for HDAC3(IC50 = 289 nM) It inhibits HDAC1 HDAC2 and HDAC6 withgreatly reduced potency (IC50s = 2 22 and gt20 μMrespectively) IC50 value 289 nM (HDAC3) 2 μM (HDAC1) 22μM (HDAC2) gt20 μM (HDAC6) Target HDAC At concentrationshellip

Bioactivity BML-210 is a novel HDAC inhibitor and its mechanism of actionhas not been characterized IC50 value 5 μM[1] Target HDAC4In vitro Cell cycle analysis indicated that HeLa celltreatment with 20 and 30 μM concentration of BML-210 increasedthe proportion of cells in G0G1 phase and causedhellip

Abexinostat (CRA 024781 PCI-24781) Cat No HY-10990

ACY-1083 Cat No HY-111791

ACY-738 Cat No HY-19327

ACY-775 Cat No HY-19328

ACY-957 Cat No HY-104008

AES-135 Cat No HY-114483

Belinostat (PXD101 PX105684) Cat No HY-10225

Benzenebutyric acid (4-Phenylbutyric acid) Cat No HY-A0281

BG45 Cat No HY-18712

BML-210 Cat No HY-19350

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9875Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9906Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BRD 4354 is a moderately potent inhibitor of andHDAC5 with of 085 and 188 μM respectivelyHDAC9 IC s50

Bioactivity BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitorof and with of 085 and 188 μMHDAC5 HDAC9 IC s50

respectively [1]

Bioactivity BRD73954 ia a potent and selective HDAC inhibitor with IC50 of36 nM and 120 nM for HDAC6 and HDAC8 respectively

Bioactivity Bufexamac is a class IIB histone deacetylases (HDAC6 andHDAC10) inhibitor used as an anti-inflammatory agent

Bioactivity CAY10603 (BML-281) is a potent and selective inhibitorHDAC6with an of 2 pM CAY10603 (BML-281) also inhibits HDAC1IC50HDAC2 HDAC3 HDAC8 HDAC10 with s of 271 252 042IC506851 907 nM

Bioactivity CHDI-390576 a potent cell permeable and CNS penetrant class inhibitor with s of 54 nMIIa histonedeacetylase (HDAC) IC50

60 nM 31 nM 50 nM for class IIa HDAC4 HDAC5 HDAC7 HDAC9respectively shows gt500-fold selectivity over class IHDACs (1 2 3) and ~150-fold selectivity over HDAC8 and thehellip

Bioactivity Citarinostat is a HDAC6 specific inhibitor with IC50 of 4 nMand 76 nM for HDAC6 and HDAC3 respectively IC50 value 4 nM(HDAC6) 76 nM (HDAC3) Target HDAC The detailed informationplease refer to WO2015061684A1 and 2015054197A1

Bioactivity CM-675 is a dual and phosphodiesterase 5 (PDE5) class I histone-selective inhibitor with values of 114 nMdeacetylases IC50

and 673 nM for PDE5 and HDAC1 respectively CM-675 haspotential to treat Alzheimerrsquos disease [1]

Bioactivity Corin is a dual inhibitor of histone lysine specificdemethylase and histone deacetylase with a(LSD1) (HDAC)

of 110 nM for LSD1 and an IC of 147 nM forK (inact)i 50HDAC1

Bioactivity CRA-026440 is a potent broad-spectrum inhibitor The HDAC Kivalues against recombinant HDAC isoenzymes HDAC1 HDAC2

and are 4 14 11 15 7 andHDAC3 HDAC6 HDAC8 HDAC1020 nM respectively

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BRD 4354 Cat No HY-112719

BRD 4354 ditrifluoroacetate Cat No HY-112719B

BRD73954 Cat No HY-18700

Bufexamac (Bufexamic acid) Cat No HY-B0494

CAY10603 (BML-281) Cat No HY-18613

CHDI-390576 Cat No HY-119939

Citarinostat (ACY241) Cat No HY-15994

CM-675 Cat No HY-114303

Corin Cat No HY-111048

CRA-026440 Cat No HY-19754

wwwMedChemExpresscom 69

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in Ethanol

2 mg 5 mg 10 mg 50 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9809Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9959Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity CUDC-101 is a potent inhibitor of and withHDAC EGFR HER2s of 44 24 and 157 nM respectivelyIC50

Bioactivity Dacinostat is a potent inhibitor with an of 32 nMHDAC IC50Dacinostat also inhibits with an of 9 nM and usedHDAC1 IC50in cancer research

Bioactivity Domatinostat (4SC-202 free base) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Domatinostat tosylate (4SC-202) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Droxinostat(NS41080) is a selective inhibitor of HDAC3 HDAC6and HDAC8 with IC50 of 169 247 and 146 μM respectivelygt 8-fold selective against HDAC3 and no inhibition toHDAC1 2 4 5 7 9 and 10 IC50 Value 169 μM(HDAC3) 247μM(HDAC6) 146 μM(HDAC8) Target HDAC368 in vitrohellip

Bioactivity EDO-S101 is a pan inhibitor inhibits HDAC1 HDAC2 andHDACHDAC3 with values of 9 9 and 25 nM respectivelyIC50

Bioactivity Entinostat is an oral and selective class I inhibitorHDACwith s of 243 nM 453 nM and 248 nM for IC50 HDAC1 HDAC2

and respectivelyHDAC3

Bioactivity Fimepinostat (CUDC-907) potently inhibits class I s as wellPI3Kas classes I and II enzymes with an of 195439 nMHDAC IC50and 17501828 nM for PI3KαPI3KβPI3Kδ andHDAC1HDAC2HDAC3HDAC10 respectively

Bioactivity FT895 is a potent and selective inhibitor with an HDAC11 IC50

of 3 nM [1]

Bioactivity Givinostat (ITF-2357) is a inhibitor with an of 198HDAC IC50and 157 nM for and respectivelyHDAC1 HDAC3

CUDC-101 Cat No HY-10223

Dacinostat (NVP-LAQ824 LAQ824) Cat No HY-13606

Domatinostat (4SC-202 (free base)) Cat No HY-16012A

Domatinostat tosylate (4SC-202) Cat No HY-16012

Droxinostat (NS 41080) Cat No HY-13267

EDO-S101 (Tinostamustine) Cat No HY-101780

Entinostat (MS-275 SNDX-275) Cat No HY-12163

Fimepinostat (CUDC-907) Cat No HY-13522

FT895 Cat No HY-112285

Givinostat (ITF-2357) Cat No HY-14842

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9849Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9609Clinical Data LaunchedSize 2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Bioactivity Givinostat hydrochloride (ITF-2357 hydrochloride) is a HDACinhibitor with an of 198 and 157 nM for andIC50 HDAC1

respectivelyHDAC3

Bioactivity Givinostat hydrochloride monohydrate (ITF-2357 hydrochloridemonohydrate) is a inhibitor with an of 198 and 157HDAC IC50nM for and respectivelyHDAC1 HDAC3

Bioactivity HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2008040934 A1

Bioactivity HDAC-IN-4 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2007045844 A1 20070426

Bioactivity HDAC-IN-5 is a histone deacetylase inhibitor(HDAC) Bioactivity HDAC-IN-7 (Chidamide impurity) is an impurity of ChidamideChidamide is a potent and orally bioavailable HDAC enzymesclass I (HDAC123) and class IIb (HDAC10) inhibitor

Bioactivity HDAC6-IN-1 is a potent and selective inhibitor for withHDAC6an of 17 nM and shows 25-fold and 200-fold selectivityIC50relative to ( =422 nM) and ( =3398 nM)HDAC1 IC50 HDAC8 IC50respectively

Bioactivity HDAC8-IN-1 is a inhibitor with an of 272 nMHDAC8 IC50

Bioactivity HDACsmTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs)and targetmammalian target of Rapamycin (mTOR)inhibitor for treating hematologic malignancies with ofIC s50019 nM 18 nM 12 nM and gt500 nM for HDAC1 HDAC6 mTORand PI3Kα respectively HDACsmTOR Inhibitor 1 stimulateshellip

Bioactivity HPOB is a highly potent and selective inhibitor of histonedeacetylase 6 (HDAC6) with IC50 of 56 nM gt30 fold lesspotent against other HDACs target HDAC6 [1] IC 50 56nM [1]In vitro HPOB causes growth inhibition of normal andtransformed cells but does not induce cell death HPOBhellip

70 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Givinostat hydrochloride (ITF-2357 hydrochloride) Cat No HY-14842A

Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) Cat No HY-14842B

HDAC-IN-3 Cat No HY-19772

HDAC-IN-4 (CXD101) Cat No HY-100748

HDAC-IN-5 Cat No HY-18362

HDAC-IN-7 (Chidamide impurity) Cat No HY-13592

HDAC6-IN-1 Cat No HY-18947

HDAC8-IN-1 Cat No HY-111342

HDACsmTOR Inhibitor 1 Cat No HY-114414

HPOB Cat No HY-19747

wwwMedChemExpresscom 71

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg 100 mg

Bioactivity IDO1 and HDAC1 Inhibitor (Compound 10) is a dual andIDO1 inhibitor with s of 690 nM and 665 nMHDAC1 IC50

respectively [1]

Bioactivity ITSA-1 is membrane permeable and specifically suppresses TSAinhibition of HDAC (histone deacetylase) but not other HDACinhibitors

Bioactivity J22352 is a PROTAC (proteolysis-targeting chimeras)-like andhighly selective inhibitor with an value of 47HDAC6 IC50nM J22352 promotes HDAC6 degradation and induces anticancereffects by inhibiting autophagy and eliciting the antitumorimmune response in glioblastoma cancers and leading to thehellip

Bioactivity JAKHDAC-IN-1 is a potent dual inhibitor exhibitsJAK2HDACantiproliferative and proapoptotic activities in severalhematological cell lines JAKHDAC-IN-1 shows s of 4 and 2IC50

nM for JAK2 and HDAC respectively [1]

Bioactivity LMK-235 is a potent and selective inhibitor inhibitsHDAC45HDAC5 HDAC4 HDAC6 HDAC1 HDAC2 HDAC11 and HDAC8 with

s of 422 nM 119 nM 557 nM 320 nM 881 nM 852 nM andIC501278 nM respectively and is used in cancer research

Bioactivity M344 (D 237) is an inhibitor of ( =100histone deacetylase IC50nM) and an inducer of terminal cell fifferentiation

Bioactivity MC1568 is a selective class II (IIa) histone deacetylas () inhibitor used for cancer researchHDAC II

Bioactivity Mocetinostat (MGCD0103) is a potent orally active andisotype-selective inhibitor with s ofHDAC (Class IIV) IC50015 029 166 and 059 μM for andHDAC1 HDAC2 HDAC3

respectively Mocetinostat shows no inhibition onHDAC11HDAC4 HDAC5 HDAC6 HDAC7 or HDAC8

Bioactivity Nanatinostat (CHR-3996) is a potent class I selective andorally active inhibitor with anhistone deacetylase (HDAC)

of 8 nM IC50[1]

Bioactivity Nexturastat A is a potent and selective HDAC6 inhibitor withIC50 of 5 nM no inhibition on other HDAC forms

IDO1 and HDAC1 Inhibitor Cat No HY-112147

ITSA-1 Cat No HY-100508

J22352 Cat No HY-126147

JAKHDAC-IN-1 Cat No HY-126141

LMK-235 Cat No HY-18998

M344 (D 237 MS 344) Cat No HY-13506

MC1568 Cat No HY-16914

Mocetinostat (MGCD0103) Cat No HY-12164

Nanatinostat (CHR-3996) Cat No HY-13432

Nexturastat A Cat No HY-16699

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9907Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9867Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9797Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NKL 22 is a HDAC inhibitor The value of IC 50 is 78 uM NKL 22increase frataxin protein concentrations NKL 22 inhibitorsincrease FXN mRNA in FRDA lymphocytes HDAC inhibitors actdirectly on FXN [1]

Bioactivity Oxamflatin (Metacept-3) is a potent inhibitor with anHDAC of 157 nMIC50

Bioactivity Panobinostat is a non-selective histone deacetylase ( )HDACinhibitor

Bioactivity PCI-34051 is a potent and selective inhibitor with HDAC8 IC50of 10 nM with gt200-fold selectivity over the other HDACisoforms

Bioactivity PI3KHDAC-IN-1 is a potent dual inhibitor of PI3KHDACpotently inhibits PI3Kδ and HDAC1 with s of 81 nM and 14IC50

nM respectively [1]

Bioactivity Pimelic diphenylamide 106 is a slow tight-binding inhibitorof class I HDAC (HDAC 1 2 and 3 with IC50 values of 150 nM 760nM and 370 nM respectively) demonstrating no activityagainst class II HDACs

Bioactivity Pracinostat is a potent inhibitorhistone deacetylase (HDAC)with s of 40-140 nM used for cancer researchIC50

Bioactivity PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDACPTACH exerts potent growth inhibition against various humancancer cells with EC50 values ranging from 1 to 10 μM

Bioactivity Quisinostat (JNJ-26481585) is an orally available potent inhibitor with an of 011 nM for HDAC1HDAC IC50

Bioactivity Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of which is under developmenthistone deacetylase enzymes (HDAC)

for the treatment of cutaneous T-cell lymphoma [1]

72 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NKL 22 Cat No HY-100384

Oxamflatin (Metacept-3) Cat No HY-102033

Panobinostat (LBH589 NVP-LBH589) Cat No HY-10224

PCI-34051 Cat No HY-15224

PI3KHDAC-IN-1 Cat No HY-128582

Pimelic Diphenylamide 106 (RGFA-8 TC-H 106 Histone Deacetylase Inhibitor VII) Cat No HY-19348

Pracinostat (SB939) Cat No HY-13322

PTACH (NCH-51) Cat No HY-12954

Quisinostat (JNJ-26481585) Cat No HY-15433

Remetinostat (SHP-141) Cat No HY-100365

wwwMedChemExpresscom 73

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9970Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Bioactivity Resminostat is a potent inhibitor of andHDAC1 HDAC3 with mean values of 425 501 718 nMHDAC6 IC50

respectively and shows less potent activities against HDAC8with an of 877 nMIC50

Bioactivity Resminostat hydrochloride is a potent inhibitor of HDAC1 and with mean values of 425 501 718HDAC3 HDAC6 IC50

nM respectively and shows less potent activities againstHDAC8 with an of 877 nMIC50

Bioactivity RG2833 is a brain-penetrant inhibitor with of 60 nMHDAC IC50and 50 nM for HDAC1 and HDAC3 respectively

Bioactivity RGFP966 is a highly selective inhibitor with an ofHDAC3 IC5080 nM and shows no inhibition to other HDACs at concentrationsup to 15 μM

Bioactivity Ricolinostat (ACY-1215) is a potent and selective HDAC6inhibitor with an of 5 nM ACY-1215 also inhibitsIC50

and with s of 58 48 and 51 nMHDAC1 HDAC2 HDAC3 IC50respectively

Bioactivity Romidepsin is a potent and inhibitor with sHDAC1 HDAC2 IC50of 36 and 47 nM respectively

Bioactivity RTS-V5 is a dual inhibitor with s ofHDACproteasome IC5069 18 15 027 053 μM for HDAC1 HDAC2 HDAC3 HDAC6HDAC8 respectively

Bioactivity Santacruzamate A (CAY-10683) is a potent and selective HDAC2inhibitor with an of 119 pM IC50

[1]

Bioactivity Scriptaid is a potent inhibitorhistone deacetylase (HDAC)used in cancer research

Bioactivity Sinapinic acid (Sinapic acid) is a phenolic compound isolatedfrom Jack Rhizome acts as anHydnophytum formicaruminhibitor of with an of 227 mM and alsoHDAC IC50

[1]

inhibits activity Sinapinic acid posssess pothellipACE-I [2]

Resminostat (RAS2410 4SC-201) Cat No HY-14718

Resminostat hydrochloride (RAS2410 hydrochloride 4SC-201 hydrochloride) Cat No HY-14718A

RG2833 (RGFP109) Cat No HY-16425

RGFP966 Cat No HY-13909

Ricolinostat (ACY-1215 Rocilinostat) Cat No HY-16026

Romidepsin (FK 228 FR 901228 NSC 630176) Cat No HY-15149

RTS-V5 Cat No HY-112908

Santacruzamate A (CAY-10683) Cat No HY-N0931

Scriptaid (Scriptide GCK1026) Cat No HY-15489

Sinapinic acid (Sinapic acid) Cat No HY-W009732

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg

Purity 9800Clinical Data Phase 3Size 10mM x 1mL in Water

1 g 5 g 500 g

Bioactivity Butyric acid is a inhibitor withhistone deacetylase (HDAC)anti-tumor effects in several cancers

Bioactivity Sodium phenylbutyrate is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity SR-4370 is an inhibitor of with s of 013 μM 058HDAC IC50μM 0006 μM 23 μM and 34 μM for HDAC1 HDAC2 HDAC3HDAC8 and HDAC6 respectively

Bioactivity ST8154AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity ST8155AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity Sulforaphane is an isothiocyanate present naturally in widelyconsumed vegetables has shown anticancer and cardioprotectiveactivities

Bioactivity SW-100 a selective inhibitorhistone deacetylase 6 (HDAC6)with an of 23 nM shows at least 1000-fold selectivityIC50for HDAC6 relative to all other HDAC isozymes SW-100 displaysa significantly improved ability to cross hellip

Bioactivity Tacedinaline (N-acetyldinaline) is an inhibitor of the histonedeacetylase ( ) with s of 09 09 12 μM forHDAC IC50recombinant HDAC 1 2 and 3 respectively

Bioactivity Tasquinimod is an oral antiangiogenic agent in clinical trialsfor the treatment of castration-resistant prostate cancerTasquinimod binds to the regulatory Zn binding domain of2+

with of 10-30 nMHDAC4 Kd

Bioactivity TH34 an inhibitor with s of 46 μM 19HDAC6 8 10 IC50μM and 77 μM respectively shows high selectivity overHDAC123 [1]

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Sodium Butyrate (Butanoic acid sodium salt) Cat No HY-B0350A

Sodium phenylbutyrate (Sodium 4-phenylbutyrate TriButyrate) Cat No HY-15654

SR-4370 Cat No HY-111400

ST8154AA1 Cat No HY-112805

ST8155AA1 Cat No HY-112806

Sulforaphane Cat No HY-13755

SW-100 Cat No HY-115475

Tacedinaline (N-acetyldinaline CI-994 Goe-5549) Cat No HY-50934

Tasquinimod (ABR-215050) Cat No HY-10528

TH34 Cat No HY-111818

wwwMedChemExpresscom 75

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g 25 g

Purity 9867Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g 25 g

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9887Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TMP195 is a selective class IIa histone deacetylase ( )HDACinhibitor with s of 59 60 26 15 nM for HDAC4 HDAC5KiHDAC7 and HDAC9 respectively

Bioactivity TMP269 is a novel and selective class IIa histone deacetylase inhibitor with s of 157 nM 97 nM 43 nM and 23 nM(HDAC) IC50

for HDAC4 HDAC5 HDAC7 and HDAC9 respectively

Bioactivity Trichostatin A is a potent and specific inhibitor of HDAC with an value of 18 nM for HDACclass III IC50

Bioactivity Tubacin is a potent and selective inhibitor of with anHDAC6 value of 4 nM and approximately 350-fold selectivity overIC50

HDAC1

Bioactivity Tubastatin A (Hydrochloride) is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tubastatin-A is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tucidinostat is a potent and orally bioavailable enzymesHDACclass I ( ) and class IIb ( ) inhibitor withHDAC123 HDAC10

s of 95 160 67 and 78 nM less active on HDAC8 andIC50HDAC11 ( s 733 nM 432 nM respectively) and showshellipIC50

Bioactivity UF010 is a potent and selective HDAC inhibitor with IC50 ~006μM 01 μM 05 μM and 15 μM for HDACs 3 2 1 and 8respectively It has gt 6-fold selectivity over other HDACsIC50 value 006 μM (HDAC3) 01 μM (HDAC2) 05 μM (HDAC1)15 μM(HDAC 8) Target HDAC in vitro UF010 is a competitivehellip

Bioactivity Valproic acid is an inhibitor with in the range ofHDAC IC5005 and 2 mM also inhibits ( 400 μM) andHDAC1 IC50induces proteasomal degradation of Valproic acidHDAC2sodium salt is used in the treatment of epilepsy bipohellip

Bioactivity Valproic acid sodium salt is an anticonvulsants used to treatepilepsy bipolar disorder and migraines Valproic acidinhibits with an of 04 mMhistone deacetylase 1 (HDAC1) IC50

TMP195 Cat No HY-18361

TMP269 Cat No HY-18360

Trichostatin A (TSA) Cat No HY-15144

Tubacin Cat No HY-13428

Tubastatin A Hydrochloride (Tubastatin A HCl TSA HCl) Cat No HY-13271

Tubastatin-A Cat No HY-13271A

Tucidinostat (Chidamide HBI-8000 CS 055) Cat No HY-109015

UF010 Cat No HY-18976

Valproic acid (VPA 2-Propylpentanoic Acid) Cat No HY-10585

Valproic acid sodium salt (Sodium Valproate) Cat No HY-10585A

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

250 mg 500 mg 1 g 5 g

Bioactivity Vorinostat is a potent and orally available inhibitor of and andHDAC1 HDAC2 HDAC3 (Class I) HDAC7 (Class II)

with values of 10 nM and 20 nM forHDAC11 (Class IV ) ID50HDAC1 and HDAC3 respectively

Bioactivity WT-161 is a potent and selective inhibitor with an HDAC6 IC50of 040 nM

76 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Vorinostat (SAHA) Cat No HY-10221

WT-161 Cat No HY-100871

wwwMedChemExpresscom 77

HSPHeat shock proteins

HSP (Heat shock proteins) are a group of proteins induced by heatshock the most prominent members of this group are a class offunctionally related proteins involved in the folding and unfolding ofother proteins HSP expression is increased when cells are exposed toelevated temperatures or other stress This increase in expression istranscriptionally regulated The dramatic upregulation of the heatshock proteins is a key part of the heat shock response and is inducedprimarily by heat shock factor (HSF) HSPs are found in virtually allliving organisms from bacteria to humans Heat shock proteinsappear to serve a significant cardiovascular role Hsp90 Hsp84Hsp70 Hsp27 Hsp20 and alpha B crystallin all have been reported as

having roles in the cardiovasculature

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 g

Purity 9997Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9932Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 1 mg

HSP Inhibitors amp Modulators

Bioactivity Alvespimycin is a potent inhibitor of binding to Hsp90Hsp90with an of 62 plusmn 29 nMEC50

Bioactivity Alvespimycin hydrochloride is a potent inhibitor of Hsp90binding to Hsp90 with of 62plusmn29 nMEC50

Bioactivity Apoptozole is an inhibitor of the ATPase domain of andHsc70 with s of 021 and 014 μM respectively and canHsp70 Kd

induce apoptosis

Bioactivity Arimoclomol maleate (BRX-220) is a co-inducer of heat shockproteins ( )HSP

Bioactivity BIIB021 is an orally available fully synthetic inhibitor of with and of 17 nM and 38 nM respectivelyHSP90 Ki EC50

Bioactivity Bimoclomol is a coinducer used forheat shock protein (HSP)treatment of cardiovascular diseases

Bioactivity CCT251236 is an orally available pirin ligand from a heatshock transcription factor 1 (hsf1) phenotypic screen with an

of 19 nM for inhibition of HSF1-mediated IC50 HSP72

induction

Bioactivity Col003 is a potent inhibitor of competitively binds toHsp47the collagen binding site on Hsp47 ( 18 μM) andIC50inhibits collagen secretion by destabilizing the collagentriple helix [1]

Bioactivity Debio 0932 is an orally active inhibitor with s ofHSP90 IC50100 and 103 nM for HSP90α and HSP90β respectively

Bioactivity Ethoxyquin is an antioxidant which has been used in animalfeed for many years and also an inhibitor of heat shock

( )protein 90 Hsp90

78 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Alvespimycin (17-DMAG NSC 707545) Cat No HY-10389

Alvespimycin hydrochloride (17-DMAG hydrochloride KOS-1022 BMS 826476) Cat No HY-12024

Apoptozole (Apoptosis Activator VII) Cat No HY-15098

Arimoclomol maleate (BRX-220) Cat No HY-106443A

BIIB021 (CNF2024) Cat No HY-10212

Bimoclomol Cat No HY-U00398

CCT251236 Cat No HY-101026

Col003 Cat No HY-124817

Debio 0932 (CUDC-305) Cat No HY-13469

Ethoxyquin Cat No HY-B1425

wwwMedChemExpresscom 79

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9994Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Bioactivity Feretoside a phenolic compound extracted from the barks of E is a which act as cytoprotectiveulmoides HSP inducer

agent

Bioactivity Ganetespib is a heat shock protein 90 ( ) inhibitorHSP90which exhibits potent cytotoxicity in a wide variety ofhematological and solid tumor cell lines

Bioactivity Geldanamycin is a inhibitor with antimicrobial activityHsp90against many Gram-positive and some Gram-negative bacteria

Bioactivity Grp94 Inhibitor-1 is a potent selective inhibitor withGrp94an value of 2 nM and over 1000-fold selectivity to Grp94IC50

against Hsp90α [1]

Bioactivity HA15 a molecule that targets specifically BiP GRP78 HSPA5inhibits the ATPase activity of BiP HA15 strongly increasesBiP protein expression in A375 melanoma cells [1]

Bioactivity HSF1A is a cell-permeable activator of heat shocktranscription factor 1 ( )HSF1

Bioactivity HSP70-IN-1 is a heat shock protein ( ) inhibitor inhibitsHSPthe growth of Kasumi-1 cells with an of 23 μMIC50

Bioactivity JG-98 is an allosteric heat shock protein 70 (Hsp70)inhibitor with anti-cancer activities which disrupts Hsp70

and affects signalinginteraction with a co-chaperone Bag3pathways important for cancer development [1] [2] [3]

Bioactivity KNK437 is a inhibitor and inhibits the induction ofHSPHSP105 HSP70 and HSP40

Bioactivity KRIBB11 is an inhibitor of withHeat shock factor 1 (HSF1) of 12 μMIC50

Feretoside Cat No HY-N6249

Ganetespib (STA-9090) Cat No HY-15205

Geldanamycin Cat No HY-15230

Grp94 Inhibitor-1 Cat No HY-112910

HA15 Cat No HY-100437

HSF1A Cat No HY-103000

HSP70-IN-1 Cat No HY-12622

JG-98 Cat No HY-117282

KNK437 (Heat Shock Protein Inhibitor I) Cat No HY-100110

KRIBB11 Cat No HY-100872

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 100 mg

Purity 9569Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9914Clinical Data Phase 2Size 5 mg 10 mg 25 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity KU-32 is a novel novobiocin-based inhibitor that canHsp90protect against neuronal cell death

Bioactivity KW-2478 is an inhibitor of with an of 38 nMHsp90α IC50and has antitumor activity against various human hematologicaltumor cells

Bioactivity Luminespib (NVP-AUY922) is a potent inhibitor withHSP90s of 78 and 21 nM for HSP90α and HSP90β respectivelyIC50

Bioactivity MKT-077 is a rhodacyanine dye and also a heat shock protein 70( ) inhibitor which exhibits significant antitumorHsp70activity

Bioactivity NVP-HSP990 is a potent and selective inhibitor withHsp90 values of 06 08 and 85 nM for Hsp90α Hsp90β andIC50

Grp94 respectively

Bioactivity Onalespib (AT13387) is a potent inhibitor of with aHsp90 of 071 nMKd

Bioactivity p5 Ligand for Dnak and DnaJ is a nonapeptide whichcorresponds to the main binding site for the 23-residue partof the presequence of mitochondrial aspartateaminotransferase p5 Ligand for Dnak and DnaJ is ahigh-affinity ligand for DnaK and DnaJ [1]

Bioactivity Pifithrin-μ is an inhibitor of and with antitumorp53 HSP70and neuroprotective activity

Bioactivity PU-WS13 is a selective inhibitor with an ofGrp94 EC50022 μM

Bioactivity Retaspimycin is a potent and water-soluble inhibitor of with s of 119 nM for both Hsp90 and Grp9Hsp90 EC50

80 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

KU-32 Cat No HY-108248

KW-2478 Cat No HY-13468

Luminespib (NVP-AUY922 AUY922 VER-52296) Cat No HY-10215

MKT-077 (FJ-776) Cat No HY-15096

NVP-HSP990 (HSP-990) Cat No HY-15190

Onalespib (AT13387) Cat No HY-14463

p5 Ligand for Dnak and DnaJ Cat No HY-P1887

Pifithrin-μ (PFTμ 2-Phenylethynesulfonamide) Cat No HY-10940

PU-WS13 Cat No HY-18680

Retaspimycin Cat No HY-15263

wwwMedChemExpresscom 81

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9740Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9982Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9903Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Retaspimycin Hydrochloride is a potent and water-solubleinhibitor of with s of 119 nM for both Hsp90 andHsp90 EC50Grp9

Bioactivity Shepherdin (79-87) is amino acids 79 to 87 fragment ofShepherdin Shepherdin is a peptidomimetic antagonist of thecomplex between Hsp90 and Survivin Anticancer activity [1]

Bioactivity SNX-5422 Mesylate (PF-04929113 Mesylate) a prodrug ofSNX-2112 is an orally active inhibitor with a ofHsp90 Kd41 nM and also induces Her-2 degradation with an ofIC5037nM

Bioactivity Tanespimycin (17-AAG) is a potent inhibitor with anHSP90 of 5 nM having a 100-fold higher binding affinity forIC50

tumour cell derived HSP90 than normal cell derived HSP90

Bioactivity TAS-116 is an oral bioavailable ATP-competitive highlyspecific inhibitor ( s of 347 nM and 213HSP90αHSP90β KinM respectively) without inhibiting other HSP90 familyproteins such as GRP94 TAS-116 demonstrates less ocuhellip[1]

Bioactivity Teprenone is a anti-ulcer drug and works as an inducer ofheat shock proteins ( )HSPs

Bioactivity TRC051384 is a heat shock protein 70 ( ) inducerHSP70 Bioactivity VER-155008 is an inhibitor of with s of 05 μMHsp70 IC5026 μM and 26 μM for Hsc70 and Grp7 respectivelyHsp70and with a of 03 μM for Kd Hsp70

Bioactivity VER-49009 is a inhibitor with an of 25 nM and aHsp90 IC50 of 78 nMKd

Bioactivity VER-50589 is a inhibitor with an of 21 nM and aHsp90 IC50 of 45 nMKd

Retaspimycin Hydrochloride (IPI-504) Cat No HY-10210

Shepherdin 79-87 Cat No HY-P1750

SNX-5422 Mesylate (PF-04929113 (Mesylate)) Cat No HY-10213A

Tanespimycin (17-AAG NSC 330507 CP 127374) Cat No HY-10211

TAS-116 Cat No HY-15785

Teprenone (Geranylgeranylacetone) Cat No HY-B0779

TRC051384 Cat No HY-101712

VER-155008 Cat No HY-10941

VER-49009 (CCT 129397) Cat No HY-15986

VER-50589 Cat No HY-15984

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9924Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity VER-82576 (NVP-BEP800) is a potent orally available andselective inhibitor with an of 58 nM for Hsp90βHsp90 IC50VER-82576 also slightly blocks Grp94 and Trap-1 with s ofIC5041 and 55 μM respectively

Bioactivity XL888 is a heat shock protein-90 ( ) inhibitor with anHSP90 of 24 nMIC50

Bioactivity YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathwayagainst glioblastoma directly binding to heat shock protein

with an of 820 nM on NFAT nuclear90 (HSP90) IC50translocation YZ129-induced GBM cell-cycle arrest at the G2Mphase promotes apoptosis and inhibited tumor cellhellip

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VER-82576 (NVP-BEP800) Cat No HY-10942

XL888 Cat No HY-13313

YZ129 Cat No HY-114413

wwwMedChemExpresscom 83

IRE1Inositol requiring enzyme 1

The serinethreonine-protein kinaseendoribonucleaseinositol-requiring enzyme 1 (IRE1) is an enzyme that in humans isencoded by the gene IRE1 is an endoplasmic reticulum (ER)ERN1transmembrane sensor that activates UPR to maintain ER and cellularfunction While mammalian IRE1 promotes cell survive it can initiateapoptosis via decay of anti-apoptotic microRNAsIRE1 activation is initiated by homotypic interactions of thestress-sensing lumenal domain favoring transautophosphorylation ofthe kinase-extension nuclease (KEN) domain on the cytoplasmic sideof the ER membraneIRE1XBP-1 has been shown to regulate a variety of genes in various

cell types in response to ER stress mostly related to ER function and the secretory pathway although the target genesvary depending on the cell type and nature of the stress stimuli

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9875Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg

IRE1 Inhibitors amp Modulators

Bioactivity 36-DMAD hydrochloride is a inhibitor of the pathwayIRE1α-XBP1of the unfolded protein response

Bioactivity 4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor ofIRE1α

Bioactivity 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1αinhibitor with an of 008 μM extracted from patent WOIC502008154484 A1 IRE-lα inhibitor compound 3-5

Bioactivity APY29 is an allosteric modulator of which inhibits IRE1αIRE1αautophosphorylation with of 280 nM and activates IRE1αIC50RNase activity

Bioactivity B I09 is an RNase inhibitor with an of 1230 nMIRE-1 IC50 Bioactivity GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1alpha ( ) which can inhibit and IRE1α IRE1α kinase activity RNase

with s of 20 and 200 nM respectivelyactivity IC50

Bioactivity GSK2850163 hydrochloride is a novel inhibitor ofinositol-requiring enzyme-1 alpha ( ) which can inhibitIRE1α

and with s of 20 andIRE1α kinase activity RNase activity IC50200 nM respectively

Bioactivity KIRA6 allosterically inhibits activity withIRE1α RNase kinasean of 06 microMIC50

Bioactivity Kira8 is a mono-selective inhibitor that allostericallyIRE1αattenuates with an of 59 nM IRE1α RNase activity IC50

[1]Bioactivity MKC3946 is a potent and soluble inhibitor used forIRE1α

cancer research

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36-DMAD hydrochloride Cat No HY-U00460

4μ8C (IRE1 Inhibitor III) Cat No HY-19707

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) Cat No HY-107371

APY29 Cat No HY-17537

B I09 Cat No HY-107400

GSK2850163 Cat No HY-U00459

GSK2850163 hydrochloride Cat No HY-U00459B

KIRA6 Cat No HY-19708

Kira8 Cat No HY-114368

MKC3946 Cat No HY-19710

wwwMedChemExpresscom 85

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity MKC8866 is an inhibitor with an of less thanIRE1 RNase IC5001 μM for IRE1α RNase

Bioactivity MKC9989 is a ( ) inhibitor and alsoHydroxy aryl aldehydes HAAinhibits with an of 023 to 44 μMIRE1α IC50

Bioactivity STF-083010 is an inhibitor STF-083010 inhibits Ire1Ire1endonuclease activity without affecting its kinase activityafter endoplasmic reticulum stress

MKC8866 Cat No HY-104040

MKC9989 Cat No HY-12399

STF-083010 Cat No HY-15845

Kinesin

Kinesin is a protein belonging to a class of motor proteins found ineukaryotic cells Kinesins move along microtubule filaments and arepowered by the hydrolysis of ATP (thus kinesins are ATPases) Theactive movement of kinesins supports several cellular functionsincluding mitosis meiosis and transport of cellular cargo Mostkinesins walk towards the plus end of a microtubule entailstransporting cargo from the centre of the cell towards the peripheryKinesins were discovered as microtubule (MT)-based anterogradeintracellular transport motors The founding member of thissuperfamily the genomes of mammals encode more than 40 kinesinproteins organized into at least 14 families named kinesin-1 through

kinesin-14

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wwwMedChemExpresscom 87

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9871Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9973Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Kinesin Inhibitors amp Modulators

Bioactivity (R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of ARRY-520(R)-Filanesib ((R)-ARRY-520) is a synthetic kinesin spindle

inhibitor with of 6 nMprotein (KSP) IC50

Bioactivity AZ82 is a selective kinesin-like protein KIFC1 (HSETKIFC1)inhibitor with a of 43 nM and an of 300 nM for KIFC1Ki IC50

Bioactivity CW-069 is an allosteric inhibitor of microtubule motor with an of 75 μMprotein HSET IC50

Bioactivity Dimethylenastron is a potent inhibitor with ankinesin Eg5 of 200 nMIC50

Bioactivity Eg5 Inhibitor V trans-24 is a potent and specific kinesin Eg5inhibitor with an of 065 μM and can be used in theIC50research of cancer

Bioactivity EMD534085 is a potent and selective inhibitor of the mitotic with an of 8 nMkinesin-5 IC50

Bioactivity Filanesib (ARRY-520) is a synthetic kinesin spindle protein inhibitor with of 6 nM(KSP) IC50

Bioactivity Ispinesib is a specific inhibitor of kinesin spindle protein with a of 17 nM(KSP) Ki app

Bioactivity K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5with an of 13 μMIC50

Bioactivity Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member and is used for the research of cellular15 (Kif15)

proliferative diseases

(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A

AZ82 Cat No HY-12241

CW-069 Cat No HY-15857

Dimethylenastron Cat No HY-19944

Eg5 Inhibitor V trans-24 Cat No HY-112915

EMD534085 Cat No HY-15000

Filanesib (ARRY-520) Cat No HY-15187

Ispinesib (SB-715992) Cat No HY-50759

K858 Racemic Cat No HY-19966

Kif15-IN-1 Cat No HY-15948

Purity 9731Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9705Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg

Purity 9959Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9651Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Kif15-IN-2 is an inhibitor of the mitotic and iskinesin Kif15used for the research of cellular proliferative diseases

Bioactivity Litronesib is a selective mitosis-specific kinesin Eg5inhibitor with antitumor activity

Bioactivity Litronesib (Racemate) is the racemate of litronesibLitronesib is a selective allosteric inhibitor of kinesin

Eg5

Bioactivity Monastrol is a potent and cell-permeable inhibitor of themitotic with an value of 14 μMkinesin Eg5 IC50

Bioactivity Paprotrain is a cell-permeable inhibitor of the kinesin inhibits the ATPase activity of MKLP-2 with an MKLP-2 IC50

of 135 μM and a of 336 μM and shows a moderate inhibitionKiactivity on with an of 55 μMDYRK1A IC50

Bioactivity PF-2771 is a potent and selective centromere protein E inhibitor inhibiting CENP-E motor activity with an(CENP-E)

of 161 nM PF-2771 is used as an anticancer agentIC50

Bioactivity SB-743921 is a potent inhibitor of the mitotic kinesin KSP with a of 01 nM(Eg5) Ki

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Kif15-IN-2 Cat No HY-15949

Litronesib (LY-2523355 KF-89617) Cat No HY-14846

Litronesib Racemate (LY-2523355 Racemate KF-89617 Racemate) Cat No HY-14846A

Monastrol ((plusmn)-Monastrol) Cat No HY-101071A

Paprotrain Cat No HY-101298

PF-2771 Cat No HY-19530

SB-743921 Cat No HY-12069

wwwMedChemExpresscom 89

LIM Kinase (LIMK)LIMKs

LIM kinases (LIMKs) are important cell cytoskeleton regulators thatplay a prominent role in cancer manifestation and neuronal diseasesThe LIMK family consists of two homologues LIMK1 and LIMK2which differ from one another in expression profile intercellularlocalization and function The main substrate of LIMK is cofilin amember of the actin-depolymerizing factor (ADF) protein familyWhen phosphorylated by LIMK cofilin is inactive LIMKs play acontributory role in several neurodevelopmental disorders and incancer growth and metastasisLIM domain kinases (LIMK1 and 2) are substrate for Cdc42Rac-PAKand modulate actin dynamics by phosphorylating cofilin at serine-3

This modification inactivates cofilinrsquos actin severing and depolymerizing activity LIMKs also translocate into thenucleus and regulate cell cycle progression LIMKs are potential therapeutic targets for NF2 and other merlin-deficienttumors

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

LIM Kinase (LIMK) Inhibitors amp Modulators

Bioactivity BMS-3 is a potent inhibitor with s of 5 nM and 6LIMK IC50nM for and respectivelyLIMK1 LIMK2

Bioactivity BMS-5 (LIMKi 3) is a potent inhibitor with s of 7LIMK IC50nM and 8 nM for and respectivelyLIMK1 LIMK2

Bioactivity R-10015 a broad-spectrum antiviral compound for HIVinfection acts as a potent and selective inhibitor of LIM

and binds to the ATP-binding pocketdomain kinase (LIMK)with an of 38 nM for human LIMK1 IC50

[1]

Bioactivity T56-LIMKi is a selective inhibitor of inhibits theLIMK2growth of Panc-1 cells with an of 352 μMIC50

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BMS-3 Cat No HY-18304

BMS-5 (LIMKi 3) Cat No HY-18305

R-10015 Cat No HY-120097

T56-LIMKi (T5601640) Cat No HY-19352

wwwMedChemExpresscom 91

MicrotubuleTubulin

Microtubules are a component of the cytoskeleton found throughoutthe cytoplasm These tubular polymers of tubulin can grow as long as50 micrometres with an average length of 25 microm and are highlydynamic The outer diameter of a microtubule is about 24 nm whilethe inner diameter is about 12 nm Microtubules are found ineukaryotic cells and are formed by the polymerization of a dimer oftwo globular proteins alpha and beta tubulin Tubulin is one ofseveral members of a small family of globular proteins The tubulinsuperfamily includes five distinct families the alpha- beta- gamma-delta- and epsilon-tubulins and a sixth family which is present only inkinetoplastid protozoa The most common members of the tubulin

family are α-tubulin and β-tubulin the proteins that make up microtubules Microtubules are very important in anumber of cellular processes They are involved in maintaining the structure of the cell

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9987Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9920Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9982Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

MicrotubuleTubulin Inhibitors amp Modulators

Bioactivity 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivativewith improved pharmacological features and higher watersolubility IC50 value Target Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cyclearrest and apoptosis as measured by flow cytometry DNAhellip

Bioactivity 10-Oxo Docetaxel (Docetaxel Impurity) is a novel taxoid havingremarkable anti-tumor properties and a Docetaxel intermediate

Bioactivity 2-Methoxyestradiol is an inhibitor and angiogenesis apoptosisinducer with potent antineoplastic activity2-Methoxyestradiol also destablize microtubules

Bioactivity 4-Demethylepipodophyllotoxin(4-DMEP) is a key intermediatecompound for the preparation of podophyllotoxin-typeanti-cancer drugs a potent inhibitor of microtubule assembly

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity ofdocetaxel detected by high performance liquid chromatography(HPLC)

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity C 7-Epitaxotere)is a impurity of docetaxel

Bioactivity 7-epi-Taxol is an active metabolite of taxol with activitycomparable to that of taxol against cell replicationpromoting bundle formation and againstmicrotubulemicrotubule depolymerization

Bioactivity 7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel)derivative Paclitaxel binds to tubulin and inhibits thedisassembly of microtubules

Bioactivity ABT-751(E 7010) is a novel bioavailable tubulin-binding andantimitotic sulfonamide agent with IC50 of about 15 and 34μM in neuroblastoma and non-neuroblastoma cell linesrespectively IC50 Value 15 μM(neuroblastoma) 34μM(non-neuroblastoma) Target MicrotubuleTubulin in vitrohellip

Bioactivity Amphethinile is an agent The affinity constantanti-tubulinfor the association ( ) of Amphethinile with tubulin isKa13 μM

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10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol

10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584

10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674

2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033

4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435

7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675

7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676

7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227

7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574

ABT-751 (E7010) Cat No HY-13270

Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190

wwwMedChemExpresscom 93

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9903Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9949Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9751Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ansamitocin P-3 is a inhibitor Ansamitocin P-3microtubuleis a macrocyclic antitumor antibiotic

Bioactivity Auristatin E is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAE analog and cytotoxin inAntibody-drug conjugates

Bioactivity Auristatin F is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAF analog and cytotoxin inAntibody-drug conjugates

Bioactivity BNC105 is a tubulin polymerization inhibitor with potentantiproliferative and tumor vascular disrupting properties

Bioactivity BTB-1 is a potent selective and reversible mitotic motorprotein inhibitor with an of 169 μMKif18A IC50

Bioactivity Cabazitaxel is a semi-synthetic derivative of the naturaltaxoid 10-deacetylbaccatin III with potential antineoplasticactivity

Bioactivity CCB02 is a selective inhibitor bindingCPAP-tubulin interactionto tubulin and competing for the CPAP binding site ofβ-tubulin with an of 689 nM and shows potent anti-tumorIC50activity CCB02 shows no inhibition on the cell cycle- andcentrosome-related kinases or the phosphorylation status ofhellip

Bioactivity Cephalomannine is a taxol derivative with antitumorantiproliferative properties

Bioactivity Cevipabulin (TTI-237) is an oral microtubule-active antitumorcompound and inhibits the binding of [ H] vinblastine to3

tubulin with an of 18-40 nM for cytotoxicity in humanIC50

tumor cell line [1] [2]

Bioactivity Cevipabulin fumarate (TTI-237 fumarate) is an oralmicrotubule-active antitumor compound and inhibits thebinding of [ H] vinblastine to tubulin with an of3 IC50

18-40 nM for cytotoxicity in human tumor cell line [1] [2]

Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739

Auristatin E Cat No HY-15582

Auristatin F Cat No HY-15583

BNC105 Cat No HY-16114

BTB-1 Cat No HY-101770

Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459

CCB02 Cat No HY-114302

Cephalomannine Cat No HY-77554

Cevipabulin (TTI-237) Cat No HY-14949

Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C

Purity 9828Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9956Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9831Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Bioactivity Colchicine is a inhibitor and a tubulin microtubuledisrupting agent Colchicine inhibits microtubulepolymerization with an of 3 nMIC50

Bioactivity Combretastatin A4 is a -targeting agent thatmicrotubulebinds with of 04 μMβ-tubulin Kd

Bioactivity Crolibulin is a small molecule tubulin polymerizationinhibitor

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate IC50 Value NATarget tubulin ADCs For comparison purposes the ADC A1-mc-MMAD andor A1 -vc-MMAD were used The linker payloadmc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) washellip

Bioactivity D-64131 is a novel inhibitor of Tubulin polymerization thatcompetitively binds with [(3)H]colchicine to αβ-Tubulin

Bioactivity D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule

Bioactivity D8-MMAE is a deuterated labeled MMAE a potent mitoticinhibitor

Bioactivity D8-MMAF is a deuterated form of MMAF which is a disrupting agentmicrotubule

Bioactivity D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a disrupting agentmicrotubule

Bioactivity DM4 is is an agent that inhibit cell division DM4antitubulincan be used in the preparation of antibody drug conjugate

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Colchicine Cat No HY-16569

Combretastatin A4 (CRC 87-09) Cat No HY-N2146

Crolibulin (EPC2407) Cat No HY-13603

Cys-mcMMAD Cat No HY-15750

D-64131 Cat No HY-15482

D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8

Monomethyl Dolastatin 10 D8) Cat No HY-15581S

D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A

D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S

D8-MMAF hydrochloride Cat No HY-15579AS

DM4 Cat No HY-12454

wwwMedChemExpresscom 95

Purity 9897Clinical Data LaunchedSize 500u g 1 mg

Purity gt98Clinical Data LaunchedSize 1 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Purity 9988Clinical Data Phase 3Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9555Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9983Clinical Data Phase 2Size 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg

Bioactivity Docetaxel is an antineoplastic drug by inhibiting depolymerization and attenuating of themicrotubule

effects of and gene expressionbcl-2 bcl-xL

Bioactivity Docetaxel Trihydrate is a semi-synthetic taxane analogue actsas a stabilizermicrotubule

Bioactivity Angiotensin II human is a vasoconstrictor that acts on the and the receptorAT1 AT2

Bioactivity ELR510444 is a novel microtubule disruptor inhibitsMDA-MB-231 cell proliferation with IC50 of 309 nM not asubstrate for the P-glycoprotein drug transporter and retainsactivity in βIII-tubulin-overexpressing cell lines

Bioactivity Entasobulin is a polymerization inhibitor withβ-tubulinpotential anticancer activity

Bioactivity Epothilone A is a competitive inhibitor of the binding of [H] paclitaxel to polymers with a of 06-14 μM3 tubulin Ki

Bioactivity Epothilone B is a stabilizer with a ofmicrotubule Ki071μM It acts by binding to the αβ-tubulin heterodimersubunit which causes decreasing of αβ-tubulin dissociation

Bioactivity Epothilone D (KOS 862) is a potent stabilizermicrotubule

Bioactivity Eribulin (E7389) is a targeting agent that ismicrotubuleused in the treatment of metastatic breast cancer Eribulin(E7389) inhibits the proliferation of cancer cells by bindingmicrotubule proteins and microtubules

Bioactivity Eribulin mesylate (E7389 mesylate) is a microtubuletargeting agent that is used in the treatment of metastaticbreast cancer Eribulin mesylate (E7389 mesylate) inhibits theproliferation of cancer cells by binding microtubule proteinsand microtubules

Docetaxel (RP-56976) Cat No HY-B0011

Docetaxel Trihydrate (RP-56976 (Trihydrate)) Cat No HY-B0011A

Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580

ELR510444 Cat No HY-16191

Entasobulin Cat No HY-16777

Epothilone A (Epo A) Cat No HY-13503

Epothilone B (EPO 906 Patupilone) Cat No HY-17029

Epothilone D (KOS 862) Cat No HY-15278

Eribulin (B1939 E7389 ER-086526) Cat No HY-13442

Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A

Purity 9874Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9723Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9947Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9801Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Bioactivity Estramustine phosphate sodium is an antimicrotubulechemotherapy agent arrests prostate cancer cells in the G2Mphase of the cell cycle

Bioactivity Fosbretabulin disodium(CA 4DP CA 4P) is a microtubuledestabilizing drug a type of vascular-targeting agent a drugdesigned to damage the vasculature (blood vessels) of cancertumors causing central necrosis IC50 Value 4 nM [1] Targetmicrotubule in vitro Cytotoxic IC(50) values of CA-4 in humanhellip

Bioactivity Ixabepilone is an orally bioavailable inhibitor which binds to tubulin andmicrotubule

promotes tubulin polymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of the cell cycle andinduces tumor cell apoptosis

Bioactivity Lexibulin(CYT-997) is a potent tubulin polymerisationinhibitor with IC50 of 10-100 nM in cancer cell lines withpotent cytotoxic and vascular disrupting activity in vitro andin vivo

Bioactivity Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM in cancer celllines with potent cytotoxic and vascular disrupting activityin vitro and in vivo

Bioactivity Maytansinol inhibits microtubule assembly and inducesmicrotubule disassembly in vitro Target MicrotubuleTubulinin vitro Maytansinol disrupts the mitotic spindle andprevents mitotic exit in Drosophila Maytansinol reduces thegrowth andor survival of HCT116 cells in a dose-dependenthellip

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate Mc-MMAD is aprotective group (maleimidocaproyl) -conjugated MMAD IC50Value Target tubulin ADCs For comparison purposes the ADCA1 -mc-MMAD andor A1 -vc-MMAD were used The linkerpayloadhellip

Bioactivity Mc-MMAE is a protective group (maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE) which is a potent tubulininhibitor is a toxin payload in antibody drug conjugate (

)ADC

Bioactivity Mc-MMAF is a protective group-conjugated MMAF MMAF is a morepotent drug than Monomethyl auristatin E (MMAE) but ischarged and relatively membrane-impermeable is a potenttubulin inhibitor is a toxin payload in antibody drugconjugate Target MMAF is a new auristatin derivative with ahellip

Bioactivity Mertansine (DM1) is a inhibitor and is anmicrotubulinantibody-conjugatable maytansinoid that is developed toovercome systemic toxicity associated with maytansine and toenhance tumor-specific delivery Mertansine can be attached toa monoclonal antibody with a linker to create an antibody-drughellip

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Estramustine phosphate sodium Cat No HY-13627

Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449

Ixabepilone (Azaepothilone B BMS 247550 BMS 247550-1) Cat No HY-10222

Lexibulin (CYT-997) Cat No HY-10498

Lexibulin dihydrochloride (CYT-997 dihydrochloride) Cat No HY-10498A

Maytansinol (Ansamitocin P-0) Cat No HY-19474

Mc-MMAD Cat No HY-15740

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741

McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578

Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792

wwwMedChemExpresscom 97

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9957Clinical Data Phase 3Size 10mM x 1mL in Water

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 4Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity Microtubule inhibitor 1 is an antitumor agent with inhibitory activity with anmicrotubule polymerization

value of 9-16 nM in cancer cells IC50[1]

Bioactivity MMAD is a potent inhibitor is a toxin payload intubulinantibody drug conjugates ( )ADCs

Bioactivity MMAF (Monomethylauristatin F) is an antitubulin agent thatinhibit cell division inhibits H3397 cell growth with an IC50of 105 nM

Bioactivity MMAF hydrochloride is an antitubulin agent that inhibit celldivision inhibits H3397 cell growth with an of 105 nMIC50

Bioactivity Monomethyl auristatin E (MMAE SGD-1010) is a syntheticderivative of dolastatin 10 and functions as a potent

inhibitor by inhibiting tubulin polymerizationmitoticMMAE is widely used as a cytotoxic component of antibody-drug

to treat several different cancer typesconjugates (ADCs)

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity Ombrabulin (AVE8062) is a derivative of CA-4 phosphate whichis known to exhibit antivascular effects through selectivedisruption of the cytoskeleton of endothelial cellstubulin

Bioactivity Ombrabulin hydrochloride is a derivative of CA-4 phosphatewhich is known to exhibit antivascular effects throughselective disruption of the cytoskeleton of endothelialtubulincells

Bioactivity OSIP-486823 is a novel -interfering agent withmicrotubuledistinct biological effects on both protein kinase G (PKG) andmicrotubules

Bioactivity Paclitaxel (Taxol) a naturally occurring antineoplasticagent stabilizes resulting intubulin polymerizationarrest at the G2M phase of the cell cycle and apoptotic celldeath [1] [2]

Microtubule inhibitor 1 Cat No HY-114313

MMAD (Demethyldolastatin 10 Monomethylauristatin D

Monomethyl Dolastatin 10) Cat No HY-15581

MMAF (Monomethylauristatin F) Cat No HY-15579

MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat No HY-15579A

Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162

Nocodazole (Oncodazole R17934) Cat No HY-13520

Ombrabulin (AVE8062 AC7700) Cat No HY-14797

Ombrabulin hydrochloride (AVE8062 (hydrochloride) AC7700 (hydrochloride)) Cat No HY-18256

OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004

Paclitaxel (Taxol) Cat No HY-B0015

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9979Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9344Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9968Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Bioactivity Parbendazole is a potent inhibitor of assemblymicrotubuledestabilizes tubulin with an of 879nM and exhibitsEC50a broad-spectrum anthelmintic activity

Bioactivity PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX) compound acts asa -depolymerizing agent and an apoptotic agentmicrotubule

Bioactivity PE859 is a potent inhibitor of both and aggregationtau Aβwith values of 066 and 12 μM respectivelyIC50

Bioactivity PF-06380101 is a novel cytotoxic Dolastatin 10 analogue withexcellent potencies in tumor cell proliferation assays anddifferential ADME properties when compared to other syntheticauristatin analogues that are used in the preparation of ADCsIC50 value ~02 nM(GI50 in BT474 MDA-MB-361-DYT2 and N87hellip

Bioactivity Plinabulin (NPI-2358) is a vascular disrupting agents (VDA)against tubulin-depolymerizing with IC50 of 98~18 nM in tumorcells IC50 Value 98~18 nM Target MicrotubuleTubulin invitro NPI-2358 binds to the colchicine-binding site oftubulin and has potent inhibitory to human tumor cell lineshellip

Bioactivity Podofilox (Podophyllotoxin) is a potent inhibitor ofmicrotubule assembly and DNA topoisomerase II

Bioactivity Rosabulin is a potent inhibitor withmicrotubuleanti-cancer activities

Bioactivity Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10derivative and inhibitor of polymerizationtubulin

Bioactivity SSE15206 is a polymerization inhibitor (GI microtubule 50= 197 nM in HCT116 cells) that overcomes multidrug resistanceCauses aberrant mitosis resulting in G2M arrest due toincomplete spindle formation in cancer cells [1]

Bioactivity Taltobulin (HTI-286 SPA-110) is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibitedproliferation of all three hepatic tumor cell lines (mean IC50= 2 nmolL +- 1 nmolL) in vitro Interestingly no decreasehellip

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Parbendazole (SKF 29044) Cat No HY-115364

PBOX 6 Cat No HY-U00446

PE859 Cat No HY-12662

PF-06380101 Cat No HY-12522

Plinabulin (NPI-2358) Cat No HY-14444

Podofilox (Podophyllotoxin) Cat No HY-15552

Rosabulin (STA 5312) Cat No HY-14934

Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672

SSE15206 Cat No HY-111425

Taltobulin (HTI-286 SPA-110) Cat No HY-15584

wwwMedChemExpresscom 99

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9624Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9996Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Taltobulin hydrochloride is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibits proliferationof all three hepatic tumor cell lines (mean IC50 = 2 nmolL+- 1 nmolL) Interestingly no decrease in viable primaryhellip

Bioactivity Taltobulin trifluoroacetate (HTI-286 SPA-110) is an analogueof Hemiasterlin potent tubulin inhibitor ADCs cytotoxinIC50 value Target tubulin in vitro HTI-286 significantlyinhibited proliferation of all three hepatic tumor cell lines(mean IC50 = 2 nmolL +- 1 nmolL) in vitro Interestinglyhellip

Bioactivity Tasidotin hydrochloride is a peptide analog of the antimitoticdepsipeptide dolastatin 15 as an inhibitor of microtubuleassembly and microtubule dynamics

Bioactivity Tirbanibulin (KX2-391) is an inhibitor of that targetsSrcthe peptide substrate site of Src with of 9-60 nM inGI50cancer cell lines

Bioactivity Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) isan inhibitor of that targets the peptide substrate siteSrcof Src with of 9-60 nM in cancer cell linesGI50

Bioactivity Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitorof that targets the peptide substrate site of Src withSrc

of 9-60 nM in cancer cell linesGI50

Bioactivity Triclabendazole(CGA89317) is a benzimidazole it binds totubulin impairing intracellular transport mechanisms andinterferes with protein synthesis Target MicrotubuleTubulinTriclabendazole treatment produces percentage decreases of thefluke egg output by 153 43 and 366 respectively inhellip

Bioactivity Tubulin inhibitor 1 is a inhibitor occupying thetubulincolchicine binding site inhibits tubulin polymerizationTubulin inhibitor 1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase and inducescellular apoptosis [1]

Bioactivity Tubulysin A(TubA) is a myxobacterial product that can functionas an antiangiogenic agent in many in vitro assaysanti-microtubule anti-mitotic an apoptosis induceranticancer anti-angiogenic and antiproliferative IC50value Target microtubule Tubulysin A is a novel antibiotichellip

Bioactivity Valecobulin (CKD516) a valine prodrug of (S516) and avascular disrupting agent (VDA) is a potent beta-tubulin

inhibitor with marked antitumor activitypolymerizationagainst murine and human solid tumors [1] [2]

Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A

Tasidotin hydrochloride (ILX651) Cat No HY-13760

Tirbanibulin (KX2-391 KX-01) Cat No HY-10340

Tirbanibulin dihydrochloride (KX2-391 (dihydrochloride) KX-01 (dihydrochloride)) Cat No HY-10340A

Tirbanibulin Mesylate (KX2-391 (Mesylate) KX01 (Mesylate)) Cat No HY-10340B

Triclabendazole (CGA89317) Cat No HY-B0621

Tubulin inhibitor 1 Cat No HY-112607

Tubulysin A (TubA) Cat No HY-15995

Valecobulin (CKD-516) Cat No HY-13598

Purity 9958Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9914Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data LaunchedSize 10 mg 50 mg 100 mg 200 mg

Purity 9987Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9989Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Bioactivity Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulininhibitor (MMAD) Vc-MMAD is an antibody drug conjugate IC50Valu NA Target tubulin ADCs Monomethyl auristatin D(MMAD) a potent tubulin inhibitor is a toxin payload andantibody drug conjugate For comparison purposes the ADC A1hellip

Bioactivity VcMMAE is a with potentdrug-linker conjugate for ADCantitumor activity by using the anti-mitotic agent monomethylauristatin E (MMAE) linked via the lysosomally cleavabledipeptide valine-citrulline (vc)

Bioactivity Vinblastine sulfate is a cytotoxic alkaloid used againstvarious cancer types Vinblastine sulfate inhibits theformation of microtubule and suppresses nAChR with an ofIC5089 μM

Bioactivity Vincristine sulfate is an antitumor vinca alkaloid whichinhibits formation in mitotic spindlemicrotubuleresulting in an arrest of dividing cells at the metaphasestage It binds to with a of 85 nMmicrotubule Ki

Bioactivity Vinflunine is a new vinca alkaloid uniquely fluorinated withthe properties of mitotic-arresting and tubulin-interactingactivity

Bioactivity Vinflunine Tartrat is a new vinca alkaloid uniquelyfluorinated with the properties of mitotic-arresting andtubulin-interacting activity Target MicrotubuleTubulin Themajor effects of Vinflunine on dynamic instability are aslowing of the microtubule growth rate an increase in growthhellip

Bioactivity Vinorelbine is an anti-mitotic agent which inhibits theproliferation of Hela cells with IC of 125 nM50

Bioactivity Vinorelbine (ditartrate) is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC of 12550nM

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Vc-MMAD Cat No HY-15742

VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575

Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780

Vincristine sulfate (Leurocristine sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488

Vinflunine Cat No HY-B0628

Vinflunine Tartrate Cat No HY-B0628A

Vinorelbine (KW-2307 base) Cat No HY-12053

Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A

wwwMedChemExpresscom 101

Mps1Monopolar spindle 1

Monopolar spindle 1 (Mps1) also known as TTK is a serine threoninekinase which ensures proper biorientation of sister chromatids on themitotic spindle by the activation of the spindle assembly checkpoint(SAC) Mps1 has been shown to function as the key kinase thatactivates the spindle assembly checkpoint (SAC) to secure properdistribution of chromosomes to daughter cellsMps1 is a dual specificity protein kinase that is essential for thebipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomesare properly attached Mps1 is expressed at high levels during mitosisand is abundantly expressed in cancer cells Disruption of Mps1

function induces aneuploidy and cell death

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Mps1 Inhibitors amp Modulators

Bioactivity AZ3146 is a reasonably potent and selective inhibitorMps1with of 35 nM for Mps1 IC50

CatBioactivity BAY 1217389 is a potent and selective inhibitor of the

monopolar spindle 1 ( ) kinase with an value lessMPS1 IC50than 10 nM

Bioactivity BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1)checkpoint with an of 2 nMIC50

Bioactivity CCT251455 is a potent and selective mitotic kinase monopolarspindle 1 ( ) inhibitor with an of 3 nMMPS1 IC50

Bioactivity CFI-402257 is a highly selective and orally bioavailable inhibitor with an of 17 nM for TTK in vitroTTKMps1 IC50

CFI-402257 has anti-cancer activity [1]

Bioactivity CFI-402257 hydrochloride is a highly selective and orallybioavailable inhibitor with an of 17 nM forTTKMps1 IC50TTK in vitro CFI-402257 hydrochloride has anti-canceractivity [1]

Bioactivity Empesertib (BAY 1161909) is a potent inhibitor withMps1an of lt 1 nMIC50

Bioactivity MPI-0479605 is a potent and selective ATP-competitiveinhibitor of with an of 18 nMMps1 IC50

Bioactivity Mps1-IN-1 is a potent selective and ATP-competitive Mps1kinase inhibitor with an and a of 367 nM and 27 nMIC50 Kd

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

102 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

AZ3146 Cat No HY-14710

BAY1217389 Cat No HY-12859

BOS-172722 Cat No HY-112162

CCT251455 Cat No HY-12603

CFI-402257 Cat No HY-101340

CFI-402257 hydrochloride Cat No HY-101340A

Empesertib (BAY 1161909) Cat No HY-12858

MPI-0479605 Cat No HY-12660

Mps1-IN-1 Cat No HY-13298

Mps1-IN-2 Cat No HY-13994

wwwMedChemExpresscom 103

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-3 is a potent and selective kinase inhibitorMPS1with an of 50 nMIC50

Bioactivity NMS-P715 is a selective ATP-competitive inhibitor of MPS1with an of 182 nMIC50

Bioactivity NMS-P715 analog is an inhibitor of with an of 84MPS1 IC50nM

Mps1-IN-3 Cat No HY-12401

NMS-P715 Cat No HY-12382

NMS-P715 analog Cat No HY-14712

Nucleoside AntimetaboliteAnalog

Nucleoside analogues are molecules that act like nucleosides in DNAsynthesis They include a range of antiviral products used to preventviral replication in infected cells Nucleoside analogues can be usedagainst hepatitis B virus hepatitis C virus herpes simplex and HIVOnce they are phosphorylated they work as antimetabolites by beingsimilar enough to nucleotidesto be incorporated into growing DNAstrands Less selective nucleoside analogues are used aschemotherapy agents to treat cancer eg gemcitabine and 5-FUAntimetabolite is a chemical that inhibits the use of a metabolitewhich is another chemical that is part of normal metabolism Suchsubstances are often similar in structure to the metabolite that they

interfere with such as the antifolates that interfere with the use of folic acid The presence of antimetabolites can havetoxic effects on cells such as halting cell growth and cell division so these compounds are used as chemotherapy forcancer

104 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 105

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Nucleoside AntimetaboliteAnalog Inhibitors amp Modulators

Bioactivity 1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is abicyclic nucleoside

Bioactivity 1-Methylcytosine is a methylated form of the DNA base cytosineand used as a nucleobase of hachimoji DNA in which it pairswith Isoguanine [1] [2]

Bioactivity 1-Methylinosine is a modified nucleotide found at position 37in tRNA 3 to the anticodon of eukaryotic tRNA [1]

Bioactivity 2-Deoxypseudoisocytidine is a nucleoside analogue

Bioactivity 2rsquo-O4rsquo-C-Methyleneuridine (Compound 15a) is a bicyclicnucleoside

Bioactivity 3-Azido-3-deoxy-5-fluorocytidine (Compound 12) is a cytidinederivative

Bioactivity 3-Azido-3-deoxy-beta-L-uridine (Compound 25) is a nucleosidederivative

Bioactivity 3-Methylcytidine a urinary nucleoside can be used as abiomarker of four different types of cancer lung cancergastric cancer colon cancer and breast cancer [1]

Bioactivity 5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methyluridine is a derivative of LNA-type nucleoside

Bioactivity 5-Aza-7-deazaguanine is a substrate for wild-type (WT) E coli and its Ser90Ala mutant in thepurine nucleoside phosphorylase

synthesis of base-modified nucleosides [1]

1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine Cat No HY-111638

1-Methylcytosine Cat No HY-W006395

1-Methylinosine (N1-Methylinosine) Cat No HY-113139

2-Deoxypseudoisocytidine Cat No HY-101968

2rsquo-O4rsquo-C-Methyleneuridine Cat No HY-111639

3-Azido-3-deoxy-5-fluorocytidine Cat No HY-111641

3-Azido-3-deoxy-beta-L-uridine Cat No HY-111642

3-Methylcytidine Cat No HY-111645

5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methylurid

ine

Cat No HY-111807

5-Aza-7-deazaguanine Cat No HY-111627

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9874Clinical Data Phase 4Size 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 960Clinical Data LaunchedSize 50 mg 100 mg 500 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in Water

50 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Bioactivity 5-Azacytidine is a nucleoside analogue of cytidine thatspecifically inhibits DNA methylation by trapping DNA

methyltransferases

Bioactivity 5-BrdU is a nucleoside analog that competes with thymidine forincorporation into DNA 5-BrdU is commonly used in thedetection of proliferating cells

Bioactivity 5-Fluorouracil is a potent antitumor agent that affectspyrimidine synthesis by inhibiting thymidylate synthetasethus depleting intracellular dTTP pools

Bioactivity 6-Amino-5-nitropyridin-2-one is a pyridine base and used as anucleobase of hachimoji DNA in which it pairs with5-aza-7-deazaguanine [1]

Bioactivity 6-Mercaptopurine is a purine analogue which acts as anantagonist of the and has been widely usedendogenous purinesas antileukemic agent and immunosuppressive drug

Bioactivity 6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MPhydrate) is a purine analogue which acts as an antagonist ofthe and has been widely used asendogenous purinesantileukemic agent and immunosuppressive drug

Bioactivity 6-O-Methyl Guanosine is a modified nucleoside 6-O-Methyl[1]

Guanosine (6-methylguanosine) inhibit colony-forming abilityin a malignant xeroderma pigmentosum cell line [2]

Bioactivity 7-Methylguanosine is a novel cNIIIB nucleotidase inhibitorwith IC value of 878 plusmn 75 microM50

Bioactivity 8-Azaguanine is a purine analogue which shows antineoplasticactivity

Bioactivity Adenosine is a nucleoside composed of a molecule of adenineattached to a ribose sugar molecule (ribofuranose) moiety viaa β-N9-glycosidic bond Target Nucleosideantimetaboliteanalog Adenosine plays an important role inbiochemical processes such as energy transfer mdash as adenosinehellip

106 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

5-Azacytidine (Ladakamycin 5-AzaC Azacitidine) Cat No HY-10586

5-BrdU (BUdR BRDU) Cat No HY-15910

5-Fluorouracil (5-FU) Cat No HY-90006

6-Amino-5-nitropyridin-2-one Cat No HY-50071

6-Mercaptopurine (Mercaptopurine 6-MP) Cat No HY-13677

6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MP hydrate) Cat No HY-13677A

6-O-Methyl Guanosine Cat No HY-111648

7-Methylguanosine Cat No HY-122524

8-Azaguanine Cat No HY-B1468

Adenosine (Adenine riboside D-Adenosine) Cat No HY-B0228

wwwMedChemExpresscom 107

Purity 9818Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 1 g

Purity 9897Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carmofur is a derivative of fluorouracil an antimetaboliteused as an antineoplastic agent

Bioactivity Clofarabine(Clolar Clofarex) inhibits the enzymaticactivities of ribonucleotide reductase (IC50 = 65 nM) and DNApolymerase IC50 Value 65 nM Target in vitro Clofarabine isa second generation purine nucleoside analog withantineoplastic activity It is phosphorylated intracellularlyhellip

Bioactivity CNDAC is a major metabolite of oral drug sapacitabine and anucleoside analog

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Cytidine is a nucleoside molecule that is formed when cytosineis attached to a ribose ring cytidine is a component of RNATarget Nucleoside antimetaboliteanalog Cytidine is anucleoside molecule that is formed when cytosine is attachedto a ribose ring (also known as a ribofuranose) via ahellip

Bioactivity Dacarbazine(DTIC-Dome DTIC) is an antineoplastic agent Ithas significant activity against melanomas Target Nucleosideantimetaboliteanalog Approved May 1975 Dacarbazine (DTIC) isthe only single-agent approved by the Food and DrugAdministration for treating metastatic melanoma With DTIC ashellip

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Deoxypseudouridine is a nucleotide analog

Capecitabine Cat No HY-B0016

Carmofur (HCFU) Cat No HY-B0182

Clofarabine Cat No HY-A0005

CNDAC Cat No HY-16445A

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Cytidine (Cytosine β-D-riboside Cytosine-1-β-D-ribofuranoside) Cat No HY-B0158

Dacarbazine (Imidazole Carboxamide) Cat No HY-B0078

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Deoxypseudouridine Cat No HY-101970

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in Water

1000u g 2500u g 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 2500u g 5 mg 10 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 50 mg

Bioactivity DMTr-LNA-5MeU-3-CED-phosphoramidite is a nucleoside derivative[1]

Bioactivity Doxifluridine is a thymidine phosphorylase activator forPC9-DPE2 cells with IC50 of 062 μM

Bioactivity Ethynylcytidine is a new nucleoside antimetabolite Bioactivity Floxuridine (5-fluorodeoxyuridine) is an oncology drug thatbelongs to the class known as antimetabolites with an GI50 of51 μM for the inhibition of PEPT1 IC50 value TargetNucleoside antimetaboliteanalog Floxuridine (Fludara) is aprodrug of floxuridine and an oncology agent with an GI50 ofhellip

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

Bioactivity Fludarabine (phosphate) is an analogue of adenosine anddeoxyadenosine which is able to compete with dATP forincorporation into DNA and inhibit DNA synthesis

Bioactivity Forodesine(BCX-1777 freebase Immucillin-H) is an orallybioavailable PNP inhibitor with picomolar potency inducesapoptosis mainly in T cells

Bioactivity Forodesine hydrochloride is a potent and oral purine nucleoside inhibitor with s ranging from 048 tophosphorylase (PNP) IC50

157 nM

Bioactivity Fosteabine is an oral and prodrug analogue of cytarabine whichis resistant to deoxycytidine deaminase

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

108 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

DMTr-LNA-5MeU-3-CED-phosphoramidite Cat No HY-111531

Doxifluridine (Ro 21-9738 5-Fluoro-5-deoxyuridine 5-DFUR) Cat No HY-B0021

Ethynylcytidine (ECyD TAS-106 3-C-Ethynylcytidine) Cat No HY-16200

Floxuridine (5-Fluorouracil 2-deoxyriboside) Cat No HY-B0097

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Fludarabine phosphate (NSC 118218 (phosphate)) Cat No HY-B0028

Forodesine (BCX-1777 freebase Immucillin-H) Cat No HY-16210

Forodesine hydrochloride (BCX-1777 Immucillin-H hydrochloride) Cat No HY-16209

Fosteabine (Cytarabine ocfosfate YNK 01) Cat No HY-106349

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

wwwMedChemExpresscom 109

Purity 9575Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 9971Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9829Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Gemcitabine elaidate(CP-4126 CO-101) is a lipophilicunsaturated fatty acid ester derivative of gemcitabine (dFdC)an antimetabolite deoxynucleoside analogue with potentialantineoplastic activity IC50 value Target Gemcitabineanalog Upon hydrolysis intracellularly by esterases thehellip

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity Isocytosine is a non-natural nucleobase and an isomer ofcytosine It is used in combination with Isoguanine in studiesof unnatural nucleic acid analogues of the normal base pairsin DNA and used as a nucleobase of hachimoji RNA [1] [2]

Bioactivity Isoguanine is a purine base that is an isomer of guanine Abuilding block in organic synthesis

Bioactivity LY2334737 is an orally available prodrug of gemcitabine whichis a nucleoside analog used as chemotherapy

Bioactivity N2-methylguanosine is a modified nucleoside that occurs atseveral specific locations in many tRNAs

Bioactivity N6N6-Dimethyladenosine is a modified ribonucleosidepreviously found in rRNA and also exhibits in mycobacteriumbovis Bacille Calmette-Gueacuterin tRNA [1]

Bioactivity N6-Etheno 2-deoxyadenosine is a reactive oxygen species(ROS)reactive nitrogen species (RNS)-induced DNA oxidationproduct used as a biomarker to evaluate chronic inflammationand lipid peroxidation in animal or human tissues [1]

Bioactivity Nelarabine (Arranon 506U78) is a purine nucleoside analog andDNA synthesis inhibitor with IC50 from 0067-215 μM in tumorcells Nelarabine is a chemotherapy drug used in T-cell acutelymphoblastic leukemia

Bioactivity Orotic acid (OA) is an intermediate in pyrimidine metabolismIC50 Value Target Nucleoside antimetaboliteanalog in vitroOA increases cell proliferation and decreases apoptosis inserum-starved SK-Hep1 hepatocellular carcinoma cells whichmay ascribe to the inhibition of AMP-activated protein kinasehellip

Gemcitabine elaidate (CP-4126 CO-101 Gemcitabine 5-elaidate) Cat No HY-13538

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

Isocytosine Cat No HY-W002272

Isoguanine Cat No HY-124143

LY2334737 Cat No HY-13672

N2-Methylguanosine Cat No HY-111647

N6N6-Dimethyladenosine Cat No HY-101984

N6-Etheno 2-deoxyadenosine Cat No HY-111646

Nelarabine (506U78 GW 506U78 Nelzarabine) Cat No HY-13701

Orotic acid (6-Carboxyuracil Vitamin B13) Cat No HY-N0157

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9972Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9783Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9887Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9745Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity Pseudothymidine is a C-nucleoside analog of thymidine Bioactivity Raltitrexed is an antimetabolite drug used in chemotherapyacting by inhibiting thymidylate synthase

Bioactivity RX-3117(TV-1360 Fluorocyclopentenylcytosine) is novel acytidine analog shows anticancer activity in several cancercell lines including gemcitabine-resistant variants

Bioactivity Sapacitabine is an orally available prodrugnucleoside analogthat is structurally related to cytarabine

Bioactivity Tegafur (FT 207 NSC 148958) is a chemotherapeutic 5-FUprodrug used in the treatment of cancers is a component oftegafur-uracil

Bioactivity Tipiracil is a thymidine phosphorylase ( ) inhibitorTPase

Bioactivity Tipiracil (hydrochloride) is a thymidine phosphorylaseinhibitor (TPI) used for cancer research

Bioactivity Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT)is an irreversible inhibitor andthymidylate synthasethereby suppresses Trifluridine is an antiviralDNA synthesisdrug for infectionherpes simplex virus (HSV)

Bioactivity Trifluridine-tipiracil hydrochloride mixture (TAS-102) is anovel oral combination drug that consists of an antineoplasticthymidine-based nucleoside analog trifluorothymidine and apotent inhibitor tipiracil in athymidine phosphorylase105 molar ratio

Bioactivity Vidarabine (Ara-A) an antiviral drug which is active againstherpes simplex and varicella zoster viruses

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Pseudothymidine (5-Methyl-2-Deoxypseudouridin) Cat No HY-101969

Raltitrexed (ZD1694 D1694 ICI-D1694) Cat No HY-10821

RX-3117 (TV-1360 fluorocyclopentenylcytosine) Cat No HY-15228

Sapacitabine (CS682 CYC682) Cat No HY-16445

Tegafur (FT 207NSC 148958) Cat No HY-17400

Tipiracil Cat No HY-A0063A

Tipiracil hydrochloride Cat No HY-A0063

Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT) Cat No HY-A0061

Trifluridinetipiracil hydrochloride mixture (TAS-102) Cat No HY-16478

Vidarabine (Ara-A Adenine Arabinoside

9-β-D-Arabinofuranosyladenine) Cat No HY-B0277

wwwMedChemExpresscom 111

p97VCPCdc48

p97 an abundant hexameric ATPase of the AAA family is involved inhomotypic membrane fusion It is thought to disassemble SNAREcomplexes formed during the process of membrane fusion Twostructures have been reported a crystal structure of the N-terminaland D1 ATPase domains of murine p97 at 29 A resolution and acryoelectron microscopy structure of full-length rat p97 at 18 Aresolution Together these structures show that the D1 and D2hexamers pack in a tail-to-tail arrangement and that the N domain isflexible A comparison with NSF D2 (ATP complex) reveals possibleconformational changes induced by ATP hydrolysis

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9765Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

p97 Inhibitors amp Modulators

Bioactivity CB-5083 is a potent selective and orally bioavailable p97inhibitor with an value of 11 nMIC50

Bioactivity DBeQ is a selective potent reversible and ATP-competitive inhibitor with an value of 15 μM and 16 μM forp97 IC50

p97(wt) and p97(C522A) respectively DBeQ also inhibits Vps4with an of 115 μMIC50

Bioactivity ML240 is a potent inhibitor inhibiting p97 ATPase withp97 value of 100 nMIC50

Bioactivity ML241 hydrochloride is a potent inhibitor inhibiting p97p97ATPase with value of 100 nMIC50

Bioactivity NMS-859 is a potent covalent inhibitor withVCP (p97)s of 037 and 036 μM for wild-type VCP in the presence ofIC50

60 μM and 1 mM ATP in cells respectively

Bioactivity NMS-873 is a potent selective allosteric inhibitorVCPp97with value of 30 nMIC50

112 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CB-5083 Cat No HY-12861

DBeQ (JRF 12) Cat No HY-15945

ML240 Cat No HY-19795

ML241 hydrochloride Cat No HY-19797A

NMS-859 Cat No HY-15714

NMS-873 Cat No HY-15713

wwwMedChemExpresscom 113

PAKp21 activated kinases

PAKs (p21-activated kinases) are key regulators of actin dynamics cellproliferation and cell survival PAKs are SerThr kinases that areclassified into two groups on the basis of their structural andfunctional features group I (PAK1ndash3) and group II (PAK4ndash6) Group IPAKs have an auto-inhibitory domain (also called an inhibitory switchdomain) and a kinase domain (catalytic domain CD) and are activatedby the binding of the active (that is GTP-bound) forms of RhoGTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPasesBecause the deregulation of PAKs is closely associated with varioushuman diseasessmall-molecule inhibitors of these kinases have great

potential as therapeutic agents In addition these compounds can also be used as powerful tools in studies aimed atunderstanding the PAK signaling pathwayPAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actinremodelling and their ability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role intumor cell invasion and metastasis The current evidence suggests the involvement of PAKs in motility cell survivalanchorage-independent growth angiogenesis invasion migration and regulation of cell cycle and mitosisConsequently PAKs have also been implicated in a number of pathological conditions including cancer

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9902Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 1 g 5 g

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

PAK Inhibitors amp Modulators

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Fingolimod is a ( ) antagonistsphingosine 1-phosphate S1Pwith of 0033 nM in K562 and NK cells Fingolimod also isIC50a activatorpak1

Bioactivity Fingolimod hydrochloride is a ( )sphingosine 1-phosphate S1Pantagonist with an of 0033 nM in K562 and NK cellsIC50Fingolimod hydrochloride also is a activatorpak1

Bioactivity FRAX1036 is a inhibitor with s of 233 nM 724 nM andPAK Ki24 μM for PAK1 PAK2 and PAK4 respectively

Bioactivity FRAX486 is a p21-activated kinase ( ) inhibitor with sPAK IC50of 14 33 and 39 nM for PAK1 PAK2 and PAK3 respectively

Bioactivity FRAX597 is a potent group I p21-activated Kinases ( s)PAKinhibitor with of 8 13 and 19 nM for and IC50 PAK1 2 3

Bioactivity G-5555 is a potent p21-activated kinase 1 ( ) inhibitorPAK1with s of 37 nM and 11 nM for PAK1 and PAK2 respectivelyKi

Bioactivity G-5555 hydrochloride is a potent and selective p21-activatedkinase 1 ( ) inhibitor with a of 37 nMPAK1 Ki

Bioactivity IPA-3 is a selective non-ATP competitive inhibitor withPAK1 of 25 μM and shows no inhibition to group II PAKs (PAKsIC50

4-6)

Bioactivity NVS-PAK1-1 is a potent and selective allosteric PAK1inhibitor with an of 5 nMIC50

114 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Fingolimod (FTY720 free base) Cat No HY-11063

Fingolimod hydrochloride (FTY720) Cat No HY-12005

FRAX1036 Cat No HY-19538

FRAX486 Cat No HY-15542B

FRAX597 Cat No HY-15542A

G-5555 Cat No HY-19635

G-5555 hydrochloride Cat No HY-19635A

IPA-3 Cat No HY-15663

NVS-PAK1-1 Cat No HY-100519

wwwMedChemExpresscom 115

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity PAK-IN-1 is a inhibitor that displays group IIPAKselectivity PAK-IN-1 inhibits PAK4 PAK5 and PAK6 with sIC50of 75 36 126 nM respectively

Bioactivity PF-3758309 is an inhbitor of with of 13 nM forPAK IC50PAK4

PAK-IN-1 Cat No HY-12632

PF-3758309 Cat No HY-13007

PARPpoly ADP ribose polymerase

PARP is a family of proteins involved in a number of cellular processesinvolving mainly DNA repair and programmed cell death The PARPfamily comprises 17 members They have all very different structuresand functions in the cell PARP1 PARP2 VPARP (PARP4) Tankyrase-1and -2 (PARP-5a or TNKS and PARP-5b or TNKS2) have a confirmedPARP activity Others include PARP3 PARP6 TIPARP (or PARP7)PARP8 PARP9 PARP10 PARP11 PARP12 PARP14 PARP15 andPARP16 PARP is found in the cellrsquos nucleus The main role is to detectand signal single-strand DNA breaks (SSB) to the enzymaticmachinery involved in the SSB repair

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wwwMedChemExpresscom 117

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9839Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in Water

200 mg 500 mg

PARP Inhibitors amp Modulators

Bioactivity 3-Aminobenzamide is a potent inhibitor of with of appr 50 nM in CHO cellsPARP IC50

and acts as a mediator of oxidant-induced myocyte dysfunctionduring reperfusion

Bioactivity A-966492 is a novel and potent inhibitor of and with of 1 nM andPARP1 PARP2 Ki

15 nM respectively

Bioactivity AG14361 is a potent inhibitor with a of lt 5 nMPARP-1 Kiand in permeabilized SW620 and intact SW620 cells the sIC50are 29 nM and 14 nM respectively

Bioactivity AZ6102 is a potent dual and inhibitor withTNKS1 TNKS2s of 3 nM and 1 nM respectively and alao has 100-foldIC50

selectivity against other PARP family enzymes with s ofIC5020 μM 05 μM and gt3 μM for PARP1 PARP2 and PARhellip

Bioactivity AZD-2461 is a potent inhibitor with s of 5 nM 2 nMPARP IC50and 200 nM for PARP1 PARP2 and PARP3 respectively

Bioactivity BGP-15 is a inhibitor with an and a of 120 andPARP IC50 Ki57 μM respectively

Bioactivity BRCA1-IN-1 is a novel small-molecule-like inhibitorBRCA1with and of 053 μM and 071 μM respecrivelyIC50 Ki

Bioactivity Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolatedfrom traditional Chinese herb WT WangCorydalis yanhusuoDehydrocorydaline regulates protein expression of Bax Bcl-2activates and inactivates caspase-7 caspase-8 PARP

Bioactivity E7449 is a potent and inhibitor and alsoPARP1 PARP2inhibits and with s of 20 10 50 andTNKS1 TNKS2 IC5050 nM for PARP1 PARP2 TNKS1 and TNKS2 respectively using

P-NAD as substrate32 +

Bioactivity G007-LK is a potent and selective inhibitor of andTNKS1 with s of 46 nM and 25 nM respectivelyTNKS2 IC50

3-Aminobenzamide (PARP-IN-1) Cat No HY-12022

A-966492 Cat No HY-10614

AG14361 Cat No HY-12032

AZ6102 Cat No HY-12975

AZD-2461 Cat No HY-13536

BGP-15 Cat No HY-100828

BRCA1-IN-1 Cat No HY-100863

Dehydrocorydaline (13-Methylpalmatine) Cat No HY-N0674

E7449 Cat No HY-12418

G007-LK Cat No HY-12438

Purity 9952Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Bioactivity GeA-69 is a selective highly cell permeable allostericinhibitor of poly-adenosine-diphosphate-ribose polymerase 14

targeting macrodomain 2 with a of 21 microM (PARP14) Kd[1]

Bioactivity Iniparib (BSI-201) is an irreversible inhibitor of PARP1used in the research of triple negative breast cancer

Bioactivity JW 55 is a potent and selective signaling pathwayβ-catenininhibitor which functions via inhibition of the PARP domainof tankyrase 1 and tankyrase 2 (TNKS12) JW 55 decreasesauto-PARsylation of TNKS12 in vitro with s of 19 μM andIC50830 nM respectively

Bioactivity K-756 is a direct and selective ( ) inhibitortankyrase TNKSwhich inhibits the ADP-ribosylation activity of andTNKS1

with s of 31 and 36 nM respectivelyTNKS2 IC50

Bioactivity ME0328 is a potent and selective inhibitor withARTD3 PARP3an of 089plusmn028 μMIC50

Bioactivity MN-64 is a potent inhibitor with s of 6 nMtankyrase 1 IC5072 nM 191 μM and 394 μM for TNKS2 ARTD1 andTNKS1ARTD2 respectively

Bioactivity Niraparib (MK-4827) is a highly potent and PARP1 PARP2inhibitor with s of 38 and 21 nM respectivelyIC50

Bioactivity Niraparib hydrochloride (MK-4827 hydrochloride) is anexcellent and inhibitor with of 38 and 21PARP1 PARP2 IC50nM respectively

Bioactivity Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent inhibitor with of 24 nMPARP1 IC50

Bioactivity Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1and inhibitor with an of 38 and 21 nMPARP2 IC50respectively

118 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

GeA-69 Cat No HY-108708

Iniparib (BSI-201 NSC-746045 IND-71677) Cat No HY-12015

JW 55 Cat No HY-13968

K-756 Cat No HY-U00422

ME0328 Cat No HY-100225

MN-64 Cat No HY-19351

Niraparib (MK-4827) Cat No HY-10619

Niraparib hydrochloride (MK-4827 (hydrochloride)) Cat No HY-10619A

Niraparib R-enantiomer (MK 4827 (R-enantiomer)) Cat No HY-10619D

Niraparib tosylate (MK-4827 (tosylate)) Cat No HY-10619B

wwwMedChemExpresscom 119

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg

Purity 9768Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2 g

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NMS-P118 is a potent orally available and highly selective Inhibitor for cancer therapyPARP-1

Bioactivity NMS-P515 is a potent and stereospecific inhibitorPARP-1with an of 27 nM in hela cells Anti-tumor activity IC50

[1]

Bioactivity NVP-TNKS656 is a highly potent selective and orally active inhibitor with of 6 nM and is gt 300 foldTNKS2 IC50

selectivity against and PARP1 PARP2

Bioactivity Olaparib (AZD2281KU0059436) is a potent and oral PARPinhibitor with s of 5 and 1 nM for and IC50 PARP1 PARP2

respectively

Bioactivity Pamiparib is a inhibitor which can be used for thePARPtreatment of various cancers including the solid tumorextracted from patent WO 2013097225 A1

Bioactivity PARP-2-IN-1 is a potent and selective inhibitor withPARP-2an of 115 nMIC50

Bioactivity PJ34 is a potent specific inhibitor of with ofPARPl 2 IC50110 nM and 86 nM respectively

Bioactivity PJ34 hydrochloride is an inhibitor of with of 110PARPl12 IC50nM and 86 nM respectively

Bioactivity PROTAC PARP1 degrader is a degrader based on thePARP1 technology It induces significant PARP1 cleavage andPROTAC

programmed cell death PROTAC PARP1 degrader at 10 μM at 24 hinhibits MDA-MB-231 cell line with an of 612 μMIC50

Bioactivity RK-287107 is a potent and specific inhibitor withtankyrases of 143 and 106 nM for and IC50 tankyrase-1 tankyrase-2

respectively RK-287107 blocks colorectal cancer cell growth[1]

NMS-P118 Cat No HY-18954

NMS-P515 Cat No HY-128599

NVP-TNKS656 (TNKS656) Cat No HY-13990

Olaparib (AZD2281 KU0059436) Cat No HY-10162

Pamiparib (BGB-290) Cat No HY-104044

PARP-2-IN-1 Cat No HY-102035

PJ34 Cat No HY-13688A

PJ34 hydrochloride Cat No HY-13688

PROTAC PARP1 degrader Cat No HY-114324

RK-287107 Cat No HY-123892

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9962Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9888Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9508Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9983Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9989Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9981Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity Rucaparib (AG014699) is an inhibitor of with of 14 nM for PARP1 in aPARP Ki

cell-free assay and also shows binding affinity to eightother PARP domains

Bioactivity Rucaparib Camsylate is an inhibitor of with a of 14PARP KinM for PARP1 and also shows binding affinity to eight otherPARP domains

Bioactivity Rucaparib phosphate (AG-014699 phosphate) is a potent and oral inhibitor with a of 14 nM for PARP1 in cell-freePARP Ki

assay also showing binding affinity to eight other PARPdomains

Bioactivity Talazoparib (BMN-673) is a highly potent inhibitorPARP12with s of 12 nM and 087 nM respectivelyKi

Bioactivity Talazoparib 8R9S (BMN-673 8R9S) is an enantiomer ofTalazoparib less active than Talazoparib on the inhibition of

with an of 144 nMPARP1 IC50

Bioactivity Talazoparib tosylate (BMN 673ts) is a novel potent and orallyavailable inhibitor with an of 057 nM forPARP12 IC50PARP1

Bioactivity UPF 1069 is a inhibitor with s of 8 and 03 μM forPARP IC50PARP-1 and PARP-2 respectively

Bioactivity Veliparib is a potent inhibitor inhibiting andPARP PARP1 with s of 52 and 29 nM respectivelyPARP2 Ki

Bioactivity Veliparib (dihydrochloride) is a potent inhibitor of and with s of 52PARP1 PARP2 Ki

nM and 29 nM in cell-free assays respectively

Bioactivity WD2000-012547 is a selective poly(ADP-ribose)-polymerase(PARP-1) inhibitor with a pK of 8221i

120 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Rucaparib (AG014699 PF-01367338) Cat No HY-10617A

Rucaparib Camsylate Cat No HY-102003

Rucaparib phosphate (AG-014699 phosphate PF-01367338 phosphate) Cat No HY-10617

Talazoparib (BMN-673 LT-673) Cat No HY-16106

Talazoparib 8R9S (BMN-673 (8R9S) (8R9S)-LT-673) Cat No HY-16106A

Talazoparib tosylate (BMN 673ts) Cat No HY-108413

UPF 1069 Cat No HY-14478

Veliparib (ABT-888) Cat No HY-10129

Veliparib dihydrochloride (ABT-888 dihydrochloride) Cat No HY-10130

WD2000-012547 Cat No HY-U00223

wwwMedChemExpresscom 121

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity XAV-939 is a inhibitor and an indirecttankyrase (TNKS)inhibitor of with s of 5 and 2Wntβ-catenin signaling IC50nM for TNKS1 and TNKS2 respectively

XAV-939 Cat No HY-15147

PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinase

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) isactivated in response to a variety of endoplasmic reticulum stressesimplicated in numerous disease states PERK is implicated intumorigenesis and cancer cell survival GSK2606414 is an orallyavailable potent and selective PERK inhibitor GSK2606414 inhibitsPERK activation in cells and inhibits the growth of a human tumorxenograft in mice PERK activation is independent of the largeincrease in unfolded nascent proteins within the ER followingtransient global brain ischemia

122 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 123

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

PERK Inhibitors amp Modulators

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity GSK2606414 is a cell-permeable and orally available proteinkinase R-like endoplasmic reticulum (ER) kinase (PERK)inhibitor with an of 04 nMIC50

Bioactivity GSK2656157 is a selective and ATP-competitive inhibitor ofprotein kinase R (PKR)-like endoplasmic reticulum kinase (

) with an of 09 nMPERK IC50

Bioactivity ISRIB (trans-isomer) is a potent inhibitor of with anPERK of 5 nMIC50

CCT020312 Cat No HY-119240

GSK2606414 Cat No HY-18072

GSK2656157 Cat No HY-13820

ISRIB trans-isomer Cat No HY-12495

Polo-like Kinase (PLK)

Polo-like Kinases (PLKs) are important regulators of the cell cycle Plksare involved in the formation of and the changes in the mitoticspindle and in the activation of CDKcyclin complexes duringM-phase of the cell cyclePolo-like kinases (Plks) are a family ofconserved serinethreonine kinases involved in the regulation of cellcycle progression through G2 and mitosis Mammalian polo-likekinases include Plk1 (Xenopus Plx1) Plk2Snk (Xenopus Plx2)Plk3PrkFnK (Xenopus Plx3) Plk4Sak and Plk5 Plk1 is involved in theregulation of key steps during cell division DNA damage repairpathways apoptosis and the progression of the cell cycle Plk3 is amultifunctional stress response protein that responses to signals

induced by DNA damage andor mitotic spindle disruption

124 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 125

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9982Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9897Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9857Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Polo-like Kinase (PLK) Inhibitors amp Modulators

Bioactivity BI 2536 is a dual and inhibitor with s of 083PLK1 BRD4 IC50

and 25 nM respectively BI-2536 suppresses IFNB[1]

(encoding IFN-β) gene transcription [4]

Bioactivity Centrinone (LCR-263) is a selective and reversible inhibitorof polo-like kinase 4 ( ) with a of 016 nMPlK4 Ki

Bioactivity Centrinone-B (LCR-323) is a potent and highly selective PLK4inhibitor with a of 059 nMKi

Bioactivity CFI-400945 free base is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity CFI-400945 fumarate is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity GSK461364 is a selective reversible and ATP-competitive inhibitor with a value of 22 nMPolo-like kinase 1 (PLK1) Ki

Bioactivity GW843682X is a selective ATP-competitive inhibitor of PLK1and with s of 22 nM and 91 nM respectively andPLK3 IC50is also gt100-fold selective against 30 other kinases

Bioactivity HMN-214 an orally bioavailable prodrug of HMN-176 is aninhibitor of polo-like kinase-1 ( ) with antitumorplk1activity

Bioactivity LFM-A13 is a potent inhibitor inhibitsBTK JAK2 PLKrecombinant BTK Plx1 and PLK3 with s of 25 μM 10 μM andIC5061 μM LFM-A13 shows no effects on JAK1 and JAK3 Src familykinase HCK EGFR and IRK

Bioactivity MLN0905 is a potent inhibitor with an of 2 nMPLK1 IC50

BI 2536 Cat No HY-50698

Centrinone (LCR-263) Cat No HY-18682

Centrinone-B (LCR-323) Cat No HY-18683

CFI-400945 free base Cat No HY-12300

CFI-400945 fumarate Cat No HY-12300B

GSK461364 (GSK461364A) Cat No HY-50877

GW843682X (GW843682) Cat No HY-11003

HMN-214 (IVX-214) Cat No HY-12045

LFM-A13 Cat No HY-18009

MLN0905 (PLK1 Inhibitor) Cat No HY-15155

Purity 9759Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9949Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9809Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9626Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9970Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

Bioactivity NMS-1286937 is a potent selective and orally available PLK1inhibitor with an of 2 nMIC50

Bioactivity Poloxime a hydrolysis product of poloxin is anon-ATP-competitive inhibitor with moderate Plk1Plk1inhibitory activity

Bioactivity Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1)inhibitor that targets the polo-box domain with an ofIC50appr 48 μM

Bioactivity Rigosertib (ON-01910) is a multi-kinase inhibitor and aselective anti-cancer agent which induces apoptosis byinhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib is a selective andhellip[1] [2]

Bioactivity Rigosertib sodium (ON-01910 sodium) is a multi-kinaseinhibitor and a selective anti-cancer agent which inducesapoptosis by inhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib sodium is a selective andhellip[1] [2]

Bioactivity Ro3280 is a potent highly selective inhibitor of withPLK1an and a of 3 nM and 009 nM respectively andIC50 Kdnearly has no effect on PLK2 and PLK3

Bioactivity SBE13 is a potent and selective inhibitor with an ofPlk1 IC50200 pM SBE13 poorly inhibits Plk2 (IC gt66 μM) or Plk350(IC =875 nM)50

Bioactivity SBE13 Hydrochloride is a potent and selective inhibitorPlk1with an of 200 pM SBE13 Hydrochloride poorly inhibitsIC50Plk2 (IC gt66 μM) or Plk3 (IC =875 nM)50 50

Bioactivity TAK-960 is an orally available selective inhibitor of with an of 08 nM at 10 μMpolo-like kinase 1 (PLK1) IC50

ATP TAK-960 also shows inhibitory activities against PLK2and with s of 169 and 502 nM respectivelyPLK3 IC50

126 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Mps1-IN-2 Cat No HY-13994

NMS-1286937 (NMS-P937) Cat No HY-15828

Poloxime Cat No HY-77195

Poloxin Cat No HY-12134

Rigosertib (ON-01910) Cat No HY-12037A

Rigosertib sodium (ON-01910 sodium) Cat No HY-12037

Ro3280 Cat No HY-15161

SBE13 Cat No HY-15158A

SBE13 Hydrochloride Cat No HY-15158

TAK-960 Cat No HY-15160

wwwMedChemExpresscom 127

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9955Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TAK-960 dihydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 dihydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TAK-960 hydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 hydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TC-S 7005 is a inhibitor with s ofPolo-like kinases (Plks) IC504 nM 24 nM and 214 nM for Plk2 Plk3 and Plk1 respectively

[1]

Bioactivity Volasertib is a highly potent Polo-like kinase 1 (PLK1)inhibitor with an of 087 nM as well as the two closelyIC50related kinases and with s of 5 and 56 nMPLK2 PLK3 IC50respectively

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

TAK-960 dihydrochloride Cat No HY-15160B

TAK-960 hydrochloride Cat No HY-15160A

TC-S 7005 Cat No HY-108597

Volasertib (BI 6727) Cat No HY-12137

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

PPARPeroxisome proliferator-activated receptors

PPARs (Peroxisome proliferator-activated receptors) areligand-activated transcription factors of nuclear hormone receptorsuperfamily comprising of the following three subtypes PPARαPPARγ and PPARβδ PPARs play essential roles in the regulation ofcellular differentiation development and metabolism (carbohydratelipid protein) and tumorigenesis of higher organisms All PPARsheterodimerize with the retinoid X receptor (RXR) and bind to specificregions on the DNA of target genes Activation of PPAR-α reducestriglyceride level and is involved in regulation of energy homeostasisActivation of PPAR-γ enhances glucose metabolism whereasactivation of PPAR-βδ enhances fatty acids metabolism

128 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 129

Purity 9905Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9921Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 980Clinical Data Phase 4Size 50 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg

Purity gt98Clinical Data Phase 2Size 1 mg

Purity 9900Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

PPAR Inhibitors amp Modulators

Bioactivity 4-O-Methyl honokiol is a natural neolignan isolated from acts as a agonist and inhibtisMagnolia officinalis PPARγ

activity used for cancer and inflammation researchNF-κB

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Adelmidrol exerts important anti-inflammatory effects that arepartly dependent on Adelmidrol reduces PPARγ NF-κBtranslocation and expressionCOX-2

Bioactivity Aleglitazar(R1439 RO-0728804) is a new dual PPAR-αγ agonistwith IC50 of 28 nM46 nM

Bioactivity Arhalofenate (MBX 102) is a selective partial agonist ofperoxisome proliferator-activated receptor used for(PPAR)-γthe treatment of type 2 diabetes

Bioactivity Astaxanthin a red dietary carotenoid isolated from is an inhibitor of and aHaematococcus pluvialis PPARγ

potent antioxidant with antiproliferative neuroprotective andanti-inflammatory activity Astaxanthin has potential in[1]

the treatment of various diseases such as cancers andhellip

Bioactivity Astragalus polysaccharide are active components of thepolysaccharides extract of Astragulus attenuatesTNF-α-induced insulin resistance by suppressing miR-721 andactivating and in 3T3-L1 adipocytesPPAR-γ PI3KAkt

Bioactivity AVE-8134 is a potent agonist with values of 100PPARα EC50and 3000 nM for human and rodent PPARα receptor respectively

Bioactivity Balaglitazone is a selective partial agonist with anPPARγ of 1351 μM for human EC50 PPARγ

Bioactivity Bezafibrate is an agonist of with s of 50 μM 60PPAR EC50μM 20 μM for and and 90 μMhuman PPARα PPARγ PPARδ55 μM 110 μM for and murine PPARα PPARγ PPARδrespectively Bezafibrate is used as an hypolipidemic agent

4-O-Methyl honokiol Cat No HY-U00450

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Adelmidrol Cat No HY-B1026

Aleglitazar (R1439 RO0728804) Cat No HY-14728

Arhalofenate (MBX 102 JNJ 39659100) Cat No HY-14831

Astaxanthin Cat No HY-B2163

Astragalus polysaccharide (Astragalus Polysacharin) Cat No HY-N0937

AVE-8134 Cat No HY-U00014

Balaglitazone (DRF 2593 NN 2344) Cat No HY-16086

Bezafibrate (BM15075) Cat No HY-B0637

Purity 9877Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data Phase 4Size 10mM x 1mL in DMSO

500 mg 1 g 5 g 10 g

Purity 9959Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9981Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BMS-687453 is a potent and selective agonist with anPPARα and of 10 nM and 260 nM for human and 4100EC50 IC50 PPARα

nM and gt15000 nM for PPARγ in PPAR-GAL4 transactivationassays

Bioactivity CDDO-Im (CDDO-imidazolide) is an activator of and Nrf2 PPARwith s of 232 and 344 nM for PPARα and PPARγKi

Bioactivity Chiglitazar is a dual agonist with of 12PPARαγ EC s50008 17 μM for PPARα PPARγ and PPARδ respectively

Bioactivity Choline Fenofibrate (ABT-335) is the choline salt offenofibric acid under clinical development as a combinationtherapy with rosuvastatin for the management of dyslipidemia

Bioactivity Ciprofibrate is a peroxisome proliferator-activated receptoragonist

Bioactivity Ciprofibrate D6 is deuterium labeled Ciprofibrate which is aperoxisome proliferator-activated receptor agonist

Bioactivity Clofibrate is an agonist of with s of 50 μM 500PPAR EC50μM for murine PPARα and PPARγ and 55 μM 500 μM for humanPPARα and PPARγ respectively

Bioactivity Daidzein is a soy isoflavone which acts as a activatorPPAR

Bioactivity DG172 dihydrochloride is a selective antagonist withPPARβδan of 27 nMIC50

Bioactivity Elafibranor is a agonist with s of 45 and 175PPARαδ EC50nM respectively

130 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

BMS-687453 Cat No HY-10678

CDDO-Im (RTA-403 TP-235 CDDO-Imidazolide) Cat No HY-15725

Chiglitazar Cat No HY-106266

Choline Fenofibrate (ABT-335) Cat No HY-14739

Ciprofibrate (Win35833) Cat No HY-B0664

Ciprofibrate D6 Cat No HY-B0664S

Clofibrate Cat No HY-B0287

Daidzein Cat No HY-N0019

DG172 dihydrochloride Cat No HY-19737A

Elafibranor (GFT505) Cat No HY-16737

wwwMedChemExpresscom 131

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Ertiprotafib is an inhibitor of PTP1B IkB kinase β (IKK-β)and a dual agonist with an of 16 μMPPARα and PPARβ IC50for PTP1B 400 nM for IKK-β an of ~1 μM forEC50PPARαPPARβ

Bioactivity Eupatilin a lipophilic flavonoid isolated from Artemisiaspecies is a agonist and possesses anti-apoptoticPPARαanti-oxidative and anti-inflammatory activities

Bioactivity Fenofibrate is a agonist with an of 30 μMPPARα EC50 Bioactivity Fenofibric acid an active metabolite of fenofibrate is a activitor with s of 224 microM 147 microM and 106 microMPPAR EC50

for PPARα PPARγ and PPARδ respectively Fenofibric acid alsoinhibits enzyme activity with an of 48 nMCOX-2 IC50

Bioactivity FH535 is an inhibitor of and withWntβ-catenin PPARanti-tumor activities

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Fonadelpar is a agonist used in the research ofPPARδneuroparalytic keratopathy

Bioactivity Gemfibrozil is an activator of used as aPPAR-αlipid-lowering drug Gemfibrozil is also a nonselectiveinhibitor of several isoforms with values forP450 KiCYP2C9 2C19 2C8 and 1A2 of 58 24 69 and 82 μMrespectively

Bioactivity Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2Sanchinoside Rh1) is isolated from the root of Panax GinsengGinsenoside Rh1 inhibits the expression of PPAR-γ TNF-α

and IL-6 IL-1β

Bioactivity Glabridin is a natural isoflavan from bindsGlycyrrhiza glabrato and activates with an of 6115 nM GlabridinPPARγ EC50exhibits antioxidant anti-bacterial anti-nephriticanti-diabetic anti-fungal antitumor anti-inflammatoryantiosteoporotic cardiovascular protective neuroprotectivehellip

Ertiprotafib (PTP 112) Cat No HY-19383

Eupatilin Cat No HY-N0783

Fenofibrate Cat No HY-17356

Fenofibric acid (FNF acid) Cat No HY-B0760

FH535 Cat No HY-15721

Fisetin Cat No HY-N0182

Fonadelpar (NPS-005 SJP-0035) Cat No HY-17633

Gemfibrozil (CI-719) Cat No HY-B0258

Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2 Sanchinoside Rh1) Cat No HY-N0604

Glabridin Cat No HY-N0393

Purity 9875Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9727Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9667Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity GSK0660 is a potent antagonist of and withPPARβ PPARδs of 155 nM for both isoformsIC50

Bioactivity GSK376501A is a selective peroxisome proliferator-activatedreceptor gamma ( ) modulator for the treatment of type 2PPARγdiabetes mellitus

Bioactivity GSK3787 is a selective and irreversible peroxisomeproliferator-activated receptor δ ( ) antagonist withPPARδ

of 66pIC50

Bioactivity GW 501516 is a agonist with an of 11 nMPPARδ EC50

Bioactivity GW 6471 is a potent antagonistPPARα Bioactivity GW0742 is a potent and agonist with an ofPPARβ PPARδ IC501 nM for human in binding assay and s of 1 nMPPARδ EC5011 μM and 2 μM for human PPARα and PPARγPPARδrespectively

Bioactivity GW1929 is a potent agonist with a of 884 forPPAR-γ pKihuman and s of 856 and 827 for human PPAR-γ pEC50 PPAR-γ

and murine respectivelyPPAR-γ

Bioactivity GW7647 is a potent agonist with s of 6 nM 11PPARα EC50μM and 62 μM for human PPARα PPARγ and PPARδ respectively

Bioactivity GW9662 is a potent and selective antagonist with anPPARγ of 33 nM showing 10 and 1000-fold selectivity overIC50

PPARα and PPARδ respectively

Bioactivity Icariin is a flavonol glycoside Icariin inhibits andPDE5 activities with s of 432 nM and 7350 μMPDE4 IC50

respectively Icariin also is a activatorPPARα

132 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

GSK0660 Cat No HY-12377

GSK376501A Cat No HY-101746

GSK3787 Cat No HY-15577

GW 501516 (GW 1516 GSK-516) Cat No HY-10838

GW 6471 Cat No HY-15372

GW0742 (GW610742) Cat No HY-13928

GW1929 Cat No HY-15655

GW7647 Cat No HY-13861

GW9662 Cat No HY-16578

Icariin (Ieariline) Cat No HY-N0014

wwwMedChemExpresscom 133

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9889Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9921Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 2Size 5 mg

Purity 9942Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Bioactivity Imiglitazar (TAK559) is a potent and dual human andPPARα agonist with values of 67 and 31 nMPPARγ1 EC50

Bioactivity Indeglitazar is an orally available peroxisomeproliferator-activated receptor ( ) pan-agonist for allPPARthree PPAR subtypes alpha (α) delta (δ) and gamma (γ)

Bioactivity Inolitazone a novel high-affinity agonist that isPPARγdependent upon PPARγ for its biological activity with ofIC5008 nM for growth inhibition

Bioactivity Inolitazone dihydrochloride is a novel high-affinity PPARγagonist that is dependent upon PPARγ for its biologicalactivity with of 08 nM for growth inhibitionIC50

Bioactivity KD3010 is a potent orally active and selective PPARδagonist

Bioactivity L-165041 is a cell permeable agonist with s of 6 nMPPARδ Kiand appr 730 nM for PPARδ and PPARγ respectively and inducesadipocyte differentiation in NIH-PPARδ cells

Bioactivity Lanifibranor is a pan peroxisome proliferator-activated ( ) agonist with s of 15 087 and 021receptor PPAR EC50

μM for human and respectivelyPPARα PPARσ PPARγ

Bioactivity LJ570 is a dual agonist with s of 105PPARα PPARγ EC50

and 012 μM respectively [1]

Bioactivity MA-0204 is a potent highly selective and orally availableperoxisome proliferator activated receptor δ ( )PPARδmodulator with s of 04 nM 79 nM and 10 nM for humanEC50mouse and rat PPARδ respectively Potential treatment hellip

Bioactivity Magnolol a natural lignan isolated from the stem bark of is a dual agonist of both andMagnolia officinalis RXRα

with values of 104 microM and 177 microMPPARγ EC50respectively

Imiglitazar (TAK-559) Cat No HY-101649

Indeglitazar (PPM 204) Cat No HY-14817

Inolitazone (Efatutazone CS-7017 RS5444) Cat No HY-14792

Inolitazone dihydrochloride (Efatutazone (dihydrochloride)

CS-7017 (dihydrochloride) RS5444 (dihydrochloride)) Cat No HY-14792B

KD-3010 Cat No HY-111068

L-165041 Cat No HY-20019

Lanifibranor (IVA337) Cat No HY-104049

LJ570 Cat No HY-111775

MA-0204 Cat No HY-114739

Magnolol Cat No HY-N0163

Purity 9639Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9918Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in Ethanol

10 mg

Purity gt98Clinical DataSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9872Clinical Data Phase 1Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Bioactivity Naringenin is the predominant flavanone in grapefruitdisplays strong anti-inflammatory and antioxidant activities

Bioactivity Naveglitazar racemate is the racemate of NaveglitazarNaveglitazar is a nonthiozolidinedione peroxisomeproliferator-activated receptor ( ) α-γ dual γ-dominantPPARagonist that has shown glucose-lowering potential in animalmodels and in the clinic

Bioactivity NXT629 is a potent selective and competitive PPAR-αantagonist with an of 77 nM for human PPARα shows highIC50selectivity over other nuclear hormone receptor such asPPARδ PPARγ ERβ GR and TRβ s are 60 15 152 3hellipIC50

Bioactivity Oleoylethanolamide is a high affinity endogenous PPAR-αagonist which plays an important role in the treatment ofobesity and arteriosclerosis

Bioactivity Palmitelaidic acid is the trans isomer of palmitoleic acidPalmitoleic acid is one of the most abundant fatty acids inserum and tissue

Bioactivity Peliglitazar racemate is the racemate of PeliglitazarPeliglitazar is a novel dual αγ PPAR activator

Bioactivity Pemafibrate is a highly selective agonist with anPPARα of 1 nMEC50

Bioactivity Pemafibrate racemate is the racemate of pemafibrate andactivates activity with s of 1 nM gt10 μM andPPARα EC5017 μM for h-PPARα h-PPARγ and h-PPARδ respectively

Bioactivity Pioglitazone is a potent and selective agonist withPPARγhigh affinity binding to the PPARγ ligand-binding domain with

of 093 and 099 μM for human and mouse PPARγEC50respectively

Bioactivity Pioglitazone hydrochloride is a potent and selective PPARγagonist with s of 093 and 099 μM for human and mouseEC50PPARγ respectively

134 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Naringenin Cat No HY-N0100

Naveglitazar racemate Cat No HY-U00036

NXT629 Cat No HY-114263

Oleoylethanolamide (N-(2-Hydroxyethyl)oleamide

N-Oleoyl-2-aminoethanol N-Oleoylethanolamide hellip) Cat No HY-107542

Palmitelaidic Acid (9-trans-Hexadecenoic acid trans-Palmitoleic acid) Cat No HY-N2341

Peliglitazar racemate (BMS 426707-01 racemate) Cat No HY-101738A

Pemafibrate ((R)-K-13675) Cat No HY-17618

Pemafibrate racemate (K13675 (racemate)) Cat No HY-17618A

Pioglitazone (U 72107) Cat No HY-13956

Pioglitazone hydrochloride (U 72107A AD 4833) Cat No HY-14601

wwwMedChemExpresscom 135

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9836Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 250 mg

Bioactivity Pirinixic acid (Wy-14643) is a potent agonist of withPPARαs of 063 μM 32 μM for murine and PPARγ and 50EC50 PPARα

μM 60 μM 35 μM for human PPARγ and PPARδPPARαrespectively

Bioactivity PPAR agonist 1 is an agonist of and usedPPAR α PPAR γfor reducing blood glucose lipid levels lowering cholesteroland reducing body weight

Bioactivity PPARα-MO-1 is a potent modulator extracted from patentPPARαWO2004110982A1 formula I

Bioactivity PPARδ agonist is a agonist extracted from patentPPARδUS20180071304 compound example 10

Bioactivity Pparδ agonist 1 is a agonist with an of 506PPAR-δ EC50nM used in the research of PPAR-delta related diseases suchas mitochondrial diseases muscular diseases vasculardiseases demyelinating diseases and metabolic diseases

Bioactivity Pparδ agonist 2 is a agonist extracted from patent WOPPARδ2016057656 A1

Bioactivity Raspberry ketone is a major aromatic compound of redraspberry widely used as a fragrance in cosmetics and as aflavoring agent in foodstuff also shows agonisticPPAR-αactivity

Bioactivity Retinoic acid is a metabolite of vitamin A that playsimportant roles in cell growth differentiation andorganogenesis Retinoic acid is a natural agonist of RARnuclear receptors with s of 14 nM for RARαβγ RetinhellipIC50

Bioactivity RG-12525 is a a specific competitive and orally effectiveantagonist of the and peptidoleukotrienes LTC4 LTD4 LTE4inhibiting LTC4- LTD4- and LTE4-inducd guinea pig parenchymalstrips contractions with s of 26 nM 25 nM and 7 nMIC50respectively RG-12525 is also a peroxisomehellip

Bioactivity Rosiglitazone (BRL49653) is a selective agonist withPPARγs of 30 nM 100 nM and 60 nM for andEC50 PPARγ1 PPARγ2

respectivelyPPARγ

Pirinixic acid (Wy-14643) Cat No HY-16995

PPAR agonist 1 Cat No HY-U00340

PPARα-MO-1 Cat No HY-U00068

Pparδ agonist Cat No HY-112597

Pparδ agonist 1 Cat No HY-107901

Pparδ agonist 2 Cat No HY-100120

Raspberry ketone (Frambione 4-(4-Hydroxyphenyl)-2-butanone) Cat No HY-N1426

Retinoic acid (ATRA Tretinoin Vitamin A acid all-trans-Retinoic acid) Cat No HY-14649

RG-12525 (NID 525) Cat No HY-101676

Rosiglitazone (BRL49653) Cat No HY-17386

Purity 9953Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9852Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9885Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9803Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9925Clinical Data LaunchedSize 100 mg 500 mg

Bioactivity Rosiglitazone maleate is a potent and selective activator of with s of 30 nM 100 nM and 60 nM for PPARγ EC50 PPARγ1

and respectively and a of appr 40 nMPPARγ2 PPARγ Kdfor Rosiglitazone maleate is also an modulator of PPARγ hellip

Bioactivity Saroglitazar is a novel peroxisome proliferator-activatedreceptor ( ) agonist with predominant PPARα and moderatePPARPPARγ activity with values of 065 pM and 3 nM in HepG2EC50cells respectively

Bioactivity Saroglitazar magnesium is a novel peroxisomeproliferator-activated receptor ( ) agonist withPPARpredominant PPARα and moderate PPARγ activity with EC50values of 065 pM and 3 nM in HepG2 cells respectively

Bioactivity Seladelpar is an orally active potent (50 effectconcentration 2 nM) and specific agonistEC50 PPAR-δ

Bioactivity Seladelpar sodium salt (MBX-8025) is an orally active potentand specific agonist with an of 2 nM showingPPARδ EC50more than 750-fold and 2500-fold selectivity over the PPARαand PPARγ receptors respectively

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

Bioactivity Troglitazone is a agonist with s of 550 nM andPPARγ EC50780 nM for human and murinePPARγ receptor respectively

136 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Rosiglitazone maleate (BRL 49653C) Cat No HY-14600

Saroglitazar Cat No HY-19937

Saroglitazar Magnesium Cat No HY-19937A

Seladelpar (MBX-8025) Cat No HY-19522

Seladelpar sodium salt (MBX-8025 sodium salt RWJ-800025 sodium salt) Cat No HY-19522A

T0070907 Cat No HY-13202

Troglitazone (CS-045) Cat No HY-50935

wwwMedChemExpresscom 137

RAD51

RAD51 protein family assist in repair of DNA double strand breaksRAD51 family members are homologous to the bacterial RecA andyeast Rad51 In humans RAD51 is a 339-amino acid protein that playsa major role in homologous recombination of DNA during doublestrand break repair RAD51 is involved in the search for homologyand strand pairing stages of the process RAD51 can interact with thessDNA-binding protein RPA BRCA2 PALB2 and RAD52 Recentstudies using fluorescent labeled Rad5 has indicated that Rad51fragments elongate via multiple nucleation events followed bygrowth with the total fragment terminating when it reaches about 2μm in length

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

500 mg

RAD51 Inhibitors amp Modulators

Bioactivity Harmine is a natural dual-specificity tyrosinephosphorylation-regulated kinase ( ) inhibitor with(DYRK)anticancer and anti-inflammatory activities

Bioactivity IBR2 is a specific inhibitorRAD51

Bioactivity RAD51 Inhibitor B02 (B02) is an inhibitor of human withRAD51an of 274 μMIC50

Bioactivity RAD51-IN-2 (compound example 67A) is a inhibitorRAD51extracted from patent WO2019051465A1 [1]

Bioactivity RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM Bioactivity RI-2 is a reversible inhibitor with an of 4417RAD51 IC50μM and specifically inhibits homologous recombination repairin human cells

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

138 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Harmine (Telepathine) Cat No HY-N0737A

IBR2 Cat No HY-103710

RAD51 Inhibitor B02 (B02) Cat No HY-101462

RAD51-IN-2 Cat No HY-111887

RI-1 Cat No HY-15317

RI-2 Cat No HY-16904

RS-1 Cat No HY-19793

T0070907 Cat No HY-13202

wwwMedChemExpresscom 139

ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROK

ROCK (Rho-associated protein kinase) is a kinase belonging to theAGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopusinvertebrates and chicken Human ROCK1 has a molecular mass of158 kDa and is a major downstream effector of the small GTPaseRhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces thekinase activity of ROCKs by an autoinhibitory intramolecular fold ifRhoA-GTP is not present ROCK plays a role in a wide range ofdifferent cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators

of the cytoskeleton

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9954Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

ROCK Inhibitors amp Modulators

Bioactivity AT13148 is an orally active and ATP-competitive multi- AGC inhibitor with s of 38 nM402 nM50 nM 8 nM 3 nMkinase IC50

and 6 nM4 nM for Akt123 p70S6K PKA and ROCKIIIrespectively

Bioactivity Azaindole 1 is an orally active and ATP-competitive ROCKinhibitor with s of 06 and 11nM for human andIC50 ROCK-1

respectivelyROCK-2

Bioactivity BDP5290 is a potent inhibitor of both and withROCK MRCKs of 5 nM 50 nM 10 nM and 100 nM for IC50 ROCK1 ROCK2

and respectivelyMRCKα MRCKβ

Bioactivity Chroman 1 is a highly potent inhibitor with an ofROCK2 IC501 nM

Bioactivity Fasudil (HA-1077 AT877) a potent inhibitor of with aROCK of 033 μM for ROCK1 which is also a potent Ki Ca channel2+

antagonist and vasodilator

Bioactivity Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877Hydrochloride) a potent inhibitor of with a of 033ROCK Ki

μM for ROCK1 which is also a potent antagonistCa channel2+

and vasodilator

Bioactivity GSK180736A is a G protein-coupled receptor kinase 2 ( )GRK2inhibitor with an of 077 μMIC50

Bioactivity GSK269962A is a potent inhibitor with s of 16 and 4ROCK IC50nM for recombinant human and respectivelyROCK1 ROCK2

Bioactivity GSK429286A is a selective inhibitor of with an ROCK1 IC50value of 14 nM

Bioactivity H-1152 is a membrane-permeable and selective inhibitorROCKwith a value of 16 nM and an value of 12 nM forKi IC50

ROCK2

140 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

AT13148 Cat No HY-16071

Azaindole 1 (TC-S 7001) Cat No HY-10319

BDP5290 Cat No HY-12437

Chroman 1 Cat No HY-15392

Fasudil (HA-1077 AT877) Cat No HY-10341A

Fasudil Hydrochloride (HA-1077 (Hydrochloride) AT-877 (Hydrochloride)) Cat No HY-10341

GSK180736A Cat No HY-18990

GSK269962A (GSK 269962) Cat No HY-15556

GSK429286A Cat No HY-11000

H-1152 Cat No HY-15720

wwwMedChemExpresscom 141

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9726Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical DataSize 10 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9929Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9940Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9813Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity H-1152 dihydrochloride is a membrane-permeable and selective inhibitor with a value of 16 nM and an valueROCK Ki IC50

of 12 nM for ROCK2

Bioactivity Hydroxyfasudil is a inhibitor with s of 073 andROCK IC50072 μM for and respectivelyROCK1 ROCK2

Bioactivity Hydroxyfasudil hydrochloride is a inhibitor with sROCK IC50of 073 and 072 μM for and respectivelyROCK1 ROCK2

Bioactivity LX7101 is a potent inhibitor of and with LIMK ROCK2 IC50values of 24 16 and 10 nM for LIMK1 LIMK2 and ROCK2respectively also inhibits with an less than 1 nMPKA IC50

Bioactivity Narciclasine is a plant growth modulator Narciclasinemodulates the RhoRho kinaseLIM kinasecofilin signalingpathway greatly increasing GTPase RhoA activity as well asinducing actin stress fiber formation in a RhoA-dependentmanner

Bioactivity Pentanoic acid a short-chain fatty acid is a product ofbacterial metabolism and are associated with allergic skindisorders Pentanoic acid activates signaling pathwayROCK

Bioactivity Ripasudil (K-115) is a specific inhibitor of with sROCK IC50of 19 and 51 nM for and respectivelyROCK2 ROCK1

Bioactivity Ripasudil free base (K-115 free base) is a specific inhibitorof with s of 19 and 51 nM for and ROCK IC50 ROCK2 ROCK1

respectively

Bioactivity RKI-1447 is a potent small molecule inhibitor of andROCK1 with values of 145 nM and 62 nM respectivelyROCK2 IC50

Bioactivity ROCK inhibitor-2 is a selective dual and ROCK1 ROCK2inhibitor with s of 17 nM and 2 nM respectively IC50

[1]

H-1152 dihydrochloride Cat No HY-15720A

Hydroxyfasudil (HA-1100) Cat No HY-13911

Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100

hydrochloride HA1100 hydrochloride) Cat No HY-13911A

LX7101 Cat No HY-12659

Narciclasine (Lycoricidinol) Cat No HY-16563

Pentanoic acid Cat No HY-N6056

Ripasudil (K-115) Cat No HY-15685

Ripasudil free base (K-115 (free base)) Cat No HY-15685A

RKI-1447 Cat No HY-15755

ROCK inhibitor-2 Cat No HY-119937

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2g

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9843Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Bioactivity ROCK-IN-1 is a potent inhibitor of with an of 12ROCK IC50nM for ROCK2

Bioactivity ROCK2-IN-2 is a selective inhibitor extracted fromROCK2patent US20180093978A1 Compound A-30 has an of lt1IC50μM

Bioactivity SAR407899 is a selective potent and ATP-competitive ROCKinhibitor with an of 135 nM for and s of 36IC50 ROCK-2 KinM and 41 nM for human and rat respectivelyROCK-2

Bioactivity SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an of 135 nM forROCK IC50

and s of 36 nM and 41 nM for human and rat ROCK-2 Ki ROCK-2

respectively

Bioactivity SB-772077B dihydrochloride is an aminofurazan-based Rho inhibitor with s of 56 nM and 6 nM towardkinase( ROCK) IC50

ROCK1 and ROCK2 respevtively [1]

Bioactivity SLx-2119 (KD-025) is a selective inhibitor of with anROCK2 of 105 nMIC50

Bioactivity SR-3677 is a potent and selective inhibitor with anROCK-II of ~3 nMIC50

Bioactivity Thiazovivin is a potent inhibitor which can protectROCKhuman embryonic stem cells

Bioactivity Y-27632 is an ATP-competitive inhibitor of and ROCK-I ROCK-IIwith of 220 nM and 300 nM for and Ki ROCK-I ROCK-II

respectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

Bioactivity Y-27632 dihydrochloride is a cell-permeable ATP-competitiveinhibitor of and with s of 220 and 300 nMROCK-I ROCK-II Kirespectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

142 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

ROCK-IN-1 Cat No HY-U00351

ROCK2-IN-2 Cat No HY-103620

SAR407899 Cat No HY-15687A

SAR407899 hydrochloride Cat No HY-15687

SB-772077B dihydrochloride Cat No HY-108518

SLx-2119 (KD-025) Cat No HY-15307

SR-3677 Cat No HY-13300

Thiazovivin Cat No HY-13257

Y-27632 Cat No HY-10071

Y-27632 dihydrochloride Cat No HY-10583

wwwMedChemExpresscom 143

Purity 9923Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity Y-33075 is a selective inhibitor derived from Y-27632ROCKand is more potent than Y-27632 with an of 36 nMIC50

Bioactivity Y-33075 dihydrochloride is a selective inhibitor with anROCK of 36 nMIC50

Bioactivity ZINC00881524 is a inhibitorROCK

Y-33075 (Y 39983) Cat No HY-10067

Y-33075 dihydrochloride Cat No HY-10069

ZINC00881524 Cat No HY-101244

Sirtuin

Sirtuin (Sir2 proteins) are a class of proteins that possess eithermono-ADP-ribosyltransferase or deacylase activity includingdeacetylase desuccinylase demalonylase demyristoylase anddepalmitoylase activity Sirtuins regulate important biologicalpathways in bacteria archaeaand eukaryotes Sirtuins have beenimplicated in influencing a wide range of cellular processes like agingtranscription apoptosis inflammation and stress resistance as well asenergy efficiency and alertness during low-calorie situations Sirtuinscan also control circadian clocks and mitochondrial biogenesis

144 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 145

Purity 9891Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9909Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Sirtuin Inhibitors amp Modulators

Bioactivity 3-TYP is a selective inhibitor with an of 16 nMSIRT3 IC50more potent over SIRT1 ( =88 nM) SIRT2 ( =92 nM)IC50 IC50

Bioactivity AGK2 is a selective inhibitor with of 35 μM AGK2SIRT2 IC50can also inhibit and with of 30 and 91 μMSIRT1 SIRT3 IC50respectively

Bioactivity AK-1 is a potent specific and cell-permeable inhibitorSIRT2with an of 125 μMIC50

Bioactivity AK-7 is a selective cell- and brain-permeable inhibitorSIRT2with an of 155 μMIC50

Bioactivity Cambinol is a and inhibitor with values of 56SIRT1 SIRT2 IC50and 59 μM respectively

Bioactivity CAY10602 is a activatorSIRT1

Bioactivity Dihydrocoumarin is a compound found in Melilotus Dihydrocoumarin is a inhibitorofficinalis yeast Sir2p

Dihydrocoumarin also inhibits and withhuman SIRT1 SIRT2s of 208 μM and 295 μM respectively IC50

[1]

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Ginkgolide C is a flavone isolated from leavesGinkgo bilobapossessing multiple biological functions such as decreasingplatelet aggregation and ameliorating Alzheimer disease

Bioactivity Inauhzin is a dual inhibitor and acts as anSirT1IMPDH2activator used in the research of cancerp53

3-TYP Cat No HY-108331

AGK2 Cat No HY-100578

AK-1 Cat No HY-101465

AK-7 Cat No HY-16691

Cambinol Cat No HY-100732

CAY10602 Cat No HY-104073

Dihydrocoumarin (Hydrocoumarin Chroman-2-one) Cat No HY-N1926

Fisetin Cat No HY-N0182

Ginkgolide C (BN-52022 Ginkgolide-C) Cat No HY-N0785

Inauhzin (INZ) Cat No HY-15869

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9876Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity MC3482 is a specific sirtuin5 ( ) inhibitorSIRT5 Bioactivity Nicotinamide is a form of vitamin B3 that plays essentialroles in cell physiology through facilitating NAD+ redoxhomeostasis and providing NAD+ as a substrate to a class ofenzymes that catalyze non-redox reactions Nicotinamide is aninhibitor of SIRT1

Bioactivity OSS_128167 is a selective inhibitor with s of 89SIRT6 IC501578 and 751 μM for and respectivelySIRT6 SIRT1 SIRT2

Bioactivity PROTAC Sirt2 Degrader-1 is a SirReal-based acts as aPROTAC degrader composed of a highly potent andSirt2

isotype-selective inhibitor a linker and a bona fideSirt2cereblon ligand for E3 ubiquitin ligase PROTAC Sirt2Degrader-1 shows an of 025 μM for Sirt2 with no effecthellipIC50

Bioactivity Salermide is an inhibitor of and can cause strongSirt1 Sirt2cancer-specific apoptotic cell death

Bioactivity Selisistat (EX-527) is a potent and selective inhibitorSIRT1with of 98 nMIC50

Bioactivity Selisistat S-enantiomer (EX-527 S-enantiomer) is theS-enantiomer of Selisistat with an of 123 nM for SIRT1IC50Selisistat S-enantiomer is much more potent than SelisistatR-enantiomer

Bioactivity SIRT-IN-1 is a potent inhibitor of with of 15SIRT123 IC s5010 33 μM respectively

Bioactivity SIRT-IN-2 is a potent inhibitor of with of 4SIRT123 IC s504 7 μM respectively

Bioactivity Sirt2-IN-1 (Compound 9) is a ( ) inhibitor withsirtuin 2 Sirt2an of 163 nM IC50

[1]

146 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

MC3482 Cat No HY-112587

Nicotinamide (Niacinamide Nicotinic acid amide Vitamin B3) Cat No HY-B0150

OSS_128167 Cat No HY-107454

PROTAC Sirt2 Degrader-1 Cat No HY-103636

Salermide Cat No HY-101073

Selisistat (EX-527) Cat No HY-15452

Selisistat S-enantiomer (EX-527 (S-enantiomer)) Cat No HY-15452A

SIRT-IN-1 Cat No HY-16615

SIRT-IN-2 Cat No HY-16616

Sirt2-IN-1 Cat No HY-112427

wwwMedChemExpresscom 147

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9939Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9887Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9944Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity SIRT5 inhibitor 1 is a potent Human deacylaseSirtuin 5inhibitor with an of 011 μMIC50

Bioactivity Sirtinol is a inhibitor with s of 48 μM 577 μMsirtuin IC50and 131 μM for ySir2 hSIRT2 and hSIRT2 respectively

Bioactivity Sirtuin modulator 1 is a modulator of a homolog of SIRTl SIRT3with EC of lt 1 μM extracted from patent WO 201007185315A1 Compound No4

Bioactivity SRT 1460 a potent activator with an Sirtuin-1 (SIRT1) EC15value of 29 μM shows good selectivity for activation ofSIRT1 versus SIRT2 and SIRT3 (EC15 gt 300 μM) and is morepotent than Resveratrol and the closest sirtuin homologhellip

Bioactivity SRT 1720 is a selective activator of human with anSIRT1 of 016 μM and shows less potent activities agaiinstEC15

SIRT2 and SIRT3 with EC s of 37 μM and gt 300 μM15respectively

Bioactivity SRT 1720 Hydrochloride is a selective activator of withSIRT1an of 016 μM and shows less potent activities onEC15SIRT2 and SIRT3 with EC s of 37 μM and 300 μM15respectively

Bioactivity SRT 2104 is a first-in-class highly selective andbrain-permeable activator of the NAD dependent deacetylase+

increases Sirt1 protein but shows no effect on Sirt1Sirt1mRNA Used in the research of diabetes mellitus hellip

Bioactivity SRT 2183 is a selective activator with anSirtuin-1 (SIRT1) value of 036 μM SRT 2183 induces growth arrestEC15

[1]

and apoptosis concomitant with deacetylation of STAT3 andNF-κB and reduction of c-Myc protein levels [2]

Bioactivity Tenovin-1 is an inhibitor of and ansirtuin 1 sirtuin 2activator of and may have potential in the management ofp53cancer

Bioactivity Tenovin-6 is an inhibitor of and slightly inhibitsSIRT1 SIRT2 and is also a potent activator of with s ofHDAC8 p53 IC50

21 μM 10 μM and 67 μM for SirT1 SirT2 and SirT3respectively

SIRT5 inhibitor 1 Cat No HY-112634

Sirtinol Cat No HY-13515

Sirtuin modulator 1 Cat No HY-19758A

SRT 1460 Cat No HY-124037

SRT 1720 Cat No HY-10532

SRT 1720 Hydrochloride Cat No HY-15145

SRT 2104 Cat No HY-15262

SRT 2183 Cat No HY-19759

Tenovin-1 Cat No HY-13423

Tenovin-6 Cat No HY-15510

Purity 9855Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Tenovin-6 Hydrochloride is an inhibitor of and SIRT1 SIRT2slightly inhibits and is also a potent activator ofHDAC8

with s of 21 μM 10 μM and 67 μM for SirT1 SirT2p53 IC50and SirT3 respectively

Bioactivity Thiomyristoyl is a potent and specific inhibitor with anSIRT2 of 28 nMIC50

Bioactivity UBCS039 is the first synthetic specific Sirtuin 6 (SIRT6)activator inducing autophagy in human tumor cells with an

of 38 μM EC50[1]

148 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Tenovin-6 Hydrochloride Cat No HY-15510B

Thiomyristoyl Cat No HY-101278

UBCS039 Cat No HY-115453

wwwMedChemExpresscom 149

SRPKSerine-arginine protein kinases

SRPKs is a critical enzyme family that regulates splicing activity in thecell The first serine-arginine (SR) protein kinase identified is SRPK1which is isolated from mitotic cells and it is described tophosphorylate SR proteins and to promote their release from nuclearspeckles during the G2M phase of the cell cycle SRPK1 is theprototype of the SRPK family which also includes the twohomologous SRPK2 and SRPK3 proteins SRPKs are characterized by abipartite catalytic domain separated by a unique spacer sequence andare mainly localized in the cytoplasm of mammalian cellsSRPKs can translocate into the nucleus of cells under severalconditions such as during the G2M phase of the cell cycle or after

osmotic stress or as a consequence of activation of the epidermal growth factor (EGF) signal transduction pathway

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9917Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

SRPK Inhibitors amp Modulators

Bioactivity SPHINX31 is a potent and selective inhibitor of with an ofserinearginine-rich protein kinase 1 (SRPK1) IC50

59 nM SPHINX31 inhibits phosphorylation ofserinearginine-rich splicing factor 1 (SRSF1) SPHINX31 is apotential topical therapeutic for neovascular eye diseasehellip

Bioactivity SRPIN340 is an ATP-competitive serine-arginine-rich proteinkinase ( ) inhibitor with a of 089 μM for SRPK1SRPK Ki

Bioactivity SRPKIN-1 is a covalent and irreversible inhibitorSRPK12with s of 356 and 98 nM respectively Anti-angiogenesisIC50

effect [1]

150 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SPHINX31 Cat No HY-117661

SRPIN340 (SRPK inhibitor) Cat No HY-13949

SRPKIN-1 Cat No HY-116856

wwwMedChemExpresscom 151

Telomerase

Telomerase is a ribonucleoprotein that is an enzyme that adds DNAsequence repeats (TTAGGG in all vertebrates) to the 3 end of DNAstrands in the telomere regions which are found at the ends ofeukaryotic chromosomes This region of repeated nucleotide calledtelomeres contains noncoding DNA and hinders the loss of importantDNA from chromosome ends As a result every time the chromosomeis copied only 100ndash200 nucleotides are lost which causes no damageto the organisms DNA Telomerase is a reverse transcriptase thatcarries its own RNA molecule which is used as a template when itelongates telomeres which are shortened after each replication cycleTelomerase a eukaryotic ribonucleoprotein (RNP) complex contains

both an essential RNA and a protein reverse transcriptase subunit By reverse transcription the telomerase RNPmaintains telomere length stability in almost all cancer cells

Purity 980Clinical Data No Development ReportedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Telomerase Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity BIBR 1532 is a potent selective and non-competitive inhibitor with of 100 nM intelomerase IC50

a cell-free assay

Bioactivity Telomerase-IN-1 is a inhibitor with an ofTelomerase IC50019 μM

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

152 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

BIBR 1532 Cat No HY-17353

Telomerase-IN-1 Cat No HY-U00268

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

wwwMedChemExpresscom 153

TOPKT-LAK cell-originated protein kinase

TOPK (T-lymphokine-activated killer cellndashoriginated protein kinasealso known as PBK or PDZ-binding kinase) is a SerThr protein kinasethat is highly expressed in many types of human cancer includingbreast and lung cancers TOPK is included in the ldquoconsensus stemnessranking signaturerdquo gene list that is up-regulated in cancer stemcell-enriched tumors and is associated with poor prognosis inmultiple types of cancerTOPKPBK is an oncogenic kinase upregulated in most humancancers TOPK is important for mitotic cell division and thatphosphorylation by Cdk1 is needed for its activationTOPK a member of the MEK36-related MAPKK family is expressed in

a wide range of proliferating cells and tissues including cancer cells and testis TOPK negatively regulates the activityof p38α by phosphorylating the p38α-specific phosphatase MKP1 and enhancing the stability of MKP1 The MAPKphosphatase MKP1 an archetypal member of the MKP family plays a pivotal role in the deactivation of p38 through adephosphorylation reaction

Purity 9563Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

TOPK Inhibitors amp Modulators

Bioactivity HI-TOPK-032 is a potent and specific inhibitorTOPK Bioactivity OTS-964 is a potent T-lymphokine-activated killer inhibitor ( =28cell-originated protein kinase (TOPK) IC50

nM) which inhibits TOPK kinase activity with high affinityand selectivity

Bioactivity OTS514 is a highly potent inhibitor which inhibits TOPKTOPKkinase activity with a median inhibitory concentration ( )IC50value of 26 nM

154 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

HI-TOPK-032 Cat No HY-101550

OTS-964 Cat No HY-12467

OTS514 Cat No HY-18621

wwwMedChemExpresscom 155

Topoisomerase

Topoisomerases are enzymes that regulate the overwinding orunderwinding of DNA The winding problem of DNA arises due to theintertwined nature of its double-helical structure Topoisomerases areisomerase enzymes that act on the topology of DNA Type Itopoisomerase cuts one strand of a DNA double helix relaxationoccurs and then the cut strand is reannealed Type I topoisomerasesare subdivided into two subclasses type IA topoisomerases whichshare many structural and mechanistic features with the type IItopoisomerases and type IB topoisomerases which utilize acontrolled rotary mechanism Type II topoisomerase cuts both strandsof one DNA double helix pass another unbroken DNA helix through

it and then reanneal the cut strands This class is also split into two subclasses type IIA and type IIB topoisomeraseswhich possess similar structure and mechanisms

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 1 mg 5 mg

Purity 980Clinical Data LaunchedSize 1 mg 5 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9243Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 9808Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9889Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Topoisomerase Inhibitors amp Modulators

Bioactivity 9-Aminocamptothecin is a inhibitor withtopoisomerase Ipotent anticancer activity

Bioactivity Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) afluorescent molecule and the first described non-peptidicinhibitor showing discrete specificity for the CTRL(chymotrypsin-like) activity of the 20S proteasome [1]

Aclacinomycin A hydrochloride is also a dual inhibitor ofhellip

Bioactivity Aldoxorubicin (INNO-206) is an albumin-binding prodrug ofdoxorubicin which is released from albumin under acidicconditions Aldoxorubicin (INNO-206) has potent antitumoractivities in various cancer cell lines and in murine tumormodels

Bioactivity Amonafide is a inhibitor and DNAtopoisomerase IIintercalator that induces apoptotic signaling by blocking thebinding of Topo II to DNA

Bioactivity Amrubicin (SM-5887) is a DNA inhibitortopoisomerase IIused for the research of cancer

Bioactivity Amrubicin (hydrochloride) (SM-5887 (hydrochloride)) is a DNA inhibitor used for the research of cancertopoisomerase II

Bioactivity Amsacrine (m-AMSA) is an inhibitor of andtopoisomerase IIacts as an antineoplastic agent which can intercalates intothe DNA of tumor cells

Bioactivity Amsacrine hydrochloride (mAMSA hydrochloride) is an inhibitorof and acts as an antineoplastic agenttopoisomerase IIwhich can intercalates into the DNA of tumor cells

Bioactivity Banoxantrone D12 (AQ4N D12) is the deuterium labeledbanoxantrone Banoxantrone is a novel bioreductive agent thatcan be reduced to a stable DNA-affinic compound AQ4 which isa potent inhibitortopoisomerase II

Bioactivity Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) isthe deuterium labeled banoxantrone dihydrochlorideBanoxantrone is a novel bioreductive agent that can be reducedto a stable DNA-affinic compound AQ4 which is a potent

inhibitortopoisomerase II

156 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

9-amino-CPT (9-amino-20(S)-camptothecin) Cat No HY-100309

Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) Cat No HY-N2306A

Aldoxorubicin (INNO-206 DOXO-EMCH) Cat No HY-16261

Amonafide (AS1413) Cat No HY-10982

Amrubicin (SM-5887 AMR) Cat No HY-B0067

Amrubicin hydrochloride (SM-5887 (hydrochloride) AMR (hydrochloride)) Cat No HY-B0067A

Amsacrine (m-AMSA acridinyl anisidide) Cat No HY-13551

Amsacrine hydrochloride (m-AMSA hydrochloride acridinyl anisidide hydrochloride) Cat No HY-13551A

Banoxantrone D12 (AQ4N D12) Cat No HY-13562S

Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) Cat No HY-13562AS

wwwMedChemExpresscom 157

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity 9826Clinical Data Phase 4Size 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9635Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg

Purity 9818Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9880Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg

Bioactivity Banoxantrone dihydrochloride is a novel bioreductive agentthat can be reduced to a stable DNA-affinic compound AQ4which is a potent inhibitortopoisomerase II

Bioactivity Belotecan hydrochloride (CKD-602 hydrochloride) a inhibitor is a synthetic and water-solubleTopoisomerase I

camptothecin derivative

Bioactivity Berberine chloride is an alkaloid isolated from the Chineseherbal medicine Huanglian as an Berberine chlorideantibioticinduces reactive oxygen species ( ) generation andROSinhibits Antineoplastic propertiesDNA topoisomerase

[1]

Bioactivity Berberine chloride hydrate is an alkaloid isolated from theChinese herbal medicine Huanglian as an Berberineantibioticchloride hydrate induces reactive oxygen species ( )ROSgeneration and inhibits AntineoplasticDNA topoisomeraseproperties [1]

Bioactivity Betulinic acid is a natural pentacyclic triterpenoid acts asa eukaryotic inhibitor with an of 5topoisomerase I IC50μM and possesses anti-HIV anti-malarial anti-inflammatoryand anti-tumor properties

Bioactivity Bisantrene is a highly effective antitumor drug targetseukaryotic type II topoisomerases

Bioactivity Campathecin is a potent DNA enzyme topoisomerase Iinhibitor with an of 679 nMIC50

Bioactivity Daun02 is a prodrug of the inhibitortopoisomeraseDaunorubicin

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Banoxantrone dihydrochloride (AQ4N dihydrochloride) Cat No HY-13562A

Belotecan hydrochloride (CKD-602) Cat No HY-13566A

Berberine chloride (Natural Yellow 18 (chloride)) Cat No HY-18258

Berberine chloride hydrate (Natural Yellow 18 (chloride hydrate)) Cat No HY-17577

Betulinic acid (Lupatic acid Betulic acid) Cat No HY-10529

Bisantrene (CL216942) Cat No HY-100875

Campathecin (Camptothecin (S)-(+)-Camptothecin CPT) Cat No HY-16560

Daun02 Cat No HY-13061

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9965Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9888Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9839Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9947Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Doxorubicin is a cytotoxic anthracycline antibiotic for thetreatment of multiple cancers The possible mechanisms bywhich doxorubicin acts in the cancer cell are intercalationinto DNA and disruption of -mediated DNAtopoisomerase-IIrepair

Bioactivity Doxorubicin hydrochloride is a cytotoxic anthracyclineantibiotic for the treatment of multiple cancers The possiblemechanisms by which doxorubicin acts in the cancer cell areintercalation into DNA and disruption of

-mediated DNA repairtopoisomerase-II

Bioactivity Dxd is a potent inhibitor with an ofDNA topoisomerase I IC50031 μM used as a conjugated drug of HER2-targeting ADC(DS-8201a)

Bioactivity Edotecarin is a potent inhibitor of that cantopoisomerase Iinduces single-strand DNA cleavage with of 50 nMIC50

Bioactivity Ellipticine (NSC 71795) is a potent antineoplastic agentinhibits activitiesDNA topoisomerase II

Bioactivity Ellipticine (NSC 71795) hydrochloride is a potentantineoplastic agent inhibits DNA topoisomerase IIactivities

Bioactivity Epirubicin is a semisynthetic L-arabino derivative ofdoxorubicin and an antineoplastic agent by inhibiting

Topoisomerase

Bioactivity Epirubicin (hydrochloride) is a semisynthetic L-arabinoderivative of doxorubicin and an antineoplastic agent byinhibiting Topoisomerase

Bioactivity Etoposide (VP-16 VP-16-213) a chemotherapy medication usedfor the treatments of a number of types of cancer inhibits

by forming a complex with topoisomerase II andDNA synthesisDNA Etoposide arrests cell cycle in G2 and induces apoptoshellip

Bioactivity Exatecan is a water soluble inhibitor withtopoisomerase Ian of 22 μM (0975 μgmL) and can be used in cancerIC50research

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Doxorubicin (Hydroxydaunorubicin) Cat No HY-15142A

Doxorubicin hydrochloride (Hydroxydaunorubicin (hydrochloride)) Cat No HY-15142

Dxd (Exatecan derivative for ADC) Cat No HY-13631D

Edotecarin (J 107088 PF 804950) Cat No HY-13618

Ellipticine (NSC 71795) Cat No HY-15753

Ellipticine hydrochloride (NSC 71795 (hydrochloride)) Cat No HY-15753A

Epirubicin Cat No HY-13624

Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride) Cat No HY-13624A

Etoposide (VP-16 VP-16-213) Cat No HY-13629

Exatecan (DX-8951) Cat No HY-13631

wwwMedChemExpresscom 159

Purity 9830Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9803Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9912Clinical Data Phase 3Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg 500 mg

Bioactivity Exatecan Mesylate is a water soluble topoisomerase Iinhibitor with an of 22 μM (0975 μgmL) and can beIC50used in cancer research

Bioactivity Flumequine (R-802) is a quinolone antibiotic and acts as a inhibitor with an of 15 μM (392topoisomerase II IC50

μgmL)

Bioactivity Genz-644282 is a non-camptothecin inhibitortopoisomerase Iused for cancer research

Bioactivity Idarubicin hydrochloride is an anthracycline antileukemicdrug It inhibits the interfering with thetopoisomerase IIreplication of DNA and RNA transcription

Bioactivity Indotecan (LMP-400) is a potent topoisomerase 1(Top1)inhibitor with values of 300 1200 560 nM for P388IC50HCT116 MCF-7 cell lines respectively

Bioactivity Intoplicine is a and inhibitorDNA topoisomerase I II

Bioactivity Irinotecan is a water soluble inhibitortopoisomerase Ipreventing religation of the DNA strand by binding totopoisomerase I-DNA complex

Bioactivity Irinotecan hydrochloride is a water soluble topoisomerase Iinhibitor mainly used to treat colon cancer and rectal cancer

Bioactivity Irinotecan hydrochloride trihydrate is a water soluble inhibitor with antitumor activitytopoisomerase I

Bioactivity Karenitecin (Cositecan) is a inhibitor withtopoisomerase Ipotent anti-cancer activity

Exatecan Mesylate (DX8951f) Cat No HY-13631A

Flumequine (R-802) Cat No HY-B0526

Genz-644282 Cat No HY-16228

Idarubicin hydrochloride (4-Demethoxydaunorubicin hydrochloride) Cat No HY-17381

Indotecan (LMP-400 NSC-724998) Cat No HY-18351

Intoplicine Cat No HY-101647

Irinotecan ((+)-Irinotecan CPT-11) Cat No HY-16562

Irinotecan hydrochloride (CPT-11 hydrochloride Camptothecin 11 hydrochloride) Cat No HY-16562A

Irinotecan hydrochloride trihydrate Cat No HY-16568

Karenitecin (Cositecan BNP 1350) Cat No HY-14812

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9690Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9902Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9702Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg

Bioactivity LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I inhibitor with antitumor activity (Top1) [1]

Bioactivity LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNAintercalator and inhibitor withTopoisomerase I (Top1)antitumor activity [1]

Bioactivity MC-DOXHZN is an albumin-binding prodrug of Doxorubicin withacid-sensitive properties [1]

Bioactivity MC-DOXHZN hydrochloride is an albumin-binding prodrug ofDoxorubicin with acid-sensitive properties [1]

Bioactivity Mitoxantrone is a inhibitor also inhibitstopoisomerase IIprotein kinase C ( ) activity with an of 85 μMPKC IC50

Bioactivity Mitoxantrone dihydrochloride is a topoisomerase IIinhibitor also inhibits protein kinase C ( ) activityPKCwith an of 85 μMIC50

Bioactivity Namitecan is a potent inhibitor withtopoisomerase Iantitumor property

Bioactivity Pirarubicin is an anthracycline antibiotics acts as a inhibitor and is a widely used fortopoisomerase II

treatment of various cancers in particular solid tumors

Bioactivity Pirarubicin Hydrochloride is an anthracycline antibioticsacts as a inhibitor and is a widely usedtopoisomerase IIfor treatment of various cancers in particular solid tumors

Bioactivity Pixantrone is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

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LMP744 (MJ-III65 NSC706744) Cat No HY-U00248

LMP744 hydrochloride (MJ-III65 hydrochloride NSC706744 hydrochloride) Cat No HY-U00248A

MC-DOXHZN (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat No HY-16261A

MC-DOXHZN hydrochloride (Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat No HY-16261B

Mitoxantrone (mitozantrone) Cat No HY-13502

Mitoxantrone dihydrochloride (mitozantrone dihydrochloride) Cat No HY-13502A

Namitecan (ST-1968) Cat No HY-14821

Pirarubicin (THP) Cat No HY-13725

Pirarubicin Hydrochloride (THP Hydrochloride) Cat No HY-13725A

Pixantrone (BBR 2778) Cat No HY-13727

wwwMedChemExpresscom 161

Purity 9920Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 100 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 50 mg 100 mg 200 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9960Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Pixantrone dimaleate is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

Bioactivity Podocarpusflavone A is a DNA topoisomerase I inhibitor havemoderated anti-proliferative activity induce cell apoptosis inMCF-7 is developing anti-tumor drugs target DNAtopoisomerase I In vitro podocarpusflavone-A show significantinhibitions against DLD KB MCF-7 HEp-2 tumor cell lineshellip

Bioactivity SN-38 (NK012) is an active metabolite of the Topoisomerase Iinhibitor Irinotecan SN-38 (NK012) inhibits and DNA RNA

with s of 0077 and 13 μM respectivelysynthesis IC50

Bioactivity SW044248 is a non-canonical inhibitor andtopoisomerase Iselectively toxic for certain non-small cell lung cancer(NSCLC) cell lines

Bioactivity TAS-103 is a dual inhibitor of DNA usedtopoisomerase IIIfor cancer research

Bioactivity TAS-103 dihydrochloride is a dual inhibitor of DNA used for cancer researchtopoisomerase III

Bioactivity Teniposide is a podophyllotoxin derivative acts as a inhibitor and used as a chemotherapeutictopoisomerase II

agent

Bioactivity Top1 inhibitor 1 (compound 28) is a potent human inhibitor with an value of 29topoisomerase I (Top1) IC50

nM [1]

Bioactivity Topotecan (SKF 104864A NSC 609669) is a Topoisomerase Iinhibitor The values of Topotecan at 24 h are 273plusmn025IC50μM of U251 cells 295plusmn023 μM of U87 cells 546plusmn041 μM ofGSCs-U251 and 595plusmn024 μM of GSCs-U87

Bioactivity Topotecan Hydrochloride (SKF 104864A Hydrochloride NSC 609669Hydrochloride) is a inhibitor with potentTopoisomerase Iantineoplastic activities

Pixantrone dimaleate (BBR 2778 dimaleate) Cat No HY-13727A

Podocarpusflavone A Cat No HY-N2198

SN-38 (NK012) Cat No HY-13704

SW044248 Cat No HY-19637

TAS-103 (BMS-247615) Cat No HY-13758

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) Cat No HY-13758A

Teniposide (VM26) Cat No HY-13761

Top1 inhibitor 1 Cat No HY-126142

Topotecan (SKF 104864A NSC 609669) Cat No HY-13768

Topotecan Hydrochloride (SKF 104864A (Hydrochloride) NSC 609669 (Hydrochloride)) Cat No HY-13768A

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Bioactivity Voreloxin is a first-in-class inhibitortopoisomerase IIthat intercalates DNA and induces site-selective DNA DSB G2arrest and apoptosis

Bioactivity Voreloxin Hydrochloride is a first-in-class topoisomerase IIinhibitor that intercalates DNA and induces site-selective DNADSB G2 arrest and apoptosis

Bioactivity β-Lapachone is a naturally occurring O-naphthoquinone acts asa inhibitor and induces apoptosis bytopoisomerase Iinhibiting cell cycle progression

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Voreloxin (SNS-595 Vosaroxin AG 7352) Cat No HY-10534

Voreloxin Hydrochloride (SNS-595 Hydrochloride Vosaroxin

Hydrochloride AG 7352 Hydrochloride) Cat No HY-16518

β-Lapachone (ARQ-501 NSC-26326) Cat No HY-13555

wwwMedChemExpresscom 163

Wee1

Wee1 is a nuclear kinase belonging to the SerThr family of proteinkinases in the fission yeast ( )Schizosaccharomyces pombe S pombeWee1 has amolecular mass of 96 kDa and it is a key regulator of cellcycle progression Wee1 influences cell size by inhibiting the entryinto mitosis through inhibiting Cdk1 Wee1 has homologues in manyother organisms including mammals Wee1 inhibits Cdk1 byphosphorylating it on two different sites Tyr15 and Thr14 Cdk1 iscrucial for the cyclin-dependent passage of the various cell cyclecheckpoints At least three checkpoints exist for which the inhibitionof Cdk1 by Wee1 is important G M checkpoint Cell size checkpoint2DNA damage checkpoint Wee1 is shown to phosphorylate histone

H2B at tyrosine 37 residue which regulates global expression of histones

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Wee1 Inhibitors amp Modulators

Bioactivity Adavosertib (AZD-1775 MK-1775) is a potent inhibitorWee1with an of 52 nMIC50

Bioactivity PD0166285 is a inhibitor and a weak inhibitorWEE1 Myt1with s of 24 and 72 nM respectivelyIC50

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Adavosertib (AZD1775 MK-1775) Cat No HY-10993

PD0166285 Cat No HY-13925

Page 6: Cell Cycle/DNA Damage - MedchemExpress.com · 2019. 7. 2. · G2/M transition that commits cells to division is a default consequence of initiating the cell cycle at the G1/S transition,

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9923Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 500 mg

Purity 9977Clinical Data LaunchedSize 10mM x 1mL in Water

50 mg 100 mg 200 mg

Purity 9930Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity LY 254155 an antifolate inhibits and binds tohGARFT with s of 21plusmn02 and 17plusmn01 nM respectivelymFBP Ki

Bioactivity LY309887 is a potent inhibitor of glycinamide ribonucleotideformyltransferase ( ) with a of 65 nM and hasGARFT Kiantitumor activity

Bioactivity Methotrexate is a antagonist with median of 78 nMfolate IC50in assayin vitro

Bioactivity Pemetrexed is a novel the values of theantifolate Kipentaglutamate of LY231514 are 13 72 and 65 nM forinhibits thymidylate synthase ( ) dihydrofolate reductaseTS( ) and glycinamide ribonucleotide formyltransferase (DHFR

) respectivelyGARFT

Bioactivity Pemetrexed disodium is a novel that inhibits theantifolatefolatedependent enzymes thymidylate synthase dihydrofolate

and reductase glycinamide ribonucleotide with s of 13 72 and 65 nMformyltransferase Ki

respectively

Bioactivity Pemetrexed disodium hemipenta hydrate is a novel antifolatethe values of the pentaglutamate of LY231514 are 13 72Kiand 65 nM for inhibits thymidylate synthase ( )TSdihydrofolate reductase ( ) and glycinamideDHFRribonucleotide formyltransferase ( ) respectivelyGARFT

Bioactivity Pralatrexate(Folotyn) is an antifolate and structurally afolate analog Its IC50 is lt 300 nM in some cell linesIC50 Value lt 300 nM Target Antifolate Pralatrexate is anantifolate (a folate analogue metabolic inhibitor) designed toaccumulate preferentially in cancer cells Based onhellip

Bioactivity Pyrimethamine(RP4753) is a medication used for protozoalinfections interferes with tetrahydrofolic acid synthesisfrom folic acid by inhibiting the enzyme dihydrofolatereductase (DHFR) IC50 Value 154 nM (Plasmodium falciparum)[1] Target DHFR antifolate in vitro Three susceptibilityhellip

Bioactivity Trimethoprim is a bacteriostatic antibiotic used mainly in theprophylaxis and treatment of urinary tract infections

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LY 254155 Cat No HY-14523

LY309887 Cat No HY-10818

Methotrexate (Amethopterin CL14377 WR19039) Cat No HY-14519

Pemetrexed (LY231514) Cat No HY-10820

Pemetrexed disodium (LY231514 disodium) Cat No HY-10820A

Pemetrexed disodium hemipenta hydrate (LY231514 (disodium hemipenta hydrate)) Cat No HY-13781

Pralatrexate Cat No HY-10446

Pyrimethamine (Pirimecidan Pirimetamin RP 4753) Cat No HY-18062

Trimethoprim Cat No HY-B0510

wwwMedChemExpresscom 7

APCAnaphase promoting complex

APC (Anaphase-Promoting Complex) is an E3 ubiquitin ligase thatmarks target cell cycle proteins for degradation by the 26Sproteasome The APCC is a large complex of 11ndash13 subunit proteinsincluding a cullin (Apc2) and RING (Apc11) subunit much like SCF TheAPCCs main function is to trigger the transition from metaphase toanaphase by tagging specific proteins for degradation The twoproteins of most importance that get degraded in this process assubstrates of the APCC are securin and S and M cyclins Securinreleases separase a protease after being degraded which in turntriggers the cleavage of cohesin the protein complex that binds sisterchromatids together During metaphase sister chromatids are linked

by intact cohesin complexes When securin undergoes ubiquitination by the APCC and releases separase whichdegrades cohesin sister chromatids become free to move to opposite poles for anaphase The APCC also targets themitotic cyclins for degradation resulting in the inactivation of M-CdK (mitotic cyclin-dependent kinase) complexespromoting exit from mitosis and cytokinesis

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9911Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

APC Inhibitors amp Modulators

Bioactivity TAME is a inhibitor and can be also utilizedserine proteaseas a substrate for the serine proteases trypsin plasmin andthrombin TAME is an inhibitor of[1] [2] [3]

which binds to the hellipanaphase-promoting complex (APC)

Bioactivity TAME hydrochloride is a inhibitor and can beserine proteasealso utilized as a substrate for the serine proteases trypsinplasmin and thrombin TAME hydrochloride is an[1] [2] [3]

inhibitor of which bihellipanaphase-promoting complex (APC)

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TAME Cat No HY-13255

TAME hydrochloride Cat No HY-13255A

wwwMedChemExpresscom 9

ATMATRAtaxia telangiectasia mutatedATM and RAD3 related

ATMATR are members of the PI3 family of serine-threonine kinasesand function as essential links between the sensors and effectors ofthe DNA damage response The roles of ATM and ATR partiallyoverlap and are cooperative however they are also known to playdistinct roles in protecting the cell from DNA damage ATM is mostlyresponsible for sending signals from DSBs (double-strand breaks)induced by ionizing radiation while the closely related ATR respondsto UV damage or stalled replication forks ATM and ATR are known tophosphorylate common as well as specific substrates to activatecheckpoint signaling The G1 S and G2 cell cycle checkpoints areprimarily regulated by the ATM (ataxia telangiectasia mutated) and

ATR (ATM and Rad3-related) protein kinases

Purity 9976Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9904Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9960Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

ATMATR Inhibitors amp Modulators

Bioactivity ATM Inhibitor-1 is a highly potent selective and orallyactive inhibitor with an of 07 nM shows weakATM IC50activity against mTOR (IC 21 μM) DNAPK (IC 28 μM)50 50PI3Kα (IC 38 μM) PI3Kβ (IC 103 μM) PI3Kγ hellip50 50

Bioactivity ATR inhibitor 1 is a inhibitor extracted from patentATRWO2015187451A1 compound I-l has a value below 1 microΜ Ki

[1]

Bioactivity AZ20 is a potent and selective inhibitor of with an ATR IC50of 5 nM and has 8-fold selectivity against (IC =38mTOR 50nM)

Bioactivity AZ32 is an orally bioavailable and blood-brainbarrier-penetrating inhibitor with an of lt62ATM IC50nM for ATM enzyme and an of 031 μM for ATM in cellIC50

Bioactivity AZD0156 is an oral potent and selective inhibitor withATMan of 058 nMIC50

Bioactivity AZD1390 is an inhibitorATM

Bioactivity BAY-1895344 is a potent orally available and selective ATRinhibitor with of 7 nM Anti-tumor activity IC50

[1]Bioactivity BAY-1895344 hydrochloride is a potent orally available and

selective inhibitor with of 7 nM Anti-tumorATR IC50

activity [1]

Bioactivity Berzosertib (VE-822) is an inhibitor with a value ofATR Kiless than 02 nM It also inhibits with a of 34 nMATM Ki

Bioactivity Ceralasertib (AZD6738) is a potent inhibitor of kinaseATRwith an of 1 nMIC50

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ATM Inhibitor-1 Cat No HY-112614

ATR inhibitor 1 Cat No HY-111451

AZ20 Cat No HY-15557

AZ32 Cat No HY-112305

AZD0156 Cat No HY-100016

AZD1390 Cat No HY-109566

BAY-1895344 Cat No HY-101566

BAY-1895344 hydrochloride Cat No HY-101566A

Berzosertib (VE-822 VX-970) Cat No HY-13902

Ceralasertib (AZD6738) Cat No HY-19323

wwwMedChemExpresscom 11

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9947Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9988Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9840Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity CGK733 is a potent inhibitor used for the researchATMATRof cancer

Bioactivity CP-466722 is a rapidly reversible inhibitor of with anATM of 41 μM and has no effects on PI3K or closely relatedIC50

PI3K-like protein kinase (PIKK) family members

Bioactivity ETP-46464 is an effective and inhibitor withmTOR ATRs of 06 and 14 nM respectivelyIC50

Bioactivity KU 59403 is a potent inhibitor with an of 3 nMATM IC50

Bioactivity KU-55933 is a potent inhibitor with an and ofATM IC50 Ki129 and 22 nM respectively and is highly selective for ATMas compared to DNA-PK PI3KPI4K ATR and mTOR

Bioactivity KU-60019 is an improved kinase-specific inhibitor withATM of 63 nMIC50

Bioactivity VE-821 is a potent ATP-competitive inhibitor of with ATR Ki of 13 nM26 nMIC50

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

CGK733 Cat No HY-15520

CP-466722 Cat No HY-11002

ETP-46464 Cat No HY-15521

KU 59403 Cat No HY-18650

KU-55933 Cat No HY-12016

KU-60019 Cat No HY-12061

VE-821 Cat No HY-14731

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

Aurora Kinase

Aurora kinases are serinethreonine kinases that are essential for cellproliferation Aurora kinase helps the dividing cell dispense its geneticmaterials to its daughter cells More specifically Aurora kinases play acrucial role in cellular division by controlling chromatid segregationDefects in this segregation can cause genetic instability a conditionwhich is highly associated with tumorigenesis Three Aurora kinaseshave been identified in mammalian cells to date Aurora A Aurora BAurora C Besides being implicated as mitotic regulators these threekinases have generated significant interest in the cancer research fielddue to their elevated expression profiles in many human cancers Thehuman Aurora kinases present a similar domain organization with a

N-terminal domain of 39 to 129 residues in length a protein kinase domain and a short C-terminal domain containing15 to 20 residues The N-terminal domain of three proteins share low sequence conservation which determinesselectivity during protein-protein interactions

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Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9895Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9874Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Aurora Kinase Inhibitors amp Modulators

Bioactivity Alisertib (MLN 8237) is an oral active and selective Aurora A inhibitor with an of 12 nMkinase IC50

Bioactivity AMG 900 is a potent and highly selective kinasespan-Aurorainhibitor with of 5 nM 4 nM and 1 nM for IC50 Aurora A B

and respectivelyC

Bioactivity AT9283 is a multitargeted kinase inhibitor which potentlyinhibits ( =12 nM 11 nM)aurora kinase AB JAK23 IC50

Bioactivity Aurora A inhibitor I is a potent and highly selective Aurora inhibitor with with an of 34 nMA IC50

Bioactivity Aurora B inhibitor 1 is an (Aurora-1) inhibitorAurora Bextracted from patent WO2007059299A1 compound 1-3 has a Kivalue of lt0010 uM

Bioactivity Aurora inhibitor 1 is a potent inhibitor with an Aurora IC50of le 4 nM and le13 nM for and kinaseAurora A Aurora Brespectively [1]

Bioactivity AZD1152 is a pro-drug of Barasertib-hQPA which is a highlyselective inhibitor with of 037 nM in aAurora B IC50cell-free assay

Bioactivity AZD1152-HQPA is a highly selective Aurora inhibitor with an of 037 nM in aB IC50

cell-free assay and shows 3700-fold selectivity for Aurora Bover Aurora A

Bioactivity BI-847325 is an ATP competitive dual inhibitor of andMEKaurora kinases ( ) with values of 4 and 15 nM forAK IC50human MEK2 and AK-C respectively

Bioactivity CCT 137690 is a potent and orally available kinaseaurorainhibitor with s of 15 25 and 19 nM for aurora A B andIC50C respectively

Alisertib (MLN 8237) Cat No HY-10971

AMG 900 Cat No HY-13253

AT9283 Cat No HY-50514

Aurora A inhibitor I Cat No HY-70061

Aurora B inhibitor 1 Cat No HY-U00304

Aurora inhibitor 1 Cat No HY-111506

AZD1152 (Barasertib) Cat No HY-10127

Barasertib-HQPA (AZD2811 INH-34 AZD1152-HQPA) Cat No HY-10126

BI-847325 Cat No HY-18955

CCT 137690 Cat No HY-10804

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 1 mg 5 mg 10 mg 20 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9859Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9923Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9944Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data Phase 1Size 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 950Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity CCT129202 is an kinase inhibitor with s of 42aurora IC50198 and 227 nM for aurora A B and C respectively

Bioactivity CCT241736 is a potent and orally bioavailable dual andFLT3 inhibitor which inhibits Aurora kinasesAurora kinase

(Aurora-A 75 nM 38 nM Aurora-B 48 nM)Kd IC50 KdFLT3 kinase ( 62 nM) and FLT3 mutants includhellipKd

Bioactivity CYC-116 is a potent and inhibitor withaurora A aurora Bs of 8 and 9 nM respectivelyKi

Bioactivity Danusertib is a pyrrolo-pyrazole and inhibitoraurora kinasewith of 13 79 and 61 nM for Aurora A B and CIC50respectively

Bioactivity ENMD-2076 is a multi-targeted kinase inhibitor with s ofIC50186 14 582 159 927 708 564 nM for Aurora A Flt3

KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src PDGFRαrespectively

Bioactivity ENMD-2076 Tartrate is a multi-targeted kinase inhibitor withs of 186 14 582 159 927 708 564 nM for IC50 Aurora

A Flt3 KDRVEGFR2 Flt4VEGFR3 FGFR1 FGFR2 Src respectivelyPDGFRα

Bioactivity GSK-1070916 is a potent and selective ATP-competitiveinhibitor of and with s of 038 andaurora B aurora C Ki15 nM respectively and is gt250- fold selective overAurora A

Bioactivity Hesperadin is an ATP-competitive inhibitor of aurora Bkinase with an of 250 nMIC50

Bioactivity Ilorasertib (ABT-348) is an ATP-competitive multitargetedkinase inhibitor with s for inhibiting binding Aurora B (7IC50nM) C (1 nM) and A (120 nM) and also inhibits RET tyrosinekinase PDGFRβ and Flt1 with s of 7 nM 3 nM and 32 nMIC50

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

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CCT129202 Cat No HY-12049

CCT241736 Cat No HY-18161

CYC-116 Cat No HY-10558

Danusertib (PHA-739358) Cat No HY-10179

ENMD-2076 Cat No HY-10987A

ENMD-2076 Tartrate Cat No HY-10987

GSK-1070916 (GSK-1070916A) Cat No HY-70044

Hesperadin Cat No HY-12054

Ilorasertib (ABT-348) Cat No HY-16018

JNJ-7706621 Cat No HY-10329

wwwMedChemExpresscom 15

Purity 9820Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9928Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9911Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity KW-2449 is a multi-targeted kinase inhibitor of FLT3 ABL and with s of 66 14 4 and 48 nMABLT315I Aurora kinase IC50

respectively

Bioactivity LY3295668 is a potent orally active and highly specific inhibitor with values of 08 nM and 1038Aurora-A kinase Ki

nM for AurA and AurB respectively

Bioactivity MK-5108 is a highly potent and specific inhibitor of Aurora A with an value of 0064 nMkinase IC50

Bioactivity MK-8745 is an kinase inhibitor with an of 06aurora A IC50nM

Bioactivity MLN8054 is a potent selective and orally available aurora Akinase inhibitor with an of 4 nMIC50

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity PF-03814735 is a potent orally available and reversible and inhibitor with s of 08 and 05aurora A aurora B IC50

nM respectively

Bioactivity PHA-680632 is an kinase inhibitor with s of 27aurora IC50135 and 120 nM for aurora A B and C respectively

Bioactivity Reversine is a novel class of ATP-competitive Aurora kinaseinhibitor with s of 400 500 and 400 nM for IC50 Aurora A

and respectivelyAurora B Aurora C

Bioactivity SCH-1473759 is an inhibitor with s of 4 and 13 nMaurora IC50for aurora A and B respectively

KW-2449 Cat No HY-10339

LY3295668 (AK-01) Cat No HY-114258

MK-5108 (VX-689) Cat No HY-13252

MK-8745 Cat No HY-13819

MLN8054 Cat No HY-10180

NU6140 Cat No HY-107419

PF-03814735 Cat No HY-14574

PHA-680632 Cat No HY-10178

Reversine Cat No HY-14711

SCH-1473759 Cat No HY-10482

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg

Purity 9980Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9981Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity SCH-1473759 hydrochloride is an inhibitor with saurora IC50of 4 and 13 nM for aurora A and B respectively

Bioactivity SNS-314 is a potent and selective kinase inhibitoraurorawith s of 9 31 and 6 nM for aurora A B and CIC50respectively

Bioactivity TAK-632 is a potent inhibitor with of 14 24pan-RAF IC50

and 83 nM for respectivelyCRAF BRAFV600E BRAFWT

Bioactivity TAK-901 is a multi-targeted inhibitor with s of 21aurora IC50and 15 nM for aurora A and B respectively

Bioactivity Tozasertib (VX 680 MK-0457) is an inhibitor of Aurora ABC with s of 06 18 46 nM respectivelykinases Ki

Bioactivity XL228 is a multi-targeted tyrosine kinase inhibitor with sIC50of 5 31 16 61 2 nM for Bcr-Abl Aurora A IGF-1R Srcand respectivelyLyn

Bioactivity ZM-447439 is an kinase inhibitor with s of 110 andaurora IC50130 nM for aurora A and B respectively

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SCH-1473759 hydrochloride Cat No HY-10483

SNS-314 (SNS-314 Mesylate) Cat No HY-12003

TAK-632 Cat No HY-15767

TAK-901 Cat No HY-12201

Tozasertib (VX 680 MK-0457) Cat No HY-10161

XL228 Cat No HY-15749

ZM-447439 Cat No HY-10128

wwwMedChemExpresscom 17

Casein Kinase

Casein Kinases (CKs) are serinethreonine-selective enzymes thatfunction as regulators of signal transduction pathways in mosteukaryotic cell types

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9967Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9992Clinical Data Phase 2Size 1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Casein Kinase Inhibitors amp Modulators

Bioactivity Casein Kinase II Inhibitor IV is a small-molecule inducer ofepidermal keratinocyte differentiation

Bioactivity Casein Kinase II Inhibitor IV Hydrochloride is asmall-molecule inducer of epidermal keratinocytedifferentiation

Bioactivity CK1-IN-1 is a inhibitor extracted fromcasein kinase 1 (CK1)patent WO2015119579A1 compound 1c has s of 15 nM 16 nMIC50

73 nM for CK1δ and CK1ε p38σ MAPK respectively [1]

Bioactivity D4476 is a potent selective and cell-permeable inhibitor ofcasein kinase 1( ) with an value of 03 μM CK1 IC50 in vitro

Bioactivity DMAT is a potent and specific inhibitor with an CK2 IC50value of 130 nM

Bioactivity Ellagic acid is a natural antioxidant and acts as a potentand ATP-competitive inhibitor with an of 40 nM andCK2 IC50a of 20 nMKi

Bioactivity Emodin is a broad-spectrum anticancer agent Emodin inhibits II (CKII) activity with of 2 μMcasein kinase IC50

Bioactivity IC261 is a selective ATP-competitive inhibitor withCK1s of 1 μM 1 μM 16 μM for and Ckiα1IC50 Ckiδ Ckiε

respectively

Bioactivity LH846 is a selective inhibitor of with an of 290 nMCKIδ IC50and less potently inhibits CKIα and CKIε with s of 25 μMIC50and 13 μM respectively

Bioactivity Longdaysin is a and CK1α CK1δ extracellular inhibitor with s of  56signal-regulated kinase 2 (ERK2) IC50

microM 88 microM and 52 microM respectively [1] [2]

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Casein Kinase II Inhibitor IV Cat No HY-111378

Casein Kinase II Inhibitor IV Hydrochloride Cat No HY-111378A

CK1-IN-1 Cat No HY-111820

D4476 (Casein Kinase I Inhibitor) Cat No HY-10324

DMAT (Casein kinase II Inhibitor CK2 Inhibitor) Cat No HY-15535

Ellagic acid Cat No HY-B0183

Emodin (Frangula emodin) Cat No HY-14393

IC261 Cat No HY-12774

LH846 Cat No HY-15704

Longdaysin Cat No HY-18285

wwwMedChemExpresscom 19

Purity 9701Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9827Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Bioactivity NCC007 is a dual and inhibitorcasein kinase Iα (CKIα) δ (CKIδ)with s of 18 and 36 μM respectively and can be used inIC50

research of modulating mammalian circadian rhythms [1]

Bioactivity PF-4800567 is a potent and selective inhibitor of caseinkinase 1ϵ ( ) with an of 32 nM which is greaterCK1ϵ IC50than 20-fold selectivity over CK1δ ( 711 nM)IC50

Bioactivity PF-670462 is a potent and selective inhibitor of casein kinase with s of 77 nM and 14 nM( and )CK1ε CK1δ IC50

respectively

Bioactivity Silmitasertib (CX-4945) is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity Silmitasertib sodium salt is an orally bioavailable highlyselective and potent inhibitor with values of 1 nMCK2 IC50against CK2α and CK2α

Bioactivity SR-3029 is a potent and ATP competitive and CK1δ CK1εinhibitor with s of 44 nM and 260 nM respectively andIC50

s of 97 nM for both kinasesKi

Bioactivity TA-01 is a potent and inhibitor with sCK1 p38 MAPK IC50of 64 nM 68 nM 67 nM for CK1ε CK1δ and p38 MAPKrespectively

Bioactivity TBB is a cell-permeable and ATP-competitive inhibitorCK2with an of 015 μM for rat liver CK2IC50

Bioactivity TTP 22 is a potent inhibitor with an of 100 nM andCK2 IC50a of 40 nMKi

NCC007 Cat No HY-128677

PF-4800567 Cat No HY-12470

PF-670462 Cat No HY-15490

Silmitasertib (CX-4945) Cat No HY-50855

Silmitasertib sodium salt (CX-4945 (sodium salt)) Cat No HY-50855B

SR-3029 Cat No HY-100011

TA-01 Cat No HY-100114

TBB (NSC 231634 Casein Kinase II Inhibitor I) Cat No HY-14394

TTP 22 Cat No HY-15479

CDKCyclin dependent kinase

CDKs (Cyclin-dependent kinases) are serine-threonine kinases firstdiscovered for their role in regulating the cell cycle They are alsoinvolved in regulating transcription mRNA processing and thedifferentiation of nerve cells CDKs are relatively small proteins withmolecular weights ranging from 34 to 40 kDa and contain little morethan the kinase domain In fact yeast cells can proliferate normallywhen their CDK gene has been replaced with the homologous humangene By definition a CDK binds a regulatory protein called a cyclinWithout cyclin CDK has little kinase activity only the cyclin-CDKcomplex is an active kinaseThere are around 20 Cyclin-dependent kinases (CDK1-20) known till

date CDK1 4 and 5 are involved in cell cycle and CDK 7 8 9 and 11 are associated with transcriptionCDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational Mostknowledge of CDK structure and function is based on CDKs of (Cdc2) (CDC28) and vertebratesS pombe S cerevisia(CDC2 and CDK2) The four major mechanisms of CDK regulation are cyclin binding CAK phosphorylation regulatoryinhibitory phosphorylation and binding of CDK inhibitory subunits (CKIs)

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wwwMedChemExpresscom 21

Purity 9815Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9969Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9973Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

CDK Inhibitors amp Modulators

Bioactivity (+)-BAY-1251152 is a inhibitor extracted from patent WOCDK92014076091 A1 example 1

Bioactivity (-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation(-) BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity (plusmn)-BAY-1251152 is a racemic mixture of BAY-1251152BAY-1251152 is a potent and highly selective PTEFCDK9inhibitor

Bioactivity 5-Iodo-indirubin-3-monoxime is a potent GSK-3β CDK5P25and inhibitor competing with ATP for binding toCDK1cyclin Bthe catalytic site of the kinase with s of 9 20 and 25IC50

nM respectively [1]

Bioactivity Abemaciclib (LY2835219) is a selective inhibitor withCDK46 values of 2 nM and 10 nM for CDK4 and CDK6 respectivelyIC50

Bioactivity Abemaciclib Metabolites M2 is a metabolite of abemaciclibacts as a potent and inhibitor with s in theCDK4 CDK6 IC50

range of 1-3 nM Anti-cancer activity [1]

Bioactivity Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is aselective inhibitor with s of 2 nM and 10 nM forCDK46 IC50CDK4 and CDK6 respectively

Bioactivity AMG 925 is a potent selective and orally available FLT3 dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMCDK4 IC50

respectively

Bioactivity AMG 925 HCl is a potent selective and orally available dual inhibitor with s of 2plusmn1 nM and 3plusmn1 nMFLT3 CDK4 IC50

respectively

Bioactivity AT7519 as a potent inhibitor of with s of 210 47CDKs IC50100 13 170 and lt10 nM for CDK1 CDK2 CDK4 to CDK6 andCDK9 respectively

(+)-BAY-1251152 Cat No HY-103019

(-)-BAY-1251152 Cat No HY-103019B

(plusmn)-BAY-1251152 Cat No HY-103019A

5-Iodo-indirubin-3-monoxime Cat No HY-111930

Abemaciclib (LY2835219) Cat No HY-16297A

Abemaciclib Metabolites M2 Cat No HY-128669

Abemaciclib methanesulfonate (LY2835219 (methanesulfonate)) Cat No HY-16297

AMG 925 Cat No HY-15889

AMG 925 HCl Cat No HY-15889A

AT7519 Cat No HY-50940

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9984Clinical Data Phase 1Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9999Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9700Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9848Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9816Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity AT7519 Hydrochloride is a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity AT7519 trifluoroacetate as a potent inhibitor of withCDKss of 210 47 100 13 170 and lt10 nM for CDK1 CDK2IC50

CDK4 to CDK6 and CDK9 respectively

Bioactivity Atuveciclib (BAY-1143572) is a potent and highly selectiveoral inhibitor Atuveciclib (BAY-1143572)PTEFb CDK9inhibits with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib Racemate (BAY-1143572 Racemate) is the racematemixture of Atuveciclib Atuveciclib is a potent and highlyselective oral inhibitor which supressesP-TEFb CDK9

with an of 13 nMCDK9 CycT1 IC50

Bioactivity Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is apotent and selective inhibitor which inhibits CDK9 CDK9

with an of 16 nMCycT1 IC50

Bioactivity AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 82nM AUZ 454 (K03861) inhibits CDK2 activity by competing withbinding of activating cyclins

Bioactivity AZD-5438 is a potent inhibitor of with of 16CDK129 IC50nM6 nM20 nM in cell-free assays AZD-5438 shows lessinhibition activity against GSK3β CDK5 and CDK6

Bioactivity AZD4573 is a inhibitor with an of lt3 nMCDK9 IC50extracted from patent US 20160376287 A1 example 14

Bioactivity BGG463 is a inhibitorCDK2 Bioactivity BI-1347 is a potent inhibitor extracted from patentCDK8WO2017202719A1 product I-003 has an of 11 nM IC50

[1]

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AT7519 Hydrochloride Cat No HY-50943

AT7519 trifluoroacetate Cat No HY-50940A

Atuveciclib (BAY-1143572) Cat No HY-12871B

Atuveciclib Racemate (BAY-1143572 Racemate) Cat No HY-12871

Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) Cat No HY-12871C

AUZ 454 (K03861) Cat No HY-15004

AZD-5438 Cat No HY-10012

AZD4573 Cat No HY-112088

BGG463 Cat No HY-100600

BI-1347 Cat No HY-120350

wwwMedChemExpresscom 23

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9754Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9747Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity BMS-265246 is a potent and selective CDK12 inhibitor forCDK1cyclin B and CDK2cyclin E with IC50 of 6 nM and 9 nMrespectively

Bioactivity BS-181 is a highly selective inhibitor with an ofCDK7 IC5021 nM showing 40-fold selective over CDK1 2 4 5 6 or 9

Bioactivity BS-181 hydrochloride is a highly selective inhibitorCDK7with of 21 nM and gt 40-fold selective for CDK7 thanIC50CDK1 2 4 5 6 or 9

Bioactivity BSJ-03-123 is a potent and novel -selective small-moleculeCDK6degrader

Bioactivity Ca channel agonist 1 is an agonist of 2+ N-type Ca channel2+

and an inhibitor of with s of 1423 μM and 334Cdk2 EC50μM respectively and is used as a potential treatment formotor nerve terminal dysfunction

Bioactivity CC-671 is a dual ( )TTK protein kinase CDC2-like kinase CLK2inhibitor with s of 0005 and 0006 μM for TTK and CLK2IC50respectively

Bioactivity CCT-251921 is a potent selective and orally bioavailable inhibitor with an of 23 nMCDK8 IC50

Bioactivity CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 oflt8 nM extracted from reference 1 example 4 IC50 Valuelt8 nM [1] Target CDK9 In vitro In vivo

Bioactivity CDK46-IN-2 is a potent and inhibitor extractedCDK4 CDK6from patent US20180000819A1 Compound 1 has s of 27 andIC50

16 nM for CDK4 and CDK6 respectively [1]

Bioactivity CDK461 Inhibitor is a inhibitor with s of 3 andCDK46 IC501 nM respectively

BMS-265246 Cat No HY-15275

BS-181 Cat No HY-13266

BS-181 hydrochloride Cat No HY-13266A

BSJ-03-123 Cat No HY-111556

Ca2+ channel agonist 1 Cat No HY-41076

CC-671 Cat No HY-108709

CCT-251921 Cat No HY-19984

CDK-IN-2 (CDK inhibitor II) Cat No HY-13033

CDK46-IN-2 Cat No HY-114339

CDK461 Inhibitor Cat No HY-112280

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9548Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CDK8-IN-1 is a potent and selective inhibitor with anCDK8 of 3 nMIC50

Bioactivity CDK8-IN-3 is an inhibitor of extracted from patentCDK8WO2016041618A1 compound example 17

Bioactivity CDK8-IN-4 is an inhibitor of extracted from patentCDK8WO2014090692A1 compound example 16 with an of 02 nMIC50

Bioactivity CDK819-IN-1 is a potent selective and oral bioavailable dual inhibitor with s of 046 nM 099 nM andCDK819 IC50

270 nM for CDK8 CDK19 and CDK9 respectively

Bioactivity CDK9 Antagonist-1 (compounds 11c) is a potent and selective degrader based on PROTAC with an of 17 μM in MCF-7CDK9 IC50

cell lines Natural product Wogonin binds ubiquitin E3 ligasecereblon (CRBN) via a linker to form PROTAC [1]

Bioactivity CDK9-IN-1 is a novel selective inhibitor for theCDK9treatment of HIV infection with an of 39 nM forIC50CDK9CycT1 extracted from reference compound 87

Bioactivity CDK9-IN-2 is a special cyclin-dependent kinase 9 ( )CDK9inhibitor extracted from patent WO2012131594A1 compoundCDKI(8) has an of 5 nM and 7 nM in H929 multipleIC50myeloma(MM) cell line (72 hours) and A2058 skin cell line (72hours) respectively

Bioactivity CDK9-IN-8 is a highly effective and selective inhibitorCDK9with an of 12 nMIC50

Bioactivity CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM showsselective toxicity to CLL cells(LD50=80 nM) versus normal Bcell and normal CD34+ cell(LD50gt20 uM) IC50 value 4 nM80nM(KiLD50) [1] Target CDK9 inhibitor in vitro CDKI-73 wascytotoxic to all of the CLL samples tested (n = 38) with ahellip

Bioactivity CLK1-IN-1 is a potent and selective of Cdc2-like kinase 1 () inhibitor with an IC of 2 nMCLK1 50

24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CDK8-IN-1 Cat No HY-103492

CDK8-IN-3 Cat No HY-111463

CDK8-IN-4 Cat No HY-111465

CDK819-IN-1 Cat No HY-111427

CDK9 Antagonist-1 Cat No HY-112811

CDK9-IN-1 Cat No HY-13231

CDK9-IN-2 Cat No HY-16462

CDK9-IN-8 Cat No HY-102039

CDKI-73 Cat No HY-12445

CLK1-IN-1 Cat No HY-103082

wwwMedChemExpresscom 25

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9900Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9973Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9998Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity CMPD 7 is a potent and selective inhibitor with an CDK12 IC50of 491 nM in enzymatic assay

Bioactivity CT7001 hydrochloride is a selective inhibitor withCDK7s of 41 nM and 578 nM for andIC50 CDK7CycHMAT1

respectivelyCDK2cycE1

Bioactivity Cucurbitacin E is a natural compound which from the climbingstem of Cucurbitacin E significantlyCucumic melo Lsuppresses the activity of the complexcyclin B1 CDC2

Bioactivity CVT-313 is a potent selective reversible andATP-competitive inhibitor of with of 05 μMCDK2 IC50

Bioactivity CYC065 is a second-generation orally availableATP-competitive inhibitor of kinasesCDK2 CDK 9

Bioactivity Dinaciclib is a potent inhibitor of with s of 1 1CDK IC503 and 4 nM for and respectivelyCDK2 CDK5 CDK1 CDK9

Bioactivity EHT 5372 is a strong inhibitor of family kinases withDYRKrsquos of 022 028 nM for DYRK1A and DYRK1B respectivelyIC s50

Bioactivity Flavopiridol is a broad spectrum and competitive inhibitor of inhibiting CDK1 CDK2 CDK4 with s of 30 170 100CDKs IC50

nM respectively

Bioactivity Flavopiridol Hydrochloride is a broad inhibitor of CDKcompeting with ATP to inhibit CDKs including CDK1 CDK2 CDK4with s of 30 170 100 nM respectivelyIC50

Bioactivity FMF-04-159-2 is a covalent inhibitor FMF-04-159-2CDK14inhibits CDK14 and CDK2 with s of 396 nM and 256 nM inIC50

NanoBRET assay respectively [1]

CMPD 7 Cat No HY-112261

CT7001 hydrochloride (ICEC0942 hydrochloride) Cat No HY-103712A

Cucurbitacin E (α-Elaterin α-Elaterine) Cat No HY-N0417

CVT-313 (Cdk2 Inhibitor III) Cat No HY-15339

CYC065 Cat No HY-101212

Dinaciclib (SCH 727965) Cat No HY-10492

EHT 5372 Cat No HY-111380

Flavopiridol (L868275 HMR-1275 Alvocidib) Cat No HY-10005

Flavopiridol Hydrochloride (HL 275 NSC 649890 MDL 107826A

FLAVOPIRIDOL HCL Alvocidib Hydrochloride) Cat No HY-10006

FMF-04-159-2 Cat No HY-127104

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9204Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9880Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 251 mg 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9841Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity FN-1501 is a potent inhibitor of and with s ofFLT3 CDK IC50247 085 196 and 028 nM for CDK2cyclin A CDK4cyclinD1 CDK6cyclin D1 and FLT3 respectively FN-1501 hasanticancer activity

Bioactivity GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO) is apotent selective reversible and ATP-competitive inhibitor of

and complex with s of 5 nM320GSK-3αβ CDK1-cyclinB IC50nM80nM for (GSK-3αβ)CDK1CDK5 respectively

Bioactivity GSK3186899 is an inhibitor of cdc-2-related kinase 12 () with an of 14 μM for in anCRK12 EC50 L donovani

intra-macrophage assay

Bioactivity IIIM-290 is a potent and oral inhibitor with s of 90CDK IC50and 94 nM for CDK2A and CDK9T1

Bioactivity Indirubin-3-monoxime-5-sulphonic acid is a potent andselective inhibitor of and with s ofCDK1 CDK5 GSK-3β IC50

5 nM 7 nM and 80 nM respectively [1]

Bioactivity Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK)inhibitor with values of 55 nM 35 nM 150 nM 300 nMIC50and 65 nM for CDK1cyclin B CDK2cyclin A CDK2cyclin ECDK4cyclin D1 and CDK5p35 respectively [1]

Bioactivity JH-XI-10-02 is a potent and selective degrader of withCDK8an of 159 nM based on JH-XI-10-02 causesIC50 PROTAC

proteasomal degradation does not affect CDK8 mRNA levelsJH-XI-10-02 shows no effect on CDK19 [1]

Bioactivity JNJ-7706621 is a potent inhibitor and alsoaurora kinaseinhibits and with s of 9 3 11 and 15 nMCDK1 CDK2 IC50for CDK1 CDK2 Aurora-A and Aurora-B respectively

Bioactivity JSH-150 is a highly selective and potent inhibitor withCDK9an IC of 1 nM50

Bioactivity Kenpaullone is a potent inhibitor of andCDK1cyclin B with s of 04 μM and 23 nM and also inhibitsGSK-3β IC50

CDK2cyclin A CDK2cyclin E and CDK5p25 with s of 068IC50μM 75 μM 085 μM respectively

26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

FN-1501 Cat No HY-111361

GSK 3 Inhibitor IX (6-Bromoindirubin-3-oxime BIO MLS 2052) Cat No HY-10580

GSK3186899 (DDD-853651) Cat No HY-112622

IIIM-290 Cat No HY-111356

Indirubin-3-monoxime-5-sulphonic acid Cat No HY-111931

Indirubin-5-sulfonate Cat No HY-111932

JH-XI-10-02 Cat No HY-111518

JNJ-7706621 Cat No HY-10329

JSH-150 Cat No HY-X0150

Kenpaullone (9-Bromopaullone NSC-664704) Cat No HY-12302

wwwMedChemExpresscom 27

Purity 9861Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9847Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Bioactivity KH-CB19 is a potent and highly specific inhibitor of theCDC2-like kinase isoforms 1 and 4 (CLK1CLK4) IC50 value 20nM (CLK1) [1] Target CLK14 inhibitor in vitro KH-CB19showed potent inhibition of CLK1 with an IC50 of 20 nM andfor the pure isomer KH-CB19 almost 100-fold selectivityhellip

Bioactivity LDC000067 is a highly specific inhibitor with an CDK9 IC50value of 44plusmn10 nM in vitro

Bioactivity LDC4297 is a potent and selective inhibitor with an CDK7 IC50of 013 nM

Bioactivity Lerociclib (G1T38) is a potent and selective inhibitor of with of 1 nM 2 nM for CDK4CyclinD1 andCDK46 IC s50

CDK6CyclinD3 respectively

Bioactivity Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potentand selective inhibitor of with of 1 nMCDK4 CDK6 IC s50and 2 nM for and respectivelyCDK4 CyclinD1 CDK6 CyclinD3

Bioactivity LY2857785 is a type I reversible and competitive ATP kinaseinhibitor against ( 11 nM) and other transcriptionCDK9 IC50kinases ( 16 nM) and ( 246 nM)CDK8 IC50 CDK7 IC50

Bioactivity LY3177833 is an and inhibitor extracted fromCDC7 pMCM2patent US 20140275131and patent WO 2014143601 A1 compoundexample 4 has values of 33 nM and 290 nM respectivelyIC50

Bioactivity MBQ-167 is a dual inhibitor with of 103 nMRacCdc42 IC s50for Rac 123 and 78 nM for Cdc42 in MDA-MB-231 cellsrespectively

Bioactivity MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin inhibitor with an of 5 nM at least 22-fold moreT1 IC50

selective for CDK9 over other CDKs MC180295 also inhibitsGSK-3α and GSK-3β MC180295 ((rel)-MC180295) has pothellip

Bioactivity Milciclib (PHA-848125) is a potent dual inhibitor of andCDK with s of 45 150Tropomyosin receptor kinase (TRK) IC50

160 363 398 nM and 53 nM for cyclin ACDK2 cyclin HCDK7cyclin D1CDK4 cyclin ECDK2 cyclin BCDK1 and TRKArespectively

KH-CB19 Cat No HY-12828

LDC000067 (LDC067) Cat No HY-15878

LDC4297 Cat No HY-12653

Lerociclib (G1T38) Cat No HY-112272

Lerociclib dihydrochloride (G1T38 dihydrochloride) Cat No HY-112272A

LY2857785 Cat No HY-12293

LY3177833 Cat No HY-100023

MBQ-167 Cat No HY-112842

MC180295 ((rel)-MC180295) Cat No HY-119940

Milciclib (PHA-848125) Cat No HY-10424

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9703Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 5 mg

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9851Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Bioactivity ML167 is a highly selective Cdc2-like kinase 4 ( )Clk4inhibitor with of 136 nM gt10-fold selectivity forIC50closely related kinases Clk1 Clk2 Clk3 and Dyrk1A1B

Bioactivity MSC2530818 is a potent selective and orally available CDK8inhibitor with an of 26 nM for CDK8IC50

Bioactivity NG 52 (Compound 52 ) is a potent cell-permeable reversibleselective and ATP-compatible inhibitor of the cellcycle-regulating kinase Cdc28p (IC50 = 7 μM) and the relatedPho85p kinase (IC50 = 2 μM)

Bioactivity Nimbolide is a triterpene derived from the leaves and flowersof neem ( L) Nimbolide induces apoptosisAzadirachta indicathrough inactivation of Nimbolide inhibits NF-κB CDK4

kinase activity Nimbolide suppresses the NF-κB WntCDK6PI3K-Akt MAPK and JAK-STAT signaling pathways [1]

Bioactivity NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and26 μM for CDK2 and CDK1 IC50 value 17μM (CDK2) 26μM (CDK1)Target CDK in vitro NU2058 is a competitive inhibitor ofCDK2 with respect to ATP (Ki value CDK2 12 3 μM) that bindsin the ATP binding pocket in a different orientation fromhellip

Bioactivity NU6140 is a selective inhibitor ( 041CDK2-cyclin A IC50

μM) exhibits 10- to 36-fold selectivity over other CDKs [1]

NU6140 also potently inhibits and withAurora A Aurora Bs of 67 and 35 nM respectively Enhances hellipIC50

[2]

Bioactivity NU6300 is the first covalent ATP-competitive CDK2 inhibitorIC50 value Target CDK2 in vitro NU6300 is a covalent CDK2inhibitor that illustrates the potential of using vinylsulfones to mediate irreversible inhibition NU6300 blocks theinhibitor binding site The effect was time dependent andhellip

Bioactivity NVP-2 is a inhibitor with an of 05 nMCDK9 IC50

Bioactivity NVP-LCQ195 (AT9311 LCQ195) is a small molecule heterocyclicinhibitor of CDK1 CDK2 CDK3 and CDK5 with IC50 of 1-42 nM

Bioactivity ON-013100 an antineoplastic drug acts a mitotic inhibitorthat could inhibit expressionCyclin D1

28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

ML167 (CID44968231 NCGC00188654) Cat No HY-15951

MSC2530818 Cat No HY-101611

NG 52 (Compound 52) Cat No HY-15154

Nimbolide Cat No HY-116035

NU2058 (O6-(Cyclohexylmethyl)guanine) Cat No HY-19316

NU6140 Cat No HY-107419

NU6300 Cat No HY-18930

NVP-2 Cat No HY-12214A

NVP-LCQ195 (LCQ-195 AT9311) Cat No HY-15241

ON-013100 Cat No HY-112822

wwwMedChemExpresscom 29

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9996Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity ON123300 is a potent inhibitor of CDK4 with an IC50 of 38nM with little inhibitory activity against CDKs 125 and 8

Bioactivity Palbociclib (PD 0332991) is a selective and CDK4 CDK6inhibitor with s of 11 and 16 nM respectivelyIC50Palbociclib is a drug for the treatment of ER-positive andHER2-negative breast cancer

Bioactivity Palbociclib hydrochloride is a highly selective CDK46inhibitor with s of 11 nM and 16 nM respectivelyIC50

Bioactivity Palbociclib isethionate is a highly selective inhibitorof with s of 11 nM16 nMCDK46 IC50respectively

Bioactivity PF-06873600 is a selective and orally bioavailable inhibitorof cyclin-dependent kinase with values of 009 nM(CDK) Ki013 nM and 016 nM for CDK2 CDK4 and CDK6 respectivelyPF-06873600 has potential antineoplastic activity [1] [2]

Bioactivity PHA-767491 is a dual inhibitor with s of 10 nMCdc7Cdk9 IC50and 34 nM respectively

Bioactivity PHA-767491 hydrochloride is a dual inhibitor withCdc7Cdk9s of 10 nM and 34 nM respectivelyIC50

Bioactivity PHA-793887 is a potent ATP-competitive inhibitor canCDKinhibit Cdk2 Cdk1 Cdk4 and Cdk9 with s of 8 nM 60 nMIC5062 nM and 138 nM respectively and also inhibits glycogensynthase kinase 3β with an of 79 nMIC50

Bioactivity PROTAC CDK9 Degrader-1 is a selective degraderCDK9 Bioactivity Purvalanol A is a potent inhibitor which inhibitsCDKcdc2-cyclin B cdk2-cyclin A cdk2-cyclin E cdk4-cyclin D1and cdk5-p35 with s of 4 70 35 850 75 nMIC50resepctively

ON123300 Cat No HY-12624

Palbociclib (PD 0332991) Cat No HY-50767

Palbociclib hydrochloride (PD 0332991 hydrochloride) Cat No HY-50767A

Palbociclib isethionate (PD 0332991 isethionate) Cat No HY-A0065

PF-06873600 Cat No HY-114177

PHA-767491 (CAY10572) Cat No HY-13461

PHA-767491 hydrochloride (CAY-10572 hydrochloride) Cat No HY-13461A

PHA-793887 Cat No HY-11001

PROTAC CDK9 Degrader-1 Cat No HY-103628

Purvalanol A (NG-60) Cat No HY-18299A

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9900Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9983Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitorwith IC50 values of 6 6 9 gt 10000 and 6 nM forcdc2cyclin B cdk2cyclin A cdk2cyclin E cdk4cyclin D1and cdk5-p35 respectively

Bioactivity R547 is a potent ATP-competitive inhibitor of CDK124 with Kiof 2 nM3 nM1 nM

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2

and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip

Bioactivity Ribociclib (LEE011) is a highly specific inhibitorCDK46with s of 10 nM and 39 nM respectivelyIC50

Bioactivity Ribociclib hydrochloride (LEE011 hydrochloride) is a highlyspecific inhibitor with values of 10 nM and 39CDK46 IC50nM respectively and is over 1000-fold less potent againstthe cyclin BCDK1 complex

Bioactivity Ribociclib succinate (LEE011 succinate) is a highly specific inhibitor with values of 10 nM and 39 nMCDK46 IC50

respectively and is over 1000-fold less potent against thecyclin BCDK1 complex

Bioactivity Ribociclib succinate hydrate (LEE011 succinate hydrate) is ahighly specific inhibitor with values of 10 nMCDK46 IC50and 39 nM respectively and is over 1000-fold less potentagainst the cyclin BCDK1 complex

Bioactivity Riviciclib (P276-00 free base) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib shows antituhellip[1] [2]

Bioactivity Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1

and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50

and 79 nM respectively Riviciclib hydrochlorhellip[1] [2]

30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Purvalanol B (NG 95) Cat No HY-18299

R547 Cat No HY-10014

RGB-286638 Cat No HY-15504

RGB-286638 free base Cat No HY-15504A

Ribociclib (LEE011) Cat No HY-15777

Ribociclib hydrochloride (LEE011 (hydrochloride)) Cat No HY-15777A

Ribociclib succinate (LEE011 (succinate)) Cat No HY-15777B

Ribociclib succinate hydrate (LEE011 (succinate hydrate)) Cat No HY-15777C

Riviciclib (P276-00 (free base)) Cat No HY-16559A

Riviciclib hydrochloride (P276-00) Cat No HY-16559

wwwMedChemExpresscom 31

Purity 9850Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9907Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9677Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ro-3306 is a potent and selective inhibitor of with sCDK1 Kiof 20 nM 35 nM and 340 nM for CDK1 CDK1cyclin B1 andCDK2cyclin E respectively

Bioactivity Roniciclib is an orally bioavailable pan-cyclin dependentkinase inhibitor with of 5-25 nM for CDK1 CDK2(CDK) IC s50CDK3 CDK4 CDK7 and CDK9

Bioactivity SB1317 is a potent inhibitor of and forCDK2 JAK2 FLT3the treatment of cancer with of 13 73 and 56 nM forIC50CDK2 JAK2 and FLT3 respectively

Bioactivity SEL120-34A is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A HCl is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity

Bioactivity SEL120-34A monohydrochloride is an ATP-competitive andselective inhibitor inhibits kinase activities ofCDK8CDK8CycC and CDK19CycC complexes with s of 44 nM andIC50104 nM respectively with a of 3 nM for CDhellipKd

Bioactivity Seliciclib (Roscovitine) is a potent and selective CDKsinhibitor with s of 02 μM 065 μM and 07 μM for IC50 CDK5

and respectivelyCdc2 CDK2

Bioactivity Senexin A is a inhibitor with an of 280 nMCDK8 IC50

Bioactivity Simurosertib (TAK-931) is a selective cycle 7 kinase(CDC7)inhibitor with an lt03 nMIC50

Bioactivity SNS-032 (BMS-387032) is a selective inhibitor of CDK2 and with s of 38 nM 62 nM and 4CDK7 CDK9 IC50

nM respectively

Ro-3306 Cat No HY-12529

Roniciclib (BAY 1000394) Cat No HY-13914

SB1317 (TG02) Cat No HY-15166

SEL120-34A Cat No HY-111388

SEL120-34A HCl Cat No HY-111388B

SEL120-34A monohydrochloride Cat No HY-111388A

Seliciclib (Roscovitine CYC202 R-roscovitine) Cat No HY-30237

Senexin A Cat No HY-15681

Simurosertib (TAK-931) Cat No HY-100888

SNS-032 (BMS-387032) Cat No HY-10008

Purity 9846Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9796Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9882Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity SU9516 is a potent inhibitor with an of 22 nM andCDK2 IC50also shows inhibitory effects on CDK1 and CDK4 with s ofIC5040 200 nM respectively

Bioactivity SY-1365 is a highly selective covalent inhibitor of CDK7SY-1365 possesses therapeutic potential in both hematologicaland solid tumors [1]

Bioactivity T025 is an orally available and highly potent Cdc2-like kinase inhibitor with s of 48 0096 65 and 061 nM(CLK) Kd

for CLK1 CLK2 CLK3 and CLK4 respectively

Bioactivity THAL-SNS-032 is a selective degrader PROTAC consistingCDK9of a CDK-binding SNS-032 ligand linked to a thalidomidederivative that binds the E3 ubiquitin ligase Cereblon (CRBN)

[1]

Bioactivity THZ1 is a selective and potent covalent inhibitor withCDK7an of 32 nMIC50

Bioactivity THZ1 Hydrochloride is a selective and potent inhibitorCDK7with an of 32 nMIC50

Bioactivity THZ1-R is a non-cysteine reactive analog of THZ1 whichdisplays diminished activity for inhibition THZ1-RCDK7binds to with a of 142 nMCDK7 Kd

Bioactivity THZ2 is a potent and selective inhibitor with an ofCDK7 IC50139 nM

Bioactivity THZ531 is a covalent inhibitor of both and withCDK12 CDK13s of 158 nM and 69 nM respectivelyIC50

Bioactivity Trilaciclib is a inhibitor with s of 1 nM and 4 nMCDK46 IC50for CDK4 and CDK6 respectively

32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SU9516 Cat No HY-18629

SY-1365 Cat No HY-128587

T025 Cat No HY-112296

THAL-SNS-032 Cat No HY-123937

THZ1 Cat No HY-80013

THZ1 Hydrochloride Cat No HY-80013A

THZ1-R Cat No HY-19988

THZ2 Cat No HY-12280

THZ531 Cat No HY-103618

Trilaciclib (G1T28) Cat No HY-101467

wwwMedChemExpresscom 33

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Trilaciclib hydrochloride is a inhibitor with s ofCDK46 IC501 nM and 4 nM for CDK4 and CDK6 respectively

Bioactivity Voruciclib hydrochloride is a clinical stage oral CDK9inhibitor Voruciclib hydrochloride represses expression ofMCL-1 in multiple models of diffuse large B-cell lymphoma(DLBCL) [1]

Bioactivity Wogonin is a naturally occurring mono-flavonoid can inhibitthe activity of and and exhibitsCDK8 Wntanti-inflammatory and anti-tumor effects

Bioactivity XL413 is a potent selective and ATP competitive inhibitor of with an of 34 nM and also shows potent effectCdc7 IC50

with s of 215 42 nM on CK2 PIM1 respectively and anIC50 of 118 nM on pMCMEC50

Bioactivity XL413 hydrochloride is a potent selective and ATP competitiveinhibitor of with an of 34 nM and also showsCdc7 IC50potent effect with s of 215 42 nM on CK2 PIM1IC50respectively and an of 118 nM on pMCMEC50

Trilaciclib hydrochloride (G1T28 hydrochloride) Cat No HY-101467A

Voruciclib hydrochloride Cat No HY-12422A

Wogonin Cat No HY-N0400

XL413 Cat No HY-15260

XL413 hydrochloride Cat No HY-15260A

Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) are protein kinases that are involved in cellcycle control Two checkpoint kinase subtypes have been identifiedChk1 and Chk2 Chk1 is a central component of genome surveillancepathways and is a key regulator of the cell cycle and cell survivalChk1 is required for the initiation of DNA damage checkpoints andhas recently been shown to play a role in the normal (unperturbed)cell cycle Chk1 impacts various stages of the cell cycle including the Sphase G2M transition and M phase In addition to mediating cellcycle checkpoints Chk1 also contributes to DNA repair processesgene transcription embryo development cellular responses to HIVinfection and somatic cell viability Chk2 is a protein kinase that is

activated in response to DNA damage and is involved in cell cycle arrest In response to DNA damage and replicationblocks cell cycle progression is halted through the control of cell cycle regulators The protein encoded by this gene isa cell cycle checkpoint regulator and putative tumor suppressor

34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 35

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9877Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9990Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Checkpoint Kinase (Chk) Inhibitors amp Modulators

Bioactivity AZD-7762 is a potent ATP-competitive checkpoint kinase ( )Chkinhibitor in with an of 5 nM for Chk1IC50

Bioactivity BML-277 is a selective checkpoint kinase 2 ( ) inhibitorChk2with an of 15 nMIC50

Bioactivity CCT241533 is a potent and selective ATP competitive inhibitorof with an of 3 nM and of 116 nMCHK2 IC50 Ki

Bioactivity CCT241533 hydrochloride is a potent and selective CHK2inhibitor with an of 3 nM and a of 116 nMIC50 Ki

Bioactivity CCT244747 is a potent orally bioavailable and highlyselective inhibitor with an of 77 nM CCT244747CHK1 IC50also abrogates G2 checkpoint with an of 29 nMIC50

Bioactivity CCT245737 is a orally active and seletive inhibitorChk1with an of 13 nMIC50

Bioactivity CHIR-124 is a potent and selective inhibitor with Chk1 IC50of 03 nM and also potently targets and withPDGFR FLT3

s of 66 nM and 58 nMIC50

Bioactivity CHK-IN-1 is an inhibitor of and withCHK1 CHK2anti-proliferative activities

Bioactivity CHK1 inhibitor is an inhibitor of CHK1 Bioactivity CHK1-IN-2 is a checkpoint kinase 1 inhibitor with an(CHK1) of 6 nMIC50

AZD-7762 Cat No HY-10992

BML-277 (Chk2 Inhibitor II) Cat No HY-13946

CCT241533 Cat No HY-14715

CCT241533 hydrochloride Cat No HY-14715B

CCT244747 Cat No HY-18175

CCT245737 Cat No HY-18958

CHIR-124 Cat No HY-13263

CHK-IN-1 Cat No HY-U00345

CHK1 inhibitor Cat No HY-104022

CHK1-IN-2 Cat No HY-111369

Purity 9965Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9791Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity CHK1-IN-3 is a inhibitor with anCheckpoint Kinase 1 (CHK1) of 04 nM IC50

[1]Bioactivity GDC-0575 (ARRY-575 RG7741) is a highly-selective oral

small-molecule inhibitor with an of 12nMChk1 IC50

Bioactivity GDC-0575 dihydrochloride is an orally bioavailable CHK1inhibitor with an of 12 nM and has antitumor activityIC50

Bioactivity PF 477736 is a potent selective ATP-competitive inhibitor of with a of 049 nM 100-fold selectivity versus Chk1 Ki Chk2

( 47 nM)Ki

Bioactivity Prexasertib (LY2606368) is a potent selective andATP-competitive inhibitor with ancheckpoint kinase 1 (Chk1)

and a of lt1 nM and 09 nM respectivelyIC50 Ki

Bioactivity Prexasertib dihydrochloride (LY2606368 dihydrochloride) is apotent and selective ATP competitive inhibitor of the Chk1protein kinase with s of lt1 nM and 8 nM for CHK1 andIC50CHK2 respectively and a of 09 nM against purified CHK1Ki

Bioactivity Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is apotent selective ATP competitive and inhibitorCHK1 CHK2with a of 09 nM for CHK1 and s of lt1 nM 8 nM forKi IC50CHK1 and CHK2 respectively Prexasertib Mesylate Hydrateinhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2hellip

Bioactivity Rabusertib (LY2603618) is a potent and selective inhibitor of with an of 7 nMChk1 IC50

Bioactivity SCH900776 is a potent selective and oral inhibitor ofcheckpoint kinase1 ( ) with an of 3 nM It shows 50-Chk1 IC50and 500-fold selectivity over CDK2 andChk2 respectively

36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CHK1-IN-3 Cat No HY-128601

GDC-0575 (ARRY-575 RG7741) Cat No HY-112167

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride RG7741 dihydrochloride) Cat No HY-112167A

PF 477736 (PF 00477736) Cat No HY-10032

Prexasertib (LY2606368) Cat No HY-18174

Prexasertib dihydrochloride (LY2606368 (dihydrochloride)) Cat No HY-18174A

Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate LY2940930) Cat No HY-18174B

Rabusertib (LY2603618 IC-83) Cat No HY-14720

SCH900776 (MK-8776) Cat No HY-15532

wwwMedChemExpresscom 37

CRISPRCas9

CRISPRCas9 (Clustered Regularly-Interspaced Short PalindromicRepeatsCas9) is a bacterial immune system that has been adaptedfor genome editing in mammalian cells Cas9 is a programmablenuclease that generates double-stranded breaks (DSB) in DNAdictated by binding of a ~20 nucleotide recombinant ldquoguide RNArdquo(gRNA) to the target site DSBrsquos produced by Cas9 are most oftenrepaired through the cellrsquos error-prone non-homologous end joining(NHEJ) pathway resulting in small insertions or deletions (indels) Thevast majority of indels shift the reading frame introducing apremature stop codon or resulting in nonsense mediated decay ofthe mRNA-effectively ldquoknocking outrdquo a gene

The CRISPRCas9 system has substantially advanced efforts in specific gene editing and has been successfully appliedto modify the episomal genomes of human and other organisms The CRISPRCas9 system utilizes a prokaryoticRNA-guided programmable nuclease that can make a double-strand DNA break (DSB) at a specific site under theguidance of a leading RNA This DSB process depends on the co-expression of two basic components a guide RNA(gRNA) and Cas9 nuclease Making a specific DSB can trigger DNA repair via either error-prone non-homologous endjoining (NHEJ) or homology-directed repair (HDR) In the presence of the CRISPRCas9 system the NHEJ inhibitorSCR7 is proven to increase the efficiency of Cas9-mediated HDR by at least by 7-fold in mammalian cells Genomeediting via CRISPRCas9 has become an efficient and reliable way to make precise targeted changes to the genome ofliving cells

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

CRISPRCas9 Inhibitors amp Modulators

Bioactivity Brefeldin A is a specific inhibitor of whichprotein traffickingblocks the protein transport from the endoplasmic reticulum tothe Golgi complex

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity L755507 is a potent selective agonist of with an β -AR3 IC50of 35 nM

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity Zidovudine is a nucleoside reverse transcriptase inhibitor () widely used to treat HIV infection Zidovudine increasesNRTI

CRISPRCas9-mediated editing frequency

38 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Brefeldin A (BFA Cyanein Decumbin) Cat No HY-16592

KU-57788 (NU7441) Cat No HY-11006

L755507 Cat No HY-19334

Nocodazole (Oncodazole R17934) Cat No HY-13520

RS-1 Cat No HY-19793

SCR7 Cat No HY-12742

Zidovudine (Azidothymidine AZT ZDV) Cat No HY-17413

wwwMedChemExpresscom 39

DeubiquitinaseDUBs

Deubiquitinases (DUBs) are a large group of proteases that cleaveubiquitin from proteins and other molecules Ubiquitin is attached toproteins in order to regulate the degradation of proteins via theproteasome and lysosome coordinate thecellular localisation ofproteins activate and inactivate proteins and modulateprotein-protein interactions DUBs can reverse these effects bycleaving the peptide or isopeptide bond between ubiquitin and itssubstrate protein In humans there are nearly 100 DUB genes whichcan be classified into two main classes cysteine proteases andmetalloproteases The cysteine proteases comprise ubiquitin-specificproteases (USPs) ubiquitin C-terminal hydrolases (UCHs)

Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU) The metalloprotease groupcontains only the Jab1Mov34Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases DUBs play several roles inthe ubiquitin pathway One of the best characterised functions of DUBs is the removal of monoubiqutin andpolyubiquitin chainsfrom proteins

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9940Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9892Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9893Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Deubiquitinase Inhibitors amp Modulators

Bioactivity 6-Thioguanine (Thioguanine) is an anti-leukemia andimmunosuppressant agent acts as an inhibitor of SARS and MERScoronavirus papain-like proteases ( ) and also potentlyPLprosinhibits activity with s of 25 μM and 40 μM forUSP2 IC50Plpros and recombinant human USP2 respectively

Bioactivity b-AP15 is a specific inhibitor of the enzymesdeubiquitinating and UCHL5 Usp14

Bioactivity BAY 11-7082 is a inhibitor which decreases NF-κB byNF-κBinhibiting TNF-α-induced phosphorylation of IκB-α BAY 11-7082inhibits ubiquitin-specific protease and withUSP7 USP21

s of 019 μM and 096 μM respectivelyIC50

Bioactivity C527 is a is a pan inhibitor with a highDUB enzymepotency for the complex ( =088 μM)USP1UAF1 IC50

Bioactivity Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB)inhibitor directly inhibiting DUB activity of USP9x USP5USP14 and UCH37 Degrasyn has been shown to downregulate theantiapoptotic proteins and Bcr-Abl JAK2

Bioactivity DUBs-IN-1 is an active inhibitor of ubiquitin-specific with an of 024 μM for USP8proteases (USPs) IC50

Bioactivity DUBs-IN-2 is a potent inhibitor with an ofdeubiquitinase IC50028 μM for USP8

Bioactivity DUBs-IN-3 is a potent enzyme inhibitordeubiquitinase (USP)extracted from reference compound 22c with an of 056 μMIC50for USP8

Bioactivity EOAI3402143 is a ( ) inhibitor whichdeubiquitinase DUBinhibits dose-dependently inhibits and Usp9x Usp24 Usp5

Bioactivity FT671 is a potent non-covalent and selective inhibitorUSP7with an of 52 nM and binds to the USP7 catalytic domainIC50with a of 65 nMKd

40 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

6-Thioguanine (Thioguanine2-Amino-6-purinethiol) Cat No HY-13765

b-AP15 (NSC 687852) Cat No HY-13989

BAY 11-7082 (BAY 11-7821) Cat No HY-13453

C527 Cat No HY-12988

Degrasyn (WP1130) Cat No HY-13264

DUBs-IN-1 Cat No HY-50736

DUBs-IN-2 Cat No HY-50737A

DUBs-IN-3 Cat No HY-50737

EOAI3402143 Cat No HY-111408

FT671 Cat No HY-107985

wwwMedChemExpresscom 41

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9773Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9684Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity FT827 is a selective and covalent ubiquitin-specific protease7 ( ) inhibitor with an of 52 nMUSP7 IC50

Bioactivity GNE-6640 is a selective and non-covalent inhibitor ofubiquitin epecific peptidase 7 with values of(USP7) IC50075 μM 043 μM 203 μM and 023 μM for full length USP7USP7 catalytic domain full length USP43 and Ub-MDM2respectively

Bioactivity GNE-6776 is a selective inhibitorUSP7 Bioactivity HBX 19818 is a specific inhibitor of ubiquitin-specific with an of 281 μMprotease 7 (USP7) IC50

Bioactivity IU1 is a special inhibitor with of 4-5 μMUsp14 IC50 Bioactivity IU1-47 is a potent inhibitor with an of 06 μMUSP14 IC50

IU1-47 induces tau elimination in cultured neurons [1]

Bioactivity LDN-57444 is a reversible competitive and site-directedinhibitor of withubiquitin C-terminal hydrolase L1 (UCH-L1)an of 088 μM and a of 040 μM LDN-57444 alsoIC50 Kisuppresses UCH-L3 activity with an of 25 μMIC50

Bioactivity MF-094 is a potent and selective inhibitor with an USP30 IC50of 120 nM

Bioactivity ML-323 is a reversible potent inhibitor with USP1-UAF1 IC50of 76 nM in a Ub-Rho assay The measured inhibition constantsof ML-323 for the free enzyme ( ) is 68 nMKi

Bioactivity ML364 is an inhibitor of ubiquitin specific peptidase 2 and can be used for the research of breast cancer(USP2)

extracted from patent WO 2016134026 A1 compound Figure 10G

FT827 Cat No HY-111350

GNE-6640 Cat No HY-112937

GNE-6776 Cat No HY-107986

HBX 19818 Cat No HY-17540

IU1 Cat No HY-13817

IU1-47 Cat No HY-122243

LDN-57444 Cat No HY-18637

MF-094 Cat No HY-112438

ML-323 Cat No HY-17543

ML364 Cat No HY-100900

Purity 9800Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9737Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9843Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NSC632839 is a nonselective isopeptidase inhibitor whichinhibits and with s of 45plusmn4 μMUSP2 USP7 SENP2 EC5037plusmn1 μM and 98plusmn18 μM respectively

Bioactivity P 22077 is a cell-permeable ubiquitin-specific protease 7 inhibitor with an of 801 μM It also inhibits(USP7) EC50

USP47 with an of 874 μMEC50

Bioactivity P005091 is a selective and potent inhibitor of with anubiquitin-specific protease 7 (USP7)

of 42 μMEC50

Bioactivity PR-619 is a broad-range inhibitor with of 393DUB EC5049 686 72 and 861 μM for USP4 USP8 USP7 USP2and respectivelyUSP5

Bioactivity SJB2-043 is an inhibitor of the native complex withUSP1UAF1 of 544 nMIC50

Bioactivity SJB3-019A is a potent and novel inhibitor 5 times moreUSP1potent than SJB2-043 in promoting ID1 degradation andcytoxicity in K562 cells with of 00781 μMIC50

Bioactivity USP7-IN-1 is a selective and reversible inhibitor of with an of 77 μMubiquitin-specific protease 7 (USP7) IC50

and can be used for the research of cancer

Bioactivity USP7-IN-3 (Compound 5) is a potent and selective allostericubiquitin-specific protease 7 ( ) inhibitor USP7 [1]

Bioactivity USP7USP47 inhibitor is a selective ubiquitin-specific protease inhibitor with s of 042 μM and 10747 (USP7USP47) EC50

μM respectively

Bioactivity VLX1570 is a competitive inhibitor of proteasomedeubiquitinases ( ) with an of approximate 10 μMDUBs IC50

42 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NSC632839 Cat No HY-100708

P 22077 Cat No HY-13865

P005091 (P5091) Cat No HY-15667

PR-619 Cat No HY-13814

SJB2-043 Cat No HY-15757

SJB3-019A Cat No HY-80012

USP7-IN-1 Cat No HY-16709

USP7-IN-3 Cat No HY-112128

USP7USP47 inhibitor Cat No HY-13487

VLX1570 Cat No HY-12471

wwwMedChemExpresscom 43

DNA AlkylatorCrosslinker

DNA alkylatorcrosslinker is a molecule that alkylates DNA or cancross link with DNA DNA alkylatorcrosslinker can have mutagenicpharmaceutical or other effects Alkylation is the transfer of an alkylgroup from one molecule to another The alkyl group may betransferred as an alkyl carbocation a free radical a carbanion or acarbene Alkylating agents are widely used in chemistry because thealkyl group is probably the most common group encountered inorganic molecules Selective alkylation or adding parts to the chainwith the desired functional groups is used especially if there is nocommonly available biological precursor Alkylation with only onecarbon is termed methylation In medicine alkylation of DNA is used

in chemotherapy to damage the DNA of cancer cells Alkylation is accomplished with the class of drugs calledalkylating antineoplastic agents Crosslinking of DNA occurs when various exogenous or endogenous agents reactwith two different positions in the DNA This can either occur in the same strand (intrastrand crosslink) or in theopposite strands of the DNA (interstrand crosslink) Crosslinks also occur between DNA and protein DNA replicationis blocked by crosslinks which causes replication arrest and cell death if the crosslink is not repaired The RAD51family plays a role in repair

Purity 990Clinical Data LaunchedSize 100 mg 500 mg

Purity 9879Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9844Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9961Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

DNA AlkylatorCrosslinker Inhibitors amp Modulators

Bioactivity Altretamine is an antineoplastic agentalkylating Bioactivity Altretamine hydrochloride is an antineoplasticalkylatingagent

Bioactivity Bendamustine D4 is the deuterium labeled BendamustineBendamustine is a agent that causes DNADNA cross-linkingbreaks with alkylating and antimetabolite properties

Bioactivity Bendamustine hydrochloride is a agent thatDNA cross-linkingcauses DNA breaks with alkylating and antimetaboliteproperties

Bioactivity Busulfan is a potent with selective immunosuppressivealkylatoreffect on bone marrow

Bioactivity Calicheamicin is a cytotoxic agent that causes double-strandDNA breaks

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity Carmustine is an antitumor chemotherapeutic agent which worksby akylating DNA and RNA

Bioactivity Chlorambucil is an agent with antitumor activityalkylating Bioactivity Cisplatin is a antineoplastic chemotherapy drug which works bycross-linking with and causing DNA damage in cancerDNAcells

44 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Altretamine (ENT-50852 RB-1515 WR-95704) Cat No HY-B0181

Altretamine hydrochloride (ENT-50852 hydrochloride RB-1515

hydrochloride WR-95704 hydrochloride) Cat No HY-B0181A

Bendamustine D4 (SDX-105 D4) Cat No HY-13567S

Bendamustine hydrochloride (SDX-105 EP-3101) Cat No HY-B0077

Busulfan Cat No HY-B0245

Calicheamicin (Calicheamicin γ1) Cat No HY-19609

Carboplatin (NSC 241240) Cat No HY-17393

Carmustine Cat No HY-13585

Chlorambucil (CB-1348 WR-139013) Cat No HY-13593

Cisplatin (CDDP cis-Diaminodichloroplatinum) Cat No HY-17394

wwwMedChemExpresscom 45

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 980Clinical Data LaunchedSize 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Bioactivity Cyclophosphamide is a synthetic agent chemicallyalkylatingrelated to the nitrogen mustards with antineoplastic andimmunosuppressive activities

Bioactivity Cyclophosphamide hydrate is a synthetic agentalkylatingchemically related to the nitrogen mustards withantineoplastic and immunosuppressive activities

Bioactivity Fotemustine is a agent with antitumor activityDNA-alkylating Bioactivity Ifosfamide is an chemotherapeutic agent withalkylatingactivity against a wide range of tumors

Bioactivity Lomustine (CCNU) is a agent with antitumorDNA alkylatingactivity

Bioactivity Melphalan is an effective agent with potentDNA alkylatingantitumor activity

Bioactivity Methylnitronitrosoguanidine (MNNG) is an agent withalkylatingtoxic and mutagenic effects [1]

Bioactivity Miriplatin is a chemotherapy agent which belongs to the classof agentsalkylating

Bioactivity Miriplatin hydrate is a chemotherapy agent which belongs tothe class of agentsalkylating

Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Cyclophosphamide Cat No HY-17420

Cyclophosphamide hydrate (Cyclophosphamide monohydrate) Cat No HY-17420A

Fotemustine (S10036) Cat No HY-B0733

Ifosfamide Cat No HY-17419

Lomustine (CCNU NSC 79037) Cat No HY-13669

Melphalan (L-PAM) Cat No HY-17575

Methylnitronitrosoguanidine (MNNG) Cat No HY-128612

Miriplatin (SM-11355) Cat No HY-16325A

Miriplatin hydrate (SM-11355 (hydrate)) Cat No HY-16325

Mitomycin C (Ametycine) Cat No HY-13316

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9926Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9986Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Oxaliplatin is a inhibitor It causes DNADNA synthesiscrosslinking damage prevents DNA replication andtranscription and causes cell death

Bioactivity Palifosfamide is a novel DNA alkylator and the activemetabolite of ifosfamide with antitumor activity

Bioactivity Procarbazine Hydrochloride is an agent withalkylatinganticancer activity

Bioactivity RITA is an inhibitor of binds top53-HDM-2 interactionp53dN with a of 15 nM and also induces Kd DNA-DNA

cross-links

Bioactivity Satraplatin is an agent with potent antitumoralkylatingeffect

Bioactivity SJG-136 is a agent with an of 45 nMDNA cross-linking XL50for pBR322 DNA SJG-136 has potent antitumor activity

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity Temozolomide (NSC 362856 CCRG 81045) is an oral DNA agent used to treat some brain cancersalkylating

Bioactivity Thio-TEPA is a agent with antitumor activityDNA alkylating Bioactivity Treosulfan (NSC 39069Treosulphan) is an agent withalkylatingactivity in ovarian cancer and other solid tumor types

46 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Oxaliplatin Cat No HY-17371

Palifosfamide (Isophosphoramide mustard IPM ZIO-201) Cat No HY-14798

Procarbazine Hydrochloride Cat No HY-13733

RITA (NSC 652287) Cat No HY-13424

Satraplatin (BMS182751 BMY45594 JM216) Cat No HY-17576

SJG-136 (NSC-694501) Cat No HY-14573

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

Temozolomide (NSC 362856 CCRG 81045 TMZ) Cat No HY-17364

Thio-TEPA Cat No HY-17574

Treosulfan (NSC 39069 Treosulphan) Cat No HY-16503

wwwMedChemExpresscom 47

Purity 980Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Uramustine is an oral agent effective in thealkylatingtreatment of lymphosarcoma chronic lymphatic leukaemia andthrombocythemia

Bioactivity VAL-083 is an agent that creates N7 methylation onalkylatingDNA with antitumor activity

Uramustine (Uracil mustard) Cat No HY-13544

VAL-083 (Dianhydrodulcitol Dianhydrogalactitol) Cat No HY-16513

DNA-PKDNA-dependent protein kinase

DNA-PKcs (DNA-dependent protein kinase catalytic subunit) is anenzyme that in humans is encoded by the PRKDC gene DNA-PKcsbelongs to the phosphatidylinositol 3-kinase-related kinase proteinfamily DNA-PKcs is the catalytic subunit of a nuclear DNA-dependentserinethreonine protein kinase called DNA-PK The secondcomponent is the autoimmune antigen Ku On its own DNA-PKcs isinactive and relies on Ku to direct it to DNA ends and trigger itskinase activity DNA-PKcs is required for the non-homologous endjoining (NHEJ) pathway of DNA repair Many proteins have beenidentified as substrates for the kinase activity of DNA-PKAutophosphorylation of DNA-PKcs appears to play a key role in NHEJ

and is thought to induce a conformational change that allows end processing enzymes to access the ends of thedouble-strand break DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNAdamage checkpoint

48 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 49

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9943Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9977Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9722Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9664Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9239Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

DNA-PK Inhibitors amp Modulators

Bioactivity (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer ofNedisertib with an in the range of 7-30 nM for IC50 DNA-PK

[1]

Bioactivity AZD-7648 is a potent and selective inhibitorDNA-PKAnti-tumor activity [1]

Bioactivity CC-115 is a potent and dual and kinaseDNA-PK mTORinhibitor with s of 13 nM and 21 nM respectively CC-115IC50blocks both and signalingmTORC1 mTORC2

Bioactivity CC-115 hydrochloride is a potent and dual and DNA-PK mTORkinase inhibitor with s of 13 nM and 21 nM respectivelyIC50CC-115 blocks both and signalingmTORC1 mTORC2

Bioactivity Compound 401 is a synthetic inhibitor of ( = 028DNA-PK IC50μM) that also targets mTOR but not PI3K in vitro

Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR

Bioactivity LTURM34 is a specific inhibitor with an of 0034DNA-PK IC50μM

Bioactivity LY3023414 potently and selectively inhibits class I PI3Kisoforms and with s of 607 nM 776DNA-PK mTORC12 IC50nM 38 nM 238 nM 424 nM and 165 nM for PI3Kα PI3KβPI3Kδ PI3Kγ DNA-PK and mTOR respectively LY3023414potently inhibits at low nanomolarhellipmTORC1 2

Bioactivity Nedisertib (M3814) is a potent and selective inhibitor of ( ) with an of lt3DNA-dependent Protein Kinase DNA-PK IC50

nM

Bioactivity NU 7026 is a novel specific inhibitor with ofDNA-PK IC50023plusmn001 μM also inhibits with of 13plusmn3 μMPI3K IC50

(R)-Nedisertib ((R)-M3814) Cat No HY-101570A

AZD-7648 Cat No HY-111783

CC-115 Cat No HY-16962

CC-115 hydrochloride Cat No HY-16962A

Compound 401 Cat No HY-19341

KU-57788 (NU7441) Cat No HY-11006

LTURM34 Cat No HY-101667

LY3023414 Cat No HY-12513

Nedisertib (M3814) Cat No HY-101570

NU 7026 (DNA-PK Inhibitor II LY293646) Cat No HY-15719

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9937Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9145Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity PI-103 is a potent and inhibitor with s of 8PI3K mTOR IC50nM 88 nM 48 nM 150 nM 20 nM and 83 nM for p110α p110β

and PI-103 also inhibitsp110δ p110γ mTORC1 mTORC2 with an of 2 nMDNA-PK IC50

Bioactivity PI-103 Hydrochloride is a dual and inhibitor withPI3K mTORs of 8 nM 88 nM 48 nM 150 nM 20 nM and 83 nM forIC50

and p110α p110β p110δ p110γ mTORC1 mTORC2PI-103 also inhibits with an of 2 nMDNA-PK IC50

Bioactivity PIK-75 is a and inhibitor which inhibits DNA-PKDNA-PK PI3K and p110γ with s of 2 58 and 76 nM respectivelyp110α IC50

PIK-75 inhibits p110α gt200-fold more potently than p110β(IC =13 μM)50

Bioactivity PIK-90 is a and inhibitor which inhibits DNA-PK PI3K p110α and with s of 11 18 and 13 nMp110γ DNA-PK IC50

respectively

Bioactivity Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib apotent inhibitor with an of lt3 nM DNA-PK IC50

[1]Bioactivity SF2523 is a highly selective and potent inhibitor of withPI3K

s of 34 nM 158 nM 9 nM 241 nM and 280 nM for IC50 PI3Kα

BRD4 and mTOR respectivelyPI3Kγ DNA-PK

Bioactivity STL127705 (Compound L) is a Ku 7080 heterodimer proteininhibitor inhibits Ku7080-DNA interaction with an ofIC5035 μM STL127705 also inhibits Ku-dependent activation ofDNA-PKCS kinase ( 25 μM) IC50

[1]

Bioactivity Torin 2 is an inhibitor with of 025 nM formTOR EC50inhibiting cellular mTOR activity and exhibits 800-foldselectivity over PI3K (EC 200 nM) Torin 2 also inhibits50

with an of 05 nM in the cell free assay TorihellipDNA-PK IC50

Bioactivity VX-984 is a potent inhibitorDNA-PK Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

50 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

PI-103 Cat No HY-10115

PI-103 Hydrochloride Cat No HY-10115A

PIK-75 (PIK-75 Hydrochloride) Cat No HY-13281

PIK-90 Cat No HY-12030

Rac-Nedisertib (Rac-M3814) Cat No HY-101570B

SF2523 Cat No HY-101146

STL127705 Cat No HY-122727

Torin 2 Cat No HY-13002

VX-984 (M9831) Cat No HY-19939S

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

wwwMedChemExpresscom 51

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity YU238259 is an inhibitor of homology-dependent DNA repair () used for cancer researchHDR

YU238259 Cat No HY-19977

DNARNA Synthesis

RNA synthesis which is also called DNA transcription is a highlyselective process Transcription by RNA polymerase II extends beyondRNA synthesis towards a more active role in mRNA maturationsurveillance and export to the cytoplasmSingle-strand breaks are repaired by DNA ligase using thecomplementary strand of the double helix as a template with DNAligase creating the final phosphodiester bond to fully repair theDNADNA ligases discriminate against substrates containing RNAstrands or mismatched base pairs at positions near the ends of thenickedDNA Bleomycin (BLM) exerts its genotoxicity by generatingfree radicals whichattack C-4prime in the deoxyribose backbone of DNA

leading to opening of the ribose ring and strand breakage it is an S-independentradiomimetic agent that causesdouble-strand breaks in DNAFirst strand cDNA is synthesized using random hexamer primers and M-MuLV Reverse Transcriptase (RNase H)Second strand cDNA synthesis is subsequently performed using DNA Polymerase I and RNase H The remainingoverhangs are converted into blunt ends using exonucleasepolymerase activity After adenylation of the 3prime ends ofDNA fragments NEBNext Adaptor with hairpin loop structure is ligated to prepare the samples for hybridization Cellcycle and DNA replication are the top two pathways regulated by BET bromodomain inhibition Cycloheximide blocksthe translation of mRNA to protein

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wwwMedChemExpresscom 53

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

250 mg 1 g

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9979Clinical Data No Development ReportedSize 1 mg 2 mg 5 mg

Purity 9876Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9989Clinical Data LaunchedSize 5 mg 10 mg 50 mg

Purity 9968Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

25 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

DNARNA Synthesis Inhibitors amp Modulators

Bioactivity 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is amodified nucleoside 2-(Methylamino)-1H-purin-6(7H)-one is anendogenous methylated nucleoside found in human fluids

Bioactivity 374-Trihydroxyflavone isolated from Rhus javanica var is a flavonoid with DNA strand-scission activityroxburghiana

[1]

Bioactivity 5-Methoxyflavone belonged to Flavonoid family is a DNApolymerase-beta inhibitor and neuroprotective agent againstbeta-amyloid toxicity possess central nervous system (CNS)depressant effect mediated through the ionotropic GABA Areceptors

Bioactivity 6-Thio-2-Deoxyguanosine is a nucleoside analogue that can beincorporated into de novo-synthesized telomeres by telomerase

Bioactivity Acelarin (NUC-1031) is a ProTide transformation andenhancement of the widely-used nucleoside analoguegemcitabine

Bioactivity Actinomycin D inhibits with an of 042 μMDNA repair IC50

Bioactivity Adenine is a purine derivative and a nucleobase with a varietyof roles in biochemistry Target Nucleosideantimetaboliteanalog Adenine is a nucleobase with a varietyof roles in biochemistry including cellular respiration inthe form of both the energy-rich adenosine triphosphate (ATP)hellip

Bioactivity alpha-Amanitin is the principal toxin of several deadlypoisonous mushrooms exerting its toxic function by inhibiting

RNA-polymerase II

Bioactivity Anisomycin is a potent inhibitor whichprotein synthesisinterferes with protein and by inhibitingDNA synthesispeptidyl transferase or the 80S ribosome system Anisomycin isa JNK activator which increases phospho-JNK

Bioactivity Beaucage reagent is found to be potent in causing DNAcleavage

2-(Methylamino)-1H-purin-6(7H)-one (N2-methylguanine) Cat No HY-101412

374-Trihydroxyflavone (5-Deoxykampferol) Cat No HY-111806

5-Methoxyflavone Cat No HY-107790

6-Thio-2-Deoxyguanosine (6-thio-dG β-TGdR) Cat No HY-18762

Acelarin (NUC-1031) Cat No HY-100885

Actinomycin D (Dactinomycin Actinomycin IV) Cat No HY-17559

Adenine (6-Aminopurine Vitamin B4) Cat No HY-B0152

alpha-Amanitin (α-Amanitin α-Amatoxin) Cat No HY-19610

Anisomycin (Flagecidin Wuningmeisu C) Cat No HY-18982

Beaucage reagent Cat No HY-100951

Purity 9847Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity 9804Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9896Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Bioactivity Bleomycin sulfate is a inhibitor with potentDNA synthesisantitumor activity

Bioactivity BMH-21 is a small molecule DNA intercalator that bindsribosomal DNA and inhibits RNA polymerase I (Pol I)transcription does not cause phosphorylation of H2AX

Bioactivity Branaplam (LMI070) is a highly potent selective and orallyactive small molecule modulatorSMN2 splicing

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent

Bioactivity CeMMEC1 is an inhibitor of and also has high affinityBRD4for with an of 09 μM for TAF1 and a of 18TAF1 IC50 KdμM for TAF1 (2)

Bioactivity CeMMEC13 is a potent inhibitor of bromodomain withTAF1 (2)an of 21 μMIC50

Bioactivity Chebulinic acid is a potent natural inhibitor of Mtuberculosis DNA gyrase also can inhibit SMAD-3phosphorylation inhibit H+ K+-ATPase activity

Bioactivity COH29 is a potent ribonucleotide reductase ( ) inhibitorRNRwith anticancer activity COH29 inhibits α and β subunit ofRNR with s of 16 μMIC50

Bioactivity CX-5461 is a potent and oral inhibitor ItrRNA synthesisinhibits RNA polymerase I-driven transcription of rRNA with

s of 142 113 and 54 nM in HCT-116 A375 and MIA PaCa-2IC50cells respectively

54 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Bleomycin sulfate Cat No HY-17565

BMH-21 Cat No HY-12484

Branaplam (LMI070 NVS-SM1) Cat No HY-19620

Capecitabine Cat No HY-B0016

Carboplatin (NSC 241240) Cat No HY-17393

CeMMEC1 Cat No HY-111445

CeMMEC13 Cat No HY-101088

Chebulinic acid Cat No HY-N2033

COH29 (RNR Inhibitor COH29) Cat No HY-19931

CX-5461 Cat No HY-13323

wwwMedChemExpresscom 55

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9872Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9963Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9945Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg

Bioactivity CX-5461 dihydrochloride is a potent and orally bioavailableinhibitor of Pol I-mediated with s of 142rRNA synthesis IC50nM in HCT-116 113 nM in A375 and 54 nM in MIA PaCa-2 cellsand shows little or no effect on Pol II ( ge25 μM)IC50

Bioactivity Cycloheximide (Naramycin A) is an eukaryote protein synthesisinhibitor with s of 5325 nM and 2880 nM for proteinIC50synthesis and RNA synthesis respectivelyin vivo

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Datelliptium chloride is a DNA-intercalating agent derivedfrom ellipticine with anti-tumor activities

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Didox (NSC-324360) is a synthetic (ribonucleotide reductase) inhibitorRR

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

CX-5461 dihydrochloride Cat No HY-13323A

Cycloheximide (Naramycin A Actidione CHX) Cat No HY-12320

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Datelliptium chloride Cat No HY-U00337

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Didox (NSC-324360) Cat No HY-19387

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

1 mg 5 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Bioactivity Folic acid(Vitamin M Vitamin B9) is a B vitamin is necessaryfor the production and maintenance of new cells for DNAsynthesis and RNA synthesis

Bioactivity GC7 Sulfate is a ( ) inhibitordeoxyhypusine synthase DHPS

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity GNE-371 is a potent and selective chemical probe for thesecond bromodomains of human transcription-initiation-factor

subunit 1 and transcription-initiation-factor TFIID TFIIDsubunit 1-like with an of 10 nM for TAF1(2)IC50

Bioactivity Guanine is one of the fundamental components of nucleic acids( and ) Guanine is a purine derivative consistingDNA RNAof a fused pyrimidine-imidazole ring system with conjugateddouble bonds

Bioactivity Halofuginone (RU-19110) is a less-toxic form of Febrifuginewhich is isolated from the plant Dichroa febrifuga [1]

Halofuginone inhibits in anprolyl-tRNA synthetaseATP-dependent manner with a of 183 nM HalofuginhellipKi

[2]

Bioactivity Halofuginone hydrobromide (RU-19110 hydrobromide) is aless-toxic form of Febrifugine which is isolated from theplant Halofuginone inhibits Dichroa febrifuga [1] prolyl-tRNA

in an ATP-dependent manner with a of 183hellipsynthetase Ki

Bioactivity Hydroxyurea is a cell apoptosis inducer that inhibit DNAsynthesis through inhibition of ribonucleotide reductase

Bioactivity L189 is a novel human DNA ligase inhibitor inhibitshLigIIIIIV with IC50 of 595 μM

56 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Folic acid (Vitamin B9 Vitamin M) Cat No HY-16637

GC7 Sulfate Cat No HY-108314A

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

GNE-371 Cat No HY-112803

Guanine Cat No HY-Y1055

Halofuginone (RU-19110) Cat No HY-N1584

Halofuginone hydrobromide (RU-19110 (hydrobromide)) Cat No HY-N1584A

Hydroxyurea (Hydroxycarbamide) Cat No HY-B0313

L189 Cat No HY-15588

wwwMedChemExpresscom 57

Purity 990Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9839Clinical Data No Development ReportedSize 1 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 9977Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9988Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity L67 is a novel competitive human DNA ligase inhibitorinhibits DNA ligases I and III with IC50 of 10 μM and 10 μM

Bioactivity Madrasin is a potent and cell penetrant splicing inhibitorthat interferes with the early stages of spliceosome assemblyMadrasin is cytotoxic at higher concentrations although atlower concentrations it induces cell cycle arrest promotes aspecific reorganization of subnuclear protein localizationhellip

Bioactivity MB-7133 is a inhibitorDNA synthesis Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging

Bioactivity ML216(CID-49852229) is a potent inhibitor of the DNA unwindingactivity of BLM helicase showing similar IC50s of 30 and097 μM for full length BLM and BLM636ndash1298 respectively IC50value 30097 uM(Full length636ndash1298 BLM) Target BLMhelicase inhibitor ML216 shows cell-based activity and canhellip

Bioactivity Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNAdamage agent

Bioactivity NITD008 is a potent and selective inhibitor whichflavivirusecan inhibit with an ofDengue Virus Type 2 (DENV-2) EC50064 μM

Bioactivity Oxolinic acid is a potent inhibitor of DNA gyrase and DNAsynthesis lead to DNA cleavage when extracted chromosomes areincubated with sodium dodecyl sulfate

Bioactivity Phen-DC3 is a (G4) specific ligand which canG-quadruplexinhibit and helicases with s of 65plusmn6 and 50plusmn10FANCJ DinG IC50nM respectively

Bioactivity Plicamycin is a selective specificity protein 1 ( )Sp1inhibitor Plicamycin inhibits the growth of various cancersby decreasing Sp1 protein

L67 (DNA Ligase Inhibitor) Cat No HY-15586

Madrasin (DDD00107587) Cat No HY-100236

MB-7133 Cat No HY-16311

Mitomycin C (Ametycine) Cat No HY-13316

ML216 (CID-49852229) Cat No HY-12342

Nedaplatin (NSC 375101D) Cat No HY-13700

NITD008 (7-Deaza-2-C-acetylene-adenosine) Cat No HY-12957

Oxolinic acid Cat No HY-B1002

Phen-DC3 Cat No HY-15594

Plicamycin (Mithramycin A) Cat No HY-A0122

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9762Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data LaunchedSize 100 mg 500 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9931Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Quarfloxin (CX 3543) a fluoroquinolone derivative withantineoplastic activity targets and inhibits RNA pol Iactivity with IC values in the nanomolar range in50neuroblastoma cells Quarfloxin disrupts the interactionbetween the nucleolin protein and a G-quadruplex DNA structurehellip

Bioactivity RG7800 a small molecule splicing modifier to enterSMN2human clinical trials to treat spinal muscular atrophy

Bioactivity RG7800 hydrochloride is an orally active splicingSMN2modulator with s of 23 nM and 87 nM for EC15x SMN2

splicing and RG7800 hydrochloride has theSMN proteinpotential to treat spinal muscular atrophy

Bioactivity Risdiplam (RG7916 RO7034067) is an orally administeredcentrally and peripherally distributed pre-mRNASMN2splicing modifier that increases survival motor neuron (SMN)protein levels

Bioactivity Saccharin 1-methylimidazole is an activator for DNARNASynthesis

Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]

Bioactivity SMN-C3 is an orally active splicing modulator and hasSMN2the potential to treat spinal muscular atrophy (SMA)

Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively

Bioactivity TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 valueof 08 nM less potent for MTH2 NUDT5 NUDT12 NUDT14 andNUDT16

Bioactivity TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) withan IC50 value of 08 nM less potent for MTH2 NUDT5 NUDT12NUDT14 and NUDT16

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Quarfloxin (CX 3543) Cat No HY-14776

RG7800 (RO6885247) Cat No HY-101792

RG7800 hydrochloride (RO6885247 hydrochloride) Cat No HY-101792A

Risdiplam (RG7916 RO7034067) Cat No HY-109101

Saccharin 1-methylimidazole Cat No HY-112060

SCR7 Cat No HY-12742

SMN-C3 Cat No HY-112633

Streptozocin (Streptozotocin U 9889) Cat No HY-13753

TH287 Cat No HY-16965

TH287 hydrochloride Cat No HY-16965A

wwwMedChemExpresscom 59

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9920Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 25 mg 50 mg 100 mg

Purity 9906Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 25 mg 50 mg 100 mg

Bioactivity TH588 is first-in-class nudix hydrolase family inhibitor thatpotently and selectively engage and inhibit the (MTH1

= 5 nM)IC50

Bioactivity TH588 hydrochloride is first-in-class nudix hydrolase familyinhibitor that potently and selectively engage and inhibit the

( = 5 nM)MTH1 IC50

Bioactivity Thiarabine (OSI-7836) shows potent anti-tumor activity andinhibition of synthesisDNA

Bioactivity Triapine is a novel inhibitor of the M2 subunit of ( ) and is a potentribonucleotide reductase RR

radiosensitizer

Bioactivity Triciribine is a inhibitor also inhibits DNA synthesis Aktand with of 130 nM and 002-046 μMHIV-12 IC50respectively

Bioactivity YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding tothe oncogenic transciption factor EWS-FLI1 YK-4-279 inhibitsEwings sarcoma family tumor (ESFT) cell growth YK-4-279induces apoptosis

Bioactivity Zoliflodacin (ETX0914AZD0914) is a novelspiropyrimidinetrione bacterial DNA gyrasetopoisomeraseinhibitor Zoliflodacin has potent antibacterialin vitroactivity against Gram-positive and Gram-negative organismsincluding with the of 025 μgmLS aureus MIC90

TH588 Cat No HY-12814

TH588 hydrochloride Cat No HY-12814A

Thiarabine (OSI-7836) Cat No HY-16496

Triapine (3-AP PAN-811 OCX191 NSC663249) Cat No HY-10082

Triciribine (API-2 NSC 154020 TCN) Cat No HY-15457

YK-4-279 Cat No HY-14507

Zoliflodacin (ETX0914 AZD0914) Cat No HY-17647

Eukaryotic Initiation Factor (eIF)

Eukaryotic initiation factors (eIFs) are proteins involved in theinitiation phase of eukaryotic translation These proteins help stabilizethe formation of the functional ribosome around the start codon andalso provide regulatory mechanisms in translation initiationEukaryotic initiation factor 2B (eIF2B) is a guaninenucleotide-exchange factor which mediates the exchange of GDP(bound to initiation factor eIF2) for GTP thus regenerating the active[eIF2GTP] complex that is required for peptide-chain initiation Theactivity of eIF2B is a key control point for eukaryotic protein synthesisand is altered in response to viral infection hormones nutrientsgrowth factors and certain stresses

Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis oncapped mRNAs in the cytoplasm Eukaryotic initiation factor (elF) 4A functions as a subunit of the initiation factorcomplex elF4F which mediates the binding of mRNA to the ribosome

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Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 2 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9958Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Eukaryotic Initiation Factor (eIF) Inhibitors amp Modulators

Bioactivity 4E1RCat is an inhibitor of cap-dependent translation andinhibits interaction with an an of 4 μMeIF4EeIF4GI IC50

Bioactivity 4E2RCat is an inhibitor of interaction with an eIF4E-eIF4G IC50of 135 μM

Bioactivity 4EGI-1 is an inhibitor of interaction with a eIF4EeIF4G Kdof 25 μM against eIF4E binding

Bioactivity Briciclib is a water soluble derivative of ON 013100 and hasthe potential in targeting for solid cancerseIF4E

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic inhibitor with an of 110initiation factor 4A-3 (eIF4A3) IC50

nM

Bioactivity Episilvestrol is a derivative of silvestrol isolated from thefruits and twigs of and is a specificAglaia silvestris

-targeting translation inhibitor with antitumor activityeIF4A

Bioactivity GCN2iB is an ATP-competitive inhibitor of aserinethreonine-protein kinase general control

with an of 24 nMnonderepressible 2 (GCN2) IC50

Bioactivity SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1and disrupts the eIF4F complex

Bioactivity Silvestrol is a eukaryotic translation initiation factor 4A () inhibitor isolated from the fruits and twigs of eIF4A Aglaia

foveolata

4E1RCat Cat No HY-14427

4E2RCat Cat No HY-100733

4EGI-1 Cat No HY-19831

Briciclib (ON 014185) Cat No HY-16366

CCT020312 Cat No HY-119240

eIF4A3-IN-2 Cat No HY-101785

Episilvestrol Cat No HY-15359

GCN2iB Cat No HY-112654

SBI-0640756 (SBI-756) Cat No HY-19560

Silvestrol ((-)-Silvestrol) Cat No HY-13251

G-quadruplex

G-quadruplexes (G-tetrads or G4-DNA) are nucleic acid sequencesthat are rich in guanine and are capable of forming a four-strandedstructure Four guanine bases can associate through Hoogsteenhydrogen bonding to form a square planar structure called a guaninetetrad and two or more guanine tetrads can stack on top of eachother to form a G-quadruplex The quadruplex structure is furtherstabilized by the presence of a cation especially potassium which sitsin a central channel between each pair of tetradsThey can be formedof DNA RNA LNA and PNA and may be intramolecular bimolecularor tetramolecular Depending on the direction of the strands or partsof a strand that form the tetrads structures may be described as

parallel or antiparallel

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Purity 980Clinical Data No Development ReportedSize 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity 9680Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

G-quadruplex Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity APTO-253 is an inducer of andKruppel-like factor 4 (KLF4)also stabilizes with anti-proliferative activityGquadruplex

Bioactivity Phen-DC3 Trifluoromethanesulfonate is a (G4)G-quadruplexspecific ligand which can inhibit and helicasesFANCJ DinGwith s of 65plusmn6 and 50plusmn10 nM respectivelyIC50

Bioactivity Pyridostatin is a stabilizer with a of 490G-quadruplexe KdnM

Bioactivity Pyridostatin hydrochloride is a stabilizer withG-quadruplexea of 490 nMKd

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

APTO-253 (LOR-253 LT-253) Cat No HY-16291

Phen-DC3 Trifluoromethanesulfonate (Phen-DC3 Triflate) Cat No HY-15594A

Pyridostatin (RR82) Cat No HY-15176

Pyridostatin hydrochloride (RR-82 hydrochloride) Cat No HY-15176A

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

Haspin Kinase

Haspin is a protein kinase that regulates chromosome and spindlefunction during mitosis and meiosis Haspin expression is detected infetal liver skin kidney small intestine and in all proliferating cellsHaspin phosphorylates H3 thr3 (H3T3ph) in human cell lines anddepletion of Haspin by RNA interference reveals that Haspin isrequired for H3 thr3 phosphorylation in mitotic cells Phosphorylationof H3T3ph by Haspin is necessary for chromosomal passengercomplex (CPC) accumulation at centromeres H3T3ph then positionsthe CPC at centromeres to regulate selected targets of Aurora Bduring mitosis

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Purity 9956Clinical Data No Development ReportedSize 5 mg

Purity 9812Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Haspin Kinase Inhibitors amp Modulators

Bioactivity CHR-6494 is a potent inhibitor of inhibiting histonehaspinH3T3 phosphorylation with an of 2 nMIC50

Bioactivity LDN-192960 is a potent ( Haspin Haploid Germ Cell-Specific) inhibitor with an of 0010 microMNuclear Protein Kinase IC50

CHR-6494 Cat No HY-15217

LDN-192960 Cat No HY-13455

HDACHistone deacetylases

HDAC (Histone deacetylases) are a class of enzymes that removeacetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid onahistone allowing the histones to wrap the DNA more tightly This isimportant because DNA is wrapped around histones and DNAexpression is regulated by acetylation and de-acetylation Its action isopposite to that of histone acetyltransferase HDAC proteins are nowalso called lysine deacetylases (KDAC) to describe their functionrather than their target which also includes non-histone proteinsTogether with the acetylpolyamine amidohydrolases and the acetoinutilization proteins the histone deacetylases form an ancient proteinsuperfamily known as the histone deacetylase superfamily

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Purity 9600Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9971 Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9896Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

HDAC Inhibitors amp Modulators

Bioactivity Abexinostat (CRA 024781) is a novel pan- inhibitorHDACmostly targeting HDAC1 with of 7 nMKi

Bioactivity ACY-1083 is a selective and brain-penetrating inhibitorHDAC6with an of 3 nM and is 260-fold more selective for HDAC6IC50than all other classes of HDAC isoforms ACY-1083 effectivelyreverses chemotherapy-induced peripheral neuropathy [1]

Bioactivity ACY-738 is a potent selective and orally-bioavailable HDAC6inhibitor with an of 17 nM ACY-738 also inhibitsIC50HDAC1 HDAC2 and HDAC3 with s of 94 128 and 218 nMIC50

Bioactivity ACY-775 is a potent and selective inhibitor of the of histonedeacetylase 6 ( ) with an of 75nMHDAC6 IC50

Bioactivity ACY-957 is a selective inhibitor of and withHDAC1 HDAC2s of 7 nM 18 nM and 1300 nM against HDAC123IC50

respectively and shows no inhibition on HDAC456789

Bioactivity AES-135 is a potent inhibitor inhibits HDAC HDAC3 HDAC6 with s of 654 190 and 636 nM respectivelyHDAC11 IC50

Anti-tumor activity [1]

Bioactivity Belinostat is a potent inhibitor with an of 27 nMHDAC IC50in HeLa cell extracts

Bioactivity Benzenebutyric acid is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity BG45 is an HDAC class I inhibitor with selectivity for HDAC3(IC50 = 289 nM) It inhibits HDAC1 HDAC2 and HDAC6 withgreatly reduced potency (IC50s = 2 22 and gt20 μMrespectively) IC50 value 289 nM (HDAC3) 2 μM (HDAC1) 22μM (HDAC2) gt20 μM (HDAC6) Target HDAC At concentrationshellip

Bioactivity BML-210 is a novel HDAC inhibitor and its mechanism of actionhas not been characterized IC50 value 5 μM[1] Target HDAC4In vitro Cell cycle analysis indicated that HeLa celltreatment with 20 and 30 μM concentration of BML-210 increasedthe proportion of cells in G0G1 phase and causedhellip

Abexinostat (CRA 024781 PCI-24781) Cat No HY-10990

ACY-1083 Cat No HY-111791

ACY-738 Cat No HY-19327

ACY-775 Cat No HY-19328

ACY-957 Cat No HY-104008

AES-135 Cat No HY-114483

Belinostat (PXD101 PX105684) Cat No HY-10225

Benzenebutyric acid (4-Phenylbutyric acid) Cat No HY-A0281

BG45 Cat No HY-18712

BML-210 Cat No HY-19350

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9875Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9906Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BRD 4354 is a moderately potent inhibitor of andHDAC5 with of 085 and 188 μM respectivelyHDAC9 IC s50

Bioactivity BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitorof and with of 085 and 188 μMHDAC5 HDAC9 IC s50

respectively [1]

Bioactivity BRD73954 ia a potent and selective HDAC inhibitor with IC50 of36 nM and 120 nM for HDAC6 and HDAC8 respectively

Bioactivity Bufexamac is a class IIB histone deacetylases (HDAC6 andHDAC10) inhibitor used as an anti-inflammatory agent

Bioactivity CAY10603 (BML-281) is a potent and selective inhibitorHDAC6with an of 2 pM CAY10603 (BML-281) also inhibits HDAC1IC50HDAC2 HDAC3 HDAC8 HDAC10 with s of 271 252 042IC506851 907 nM

Bioactivity CHDI-390576 a potent cell permeable and CNS penetrant class inhibitor with s of 54 nMIIa histonedeacetylase (HDAC) IC50

60 nM 31 nM 50 nM for class IIa HDAC4 HDAC5 HDAC7 HDAC9respectively shows gt500-fold selectivity over class IHDACs (1 2 3) and ~150-fold selectivity over HDAC8 and thehellip

Bioactivity Citarinostat is a HDAC6 specific inhibitor with IC50 of 4 nMand 76 nM for HDAC6 and HDAC3 respectively IC50 value 4 nM(HDAC6) 76 nM (HDAC3) Target HDAC The detailed informationplease refer to WO2015061684A1 and 2015054197A1

Bioactivity CM-675 is a dual and phosphodiesterase 5 (PDE5) class I histone-selective inhibitor with values of 114 nMdeacetylases IC50

and 673 nM for PDE5 and HDAC1 respectively CM-675 haspotential to treat Alzheimerrsquos disease [1]

Bioactivity Corin is a dual inhibitor of histone lysine specificdemethylase and histone deacetylase with a(LSD1) (HDAC)

of 110 nM for LSD1 and an IC of 147 nM forK (inact)i 50HDAC1

Bioactivity CRA-026440 is a potent broad-spectrum inhibitor The HDAC Kivalues against recombinant HDAC isoenzymes HDAC1 HDAC2

and are 4 14 11 15 7 andHDAC3 HDAC6 HDAC8 HDAC1020 nM respectively

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BRD 4354 Cat No HY-112719

BRD 4354 ditrifluoroacetate Cat No HY-112719B

BRD73954 Cat No HY-18700

Bufexamac (Bufexamic acid) Cat No HY-B0494

CAY10603 (BML-281) Cat No HY-18613

CHDI-390576 Cat No HY-119939

Citarinostat (ACY241) Cat No HY-15994

CM-675 Cat No HY-114303

Corin Cat No HY-111048

CRA-026440 Cat No HY-19754

wwwMedChemExpresscom 69

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in Ethanol

2 mg 5 mg 10 mg 50 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9809Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9881Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9959Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity CUDC-101 is a potent inhibitor of and withHDAC EGFR HER2s of 44 24 and 157 nM respectivelyIC50

Bioactivity Dacinostat is a potent inhibitor with an of 32 nMHDAC IC50Dacinostat also inhibits with an of 9 nM and usedHDAC1 IC50in cancer research

Bioactivity Domatinostat (4SC-202 free base) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Domatinostat tosylate (4SC-202) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1

(LSD1)

Bioactivity Droxinostat(NS41080) is a selective inhibitor of HDAC3 HDAC6and HDAC8 with IC50 of 169 247 and 146 μM respectivelygt 8-fold selective against HDAC3 and no inhibition toHDAC1 2 4 5 7 9 and 10 IC50 Value 169 μM(HDAC3) 247μM(HDAC6) 146 μM(HDAC8) Target HDAC368 in vitrohellip

Bioactivity EDO-S101 is a pan inhibitor inhibits HDAC1 HDAC2 andHDACHDAC3 with values of 9 9 and 25 nM respectivelyIC50

Bioactivity Entinostat is an oral and selective class I inhibitorHDACwith s of 243 nM 453 nM and 248 nM for IC50 HDAC1 HDAC2

and respectivelyHDAC3

Bioactivity Fimepinostat (CUDC-907) potently inhibits class I s as wellPI3Kas classes I and II enzymes with an of 195439 nMHDAC IC50and 17501828 nM for PI3KαPI3KβPI3Kδ andHDAC1HDAC2HDAC3HDAC10 respectively

Bioactivity FT895 is a potent and selective inhibitor with an HDAC11 IC50

of 3 nM [1]

Bioactivity Givinostat (ITF-2357) is a inhibitor with an of 198HDAC IC50and 157 nM for and respectivelyHDAC1 HDAC3

CUDC-101 Cat No HY-10223

Dacinostat (NVP-LAQ824 LAQ824) Cat No HY-13606

Domatinostat (4SC-202 (free base)) Cat No HY-16012A

Domatinostat tosylate (4SC-202) Cat No HY-16012

Droxinostat (NS 41080) Cat No HY-13267

EDO-S101 (Tinostamustine) Cat No HY-101780

Entinostat (MS-275 SNDX-275) Cat No HY-12163

Fimepinostat (CUDC-907) Cat No HY-13522

FT895 Cat No HY-112285

Givinostat (ITF-2357) Cat No HY-14842

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9849Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9609Clinical Data LaunchedSize 2 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Bioactivity Givinostat hydrochloride (ITF-2357 hydrochloride) is a HDACinhibitor with an of 198 and 157 nM for andIC50 HDAC1

respectivelyHDAC3

Bioactivity Givinostat hydrochloride monohydrate (ITF-2357 hydrochloridemonohydrate) is a inhibitor with an of 198 and 157HDAC IC50nM for and respectivelyHDAC1 HDAC3

Bioactivity HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2008040934 A1

Bioactivity HDAC-IN-4 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2007045844 A1 20070426

Bioactivity HDAC-IN-5 is a histone deacetylase inhibitor(HDAC) Bioactivity HDAC-IN-7 (Chidamide impurity) is an impurity of ChidamideChidamide is a potent and orally bioavailable HDAC enzymesclass I (HDAC123) and class IIb (HDAC10) inhibitor

Bioactivity HDAC6-IN-1 is a potent and selective inhibitor for withHDAC6an of 17 nM and shows 25-fold and 200-fold selectivityIC50relative to ( =422 nM) and ( =3398 nM)HDAC1 IC50 HDAC8 IC50respectively

Bioactivity HDAC8-IN-1 is a inhibitor with an of 272 nMHDAC8 IC50

Bioactivity HDACsmTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs)and targetmammalian target of Rapamycin (mTOR)inhibitor for treating hematologic malignancies with ofIC s50019 nM 18 nM 12 nM and gt500 nM for HDAC1 HDAC6 mTORand PI3Kα respectively HDACsmTOR Inhibitor 1 stimulateshellip

Bioactivity HPOB is a highly potent and selective inhibitor of histonedeacetylase 6 (HDAC6) with IC50 of 56 nM gt30 fold lesspotent against other HDACs target HDAC6 [1] IC 50 56nM [1]In vitro HPOB causes growth inhibition of normal andtransformed cells but does not induce cell death HPOBhellip

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Givinostat hydrochloride (ITF-2357 hydrochloride) Cat No HY-14842A

Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) Cat No HY-14842B

HDAC-IN-3 Cat No HY-19772

HDAC-IN-4 (CXD101) Cat No HY-100748

HDAC-IN-5 Cat No HY-18362

HDAC-IN-7 (Chidamide impurity) Cat No HY-13592

HDAC6-IN-1 Cat No HY-18947

HDAC8-IN-1 Cat No HY-111342

HDACsmTOR Inhibitor 1 Cat No HY-114414

HPOB Cat No HY-19747

wwwMedChemExpresscom 71

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg 100 mg

Bioactivity IDO1 and HDAC1 Inhibitor (Compound 10) is a dual andIDO1 inhibitor with s of 690 nM and 665 nMHDAC1 IC50

respectively [1]

Bioactivity ITSA-1 is membrane permeable and specifically suppresses TSAinhibition of HDAC (histone deacetylase) but not other HDACinhibitors

Bioactivity J22352 is a PROTAC (proteolysis-targeting chimeras)-like andhighly selective inhibitor with an value of 47HDAC6 IC50nM J22352 promotes HDAC6 degradation and induces anticancereffects by inhibiting autophagy and eliciting the antitumorimmune response in glioblastoma cancers and leading to thehellip

Bioactivity JAKHDAC-IN-1 is a potent dual inhibitor exhibitsJAK2HDACantiproliferative and proapoptotic activities in severalhematological cell lines JAKHDAC-IN-1 shows s of 4 and 2IC50

nM for JAK2 and HDAC respectively [1]

Bioactivity LMK-235 is a potent and selective inhibitor inhibitsHDAC45HDAC5 HDAC4 HDAC6 HDAC1 HDAC2 HDAC11 and HDAC8 with

s of 422 nM 119 nM 557 nM 320 nM 881 nM 852 nM andIC501278 nM respectively and is used in cancer research

Bioactivity M344 (D 237) is an inhibitor of ( =100histone deacetylase IC50nM) and an inducer of terminal cell fifferentiation

Bioactivity MC1568 is a selective class II (IIa) histone deacetylas () inhibitor used for cancer researchHDAC II

Bioactivity Mocetinostat (MGCD0103) is a potent orally active andisotype-selective inhibitor with s ofHDAC (Class IIV) IC50015 029 166 and 059 μM for andHDAC1 HDAC2 HDAC3

respectively Mocetinostat shows no inhibition onHDAC11HDAC4 HDAC5 HDAC6 HDAC7 or HDAC8

Bioactivity Nanatinostat (CHR-3996) is a potent class I selective andorally active inhibitor with anhistone deacetylase (HDAC)

of 8 nM IC50[1]

Bioactivity Nexturastat A is a potent and selective HDAC6 inhibitor withIC50 of 5 nM no inhibition on other HDAC forms

IDO1 and HDAC1 Inhibitor Cat No HY-112147

ITSA-1 Cat No HY-100508

J22352 Cat No HY-126147

JAKHDAC-IN-1 Cat No HY-126141

LMK-235 Cat No HY-18998

M344 (D 237 MS 344) Cat No HY-13506

MC1568 Cat No HY-16914

Mocetinostat (MGCD0103) Cat No HY-12164

Nanatinostat (CHR-3996) Cat No HY-13432

Nexturastat A Cat No HY-16699

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9907Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9842Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9867Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9797Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NKL 22 is a HDAC inhibitor The value of IC 50 is 78 uM NKL 22increase frataxin protein concentrations NKL 22 inhibitorsincrease FXN mRNA in FRDA lymphocytes HDAC inhibitors actdirectly on FXN [1]

Bioactivity Oxamflatin (Metacept-3) is a potent inhibitor with anHDAC of 157 nMIC50

Bioactivity Panobinostat is a non-selective histone deacetylase ( )HDACinhibitor

Bioactivity PCI-34051 is a potent and selective inhibitor with HDAC8 IC50of 10 nM with gt200-fold selectivity over the other HDACisoforms

Bioactivity PI3KHDAC-IN-1 is a potent dual inhibitor of PI3KHDACpotently inhibits PI3Kδ and HDAC1 with s of 81 nM and 14IC50

nM respectively [1]

Bioactivity Pimelic diphenylamide 106 is a slow tight-binding inhibitorof class I HDAC (HDAC 1 2 and 3 with IC50 values of 150 nM 760nM and 370 nM respectively) demonstrating no activityagainst class II HDACs

Bioactivity Pracinostat is a potent inhibitorhistone deacetylase (HDAC)with s of 40-140 nM used for cancer researchIC50

Bioactivity PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDACPTACH exerts potent growth inhibition against various humancancer cells with EC50 values ranging from 1 to 10 μM

Bioactivity Quisinostat (JNJ-26481585) is an orally available potent inhibitor with an of 011 nM for HDAC1HDAC IC50

Bioactivity Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of which is under developmenthistone deacetylase enzymes (HDAC)

for the treatment of cutaneous T-cell lymphoma [1]

72 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

NKL 22 Cat No HY-100384

Oxamflatin (Metacept-3) Cat No HY-102033

Panobinostat (LBH589 NVP-LBH589) Cat No HY-10224

PCI-34051 Cat No HY-15224

PI3KHDAC-IN-1 Cat No HY-128582

Pimelic Diphenylamide 106 (RGFA-8 TC-H 106 Histone Deacetylase Inhibitor VII) Cat No HY-19348

Pracinostat (SB939) Cat No HY-13322

PTACH (NCH-51) Cat No HY-12954

Quisinostat (JNJ-26481585) Cat No HY-15433

Remetinostat (SHP-141) Cat No HY-100365

wwwMedChemExpresscom 73

Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9970Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Bioactivity Resminostat is a potent inhibitor of andHDAC1 HDAC3 with mean values of 425 501 718 nMHDAC6 IC50

respectively and shows less potent activities against HDAC8with an of 877 nMIC50

Bioactivity Resminostat hydrochloride is a potent inhibitor of HDAC1 and with mean values of 425 501 718HDAC3 HDAC6 IC50

nM respectively and shows less potent activities againstHDAC8 with an of 877 nMIC50

Bioactivity RG2833 is a brain-penetrant inhibitor with of 60 nMHDAC IC50and 50 nM for HDAC1 and HDAC3 respectively

Bioactivity RGFP966 is a highly selective inhibitor with an ofHDAC3 IC5080 nM and shows no inhibition to other HDACs at concentrationsup to 15 μM

Bioactivity Ricolinostat (ACY-1215) is a potent and selective HDAC6inhibitor with an of 5 nM ACY-1215 also inhibitsIC50

and with s of 58 48 and 51 nMHDAC1 HDAC2 HDAC3 IC50respectively

Bioactivity Romidepsin is a potent and inhibitor with sHDAC1 HDAC2 IC50of 36 and 47 nM respectively

Bioactivity RTS-V5 is a dual inhibitor with s ofHDACproteasome IC5069 18 15 027 053 μM for HDAC1 HDAC2 HDAC3 HDAC6HDAC8 respectively

Bioactivity Santacruzamate A (CAY-10683) is a potent and selective HDAC2inhibitor with an of 119 pM IC50

[1]

Bioactivity Scriptaid is a potent inhibitorhistone deacetylase (HDAC)used in cancer research

Bioactivity Sinapinic acid (Sinapic acid) is a phenolic compound isolatedfrom Jack Rhizome acts as anHydnophytum formicaruminhibitor of with an of 227 mM and alsoHDAC IC50

[1]

inhibits activity Sinapinic acid posssess pothellipACE-I [2]

Resminostat (RAS2410 4SC-201) Cat No HY-14718

Resminostat hydrochloride (RAS2410 hydrochloride 4SC-201 hydrochloride) Cat No HY-14718A

RG2833 (RGFP109) Cat No HY-16425

RGFP966 Cat No HY-13909

Ricolinostat (ACY-1215 Rocilinostat) Cat No HY-16026

Romidepsin (FK 228 FR 901228 NSC 630176) Cat No HY-15149

RTS-V5 Cat No HY-112908

Santacruzamate A (CAY-10683) Cat No HY-N0931

Scriptaid (Scriptide GCK1026) Cat No HY-15489

Sinapinic acid (Sinapic acid) Cat No HY-W009732

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9985Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg

Purity 9800Clinical Data Phase 3Size 10mM x 1mL in Water

1 g 5 g 500 g

Bioactivity Butyric acid is a inhibitor withhistone deacetylase (HDAC)anti-tumor effects in several cancers

Bioactivity Sodium phenylbutyrate is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)

Bioactivity SR-4370 is an inhibitor of with s of 013 μM 058HDAC IC50μM 0006 μM 23 μM and 34 μM for HDAC1 HDAC2 HDAC3HDAC8 and HDAC6 respectively

Bioactivity ST8154AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity ST8155AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]

Bioactivity Sulforaphane is an isothiocyanate present naturally in widelyconsumed vegetables has shown anticancer and cardioprotectiveactivities

Bioactivity SW-100 a selective inhibitorhistone deacetylase 6 (HDAC6)with an of 23 nM shows at least 1000-fold selectivityIC50for HDAC6 relative to all other HDAC isozymes SW-100 displaysa significantly improved ability to cross hellip

Bioactivity Tacedinaline (N-acetyldinaline) is an inhibitor of the histonedeacetylase ( ) with s of 09 09 12 μM forHDAC IC50recombinant HDAC 1 2 and 3 respectively

Bioactivity Tasquinimod is an oral antiangiogenic agent in clinical trialsfor the treatment of castration-resistant prostate cancerTasquinimod binds to the regulatory Zn binding domain of2+

with of 10-30 nMHDAC4 Kd

Bioactivity TH34 an inhibitor with s of 46 μM 19HDAC6 8 10 IC50μM and 77 μM respectively shows high selectivity overHDAC123 [1]

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Sodium Butyrate (Butanoic acid sodium salt) Cat No HY-B0350A

Sodium phenylbutyrate (Sodium 4-phenylbutyrate TriButyrate) Cat No HY-15654

SR-4370 Cat No HY-111400

ST8154AA1 Cat No HY-112805

ST8155AA1 Cat No HY-112806

Sulforaphane Cat No HY-13755

SW-100 Cat No HY-115475

Tacedinaline (N-acetyldinaline CI-994 Goe-5549) Cat No HY-50934

Tasquinimod (ABR-215050) Cat No HY-10528

TH34 Cat No HY-111818

wwwMedChemExpresscom 75

Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g 25 g

Purity 9867Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g 25 g

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9887Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TMP195 is a selective class IIa histone deacetylase ( )HDACinhibitor with s of 59 60 26 15 nM for HDAC4 HDAC5KiHDAC7 and HDAC9 respectively

Bioactivity TMP269 is a novel and selective class IIa histone deacetylase inhibitor with s of 157 nM 97 nM 43 nM and 23 nM(HDAC) IC50

for HDAC4 HDAC5 HDAC7 and HDAC9 respectively

Bioactivity Trichostatin A is a potent and specific inhibitor of HDAC with an value of 18 nM for HDACclass III IC50

Bioactivity Tubacin is a potent and selective inhibitor of with anHDAC6 value of 4 nM and approximately 350-fold selectivity overIC50

HDAC1

Bioactivity Tubastatin A (Hydrochloride) is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tubastatin-A is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50

cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)

Bioactivity Tucidinostat is a potent and orally bioavailable enzymesHDACclass I ( ) and class IIb ( ) inhibitor withHDAC123 HDAC10

s of 95 160 67 and 78 nM less active on HDAC8 andIC50HDAC11 ( s 733 nM 432 nM respectively) and showshellipIC50

Bioactivity UF010 is a potent and selective HDAC inhibitor with IC50 ~006μM 01 μM 05 μM and 15 μM for HDACs 3 2 1 and 8respectively It has gt 6-fold selectivity over other HDACsIC50 value 006 μM (HDAC3) 01 μM (HDAC2) 05 μM (HDAC1)15 μM(HDAC 8) Target HDAC in vitro UF010 is a competitivehellip

Bioactivity Valproic acid is an inhibitor with in the range ofHDAC IC5005 and 2 mM also inhibits ( 400 μM) andHDAC1 IC50induces proteasomal degradation of Valproic acidHDAC2sodium salt is used in the treatment of epilepsy bipohellip

Bioactivity Valproic acid sodium salt is an anticonvulsants used to treatepilepsy bipolar disorder and migraines Valproic acidinhibits with an of 04 mMhistone deacetylase 1 (HDAC1) IC50

TMP195 Cat No HY-18361

TMP269 Cat No HY-18360

Trichostatin A (TSA) Cat No HY-15144

Tubacin Cat No HY-13428

Tubastatin A Hydrochloride (Tubastatin A HCl TSA HCl) Cat No HY-13271

Tubastatin-A Cat No HY-13271A

Tucidinostat (Chidamide HBI-8000 CS 055) Cat No HY-109015

UF010 Cat No HY-18976

Valproic acid (VPA 2-Propylpentanoic Acid) Cat No HY-10585

Valproic acid sodium salt (Sodium Valproate) Cat No HY-10585A

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO

250 mg 500 mg 1 g 5 g

Bioactivity Vorinostat is a potent and orally available inhibitor of and andHDAC1 HDAC2 HDAC3 (Class I) HDAC7 (Class II)

with values of 10 nM and 20 nM forHDAC11 (Class IV ) ID50HDAC1 and HDAC3 respectively

Bioactivity WT-161 is a potent and selective inhibitor with an HDAC6 IC50of 040 nM

76 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Vorinostat (SAHA) Cat No HY-10221

WT-161 Cat No HY-100871

wwwMedChemExpresscom 77

HSPHeat shock proteins

HSP (Heat shock proteins) are a group of proteins induced by heatshock the most prominent members of this group are a class offunctionally related proteins involved in the folding and unfolding ofother proteins HSP expression is increased when cells are exposed toelevated temperatures or other stress This increase in expression istranscriptionally regulated The dramatic upregulation of the heatshock proteins is a key part of the heat shock response and is inducedprimarily by heat shock factor (HSF) HSPs are found in virtually allliving organisms from bacteria to humans Heat shock proteinsappear to serve a significant cardiovascular role Hsp90 Hsp84Hsp70 Hsp27 Hsp20 and alpha B crystallin all have been reported as

having roles in the cardiovasculature

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 g

Purity 9997Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9932Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 1 mg

HSP Inhibitors amp Modulators

Bioactivity Alvespimycin is a potent inhibitor of binding to Hsp90Hsp90with an of 62 plusmn 29 nMEC50

Bioactivity Alvespimycin hydrochloride is a potent inhibitor of Hsp90binding to Hsp90 with of 62plusmn29 nMEC50

Bioactivity Apoptozole is an inhibitor of the ATPase domain of andHsc70 with s of 021 and 014 μM respectively and canHsp70 Kd

induce apoptosis

Bioactivity Arimoclomol maleate (BRX-220) is a co-inducer of heat shockproteins ( )HSP

Bioactivity BIIB021 is an orally available fully synthetic inhibitor of with and of 17 nM and 38 nM respectivelyHSP90 Ki EC50

Bioactivity Bimoclomol is a coinducer used forheat shock protein (HSP)treatment of cardiovascular diseases

Bioactivity CCT251236 is an orally available pirin ligand from a heatshock transcription factor 1 (hsf1) phenotypic screen with an

of 19 nM for inhibition of HSF1-mediated IC50 HSP72

induction

Bioactivity Col003 is a potent inhibitor of competitively binds toHsp47the collagen binding site on Hsp47 ( 18 μM) andIC50inhibits collagen secretion by destabilizing the collagentriple helix [1]

Bioactivity Debio 0932 is an orally active inhibitor with s ofHSP90 IC50100 and 103 nM for HSP90α and HSP90β respectively

Bioactivity Ethoxyquin is an antioxidant which has been used in animalfeed for many years and also an inhibitor of heat shock

( )protein 90 Hsp90

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Alvespimycin (17-DMAG NSC 707545) Cat No HY-10389

Alvespimycin hydrochloride (17-DMAG hydrochloride KOS-1022 BMS 826476) Cat No HY-12024

Apoptozole (Apoptosis Activator VII) Cat No HY-15098

Arimoclomol maleate (BRX-220) Cat No HY-106443A

BIIB021 (CNF2024) Cat No HY-10212

Bimoclomol Cat No HY-U00398

CCT251236 Cat No HY-101026

Col003 Cat No HY-124817

Debio 0932 (CUDC-305) Cat No HY-13469

Ethoxyquin Cat No HY-B1425

wwwMedChemExpresscom 79

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9933Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9994Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Bioactivity Feretoside a phenolic compound extracted from the barks of E is a which act as cytoprotectiveulmoides HSP inducer

agent

Bioactivity Ganetespib is a heat shock protein 90 ( ) inhibitorHSP90which exhibits potent cytotoxicity in a wide variety ofhematological and solid tumor cell lines

Bioactivity Geldanamycin is a inhibitor with antimicrobial activityHsp90against many Gram-positive and some Gram-negative bacteria

Bioactivity Grp94 Inhibitor-1 is a potent selective inhibitor withGrp94an value of 2 nM and over 1000-fold selectivity to Grp94IC50

against Hsp90α [1]

Bioactivity HA15 a molecule that targets specifically BiP GRP78 HSPA5inhibits the ATPase activity of BiP HA15 strongly increasesBiP protein expression in A375 melanoma cells [1]

Bioactivity HSF1A is a cell-permeable activator of heat shocktranscription factor 1 ( )HSF1

Bioactivity HSP70-IN-1 is a heat shock protein ( ) inhibitor inhibitsHSPthe growth of Kasumi-1 cells with an of 23 μMIC50

Bioactivity JG-98 is an allosteric heat shock protein 70 (Hsp70)inhibitor with anti-cancer activities which disrupts Hsp70

and affects signalinginteraction with a co-chaperone Bag3pathways important for cancer development [1] [2] [3]

Bioactivity KNK437 is a inhibitor and inhibits the induction ofHSPHSP105 HSP70 and HSP40

Bioactivity KRIBB11 is an inhibitor of withHeat shock factor 1 (HSF1) of 12 μMIC50

Feretoside Cat No HY-N6249

Ganetespib (STA-9090) Cat No HY-15205

Geldanamycin Cat No HY-15230

Grp94 Inhibitor-1 Cat No HY-112910

HA15 Cat No HY-100437

HSF1A Cat No HY-103000

HSP70-IN-1 Cat No HY-12622

JG-98 Cat No HY-117282

KNK437 (Heat Shock Protein Inhibitor I) Cat No HY-100110

KRIBB11 Cat No HY-100872

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 100 mg

Purity 9569Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9914Clinical Data Phase 2Size 5 mg 10 mg 25 mg 100 mg 200 mg 500 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity KU-32 is a novel novobiocin-based inhibitor that canHsp90protect against neuronal cell death

Bioactivity KW-2478 is an inhibitor of with an of 38 nMHsp90α IC50and has antitumor activity against various human hematologicaltumor cells

Bioactivity Luminespib (NVP-AUY922) is a potent inhibitor withHSP90s of 78 and 21 nM for HSP90α and HSP90β respectivelyIC50

Bioactivity MKT-077 is a rhodacyanine dye and also a heat shock protein 70( ) inhibitor which exhibits significant antitumorHsp70activity

Bioactivity NVP-HSP990 is a potent and selective inhibitor withHsp90 values of 06 08 and 85 nM for Hsp90α Hsp90β andIC50

Grp94 respectively

Bioactivity Onalespib (AT13387) is a potent inhibitor of with aHsp90 of 071 nMKd

Bioactivity p5 Ligand for Dnak and DnaJ is a nonapeptide whichcorresponds to the main binding site for the 23-residue partof the presequence of mitochondrial aspartateaminotransferase p5 Ligand for Dnak and DnaJ is ahigh-affinity ligand for DnaK and DnaJ [1]

Bioactivity Pifithrin-μ is an inhibitor of and with antitumorp53 HSP70and neuroprotective activity

Bioactivity PU-WS13 is a selective inhibitor with an ofGrp94 EC50022 μM

Bioactivity Retaspimycin is a potent and water-soluble inhibitor of with s of 119 nM for both Hsp90 and Grp9Hsp90 EC50

80 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

KU-32 Cat No HY-108248

KW-2478 Cat No HY-13468

Luminespib (NVP-AUY922 AUY922 VER-52296) Cat No HY-10215

MKT-077 (FJ-776) Cat No HY-15096

NVP-HSP990 (HSP-990) Cat No HY-15190

Onalespib (AT13387) Cat No HY-14463

p5 Ligand for Dnak and DnaJ Cat No HY-P1887

Pifithrin-μ (PFTμ 2-Phenylethynesulfonamide) Cat No HY-10940

PU-WS13 Cat No HY-18680

Retaspimycin Cat No HY-15263

wwwMedChemExpresscom 81

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9740Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9982Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9903Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 25 mg 100 mg 200 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Retaspimycin Hydrochloride is a potent and water-solubleinhibitor of with s of 119 nM for both Hsp90 andHsp90 EC50Grp9

Bioactivity Shepherdin (79-87) is amino acids 79 to 87 fragment ofShepherdin Shepherdin is a peptidomimetic antagonist of thecomplex between Hsp90 and Survivin Anticancer activity [1]

Bioactivity SNX-5422 Mesylate (PF-04929113 Mesylate) a prodrug ofSNX-2112 is an orally active inhibitor with a ofHsp90 Kd41 nM and also induces Her-2 degradation with an ofIC5037nM

Bioactivity Tanespimycin (17-AAG) is a potent inhibitor with anHSP90 of 5 nM having a 100-fold higher binding affinity forIC50

tumour cell derived HSP90 than normal cell derived HSP90

Bioactivity TAS-116 is an oral bioavailable ATP-competitive highlyspecific inhibitor ( s of 347 nM and 213HSP90αHSP90β KinM respectively) without inhibiting other HSP90 familyproteins such as GRP94 TAS-116 demonstrates less ocuhellip[1]

Bioactivity Teprenone is a anti-ulcer drug and works as an inducer ofheat shock proteins ( )HSPs

Bioactivity TRC051384 is a heat shock protein 70 ( ) inducerHSP70 Bioactivity VER-155008 is an inhibitor of with s of 05 μMHsp70 IC5026 μM and 26 μM for Hsc70 and Grp7 respectivelyHsp70and with a of 03 μM for Kd Hsp70

Bioactivity VER-49009 is a inhibitor with an of 25 nM and aHsp90 IC50 of 78 nMKd

Bioactivity VER-50589 is a inhibitor with an of 21 nM and aHsp90 IC50 of 45 nMKd

Retaspimycin Hydrochloride (IPI-504) Cat No HY-10210

Shepherdin 79-87 Cat No HY-P1750

SNX-5422 Mesylate (PF-04929113 (Mesylate)) Cat No HY-10213A

Tanespimycin (17-AAG NSC 330507 CP 127374) Cat No HY-10211

TAS-116 Cat No HY-15785

Teprenone (Geranylgeranylacetone) Cat No HY-B0779

TRC051384 Cat No HY-101712

VER-155008 Cat No HY-10941

VER-49009 (CCT 129397) Cat No HY-15986

VER-50589 Cat No HY-15984

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9924Clinical Data Phase 1Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity VER-82576 (NVP-BEP800) is a potent orally available andselective inhibitor with an of 58 nM for Hsp90βHsp90 IC50VER-82576 also slightly blocks Grp94 and Trap-1 with s ofIC5041 and 55 μM respectively

Bioactivity XL888 is a heat shock protein-90 ( ) inhibitor with anHSP90 of 24 nMIC50

Bioactivity YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathwayagainst glioblastoma directly binding to heat shock protein

with an of 820 nM on NFAT nuclear90 (HSP90) IC50translocation YZ129-induced GBM cell-cycle arrest at the G2Mphase promotes apoptosis and inhibited tumor cellhellip

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VER-82576 (NVP-BEP800) Cat No HY-10942

XL888 Cat No HY-13313

YZ129 Cat No HY-114413

wwwMedChemExpresscom 83

IRE1Inositol requiring enzyme 1

The serinethreonine-protein kinaseendoribonucleaseinositol-requiring enzyme 1 (IRE1) is an enzyme that in humans isencoded by the gene IRE1 is an endoplasmic reticulum (ER)ERN1transmembrane sensor that activates UPR to maintain ER and cellularfunction While mammalian IRE1 promotes cell survive it can initiateapoptosis via decay of anti-apoptotic microRNAsIRE1 activation is initiated by homotypic interactions of thestress-sensing lumenal domain favoring transautophosphorylation ofthe kinase-extension nuclease (KEN) domain on the cytoplasmic sideof the ER membraneIRE1XBP-1 has been shown to regulate a variety of genes in various

cell types in response to ER stress mostly related to ER function and the secretory pathway although the target genesvary depending on the cell type and nature of the stress stimuli

Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9875Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg

IRE1 Inhibitors amp Modulators

Bioactivity 36-DMAD hydrochloride is a inhibitor of the pathwayIRE1α-XBP1of the unfolded protein response

Bioactivity 4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor ofIRE1α

Bioactivity 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1αinhibitor with an of 008 μM extracted from patent WOIC502008154484 A1 IRE-lα inhibitor compound 3-5

Bioactivity APY29 is an allosteric modulator of which inhibits IRE1αIRE1αautophosphorylation with of 280 nM and activates IRE1αIC50RNase activity

Bioactivity B I09 is an RNase inhibitor with an of 1230 nMIRE-1 IC50 Bioactivity GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1alpha ( ) which can inhibit and IRE1α IRE1α kinase activity RNase

with s of 20 and 200 nM respectivelyactivity IC50

Bioactivity GSK2850163 hydrochloride is a novel inhibitor ofinositol-requiring enzyme-1 alpha ( ) which can inhibitIRE1α

and with s of 20 andIRE1α kinase activity RNase activity IC50200 nM respectively

Bioactivity KIRA6 allosterically inhibits activity withIRE1α RNase kinasean of 06 microMIC50

Bioactivity Kira8 is a mono-selective inhibitor that allostericallyIRE1αattenuates with an of 59 nM IRE1α RNase activity IC50

[1]Bioactivity MKC3946 is a potent and soluble inhibitor used forIRE1α

cancer research

84 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

36-DMAD hydrochloride Cat No HY-U00460

4μ8C (IRE1 Inhibitor III) Cat No HY-19707

6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) Cat No HY-107371

APY29 Cat No HY-17537

B I09 Cat No HY-107400

GSK2850163 Cat No HY-U00459

GSK2850163 hydrochloride Cat No HY-U00459B

KIRA6 Cat No HY-19708

Kira8 Cat No HY-114368

MKC3946 Cat No HY-19710

wwwMedChemExpresscom 85

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity MKC8866 is an inhibitor with an of less thanIRE1 RNase IC5001 μM for IRE1α RNase

Bioactivity MKC9989 is a ( ) inhibitor and alsoHydroxy aryl aldehydes HAAinhibits with an of 023 to 44 μMIRE1α IC50

Bioactivity STF-083010 is an inhibitor STF-083010 inhibits Ire1Ire1endonuclease activity without affecting its kinase activityafter endoplasmic reticulum stress

MKC8866 Cat No HY-104040

MKC9989 Cat No HY-12399

STF-083010 Cat No HY-15845

Kinesin

Kinesin is a protein belonging to a class of motor proteins found ineukaryotic cells Kinesins move along microtubule filaments and arepowered by the hydrolysis of ATP (thus kinesins are ATPases) Theactive movement of kinesins supports several cellular functionsincluding mitosis meiosis and transport of cellular cargo Mostkinesins walk towards the plus end of a microtubule entailstransporting cargo from the centre of the cell towards the peripheryKinesins were discovered as microtubule (MT)-based anterogradeintracellular transport motors The founding member of thissuperfamily the genomes of mammals encode more than 40 kinesinproteins organized into at least 14 families named kinesin-1 through

kinesin-14

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wwwMedChemExpresscom 87

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9871Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9973Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Kinesin Inhibitors amp Modulators

Bioactivity (R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of ARRY-520(R)-Filanesib ((R)-ARRY-520) is a synthetic kinesin spindle

inhibitor with of 6 nMprotein (KSP) IC50

Bioactivity AZ82 is a selective kinesin-like protein KIFC1 (HSETKIFC1)inhibitor with a of 43 nM and an of 300 nM for KIFC1Ki IC50

Bioactivity CW-069 is an allosteric inhibitor of microtubule motor with an of 75 μMprotein HSET IC50

Bioactivity Dimethylenastron is a potent inhibitor with ankinesin Eg5 of 200 nMIC50

Bioactivity Eg5 Inhibitor V trans-24 is a potent and specific kinesin Eg5inhibitor with an of 065 μM and can be used in theIC50research of cancer

Bioactivity EMD534085 is a potent and selective inhibitor of the mitotic with an of 8 nMkinesin-5 IC50

Bioactivity Filanesib (ARRY-520) is a synthetic kinesin spindle protein inhibitor with of 6 nM(KSP) IC50

Bioactivity Ispinesib is a specific inhibitor of kinesin spindle protein with a of 17 nM(KSP) Ki app

Bioactivity K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5with an of 13 μMIC50

Bioactivity Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member and is used for the research of cellular15 (Kif15)

proliferative diseases

(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A

AZ82 Cat No HY-12241

CW-069 Cat No HY-15857

Dimethylenastron Cat No HY-19944

Eg5 Inhibitor V trans-24 Cat No HY-112915

EMD534085 Cat No HY-15000

Filanesib (ARRY-520) Cat No HY-15187

Ispinesib (SB-715992) Cat No HY-50759

K858 Racemic Cat No HY-19966

Kif15-IN-1 Cat No HY-15948

Purity 9731Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9705Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg

Purity 9959Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9651Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Kif15-IN-2 is an inhibitor of the mitotic and iskinesin Kif15used for the research of cellular proliferative diseases

Bioactivity Litronesib is a selective mitosis-specific kinesin Eg5inhibitor with antitumor activity

Bioactivity Litronesib (Racemate) is the racemate of litronesibLitronesib is a selective allosteric inhibitor of kinesin

Eg5

Bioactivity Monastrol is a potent and cell-permeable inhibitor of themitotic with an value of 14 μMkinesin Eg5 IC50

Bioactivity Paprotrain is a cell-permeable inhibitor of the kinesin inhibits the ATPase activity of MKLP-2 with an MKLP-2 IC50

of 135 μM and a of 336 μM and shows a moderate inhibitionKiactivity on with an of 55 μMDYRK1A IC50

Bioactivity PF-2771 is a potent and selective centromere protein E inhibitor inhibiting CENP-E motor activity with an(CENP-E)

of 161 nM PF-2771 is used as an anticancer agentIC50

Bioactivity SB-743921 is a potent inhibitor of the mitotic kinesin KSP with a of 01 nM(Eg5) Ki

88 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Kif15-IN-2 Cat No HY-15949

Litronesib (LY-2523355 KF-89617) Cat No HY-14846

Litronesib Racemate (LY-2523355 Racemate KF-89617 Racemate) Cat No HY-14846A

Monastrol ((plusmn)-Monastrol) Cat No HY-101071A

Paprotrain Cat No HY-101298

PF-2771 Cat No HY-19530

SB-743921 Cat No HY-12069

wwwMedChemExpresscom 89

LIM Kinase (LIMK)LIMKs

LIM kinases (LIMKs) are important cell cytoskeleton regulators thatplay a prominent role in cancer manifestation and neuronal diseasesThe LIMK family consists of two homologues LIMK1 and LIMK2which differ from one another in expression profile intercellularlocalization and function The main substrate of LIMK is cofilin amember of the actin-depolymerizing factor (ADF) protein familyWhen phosphorylated by LIMK cofilin is inactive LIMKs play acontributory role in several neurodevelopmental disorders and incancer growth and metastasisLIM domain kinases (LIMK1 and 2) are substrate for Cdc42Rac-PAKand modulate actin dynamics by phosphorylating cofilin at serine-3

This modification inactivates cofilinrsquos actin severing and depolymerizing activity LIMKs also translocate into thenucleus and regulate cell cycle progression LIMKs are potential therapeutic targets for NF2 and other merlin-deficienttumors

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

LIM Kinase (LIMK) Inhibitors amp Modulators

Bioactivity BMS-3 is a potent inhibitor with s of 5 nM and 6LIMK IC50nM for and respectivelyLIMK1 LIMK2

Bioactivity BMS-5 (LIMKi 3) is a potent inhibitor with s of 7LIMK IC50nM and 8 nM for and respectivelyLIMK1 LIMK2

Bioactivity R-10015 a broad-spectrum antiviral compound for HIVinfection acts as a potent and selective inhibitor of LIM

and binds to the ATP-binding pocketdomain kinase (LIMK)with an of 38 nM for human LIMK1 IC50

[1]

Bioactivity T56-LIMKi is a selective inhibitor of inhibits theLIMK2growth of Panc-1 cells with an of 352 μMIC50

90 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

BMS-3 Cat No HY-18304

BMS-5 (LIMKi 3) Cat No HY-18305

R-10015 Cat No HY-120097

T56-LIMKi (T5601640) Cat No HY-19352

wwwMedChemExpresscom 91

MicrotubuleTubulin

Microtubules are a component of the cytoskeleton found throughoutthe cytoplasm These tubular polymers of tubulin can grow as long as50 micrometres with an average length of 25 microm and are highlydynamic The outer diameter of a microtubule is about 24 nm whilethe inner diameter is about 12 nm Microtubules are found ineukaryotic cells and are formed by the polymerization of a dimer oftwo globular proteins alpha and beta tubulin Tubulin is one ofseveral members of a small family of globular proteins The tubulinsuperfamily includes five distinct families the alpha- beta- gamma-delta- and epsilon-tubulins and a sixth family which is present only inkinetoplastid protozoa The most common members of the tubulin

family are α-tubulin and β-tubulin the proteins that make up microtubules Microtubules are very important in anumber of cellular processes They are involved in maintaining the structure of the cell

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9987Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity 9920Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 9982Clinical Data Phase 2Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

MicrotubuleTubulin Inhibitors amp Modulators

Bioactivity 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivativewith improved pharmacological features and higher watersolubility IC50 value Target Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cyclearrest and apoptosis as measured by flow cytometry DNAhellip

Bioactivity 10-Oxo Docetaxel (Docetaxel Impurity) is a novel taxoid havingremarkable anti-tumor properties and a Docetaxel intermediate

Bioactivity 2-Methoxyestradiol is an inhibitor and angiogenesis apoptosisinducer with potent antineoplastic activity2-Methoxyestradiol also destablize microtubules

Bioactivity 4-Demethylepipodophyllotoxin(4-DMEP) is a key intermediatecompound for the preparation of podophyllotoxin-typeanti-cancer drugs a potent inhibitor of microtubule assembly

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity ofdocetaxel detected by high performance liquid chromatography(HPLC)

Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity C 7-Epitaxotere)is a impurity of docetaxel

Bioactivity 7-epi-Taxol is an active metabolite of taxol with activitycomparable to that of taxol against cell replicationpromoting bundle formation and againstmicrotubulemicrotubule depolymerization

Bioactivity 7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel)derivative Paclitaxel binds to tubulin and inhibits thedisassembly of microtubules

Bioactivity ABT-751(E 7010) is a novel bioavailable tubulin-binding andantimitotic sulfonamide agent with IC50 of about 15 and 34μM in neuroblastoma and non-neuroblastoma cell linesrespectively IC50 Value 15 μM(neuroblastoma) 34μM(non-neuroblastoma) Target MicrotubuleTubulin in vitrohellip

Bioactivity Amphethinile is an agent The affinity constantanti-tubulinfor the association ( ) of Amphethinile with tubulin isKa13 μM

92 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol

10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584

10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674

2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033

4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435

7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675

7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676

7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227

7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574

ABT-751 (E7010) Cat No HY-13270

Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190

wwwMedChemExpresscom 93

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9903Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9949Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9751Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Ansamitocin P-3 is a inhibitor Ansamitocin P-3microtubuleis a macrocyclic antitumor antibiotic

Bioactivity Auristatin E is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAE analog and cytotoxin inAntibody-drug conjugates

Bioactivity Auristatin F is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAF analog and cytotoxin inAntibody-drug conjugates

Bioactivity BNC105 is a tubulin polymerization inhibitor with potentantiproliferative and tumor vascular disrupting properties

Bioactivity BTB-1 is a potent selective and reversible mitotic motorprotein inhibitor with an of 169 μMKif18A IC50

Bioactivity Cabazitaxel is a semi-synthetic derivative of the naturaltaxoid 10-deacetylbaccatin III with potential antineoplasticactivity

Bioactivity CCB02 is a selective inhibitor bindingCPAP-tubulin interactionto tubulin and competing for the CPAP binding site ofβ-tubulin with an of 689 nM and shows potent anti-tumorIC50activity CCB02 shows no inhibition on the cell cycle- andcentrosome-related kinases or the phosphorylation status ofhellip

Bioactivity Cephalomannine is a taxol derivative with antitumorantiproliferative properties

Bioactivity Cevipabulin (TTI-237) is an oral microtubule-active antitumorcompound and inhibits the binding of [ H] vinblastine to3

tubulin with an of 18-40 nM for cytotoxicity in humanIC50

tumor cell line [1] [2]

Bioactivity Cevipabulin fumarate (TTI-237 fumarate) is an oralmicrotubule-active antitumor compound and inhibits thebinding of [ H] vinblastine to tubulin with an of3 IC50

18-40 nM for cytotoxicity in human tumor cell line [1] [2]

Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739

Auristatin E Cat No HY-15582

Auristatin F Cat No HY-15583

BNC105 Cat No HY-16114

BTB-1 Cat No HY-101770

Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459

CCB02 Cat No HY-114302

Cephalomannine Cat No HY-77554

Cevipabulin (TTI-237) Cat No HY-14949

Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C

Purity 9828Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9956Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9831Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9941Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Bioactivity Colchicine is a inhibitor and a tubulin microtubuledisrupting agent Colchicine inhibits microtubulepolymerization with an of 3 nMIC50

Bioactivity Combretastatin A4 is a -targeting agent thatmicrotubulebinds with of 04 μMβ-tubulin Kd

Bioactivity Crolibulin is a small molecule tubulin polymerizationinhibitor

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate IC50 Value NATarget tubulin ADCs For comparison purposes the ADC A1-mc-MMAD andor A1 -vc-MMAD were used The linker payloadmc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) washellip

Bioactivity D-64131 is a novel inhibitor of Tubulin polymerization thatcompetitively binds with [(3)H]colchicine to αβ-Tubulin

Bioactivity D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule

Bioactivity D8-MMAE is a deuterated labeled MMAE a potent mitoticinhibitor

Bioactivity D8-MMAF is a deuterated form of MMAF which is a disrupting agentmicrotubule

Bioactivity D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a disrupting agentmicrotubule

Bioactivity DM4 is is an agent that inhibit cell division DM4antitubulincan be used in the preparation of antibody drug conjugate

94 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Colchicine Cat No HY-16569

Combretastatin A4 (CRC 87-09) Cat No HY-N2146

Crolibulin (EPC2407) Cat No HY-13603

Cys-mcMMAD Cat No HY-15750

D-64131 Cat No HY-15482

D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8

Monomethyl Dolastatin 10 D8) Cat No HY-15581S

D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A

D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S

D8-MMAF hydrochloride Cat No HY-15579AS

DM4 Cat No HY-12454

wwwMedChemExpresscom 95

Purity 9897Clinical Data LaunchedSize 500u g 1 mg

Purity gt98Clinical Data LaunchedSize 1 mg

Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Purity 9988Clinical Data Phase 3Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity 9555Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9983Clinical Data Phase 2Size 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg

Bioactivity Docetaxel is an antineoplastic drug by inhibiting depolymerization and attenuating of themicrotubule

effects of and gene expressionbcl-2 bcl-xL

Bioactivity Docetaxel Trihydrate is a semi-synthetic taxane analogue actsas a stabilizermicrotubule

Bioactivity Angiotensin II human is a vasoconstrictor that acts on the and the receptorAT1 AT2

Bioactivity ELR510444 is a novel microtubule disruptor inhibitsMDA-MB-231 cell proliferation with IC50 of 309 nM not asubstrate for the P-glycoprotein drug transporter and retainsactivity in βIII-tubulin-overexpressing cell lines

Bioactivity Entasobulin is a polymerization inhibitor withβ-tubulinpotential anticancer activity

Bioactivity Epothilone A is a competitive inhibitor of the binding of [H] paclitaxel to polymers with a of 06-14 μM3 tubulin Ki

Bioactivity Epothilone B is a stabilizer with a ofmicrotubule Ki071μM It acts by binding to the αβ-tubulin heterodimersubunit which causes decreasing of αβ-tubulin dissociation

Bioactivity Epothilone D (KOS 862) is a potent stabilizermicrotubule

Bioactivity Eribulin (E7389) is a targeting agent that ismicrotubuleused in the treatment of metastatic breast cancer Eribulin(E7389) inhibits the proliferation of cancer cells by bindingmicrotubule proteins and microtubules

Bioactivity Eribulin mesylate (E7389 mesylate) is a microtubuletargeting agent that is used in the treatment of metastaticbreast cancer Eribulin mesylate (E7389 mesylate) inhibits theproliferation of cancer cells by binding microtubule proteinsand microtubules

Docetaxel (RP-56976) Cat No HY-B0011

Docetaxel Trihydrate (RP-56976 (Trihydrate)) Cat No HY-B0011A

Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580

ELR510444 Cat No HY-16191

Entasobulin Cat No HY-16777

Epothilone A (Epo A) Cat No HY-13503

Epothilone B (EPO 906 Patupilone) Cat No HY-17029

Epothilone D (KOS 862) Cat No HY-15278

Eribulin (B1939 E7389 ER-086526) Cat No HY-13442

Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A

Purity 9874Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9723Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9947Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg

Purity 9801Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Bioactivity Estramustine phosphate sodium is an antimicrotubulechemotherapy agent arrests prostate cancer cells in the G2Mphase of the cell cycle

Bioactivity Fosbretabulin disodium(CA 4DP CA 4P) is a microtubuledestabilizing drug a type of vascular-targeting agent a drugdesigned to damage the vasculature (blood vessels) of cancertumors causing central necrosis IC50 Value 4 nM [1] Targetmicrotubule in vitro Cytotoxic IC(50) values of CA-4 in humanhellip

Bioactivity Ixabepilone is an orally bioavailable inhibitor which binds to tubulin andmicrotubule

promotes tubulin polymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of the cell cycle andinduces tumor cell apoptosis

Bioactivity Lexibulin(CYT-997) is a potent tubulin polymerisationinhibitor with IC50 of 10-100 nM in cancer cell lines withpotent cytotoxic and vascular disrupting activity in vitro andin vivo

Bioactivity Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM in cancer celllines with potent cytotoxic and vascular disrupting activityin vitro and in vivo

Bioactivity Maytansinol inhibits microtubule assembly and inducesmicrotubule disassembly in vitro Target MicrotubuleTubulinin vitro Maytansinol disrupts the mitotic spindle andprevents mitotic exit in Drosophila Maytansinol reduces thegrowth andor survival of HCT116 cells in a dose-dependenthellip

Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate Mc-MMAD is aprotective group (maleimidocaproyl) -conjugated MMAD IC50Value Target tubulin ADCs For comparison purposes the ADCA1 -mc-MMAD andor A1 -vc-MMAD were used The linkerpayloadhellip

Bioactivity Mc-MMAE is a protective group (maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE) which is a potent tubulininhibitor is a toxin payload in antibody drug conjugate (

)ADC

Bioactivity Mc-MMAF is a protective group-conjugated MMAF MMAF is a morepotent drug than Monomethyl auristatin E (MMAE) but ischarged and relatively membrane-impermeable is a potenttubulin inhibitor is a toxin payload in antibody drugconjugate Target MMAF is a new auristatin derivative with ahellip

Bioactivity Mertansine (DM1) is a inhibitor and is anmicrotubulinantibody-conjugatable maytansinoid that is developed toovercome systemic toxicity associated with maytansine and toenhance tumor-specific delivery Mertansine can be attached toa monoclonal antibody with a linker to create an antibody-drughellip

96 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Estramustine phosphate sodium Cat No HY-13627

Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449

Ixabepilone (Azaepothilone B BMS 247550 BMS 247550-1) Cat No HY-10222

Lexibulin (CYT-997) Cat No HY-10498

Lexibulin dihydrochloride (CYT-997 dihydrochloride) Cat No HY-10498A

Maytansinol (Ansamitocin P-0) Cat No HY-19474

Mc-MMAD Cat No HY-15740

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741

McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578

Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792

wwwMedChemExpresscom 97

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9957Clinical Data Phase 3Size 10mM x 1mL in Water

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 4Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Bioactivity Microtubule inhibitor 1 is an antitumor agent with inhibitory activity with anmicrotubule polymerization

value of 9-16 nM in cancer cells IC50[1]

Bioactivity MMAD is a potent inhibitor is a toxin payload intubulinantibody drug conjugates ( )ADCs

Bioactivity MMAF (Monomethylauristatin F) is an antitubulin agent thatinhibit cell division inhibits H3397 cell growth with an IC50of 105 nM

Bioactivity MMAF hydrochloride is an antitubulin agent that inhibit celldivision inhibits H3397 cell growth with an of 105 nMIC50

Bioactivity Monomethyl auristatin E (MMAE SGD-1010) is a syntheticderivative of dolastatin 10 and functions as a potent

inhibitor by inhibiting tubulin polymerizationmitoticMMAE is widely used as a cytotoxic component of antibody-drug

to treat several different cancer typesconjugates (ADCs)

Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule

microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9

Bioactivity Ombrabulin (AVE8062) is a derivative of CA-4 phosphate whichis known to exhibit antivascular effects through selectivedisruption of the cytoskeleton of endothelial cellstubulin

Bioactivity Ombrabulin hydrochloride is a derivative of CA-4 phosphatewhich is known to exhibit antivascular effects throughselective disruption of the cytoskeleton of endothelialtubulincells

Bioactivity OSIP-486823 is a novel -interfering agent withmicrotubuledistinct biological effects on both protein kinase G (PKG) andmicrotubules

Bioactivity Paclitaxel (Taxol) a naturally occurring antineoplasticagent stabilizes resulting intubulin polymerizationarrest at the G2M phase of the cell cycle and apoptotic celldeath [1] [2]

Microtubule inhibitor 1 Cat No HY-114313

MMAD (Demethyldolastatin 10 Monomethylauristatin D

Monomethyl Dolastatin 10) Cat No HY-15581

MMAF (Monomethylauristatin F) Cat No HY-15579

MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat No HY-15579A

Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162

Nocodazole (Oncodazole R17934) Cat No HY-13520

Ombrabulin (AVE8062 AC7700) Cat No HY-14797

Ombrabulin hydrochloride (AVE8062 (hydrochloride) AC7700 (hydrochloride)) Cat No HY-18256

OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004

Paclitaxel (Taxol) Cat No HY-B0015

Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9979Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9344Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9968Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 25 mg 50 mg 100 mg

Bioactivity Parbendazole is a potent inhibitor of assemblymicrotubuledestabilizes tubulin with an of 879nM and exhibitsEC50a broad-spectrum anthelmintic activity

Bioactivity PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX) compound acts asa -depolymerizing agent and an apoptotic agentmicrotubule

Bioactivity PE859 is a potent inhibitor of both and aggregationtau Aβwith values of 066 and 12 μM respectivelyIC50

Bioactivity PF-06380101 is a novel cytotoxic Dolastatin 10 analogue withexcellent potencies in tumor cell proliferation assays anddifferential ADME properties when compared to other syntheticauristatin analogues that are used in the preparation of ADCsIC50 value ~02 nM(GI50 in BT474 MDA-MB-361-DYT2 and N87hellip

Bioactivity Plinabulin (NPI-2358) is a vascular disrupting agents (VDA)against tubulin-depolymerizing with IC50 of 98~18 nM in tumorcells IC50 Value 98~18 nM Target MicrotubuleTubulin invitro NPI-2358 binds to the colchicine-binding site oftubulin and has potent inhibitory to human tumor cell lineshellip

Bioactivity Podofilox (Podophyllotoxin) is a potent inhibitor ofmicrotubule assembly and DNA topoisomerase II

Bioactivity Rosabulin is a potent inhibitor withmicrotubuleanti-cancer activities

Bioactivity Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10derivative and inhibitor of polymerizationtubulin

Bioactivity SSE15206 is a polymerization inhibitor (GI microtubule 50= 197 nM in HCT116 cells) that overcomes multidrug resistanceCauses aberrant mitosis resulting in G2M arrest due toincomplete spindle formation in cancer cells [1]

Bioactivity Taltobulin (HTI-286 SPA-110) is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibitedproliferation of all three hepatic tumor cell lines (mean IC50= 2 nmolL +- 1 nmolL) in vitro Interestingly no decreasehellip

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Parbendazole (SKF 29044) Cat No HY-115364

PBOX 6 Cat No HY-U00446

PE859 Cat No HY-12662

PF-06380101 Cat No HY-12522

Plinabulin (NPI-2358) Cat No HY-14444

Podofilox (Podophyllotoxin) Cat No HY-15552

Rosabulin (STA 5312) Cat No HY-14934

Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672

SSE15206 Cat No HY-111425

Taltobulin (HTI-286 SPA-110) Cat No HY-15584

wwwMedChemExpresscom 99

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9624Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9996Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Taltobulin hydrochloride is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibits proliferationof all three hepatic tumor cell lines (mean IC50 = 2 nmolL+- 1 nmolL) Interestingly no decrease in viable primaryhellip

Bioactivity Taltobulin trifluoroacetate (HTI-286 SPA-110) is an analogueof Hemiasterlin potent tubulin inhibitor ADCs cytotoxinIC50 value Target tubulin in vitro HTI-286 significantlyinhibited proliferation of all three hepatic tumor cell lines(mean IC50 = 2 nmolL +- 1 nmolL) in vitro Interestinglyhellip

Bioactivity Tasidotin hydrochloride is a peptide analog of the antimitoticdepsipeptide dolastatin 15 as an inhibitor of microtubuleassembly and microtubule dynamics

Bioactivity Tirbanibulin (KX2-391) is an inhibitor of that targetsSrcthe peptide substrate site of Src with of 9-60 nM inGI50cancer cell lines

Bioactivity Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) isan inhibitor of that targets the peptide substrate siteSrcof Src with of 9-60 nM in cancer cell linesGI50

Bioactivity Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitorof that targets the peptide substrate site of Src withSrc

of 9-60 nM in cancer cell linesGI50

Bioactivity Triclabendazole(CGA89317) is a benzimidazole it binds totubulin impairing intracellular transport mechanisms andinterferes with protein synthesis Target MicrotubuleTubulinTriclabendazole treatment produces percentage decreases of thefluke egg output by 153 43 and 366 respectively inhellip

Bioactivity Tubulin inhibitor 1 is a inhibitor occupying thetubulincolchicine binding site inhibits tubulin polymerizationTubulin inhibitor 1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase and inducescellular apoptosis [1]

Bioactivity Tubulysin A(TubA) is a myxobacterial product that can functionas an antiangiogenic agent in many in vitro assaysanti-microtubule anti-mitotic an apoptosis induceranticancer anti-angiogenic and antiproliferative IC50value Target microtubule Tubulysin A is a novel antibiotichellip

Bioactivity Valecobulin (CKD516) a valine prodrug of (S516) and avascular disrupting agent (VDA) is a potent beta-tubulin

inhibitor with marked antitumor activitypolymerizationagainst murine and human solid tumors [1] [2]

Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A

Tasidotin hydrochloride (ILX651) Cat No HY-13760

Tirbanibulin (KX2-391 KX-01) Cat No HY-10340

Tirbanibulin dihydrochloride (KX2-391 (dihydrochloride) KX-01 (dihydrochloride)) Cat No HY-10340A

Tirbanibulin Mesylate (KX2-391 (Mesylate) KX01 (Mesylate)) Cat No HY-10340B

Triclabendazole (CGA89317) Cat No HY-B0621

Tubulin inhibitor 1 Cat No HY-112607

Tubulysin A (TubA) Cat No HY-15995

Valecobulin (CKD-516) Cat No HY-13598

Purity 9958Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9914Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data LaunchedSize 10 mg 50 mg 100 mg 200 mg

Purity 9987Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9989Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Bioactivity Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulininhibitor (MMAD) Vc-MMAD is an antibody drug conjugate IC50Valu NA Target tubulin ADCs Monomethyl auristatin D(MMAD) a potent tubulin inhibitor is a toxin payload andantibody drug conjugate For comparison purposes the ADC A1hellip

Bioactivity VcMMAE is a with potentdrug-linker conjugate for ADCantitumor activity by using the anti-mitotic agent monomethylauristatin E (MMAE) linked via the lysosomally cleavabledipeptide valine-citrulline (vc)

Bioactivity Vinblastine sulfate is a cytotoxic alkaloid used againstvarious cancer types Vinblastine sulfate inhibits theformation of microtubule and suppresses nAChR with an ofIC5089 μM

Bioactivity Vincristine sulfate is an antitumor vinca alkaloid whichinhibits formation in mitotic spindlemicrotubuleresulting in an arrest of dividing cells at the metaphasestage It binds to with a of 85 nMmicrotubule Ki

Bioactivity Vinflunine is a new vinca alkaloid uniquely fluorinated withthe properties of mitotic-arresting and tubulin-interactingactivity

Bioactivity Vinflunine Tartrat is a new vinca alkaloid uniquelyfluorinated with the properties of mitotic-arresting andtubulin-interacting activity Target MicrotubuleTubulin Themajor effects of Vinflunine on dynamic instability are aslowing of the microtubule growth rate an increase in growthhellip

Bioactivity Vinorelbine is an anti-mitotic agent which inhibits theproliferation of Hela cells with IC of 125 nM50

Bioactivity Vinorelbine (ditartrate) is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC of 12550nM

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Vc-MMAD Cat No HY-15742

VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575

Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780

Vincristine sulfate (Leurocristine sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488

Vinflunine Cat No HY-B0628

Vinflunine Tartrate Cat No HY-B0628A

Vinorelbine (KW-2307 base) Cat No HY-12053

Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A

wwwMedChemExpresscom 101

Mps1Monopolar spindle 1

Monopolar spindle 1 (Mps1) also known as TTK is a serine threoninekinase which ensures proper biorientation of sister chromatids on themitotic spindle by the activation of the spindle assembly checkpoint(SAC) Mps1 has been shown to function as the key kinase thatactivates the spindle assembly checkpoint (SAC) to secure properdistribution of chromosomes to daughter cellsMps1 is a dual specificity protein kinase that is essential for thebipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomesare properly attached Mps1 is expressed at high levels during mitosisand is abundantly expressed in cancer cells Disruption of Mps1

function induces aneuploidy and cell death

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9952Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9994Clinical Data Phase 1Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg

Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Mps1 Inhibitors amp Modulators

Bioactivity AZ3146 is a reasonably potent and selective inhibitorMps1with of 35 nM for Mps1 IC50

CatBioactivity BAY 1217389 is a potent and selective inhibitor of the

monopolar spindle 1 ( ) kinase with an value lessMPS1 IC50than 10 nM

Bioactivity BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1)checkpoint with an of 2 nMIC50

Bioactivity CCT251455 is a potent and selective mitotic kinase monopolarspindle 1 ( ) inhibitor with an of 3 nMMPS1 IC50

Bioactivity CFI-402257 is a highly selective and orally bioavailable inhibitor with an of 17 nM for TTK in vitroTTKMps1 IC50

CFI-402257 has anti-cancer activity [1]

Bioactivity CFI-402257 hydrochloride is a highly selective and orallybioavailable inhibitor with an of 17 nM forTTKMps1 IC50TTK in vitro CFI-402257 hydrochloride has anti-canceractivity [1]

Bioactivity Empesertib (BAY 1161909) is a potent inhibitor withMps1an of lt 1 nMIC50

Bioactivity MPI-0479605 is a potent and selective ATP-competitiveinhibitor of with an of 18 nMMps1 IC50

Bioactivity Mps1-IN-1 is a potent selective and ATP-competitive Mps1kinase inhibitor with an and a of 367 nM and 27 nMIC50 Kd

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

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AZ3146 Cat No HY-14710

BAY1217389 Cat No HY-12859

BOS-172722 Cat No HY-112162

CCT251455 Cat No HY-12603

CFI-402257 Cat No HY-101340

CFI-402257 hydrochloride Cat No HY-101340A

Empesertib (BAY 1161909) Cat No HY-12858

MPI-0479605 Cat No HY-12660

Mps1-IN-1 Cat No HY-13298

Mps1-IN-2 Cat No HY-13994

wwwMedChemExpresscom 103

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-3 is a potent and selective kinase inhibitorMPS1with an of 50 nMIC50

Bioactivity NMS-P715 is a selective ATP-competitive inhibitor of MPS1with an of 182 nMIC50

Bioactivity NMS-P715 analog is an inhibitor of with an of 84MPS1 IC50nM

Mps1-IN-3 Cat No HY-12401

NMS-P715 Cat No HY-12382

NMS-P715 analog Cat No HY-14712

Nucleoside AntimetaboliteAnalog

Nucleoside analogues are molecules that act like nucleosides in DNAsynthesis They include a range of antiviral products used to preventviral replication in infected cells Nucleoside analogues can be usedagainst hepatitis B virus hepatitis C virus herpes simplex and HIVOnce they are phosphorylated they work as antimetabolites by beingsimilar enough to nucleotidesto be incorporated into growing DNAstrands Less selective nucleoside analogues are used aschemotherapy agents to treat cancer eg gemcitabine and 5-FUAntimetabolite is a chemical that inhibits the use of a metabolitewhich is another chemical that is part of normal metabolism Suchsubstances are often similar in structure to the metabolite that they

interfere with such as the antifolates that interfere with the use of folic acid The presence of antimetabolites can havetoxic effects on cells such as halting cell growth and cell division so these compounds are used as chemotherapy forcancer

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wwwMedChemExpresscom 105

Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Nucleoside AntimetaboliteAnalog Inhibitors amp Modulators

Bioactivity 1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is abicyclic nucleoside

Bioactivity 1-Methylcytosine is a methylated form of the DNA base cytosineand used as a nucleobase of hachimoji DNA in which it pairswith Isoguanine [1] [2]

Bioactivity 1-Methylinosine is a modified nucleotide found at position 37in tRNA 3 to the anticodon of eukaryotic tRNA [1]

Bioactivity 2-Deoxypseudoisocytidine is a nucleoside analogue

Bioactivity 2rsquo-O4rsquo-C-Methyleneuridine (Compound 15a) is a bicyclicnucleoside

Bioactivity 3-Azido-3-deoxy-5-fluorocytidine (Compound 12) is a cytidinederivative

Bioactivity 3-Azido-3-deoxy-beta-L-uridine (Compound 25) is a nucleosidederivative

Bioactivity 3-Methylcytidine a urinary nucleoside can be used as abiomarker of four different types of cancer lung cancergastric cancer colon cancer and breast cancer [1]

Bioactivity 5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methyluridine is a derivative of LNA-type nucleoside

Bioactivity 5-Aza-7-deazaguanine is a substrate for wild-type (WT) E coli and its Ser90Ala mutant in thepurine nucleoside phosphorylase

synthesis of base-modified nucleosides [1]

1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine Cat No HY-111638

1-Methylcytosine Cat No HY-W006395

1-Methylinosine (N1-Methylinosine) Cat No HY-113139

2-Deoxypseudoisocytidine Cat No HY-101968

2rsquo-O4rsquo-C-Methyleneuridine Cat No HY-111639

3-Azido-3-deoxy-5-fluorocytidine Cat No HY-111641

3-Azido-3-deoxy-beta-L-uridine Cat No HY-111642

3-Methylcytidine Cat No HY-111645

5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methylurid

ine

Cat No HY-111807

5-Aza-7-deazaguanine Cat No HY-111627

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 50 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity 9874Clinical Data Phase 4Size 10mM x 1mL in DMSO

50 mg 100 mg 500 mg

Purity 960Clinical Data LaunchedSize 50 mg 100 mg 500 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in Water

50 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Bioactivity 5-Azacytidine is a nucleoside analogue of cytidine thatspecifically inhibits DNA methylation by trapping DNA

methyltransferases

Bioactivity 5-BrdU is a nucleoside analog that competes with thymidine forincorporation into DNA 5-BrdU is commonly used in thedetection of proliferating cells

Bioactivity 5-Fluorouracil is a potent antitumor agent that affectspyrimidine synthesis by inhibiting thymidylate synthetasethus depleting intracellular dTTP pools

Bioactivity 6-Amino-5-nitropyridin-2-one is a pyridine base and used as anucleobase of hachimoji DNA in which it pairs with5-aza-7-deazaguanine [1]

Bioactivity 6-Mercaptopurine is a purine analogue which acts as anantagonist of the and has been widely usedendogenous purinesas antileukemic agent and immunosuppressive drug

Bioactivity 6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MPhydrate) is a purine analogue which acts as an antagonist ofthe and has been widely used asendogenous purinesantileukemic agent and immunosuppressive drug

Bioactivity 6-O-Methyl Guanosine is a modified nucleoside 6-O-Methyl[1]

Guanosine (6-methylguanosine) inhibit colony-forming abilityin a malignant xeroderma pigmentosum cell line [2]

Bioactivity 7-Methylguanosine is a novel cNIIIB nucleotidase inhibitorwith IC value of 878 plusmn 75 microM50

Bioactivity 8-Azaguanine is a purine analogue which shows antineoplasticactivity

Bioactivity Adenosine is a nucleoside composed of a molecule of adenineattached to a ribose sugar molecule (ribofuranose) moiety viaa β-N9-glycosidic bond Target Nucleosideantimetaboliteanalog Adenosine plays an important role inbiochemical processes such as energy transfer mdash as adenosinehellip

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5-Azacytidine (Ladakamycin 5-AzaC Azacitidine) Cat No HY-10586

5-BrdU (BUdR BRDU) Cat No HY-15910

5-Fluorouracil (5-FU) Cat No HY-90006

6-Amino-5-nitropyridin-2-one Cat No HY-50071

6-Mercaptopurine (Mercaptopurine 6-MP) Cat No HY-13677

6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MP hydrate) Cat No HY-13677A

6-O-Methyl Guanosine Cat No HY-111648

7-Methylguanosine Cat No HY-122524

8-Azaguanine Cat No HY-B1468

Adenosine (Adenine riboside D-Adenosine) Cat No HY-B0228

wwwMedChemExpresscom 107

Purity 9818Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 1 g

Purity 9897Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 1 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase

Bioactivity Carmofur is a derivative of fluorouracil an antimetaboliteused as an antineoplastic agent

Bioactivity Clofarabine(Clolar Clofarex) inhibits the enzymaticactivities of ribonucleotide reductase (IC50 = 65 nM) and DNApolymerase IC50 Value 65 nM Target in vitro Clofarabine isa second generation purine nucleoside analog withantineoplastic activity It is phosphorylated intracellularlyhellip

Bioactivity CNDAC is a major metabolite of oral drug sapacitabine and anucleoside analog

Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase

with an of 16 nMDNA synthesis IC50

Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50

Bioactivity Cytidine is a nucleoside molecule that is formed when cytosineis attached to a ribose ring cytidine is a component of RNATarget Nucleoside antimetaboliteanalog Cytidine is anucleoside molecule that is formed when cytosine is attachedto a ribose ring (also known as a ribofuranose) via ahellip

Bioactivity Dacarbazine(DTIC-Dome DTIC) is an antineoplastic agent Ithas significant activity against melanomas Target Nucleosideantimetaboliteanalog Approved May 1975 Dacarbazine (DTIC) isthe only single-agent approved by the Food and DrugAdministration for treating metastatic melanoma With DTIC ashellip

Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing

Bioactivity Deoxypseudouridine is a nucleotide analog

Capecitabine Cat No HY-B0016

Carmofur (HCFU) Cat No HY-B0182

Clofarabine Cat No HY-A0005

CNDAC Cat No HY-16445A

Cytarabine (Cytosine β-D-arabinofuranoside Cytosine

Arabinoside Ara-C) Cat No HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside

hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A

Cytidine (Cytosine β-D-riboside Cytosine-1-β-D-ribofuranoside) Cat No HY-B0158

Dacarbazine (Imidazole Carboxamide) Cat No HY-B0078

Deoxycytidine triphosphate (dCTP) Cat No HY-101400

Deoxypseudouridine Cat No HY-101970

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9986Clinical Data LaunchedSize 10mM x 1mL in Water

1000u g 2500u g 5 mg 10 mg

Purity gt98Clinical Data LaunchedSize 2500u g 5 mg 10 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in Water

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 50 mg

Bioactivity DMTr-LNA-5MeU-3-CED-phosphoramidite is a nucleoside derivative[1]

Bioactivity Doxifluridine is a thymidine phosphorylase activator forPC9-DPE2 cells with IC50 of 062 μM

Bioactivity Ethynylcytidine is a new nucleoside antimetabolite Bioactivity Floxuridine (5-fluorodeoxyuridine) is an oncology drug thatbelongs to the class known as antimetabolites with an GI50 of51 μM for the inhibition of PEPT1 IC50 value TargetNucleoside antimetaboliteanalog Floxuridine (Fludara) is aprodrug of floxuridine and an oncology agent with an GI50 ofhellip

Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1

Bioactivity Fludarabine (phosphate) is an analogue of adenosine anddeoxyadenosine which is able to compete with dATP forincorporation into DNA and inhibit DNA synthesis

Bioactivity Forodesine(BCX-1777 freebase Immucillin-H) is an orallybioavailable PNP inhibitor with picomolar potency inducesapoptosis mainly in T cells

Bioactivity Forodesine hydrochloride is a potent and oral purine nucleoside inhibitor with s ranging from 048 tophosphorylase (PNP) IC50

157 nM

Bioactivity Fosteabine is an oral and prodrug analogue of cytarabine whichis resistant to deoxycytidine deaminase

Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively

108 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

DMTr-LNA-5MeU-3-CED-phosphoramidite Cat No HY-111531

Doxifluridine (Ro 21-9738 5-Fluoro-5-deoxyuridine 5-DFUR) Cat No HY-B0021

Ethynylcytidine (ECyD TAS-106 3-C-Ethynylcytidine) Cat No HY-16200

Floxuridine (5-Fluorouracil 2-deoxyriboside) Cat No HY-B0097

Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069

Fludarabine phosphate (NSC 118218 (phosphate)) Cat No HY-B0028

Forodesine (BCX-1777 freebase Immucillin-H) Cat No HY-16210

Forodesine hydrochloride (BCX-1777 Immucillin-H hydrochloride) Cat No HY-16209

Fosteabine (Cytarabine ocfosfate YNK 01) Cat No HY-106349

Gemcitabine (NSC 613327 LY188011) Cat No HY-17026

wwwMedChemExpresscom 109

Purity 9575Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg

Purity 9971Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg

Purity 9829Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg

Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water

100 mg 200 mg 500 mg 1 g

Purity 9924Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Bioactivity Gemcitabine elaidate(CP-4126 CO-101) is a lipophilicunsaturated fatty acid ester derivative of gemcitabine (dFdC)an antimetabolite deoxynucleoside analogue with potentialantineoplastic activity IC50 value Target Gemcitabineanalog Upon hydrolysis intracellularly by esterases thehellip

Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50

Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively

Bioactivity Isocytosine is a non-natural nucleobase and an isomer ofcytosine It is used in combination with Isoguanine in studiesof unnatural nucleic acid analogues of the normal base pairsin DNA and used as a nucleobase of hachimoji RNA [1] [2]

Bioactivity Isoguanine is a purine base that is an isomer of guanine Abuilding block in organic synthesis

Bioactivity LY2334737 is an orally available prodrug of gemcitabine whichis a nucleoside analog used as chemotherapy

Bioactivity N2-methylguanosine is a modified nucleoside that occurs atseveral specific locations in many tRNAs

Bioactivity N6N6-Dimethyladenosine is a modified ribonucleosidepreviously found in rRNA and also exhibits in mycobacteriumbovis Bacille Calmette-Gueacuterin tRNA [1]

Bioactivity N6-Etheno 2-deoxyadenosine is a reactive oxygen species(ROS)reactive nitrogen species (RNS)-induced DNA oxidationproduct used as a biomarker to evaluate chronic inflammationand lipid peroxidation in animal or human tissues [1]

Bioactivity Nelarabine (Arranon 506U78) is a purine nucleoside analog andDNA synthesis inhibitor with IC50 from 0067-215 μM in tumorcells Nelarabine is a chemotherapy drug used in T-cell acutelymphoblastic leukemia

Bioactivity Orotic acid (OA) is an intermediate in pyrimidine metabolismIC50 Value Target Nucleoside antimetaboliteanalog in vitroOA increases cell proliferation and decreases apoptosis inserum-starved SK-Hep1 hepatocellular carcinoma cells whichmay ascribe to the inhibition of AMP-activated protein kinasehellip

Gemcitabine elaidate (CP-4126 CO-101 Gemcitabine 5-elaidate) Cat No HY-13538

Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003

Isocytosine Cat No HY-W002272

Isoguanine Cat No HY-124143

LY2334737 Cat No HY-13672

N2-Methylguanosine Cat No HY-111647

N6N6-Dimethyladenosine Cat No HY-101984

N6-Etheno 2-deoxyadenosine Cat No HY-111646

Nelarabine (506U78 GW 506U78 Nelzarabine) Cat No HY-13701

Orotic acid (6-Carboxyuracil Vitamin B13) Cat No HY-N0157

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9972Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg

Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9783Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9887Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9745Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity Pseudothymidine is a C-nucleoside analog of thymidine Bioactivity Raltitrexed is an antimetabolite drug used in chemotherapyacting by inhibiting thymidylate synthase

Bioactivity RX-3117(TV-1360 Fluorocyclopentenylcytosine) is novel acytidine analog shows anticancer activity in several cancercell lines including gemcitabine-resistant variants

Bioactivity Sapacitabine is an orally available prodrugnucleoside analogthat is structurally related to cytarabine

Bioactivity Tegafur (FT 207 NSC 148958) is a chemotherapeutic 5-FUprodrug used in the treatment of cancers is a component oftegafur-uracil

Bioactivity Tipiracil is a thymidine phosphorylase ( ) inhibitorTPase

Bioactivity Tipiracil (hydrochloride) is a thymidine phosphorylaseinhibitor (TPI) used for cancer research

Bioactivity Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT)is an irreversible inhibitor andthymidylate synthasethereby suppresses Trifluridine is an antiviralDNA synthesisdrug for infectionherpes simplex virus (HSV)

Bioactivity Trifluridine-tipiracil hydrochloride mixture (TAS-102) is anovel oral combination drug that consists of an antineoplasticthymidine-based nucleoside analog trifluorothymidine and apotent inhibitor tipiracil in athymidine phosphorylase105 molar ratio

Bioactivity Vidarabine (Ara-A) an antiviral drug which is active againstherpes simplex and varicella zoster viruses

110 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Pseudothymidine (5-Methyl-2-Deoxypseudouridin) Cat No HY-101969

Raltitrexed (ZD1694 D1694 ICI-D1694) Cat No HY-10821

RX-3117 (TV-1360 fluorocyclopentenylcytosine) Cat No HY-15228

Sapacitabine (CS682 CYC682) Cat No HY-16445

Tegafur (FT 207NSC 148958) Cat No HY-17400

Tipiracil Cat No HY-A0063A

Tipiracil hydrochloride Cat No HY-A0063

Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT) Cat No HY-A0061

Trifluridinetipiracil hydrochloride mixture (TAS-102) Cat No HY-16478

Vidarabine (Ara-A Adenine Arabinoside

9-β-D-Arabinofuranosyladenine) Cat No HY-B0277

wwwMedChemExpresscom 111

p97VCPCdc48

p97 an abundant hexameric ATPase of the AAA family is involved inhomotypic membrane fusion It is thought to disassemble SNAREcomplexes formed during the process of membrane fusion Twostructures have been reported a crystal structure of the N-terminaland D1 ATPase domains of murine p97 at 29 A resolution and acryoelectron microscopy structure of full-length rat p97 at 18 Aresolution Together these structures show that the D1 and D2hexamers pack in a tail-to-tail arrangement and that the N domain isflexible A comparison with NSF D2 (ATP complex) reveals possibleconformational changes induced by ATP hydrolysis

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9765Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

p97 Inhibitors amp Modulators

Bioactivity CB-5083 is a potent selective and orally bioavailable p97inhibitor with an value of 11 nMIC50

Bioactivity DBeQ is a selective potent reversible and ATP-competitive inhibitor with an value of 15 μM and 16 μM forp97 IC50

p97(wt) and p97(C522A) respectively DBeQ also inhibits Vps4with an of 115 μMIC50

Bioactivity ML240 is a potent inhibitor inhibiting p97 ATPase withp97 value of 100 nMIC50

Bioactivity ML241 hydrochloride is a potent inhibitor inhibiting p97p97ATPase with value of 100 nMIC50

Bioactivity NMS-859 is a potent covalent inhibitor withVCP (p97)s of 037 and 036 μM for wild-type VCP in the presence ofIC50

60 μM and 1 mM ATP in cells respectively

Bioactivity NMS-873 is a potent selective allosteric inhibitorVCPp97with value of 30 nMIC50

112 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

CB-5083 Cat No HY-12861

DBeQ (JRF 12) Cat No HY-15945

ML240 Cat No HY-19795

ML241 hydrochloride Cat No HY-19797A

NMS-859 Cat No HY-15714

NMS-873 Cat No HY-15713

wwwMedChemExpresscom 113

PAKp21 activated kinases

PAKs (p21-activated kinases) are key regulators of actin dynamics cellproliferation and cell survival PAKs are SerThr kinases that areclassified into two groups on the basis of their structural andfunctional features group I (PAK1ndash3) and group II (PAK4ndash6) Group IPAKs have an auto-inhibitory domain (also called an inhibitory switchdomain) and a kinase domain (catalytic domain CD) and are activatedby the binding of the active (that is GTP-bound) forms of RhoGTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPasesBecause the deregulation of PAKs is closely associated with varioushuman diseasessmall-molecule inhibitors of these kinases have great

potential as therapeutic agents In addition these compounds can also be used as powerful tools in studies aimed atunderstanding the PAK signaling pathwayPAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actinremodelling and their ability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role intumor cell invasion and metastasis The current evidence suggests the involvement of PAKs in motility cell survivalanchorage-independent growth angiogenesis invasion migration and regulation of cell cycle and mitosisConsequently PAKs have also been implicated in a number of pathological conditions including cancer

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9902Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 1 g 5 g

Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

PAK Inhibitors amp Modulators

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Fingolimod is a ( ) antagonistsphingosine 1-phosphate S1Pwith of 0033 nM in K562 and NK cells Fingolimod also isIC50a activatorpak1

Bioactivity Fingolimod hydrochloride is a ( )sphingosine 1-phosphate S1Pantagonist with an of 0033 nM in K562 and NK cellsIC50Fingolimod hydrochloride also is a activatorpak1

Bioactivity FRAX1036 is a inhibitor with s of 233 nM 724 nM andPAK Ki24 μM for PAK1 PAK2 and PAK4 respectively

Bioactivity FRAX486 is a p21-activated kinase ( ) inhibitor with sPAK IC50of 14 33 and 39 nM for PAK1 PAK2 and PAK3 respectively

Bioactivity FRAX597 is a potent group I p21-activated Kinases ( s)PAKinhibitor with of 8 13 and 19 nM for and IC50 PAK1 2 3

Bioactivity G-5555 is a potent p21-activated kinase 1 ( ) inhibitorPAK1with s of 37 nM and 11 nM for PAK1 and PAK2 respectivelyKi

Bioactivity G-5555 hydrochloride is a potent and selective p21-activatedkinase 1 ( ) inhibitor with a of 37 nMPAK1 Ki

Bioactivity IPA-3 is a selective non-ATP competitive inhibitor withPAK1 of 25 μM and shows no inhibition to group II PAKs (PAKsIC50

4-6)

Bioactivity NVS-PAK1-1 is a potent and selective allosteric PAK1inhibitor with an of 5 nMIC50

114 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Fingolimod (FTY720 free base) Cat No HY-11063

Fingolimod hydrochloride (FTY720) Cat No HY-12005

FRAX1036 Cat No HY-19538

FRAX486 Cat No HY-15542B

FRAX597 Cat No HY-15542A

G-5555 Cat No HY-19635

G-5555 hydrochloride Cat No HY-19635A

IPA-3 Cat No HY-15663

NVS-PAK1-1 Cat No HY-100519

wwwMedChemExpresscom 115

Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity PAK-IN-1 is a inhibitor that displays group IIPAKselectivity PAK-IN-1 inhibits PAK4 PAK5 and PAK6 with sIC50of 75 36 126 nM respectively

Bioactivity PF-3758309 is an inhbitor of with of 13 nM forPAK IC50PAK4

PAK-IN-1 Cat No HY-12632

PF-3758309 Cat No HY-13007

PARPpoly ADP ribose polymerase

PARP is a family of proteins involved in a number of cellular processesinvolving mainly DNA repair and programmed cell death The PARPfamily comprises 17 members They have all very different structuresand functions in the cell PARP1 PARP2 VPARP (PARP4) Tankyrase-1and -2 (PARP-5a or TNKS and PARP-5b or TNKS2) have a confirmedPARP activity Others include PARP3 PARP6 TIPARP (or PARP7)PARP8 PARP9 PARP10 PARP11 PARP12 PARP14 PARP15 andPARP16 PARP is found in the cellrsquos nucleus The main role is to detectand signal single-strand DNA breaks (SSB) to the enzymaticmachinery involved in the SSB repair

116 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

wwwMedChemExpresscom 117

Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9839Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9992Clinical Data Phase 2Size 10mM x 1mL in Water

200 mg 500 mg

PARP Inhibitors amp Modulators

Bioactivity 3-Aminobenzamide is a potent inhibitor of with of appr 50 nM in CHO cellsPARP IC50

and acts as a mediator of oxidant-induced myocyte dysfunctionduring reperfusion

Bioactivity A-966492 is a novel and potent inhibitor of and with of 1 nM andPARP1 PARP2 Ki

15 nM respectively

Bioactivity AG14361 is a potent inhibitor with a of lt 5 nMPARP-1 Kiand in permeabilized SW620 and intact SW620 cells the sIC50are 29 nM and 14 nM respectively

Bioactivity AZ6102 is a potent dual and inhibitor withTNKS1 TNKS2s of 3 nM and 1 nM respectively and alao has 100-foldIC50

selectivity against other PARP family enzymes with s ofIC5020 μM 05 μM and gt3 μM for PARP1 PARP2 and PARhellip

Bioactivity AZD-2461 is a potent inhibitor with s of 5 nM 2 nMPARP IC50and 200 nM for PARP1 PARP2 and PARP3 respectively

Bioactivity BGP-15 is a inhibitor with an and a of 120 andPARP IC50 Ki57 μM respectively

Bioactivity BRCA1-IN-1 is a novel small-molecule-like inhibitorBRCA1with and of 053 μM and 071 μM respecrivelyIC50 Ki

Bioactivity Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolatedfrom traditional Chinese herb WT WangCorydalis yanhusuoDehydrocorydaline regulates protein expression of Bax Bcl-2activates and inactivates caspase-7 caspase-8 PARP

Bioactivity E7449 is a potent and inhibitor and alsoPARP1 PARP2inhibits and with s of 20 10 50 andTNKS1 TNKS2 IC5050 nM for PARP1 PARP2 TNKS1 and TNKS2 respectively using

P-NAD as substrate32 +

Bioactivity G007-LK is a potent and selective inhibitor of andTNKS1 with s of 46 nM and 25 nM respectivelyTNKS2 IC50

3-Aminobenzamide (PARP-IN-1) Cat No HY-12022

A-966492 Cat No HY-10614

AG14361 Cat No HY-12032

AZ6102 Cat No HY-12975

AZD-2461 Cat No HY-13536

BGP-15 Cat No HY-100828

BRCA1-IN-1 Cat No HY-100863

Dehydrocorydaline (13-Methylpalmatine) Cat No HY-N0674

E7449 Cat No HY-12418

G007-LK Cat No HY-12438

Purity 9952Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9858Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg

Bioactivity GeA-69 is a selective highly cell permeable allostericinhibitor of poly-adenosine-diphosphate-ribose polymerase 14

targeting macrodomain 2 with a of 21 microM (PARP14) Kd[1]

Bioactivity Iniparib (BSI-201) is an irreversible inhibitor of PARP1used in the research of triple negative breast cancer

Bioactivity JW 55 is a potent and selective signaling pathwayβ-catenininhibitor which functions via inhibition of the PARP domainof tankyrase 1 and tankyrase 2 (TNKS12) JW 55 decreasesauto-PARsylation of TNKS12 in vitro with s of 19 μM andIC50830 nM respectively

Bioactivity K-756 is a direct and selective ( ) inhibitortankyrase TNKSwhich inhibits the ADP-ribosylation activity of andTNKS1

with s of 31 and 36 nM respectivelyTNKS2 IC50

Bioactivity ME0328 is a potent and selective inhibitor withARTD3 PARP3an of 089plusmn028 μMIC50

Bioactivity MN-64 is a potent inhibitor with s of 6 nMtankyrase 1 IC5072 nM 191 μM and 394 μM for TNKS2 ARTD1 andTNKS1ARTD2 respectively

Bioactivity Niraparib (MK-4827) is a highly potent and PARP1 PARP2inhibitor with s of 38 and 21 nM respectivelyIC50

Bioactivity Niraparib hydrochloride (MK-4827 hydrochloride) is anexcellent and inhibitor with of 38 and 21PARP1 PARP2 IC50nM respectively

Bioactivity Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent inhibitor with of 24 nMPARP1 IC50

Bioactivity Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1and inhibitor with an of 38 and 21 nMPARP2 IC50respectively

118 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

GeA-69 Cat No HY-108708

Iniparib (BSI-201 NSC-746045 IND-71677) Cat No HY-12015

JW 55 Cat No HY-13968

K-756 Cat No HY-U00422

ME0328 Cat No HY-100225

MN-64 Cat No HY-19351

Niraparib (MK-4827) Cat No HY-10619

Niraparib hydrochloride (MK-4827 (hydrochloride)) Cat No HY-10619A

Niraparib R-enantiomer (MK 4827 (R-enantiomer)) Cat No HY-10619D

Niraparib tosylate (MK-4827 (tosylate)) Cat No HY-10619B

wwwMedChemExpresscom 119

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg

Purity 9768Clinical Data No Development ReportedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2 g

Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity NMS-P118 is a potent orally available and highly selective Inhibitor for cancer therapyPARP-1

Bioactivity NMS-P515 is a potent and stereospecific inhibitorPARP-1with an of 27 nM in hela cells Anti-tumor activity IC50

[1]

Bioactivity NVP-TNKS656 is a highly potent selective and orally active inhibitor with of 6 nM and is gt 300 foldTNKS2 IC50

selectivity against and PARP1 PARP2

Bioactivity Olaparib (AZD2281KU0059436) is a potent and oral PARPinhibitor with s of 5 and 1 nM for and IC50 PARP1 PARP2

respectively

Bioactivity Pamiparib is a inhibitor which can be used for thePARPtreatment of various cancers including the solid tumorextracted from patent WO 2013097225 A1

Bioactivity PARP-2-IN-1 is a potent and selective inhibitor withPARP-2an of 115 nMIC50

Bioactivity PJ34 is a potent specific inhibitor of with ofPARPl 2 IC50110 nM and 86 nM respectively

Bioactivity PJ34 hydrochloride is an inhibitor of with of 110PARPl12 IC50nM and 86 nM respectively

Bioactivity PROTAC PARP1 degrader is a degrader based on thePARP1 technology It induces significant PARP1 cleavage andPROTAC

programmed cell death PROTAC PARP1 degrader at 10 μM at 24 hinhibits MDA-MB-231 cell line with an of 612 μMIC50

Bioactivity RK-287107 is a potent and specific inhibitor withtankyrases of 143 and 106 nM for and IC50 tankyrase-1 tankyrase-2

respectively RK-287107 blocks colorectal cancer cell growth[1]

NMS-P118 Cat No HY-18954

NMS-P515 Cat No HY-128599

NVP-TNKS656 (TNKS656) Cat No HY-13990

Olaparib (AZD2281 KU0059436) Cat No HY-10162

Pamiparib (BGB-290) Cat No HY-104044

PARP-2-IN-1 Cat No HY-102035

PJ34 Cat No HY-13688A

PJ34 hydrochloride Cat No HY-13688

PROTAC PARP1 degrader Cat No HY-114324

RK-287107 Cat No HY-123892

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9962Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9888Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9508Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9983Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9989Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9981Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity Rucaparib (AG014699) is an inhibitor of with of 14 nM for PARP1 in aPARP Ki

cell-free assay and also shows binding affinity to eightother PARP domains

Bioactivity Rucaparib Camsylate is an inhibitor of with a of 14PARP KinM for PARP1 and also shows binding affinity to eight otherPARP domains

Bioactivity Rucaparib phosphate (AG-014699 phosphate) is a potent and oral inhibitor with a of 14 nM for PARP1 in cell-freePARP Ki

assay also showing binding affinity to eight other PARPdomains

Bioactivity Talazoparib (BMN-673) is a highly potent inhibitorPARP12with s of 12 nM and 087 nM respectivelyKi

Bioactivity Talazoparib 8R9S (BMN-673 8R9S) is an enantiomer ofTalazoparib less active than Talazoparib on the inhibition of

with an of 144 nMPARP1 IC50

Bioactivity Talazoparib tosylate (BMN 673ts) is a novel potent and orallyavailable inhibitor with an of 057 nM forPARP12 IC50PARP1

Bioactivity UPF 1069 is a inhibitor with s of 8 and 03 μM forPARP IC50PARP-1 and PARP-2 respectively

Bioactivity Veliparib is a potent inhibitor inhibiting andPARP PARP1 with s of 52 and 29 nM respectivelyPARP2 Ki

Bioactivity Veliparib (dihydrochloride) is a potent inhibitor of and with s of 52PARP1 PARP2 Ki

nM and 29 nM in cell-free assays respectively

Bioactivity WD2000-012547 is a selective poly(ADP-ribose)-polymerase(PARP-1) inhibitor with a pK of 8221i

120 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Rucaparib (AG014699 PF-01367338) Cat No HY-10617A

Rucaparib Camsylate Cat No HY-102003

Rucaparib phosphate (AG-014699 phosphate PF-01367338 phosphate) Cat No HY-10617

Talazoparib (BMN-673 LT-673) Cat No HY-16106

Talazoparib 8R9S (BMN-673 (8R9S) (8R9S)-LT-673) Cat No HY-16106A

Talazoparib tosylate (BMN 673ts) Cat No HY-108413

UPF 1069 Cat No HY-14478

Veliparib (ABT-888) Cat No HY-10129

Veliparib dihydrochloride (ABT-888 dihydrochloride) Cat No HY-10130

WD2000-012547 Cat No HY-U00223

wwwMedChemExpresscom 121

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Bioactivity XAV-939 is a inhibitor and an indirecttankyrase (TNKS)inhibitor of with s of 5 and 2Wntβ-catenin signaling IC50nM for TNKS1 and TNKS2 respectively

XAV-939 Cat No HY-15147

PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinase

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) isactivated in response to a variety of endoplasmic reticulum stressesimplicated in numerous disease states PERK is implicated intumorigenesis and cancer cell survival GSK2606414 is an orallyavailable potent and selective PERK inhibitor GSK2606414 inhibitsPERK activation in cells and inhibits the growth of a human tumorxenograft in mice PERK activation is independent of the largeincrease in unfolded nascent proteins within the ER followingtransient global brain ischemia

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Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

PERK Inhibitors amp Modulators

Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)

Bioactivity GSK2606414 is a cell-permeable and orally available proteinkinase R-like endoplasmic reticulum (ER) kinase (PERK)inhibitor with an of 04 nMIC50

Bioactivity GSK2656157 is a selective and ATP-competitive inhibitor ofprotein kinase R (PKR)-like endoplasmic reticulum kinase (

) with an of 09 nMPERK IC50

Bioactivity ISRIB (trans-isomer) is a potent inhibitor of with anPERK of 5 nMIC50

CCT020312 Cat No HY-119240

GSK2606414 Cat No HY-18072

GSK2656157 Cat No HY-13820

ISRIB trans-isomer Cat No HY-12495

Polo-like Kinase (PLK)

Polo-like Kinases (PLKs) are important regulators of the cell cycle Plksare involved in the formation of and the changes in the mitoticspindle and in the activation of CDKcyclin complexes duringM-phase of the cell cyclePolo-like kinases (Plks) are a family ofconserved serinethreonine kinases involved in the regulation of cellcycle progression through G2 and mitosis Mammalian polo-likekinases include Plk1 (Xenopus Plx1) Plk2Snk (Xenopus Plx2)Plk3PrkFnK (Xenopus Plx3) Plk4Sak and Plk5 Plk1 is involved in theregulation of key steps during cell division DNA damage repairpathways apoptosis and the progression of the cell cycle Plk3 is amultifunctional stress response protein that responses to signals

induced by DNA damage andor mitotic spindle disruption

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Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9982Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9845Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9897Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9857Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9995Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Polo-like Kinase (PLK) Inhibitors amp Modulators

Bioactivity BI 2536 is a dual and inhibitor with s of 083PLK1 BRD4 IC50

and 25 nM respectively BI-2536 suppresses IFNB[1]

(encoding IFN-β) gene transcription [4]

Bioactivity Centrinone (LCR-263) is a selective and reversible inhibitorof polo-like kinase 4 ( ) with a of 016 nMPlK4 Ki

Bioactivity Centrinone-B (LCR-323) is a potent and highly selective PLK4inhibitor with a of 059 nMKi

Bioactivity CFI-400945 free base is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity CFI-400945 fumarate is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively

Bioactivity GSK461364 is a selective reversible and ATP-competitive inhibitor with a value of 22 nMPolo-like kinase 1 (PLK1) Ki

Bioactivity GW843682X is a selective ATP-competitive inhibitor of PLK1and with s of 22 nM and 91 nM respectively andPLK3 IC50is also gt100-fold selective against 30 other kinases

Bioactivity HMN-214 an orally bioavailable prodrug of HMN-176 is aninhibitor of polo-like kinase-1 ( ) with antitumorplk1activity

Bioactivity LFM-A13 is a potent inhibitor inhibitsBTK JAK2 PLKrecombinant BTK Plx1 and PLK3 with s of 25 μM 10 μM andIC5061 μM LFM-A13 shows no effects on JAK1 and JAK3 Src familykinase HCK EGFR and IRK

Bioactivity MLN0905 is a potent inhibitor with an of 2 nMPLK1 IC50

BI 2536 Cat No HY-50698

Centrinone (LCR-263) Cat No HY-18682

Centrinone-B (LCR-323) Cat No HY-18683

CFI-400945 free base Cat No HY-12300

CFI-400945 fumarate Cat No HY-12300B

GSK461364 (GSK461364A) Cat No HY-50877

GW843682X (GW843682) Cat No HY-11003

HMN-214 (IVX-214) Cat No HY-12045

LFM-A13 Cat No HY-18009

MLN0905 (PLK1 Inhibitor) Cat No HY-15155

Purity 9759Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg

Purity 9949Clinical Data Phase 3Size 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9809Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9626Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 500 mg 1 g

Purity 9970Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd

12 nM for Mps1 and a of 61 nM for Plk1Kd

Bioactivity NMS-1286937 is a potent selective and orally available PLK1inhibitor with an of 2 nMIC50

Bioactivity Poloxime a hydrolysis product of poloxin is anon-ATP-competitive inhibitor with moderate Plk1Plk1inhibitory activity

Bioactivity Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1)inhibitor that targets the polo-box domain with an ofIC50appr 48 μM

Bioactivity Rigosertib (ON-01910) is a multi-kinase inhibitor and aselective anti-cancer agent which induces apoptosis byinhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib is a selective andhellip[1] [2]

Bioactivity Rigosertib sodium (ON-01910 sodium) is a multi-kinaseinhibitor and a selective anti-cancer agent which inducesapoptosis by inhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib sodium is a selective andhellip[1] [2]

Bioactivity Ro3280 is a potent highly selective inhibitor of withPLK1an and a of 3 nM and 009 nM respectively andIC50 Kdnearly has no effect on PLK2 and PLK3

Bioactivity SBE13 is a potent and selective inhibitor with an ofPlk1 IC50200 pM SBE13 poorly inhibits Plk2 (IC gt66 μM) or Plk350(IC =875 nM)50

Bioactivity SBE13 Hydrochloride is a potent and selective inhibitorPlk1with an of 200 pM SBE13 Hydrochloride poorly inhibitsIC50Plk2 (IC gt66 μM) or Plk3 (IC =875 nM)50 50

Bioactivity TAK-960 is an orally available selective inhibitor of with an of 08 nM at 10 μMpolo-like kinase 1 (PLK1) IC50

ATP TAK-960 also shows inhibitory activities against PLK2and with s of 169 and 502 nM respectivelyPLK3 IC50

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Mps1-IN-2 Cat No HY-13994

NMS-1286937 (NMS-P937) Cat No HY-15828

Poloxime Cat No HY-77195

Poloxin Cat No HY-12134

Rigosertib (ON-01910) Cat No HY-12037A

Rigosertib sodium (ON-01910 sodium) Cat No HY-12037

Ro3280 Cat No HY-15161

SBE13 Cat No HY-15158A

SBE13 Hydrochloride Cat No HY-15158

TAK-960 Cat No HY-15160

wwwMedChemExpresscom 127

Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9955Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg

Purity 9980Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity TAK-960 dihydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 dihydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TAK-960 hydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 hydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50

Bioactivity TC-S 7005 is a inhibitor with s ofPolo-like kinases (Plks) IC504 nM 24 nM and 214 nM for Plk2 Plk3 and Plk1 respectively

[1]

Bioactivity Volasertib is a highly potent Polo-like kinase 1 (PLK1)inhibitor with an of 087 nM as well as the two closelyIC50related kinases and with s of 5 and 56 nMPLK2 PLK3 IC50respectively

Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]

and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively

TAK-960 dihydrochloride Cat No HY-15160B

TAK-960 hydrochloride Cat No HY-15160A

TC-S 7005 Cat No HY-108597

Volasertib (BI 6727) Cat No HY-12137

Wortmannin (SL-2052 KY-12420) Cat No HY-10197

PPARPeroxisome proliferator-activated receptors

PPARs (Peroxisome proliferator-activated receptors) areligand-activated transcription factors of nuclear hormone receptorsuperfamily comprising of the following three subtypes PPARαPPARγ and PPARβδ PPARs play essential roles in the regulation ofcellular differentiation development and metabolism (carbohydratelipid protein) and tumorigenesis of higher organisms All PPARsheterodimerize with the retinoid X receptor (RXR) and bind to specificregions on the DNA of target genes Activation of PPAR-α reducestriglyceride level and is involved in regulation of energy homeostasisActivation of PPAR-γ enhances glucose metabolism whereasactivation of PPAR-βδ enhances fatty acids metabolism

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Purity 9905Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg

Purity 9921Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 980Clinical Data Phase 4Size 50 mg

Purity 980Clinical Data LaunchedSize 5 mg 10 mg

Purity gt98Clinical Data Phase 2Size 1 mg

Purity 9900Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 g

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg

PPAR Inhibitors amp Modulators

Bioactivity 4-O-Methyl honokiol is a natural neolignan isolated from acts as a agonist and inhibtisMagnolia officinalis PPARγ

activity used for cancer and inflammation researchNF-κB

Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB

Bioactivity Adelmidrol exerts important anti-inflammatory effects that arepartly dependent on Adelmidrol reduces PPARγ NF-κBtranslocation and expressionCOX-2

Bioactivity Aleglitazar(R1439 RO-0728804) is a new dual PPAR-αγ agonistwith IC50 of 28 nM46 nM

Bioactivity Arhalofenate (MBX 102) is a selective partial agonist ofperoxisome proliferator-activated receptor used for(PPAR)-γthe treatment of type 2 diabetes

Bioactivity Astaxanthin a red dietary carotenoid isolated from is an inhibitor of and aHaematococcus pluvialis PPARγ

potent antioxidant with antiproliferative neuroprotective andanti-inflammatory activity Astaxanthin has potential in[1]

the treatment of various diseases such as cancers andhellip

Bioactivity Astragalus polysaccharide are active components of thepolysaccharides extract of Astragulus attenuatesTNF-α-induced insulin resistance by suppressing miR-721 andactivating and in 3T3-L1 adipocytesPPAR-γ PI3KAkt

Bioactivity AVE-8134 is a potent agonist with values of 100PPARα EC50and 3000 nM for human and rodent PPARα receptor respectively

Bioactivity Balaglitazone is a selective partial agonist with anPPARγ of 1351 μM for human EC50 PPARγ

Bioactivity Bezafibrate is an agonist of with s of 50 μM 60PPAR EC50μM 20 μM for and and 90 μMhuman PPARα PPARγ PPARδ55 μM 110 μM for and murine PPARα PPARγ PPARδrespectively Bezafibrate is used as an hypolipidemic agent

4-O-Methyl honokiol Cat No HY-U00450

5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027

Adelmidrol Cat No HY-B1026

Aleglitazar (R1439 RO0728804) Cat No HY-14728

Arhalofenate (MBX 102 JNJ 39659100) Cat No HY-14831

Astaxanthin Cat No HY-B2163

Astragalus polysaccharide (Astragalus Polysacharin) Cat No HY-N0937

AVE-8134 Cat No HY-U00014

Balaglitazone (DRF 2593 NN 2344) Cat No HY-16086

Bezafibrate (BM15075) Cat No HY-B0637

Purity 9877Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity 9966Clinical Data Phase 4Size 10mM x 1mL in DMSO

500 mg 1 g 5 g 10 g

Purity 9959Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9981Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Bioactivity BMS-687453 is a potent and selective agonist with anPPARα and of 10 nM and 260 nM for human and 4100EC50 IC50 PPARα

nM and gt15000 nM for PPARγ in PPAR-GAL4 transactivationassays

Bioactivity CDDO-Im (CDDO-imidazolide) is an activator of and Nrf2 PPARwith s of 232 and 344 nM for PPARα and PPARγKi

Bioactivity Chiglitazar is a dual agonist with of 12PPARαγ EC s50008 17 μM for PPARα PPARγ and PPARδ respectively

Bioactivity Choline Fenofibrate (ABT-335) is the choline salt offenofibric acid under clinical development as a combinationtherapy with rosuvastatin for the management of dyslipidemia

Bioactivity Ciprofibrate is a peroxisome proliferator-activated receptoragonist

Bioactivity Ciprofibrate D6 is deuterium labeled Ciprofibrate which is aperoxisome proliferator-activated receptor agonist

Bioactivity Clofibrate is an agonist of with s of 50 μM 500PPAR EC50μM for murine PPARα and PPARγ and 55 μM 500 μM for humanPPARα and PPARγ respectively

Bioactivity Daidzein is a soy isoflavone which acts as a activatorPPAR

Bioactivity DG172 dihydrochloride is a selective antagonist withPPARβδan of 27 nMIC50

Bioactivity Elafibranor is a agonist with s of 45 and 175PPARαδ EC50nM respectively

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BMS-687453 Cat No HY-10678

CDDO-Im (RTA-403 TP-235 CDDO-Imidazolide) Cat No HY-15725

Chiglitazar Cat No HY-106266

Choline Fenofibrate (ABT-335) Cat No HY-14739

Ciprofibrate (Win35833) Cat No HY-B0664

Ciprofibrate D6 Cat No HY-B0664S

Clofibrate Cat No HY-B0287

Daidzein Cat No HY-N0019

DG172 dihydrochloride Cat No HY-19737A

Elafibranor (GFT505) Cat No HY-16737

wwwMedChemExpresscom 131

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9938Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g 10 g

Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Bioactivity Ertiprotafib is an inhibitor of PTP1B IkB kinase β (IKK-β)and a dual agonist with an of 16 μMPPARα and PPARβ IC50for PTP1B 400 nM for IKK-β an of ~1 μM forEC50PPARαPPARβ

Bioactivity Eupatilin a lipophilic flavonoid isolated from Artemisiaspecies is a agonist and possesses anti-apoptoticPPARαanti-oxidative and anti-inflammatory activities

Bioactivity Fenofibrate is a agonist with an of 30 μMPPARα EC50 Bioactivity Fenofibric acid an active metabolite of fenofibrate is a activitor with s of 224 microM 147 microM and 106 microMPPAR EC50

for PPARα PPARγ and PPARδ respectively Fenofibric acid alsoinhibits enzyme activity with an of 48 nMCOX-2 IC50

Bioactivity FH535 is an inhibitor of and withWntβ-catenin PPARanti-tumor activities

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Fonadelpar is a agonist used in the research ofPPARδneuroparalytic keratopathy

Bioactivity Gemfibrozil is an activator of used as aPPAR-αlipid-lowering drug Gemfibrozil is also a nonselectiveinhibitor of several isoforms with values forP450 KiCYP2C9 2C19 2C8 and 1A2 of 58 24 69 and 82 μMrespectively

Bioactivity Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2Sanchinoside Rh1) is isolated from the root of Panax GinsengGinsenoside Rh1 inhibits the expression of PPAR-γ TNF-α

and IL-6 IL-1β

Bioactivity Glabridin is a natural isoflavan from bindsGlycyrrhiza glabrato and activates with an of 6115 nM GlabridinPPARγ EC50exhibits antioxidant anti-bacterial anti-nephriticanti-diabetic anti-fungal antitumor anti-inflammatoryantiosteoporotic cardiovascular protective neuroprotectivehellip

Ertiprotafib (PTP 112) Cat No HY-19383

Eupatilin Cat No HY-N0783

Fenofibrate Cat No HY-17356

Fenofibric acid (FNF acid) Cat No HY-B0760

FH535 Cat No HY-15721

Fisetin Cat No HY-N0182

Fonadelpar (NPS-005 SJP-0035) Cat No HY-17633

Gemfibrozil (CI-719) Cat No HY-B0258

Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2 Sanchinoside Rh1) Cat No HY-N0604

Glabridin Cat No HY-N0393

Purity 9875Clinical Data Phase 3Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9727Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9667Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Bioactivity GSK0660 is a potent antagonist of and withPPARβ PPARδs of 155 nM for both isoformsIC50

Bioactivity GSK376501A is a selective peroxisome proliferator-activatedreceptor gamma ( ) modulator for the treatment of type 2PPARγdiabetes mellitus

Bioactivity GSK3787 is a selective and irreversible peroxisomeproliferator-activated receptor δ ( ) antagonist withPPARδ

of 66pIC50

Bioactivity GW 501516 is a agonist with an of 11 nMPPARδ EC50

Bioactivity GW 6471 is a potent antagonistPPARα Bioactivity GW0742 is a potent and agonist with an ofPPARβ PPARδ IC501 nM for human in binding assay and s of 1 nMPPARδ EC5011 μM and 2 μM for human PPARα and PPARγPPARδrespectively

Bioactivity GW1929 is a potent agonist with a of 884 forPPAR-γ pKihuman and s of 856 and 827 for human PPAR-γ pEC50 PPAR-γ

and murine respectivelyPPAR-γ

Bioactivity GW7647 is a potent agonist with s of 6 nM 11PPARα EC50μM and 62 μM for human PPARα PPARγ and PPARδ respectively

Bioactivity GW9662 is a potent and selective antagonist with anPPARγ of 33 nM showing 10 and 1000-fold selectivity overIC50

PPARα and PPARδ respectively

Bioactivity Icariin is a flavonol glycoside Icariin inhibits andPDE5 activities with s of 432 nM and 7350 μMPDE4 IC50

respectively Icariin also is a activatorPPARα

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GSK0660 Cat No HY-12377

GSK376501A Cat No HY-101746

GSK3787 Cat No HY-15577

GW 501516 (GW 1516 GSK-516) Cat No HY-10838

GW 6471 Cat No HY-15372

GW0742 (GW610742) Cat No HY-13928

GW1929 Cat No HY-15655

GW7647 Cat No HY-13861

GW9662 Cat No HY-16578

Icariin (Ieariline) Cat No HY-N0014

wwwMedChemExpresscom 133

Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9889Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9921Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg

Purity gt98Clinical Data Phase 2Size 5 mg

Purity 9942Clinical Data Phase 2Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg

Bioactivity Imiglitazar (TAK559) is a potent and dual human andPPARα agonist with values of 67 and 31 nMPPARγ1 EC50

Bioactivity Indeglitazar is an orally available peroxisomeproliferator-activated receptor ( ) pan-agonist for allPPARthree PPAR subtypes alpha (α) delta (δ) and gamma (γ)

Bioactivity Inolitazone a novel high-affinity agonist that isPPARγdependent upon PPARγ for its biological activity with ofIC5008 nM for growth inhibition

Bioactivity Inolitazone dihydrochloride is a novel high-affinity PPARγagonist that is dependent upon PPARγ for its biologicalactivity with of 08 nM for growth inhibitionIC50

Bioactivity KD3010 is a potent orally active and selective PPARδagonist

Bioactivity L-165041 is a cell permeable agonist with s of 6 nMPPARδ Kiand appr 730 nM for PPARδ and PPARγ respectively and inducesadipocyte differentiation in NIH-PPARδ cells

Bioactivity Lanifibranor is a pan peroxisome proliferator-activated ( ) agonist with s of 15 087 and 021receptor PPAR EC50

μM for human and respectivelyPPARα PPARσ PPARγ

Bioactivity LJ570 is a dual agonist with s of 105PPARα PPARγ EC50

and 012 μM respectively [1]

Bioactivity MA-0204 is a potent highly selective and orally availableperoxisome proliferator activated receptor δ ( )PPARδmodulator with s of 04 nM 79 nM and 10 nM for humanEC50mouse and rat PPARδ respectively Potential treatment hellip

Bioactivity Magnolol a natural lignan isolated from the stem bark of is a dual agonist of both andMagnolia officinalis RXRα

with values of 104 microM and 177 microMPPARγ EC50respectively

Imiglitazar (TAK-559) Cat No HY-101649

Indeglitazar (PPM 204) Cat No HY-14817

Inolitazone (Efatutazone CS-7017 RS5444) Cat No HY-14792

Inolitazone dihydrochloride (Efatutazone (dihydrochloride)

CS-7017 (dihydrochloride) RS5444 (dihydrochloride)) Cat No HY-14792B

KD-3010 Cat No HY-111068

L-165041 Cat No HY-20019

Lanifibranor (IVA337) Cat No HY-104049

LJ570 Cat No HY-111775

MA-0204 Cat No HY-114739

Magnolol Cat No HY-N0163

Purity 9639Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9918Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in Ethanol

10 mg

Purity gt98Clinical DataSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9872Clinical Data Phase 1Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Bioactivity Naringenin is the predominant flavanone in grapefruitdisplays strong anti-inflammatory and antioxidant activities

Bioactivity Naveglitazar racemate is the racemate of NaveglitazarNaveglitazar is a nonthiozolidinedione peroxisomeproliferator-activated receptor ( ) α-γ dual γ-dominantPPARagonist that has shown glucose-lowering potential in animalmodels and in the clinic

Bioactivity NXT629 is a potent selective and competitive PPAR-αantagonist with an of 77 nM for human PPARα shows highIC50selectivity over other nuclear hormone receptor such asPPARδ PPARγ ERβ GR and TRβ s are 60 15 152 3hellipIC50

Bioactivity Oleoylethanolamide is a high affinity endogenous PPAR-αagonist which plays an important role in the treatment ofobesity and arteriosclerosis

Bioactivity Palmitelaidic acid is the trans isomer of palmitoleic acidPalmitoleic acid is one of the most abundant fatty acids inserum and tissue

Bioactivity Peliglitazar racemate is the racemate of PeliglitazarPeliglitazar is a novel dual αγ PPAR activator

Bioactivity Pemafibrate is a highly selective agonist with anPPARα of 1 nMEC50

Bioactivity Pemafibrate racemate is the racemate of pemafibrate andactivates activity with s of 1 nM gt10 μM andPPARα EC5017 μM for h-PPARα h-PPARγ and h-PPARδ respectively

Bioactivity Pioglitazone is a potent and selective agonist withPPARγhigh affinity binding to the PPARγ ligand-binding domain with

of 093 and 099 μM for human and mouse PPARγEC50respectively

Bioactivity Pioglitazone hydrochloride is a potent and selective PPARγagonist with s of 093 and 099 μM for human and mouseEC50PPARγ respectively

134 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Naringenin Cat No HY-N0100

Naveglitazar racemate Cat No HY-U00036

NXT629 Cat No HY-114263

Oleoylethanolamide (N-(2-Hydroxyethyl)oleamide

N-Oleoyl-2-aminoethanol N-Oleoylethanolamide hellip) Cat No HY-107542

Palmitelaidic Acid (9-trans-Hexadecenoic acid trans-Palmitoleic acid) Cat No HY-N2341

Peliglitazar racemate (BMS 426707-01 racemate) Cat No HY-101738A

Pemafibrate ((R)-K-13675) Cat No HY-17618

Pemafibrate racemate (K13675 (racemate)) Cat No HY-17618A

Pioglitazone (U 72107) Cat No HY-13956

Pioglitazone hydrochloride (U 72107A AD 4833) Cat No HY-14601

wwwMedChemExpresscom 135

Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 200 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9836Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 500 mg 1 g 5 g

Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 250 mg

Bioactivity Pirinixic acid (Wy-14643) is a potent agonist of withPPARαs of 063 μM 32 μM for murine and PPARγ and 50EC50 PPARα

μM 60 μM 35 μM for human PPARγ and PPARδPPARαrespectively

Bioactivity PPAR agonist 1 is an agonist of and usedPPAR α PPAR γfor reducing blood glucose lipid levels lowering cholesteroland reducing body weight

Bioactivity PPARα-MO-1 is a potent modulator extracted from patentPPARαWO2004110982A1 formula I

Bioactivity PPARδ agonist is a agonist extracted from patentPPARδUS20180071304 compound example 10

Bioactivity Pparδ agonist 1 is a agonist with an of 506PPAR-δ EC50nM used in the research of PPAR-delta related diseases suchas mitochondrial diseases muscular diseases vasculardiseases demyelinating diseases and metabolic diseases

Bioactivity Pparδ agonist 2 is a agonist extracted from patent WOPPARδ2016057656 A1

Bioactivity Raspberry ketone is a major aromatic compound of redraspberry widely used as a fragrance in cosmetics and as aflavoring agent in foodstuff also shows agonisticPPAR-αactivity

Bioactivity Retinoic acid is a metabolite of vitamin A that playsimportant roles in cell growth differentiation andorganogenesis Retinoic acid is a natural agonist of RARnuclear receptors with s of 14 nM for RARαβγ RetinhellipIC50

Bioactivity RG-12525 is a a specific competitive and orally effectiveantagonist of the and peptidoleukotrienes LTC4 LTD4 LTE4inhibiting LTC4- LTD4- and LTE4-inducd guinea pig parenchymalstrips contractions with s of 26 nM 25 nM and 7 nMIC50respectively RG-12525 is also a peroxisomehellip

Bioactivity Rosiglitazone (BRL49653) is a selective agonist withPPARγs of 30 nM 100 nM and 60 nM for andEC50 PPARγ1 PPARγ2

respectivelyPPARγ

Pirinixic acid (Wy-14643) Cat No HY-16995

PPAR agonist 1 Cat No HY-U00340

PPARα-MO-1 Cat No HY-U00068

Pparδ agonist Cat No HY-112597

Pparδ agonist 1 Cat No HY-107901

Pparδ agonist 2 Cat No HY-100120

Raspberry ketone (Frambione 4-(4-Hydroxyphenyl)-2-butanone) Cat No HY-N1426

Retinoic acid (ATRA Tretinoin Vitamin A acid all-trans-Retinoic acid) Cat No HY-14649

RG-12525 (NID 525) Cat No HY-101676

Rosiglitazone (BRL49653) Cat No HY-17386

Purity 9953Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9852Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9885Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg

Purity 9803Clinical Data Phase 3Size 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9925Clinical Data LaunchedSize 100 mg 500 mg

Bioactivity Rosiglitazone maleate is a potent and selective activator of with s of 30 nM 100 nM and 60 nM for PPARγ EC50 PPARγ1

and respectively and a of appr 40 nMPPARγ2 PPARγ Kdfor Rosiglitazone maleate is also an modulator of PPARγ hellip

Bioactivity Saroglitazar is a novel peroxisome proliferator-activatedreceptor ( ) agonist with predominant PPARα and moderatePPARPPARγ activity with values of 065 pM and 3 nM in HepG2EC50cells respectively

Bioactivity Saroglitazar magnesium is a novel peroxisomeproliferator-activated receptor ( ) agonist withPPARpredominant PPARα and moderate PPARγ activity with EC50values of 065 pM and 3 nM in HepG2 cells respectively

Bioactivity Seladelpar is an orally active potent (50 effectconcentration 2 nM) and specific agonistEC50 PPAR-δ

Bioactivity Seladelpar sodium salt (MBX-8025) is an orally active potentand specific agonist with an of 2 nM showingPPARδ EC50more than 750-fold and 2500-fold selectivity over the PPARαand PPARγ receptors respectively

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

Bioactivity Troglitazone is a agonist with s of 550 nM andPPARγ EC50780 nM for human and murinePPARγ receptor respectively

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Rosiglitazone maleate (BRL 49653C) Cat No HY-14600

Saroglitazar Cat No HY-19937

Saroglitazar Magnesium Cat No HY-19937A

Seladelpar (MBX-8025) Cat No HY-19522

Seladelpar sodium salt (MBX-8025 sodium salt RWJ-800025 sodium salt) Cat No HY-19522A

T0070907 Cat No HY-13202

Troglitazone (CS-045) Cat No HY-50935

wwwMedChemExpresscom 137

RAD51

RAD51 protein family assist in repair of DNA double strand breaksRAD51 family members are homologous to the bacterial RecA andyeast Rad51 In humans RAD51 is a 339-amino acid protein that playsa major role in homologous recombination of DNA during doublestrand break repair RAD51 is involved in the search for homologyand strand pairing stages of the process RAD51 can interact with thessDNA-binding protein RPA BRCA2 PALB2 and RAD52 Recentstudies using fluorescent labeled Rad5 has indicated that Rad51fragments elongate via multiple nucleation events followed bygrowth with the total fragment terminating when it reaches about 2μm in length

Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

500 mg

RAD51 Inhibitors amp Modulators

Bioactivity Harmine is a natural dual-specificity tyrosinephosphorylation-regulated kinase ( ) inhibitor with(DYRK)anticancer and anti-inflammatory activities

Bioactivity IBR2 is a specific inhibitorRAD51

Bioactivity RAD51 Inhibitor B02 (B02) is an inhibitor of human withRAD51an of 274 μMIC50

Bioactivity RAD51-IN-2 (compound example 67A) is a inhibitorRAD51extracted from patent WO2019051465A1 [1]

Bioactivity RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM Bioactivity RI-2 is a reversible inhibitor with an of 4417RAD51 IC50μM and specifically inhibits homologous recombination repairin human cells

Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9

Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki

138 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Harmine (Telepathine) Cat No HY-N0737A

IBR2 Cat No HY-103710

RAD51 Inhibitor B02 (B02) Cat No HY-101462

RAD51-IN-2 Cat No HY-111887

RI-1 Cat No HY-15317

RI-2 Cat No HY-16904

RS-1 Cat No HY-19793

T0070907 Cat No HY-13202

wwwMedChemExpresscom 139

ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROK

ROCK (Rho-associated protein kinase) is a kinase belonging to theAGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopusinvertebrates and chicken Human ROCK1 has a molecular mass of158 kDa and is a major downstream effector of the small GTPaseRhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces thekinase activity of ROCKs by an autoinhibitory intramolecular fold ifRhoA-GTP is not present ROCK plays a role in a wide range ofdifferent cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators

of the cytoskeleton

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO

200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg

Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9954Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

ROCK Inhibitors amp Modulators

Bioactivity AT13148 is an orally active and ATP-competitive multi- AGC inhibitor with s of 38 nM402 nM50 nM 8 nM 3 nMkinase IC50

and 6 nM4 nM for Akt123 p70S6K PKA and ROCKIIIrespectively

Bioactivity Azaindole 1 is an orally active and ATP-competitive ROCKinhibitor with s of 06 and 11nM for human andIC50 ROCK-1

respectivelyROCK-2

Bioactivity BDP5290 is a potent inhibitor of both and withROCK MRCKs of 5 nM 50 nM 10 nM and 100 nM for IC50 ROCK1 ROCK2

and respectivelyMRCKα MRCKβ

Bioactivity Chroman 1 is a highly potent inhibitor with an ofROCK2 IC501 nM

Bioactivity Fasudil (HA-1077 AT877) a potent inhibitor of with aROCK of 033 μM for ROCK1 which is also a potent Ki Ca channel2+

antagonist and vasodilator

Bioactivity Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877Hydrochloride) a potent inhibitor of with a of 033ROCK Ki

μM for ROCK1 which is also a potent antagonistCa channel2+

and vasodilator

Bioactivity GSK180736A is a G protein-coupled receptor kinase 2 ( )GRK2inhibitor with an of 077 μMIC50

Bioactivity GSK269962A is a potent inhibitor with s of 16 and 4ROCK IC50nM for recombinant human and respectivelyROCK1 ROCK2

Bioactivity GSK429286A is a selective inhibitor of with an ROCK1 IC50value of 14 nM

Bioactivity H-1152 is a membrane-permeable and selective inhibitorROCKwith a value of 16 nM and an value of 12 nM forKi IC50

ROCK2

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AT13148 Cat No HY-16071

Azaindole 1 (TC-S 7001) Cat No HY-10319

BDP5290 Cat No HY-12437

Chroman 1 Cat No HY-15392

Fasudil (HA-1077 AT877) Cat No HY-10341A

Fasudil Hydrochloride (HA-1077 (Hydrochloride) AT-877 (Hydrochloride)) Cat No HY-10341

GSK180736A Cat No HY-18990

GSK269962A (GSK 269962) Cat No HY-15556

GSK429286A Cat No HY-11000

H-1152 Cat No HY-15720

wwwMedChemExpresscom 141

Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg

Purity 9726Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg 50 mg 100 mg

Purity gt98Clinical DataSize 10 mg

Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9929Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9940Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9813Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity H-1152 dihydrochloride is a membrane-permeable and selective inhibitor with a value of 16 nM and an valueROCK Ki IC50

of 12 nM for ROCK2

Bioactivity Hydroxyfasudil is a inhibitor with s of 073 andROCK IC50072 μM for and respectivelyROCK1 ROCK2

Bioactivity Hydroxyfasudil hydrochloride is a inhibitor with sROCK IC50of 073 and 072 μM for and respectivelyROCK1 ROCK2

Bioactivity LX7101 is a potent inhibitor of and with LIMK ROCK2 IC50values of 24 16 and 10 nM for LIMK1 LIMK2 and ROCK2respectively also inhibits with an less than 1 nMPKA IC50

Bioactivity Narciclasine is a plant growth modulator Narciclasinemodulates the RhoRho kinaseLIM kinasecofilin signalingpathway greatly increasing GTPase RhoA activity as well asinducing actin stress fiber formation in a RhoA-dependentmanner

Bioactivity Pentanoic acid a short-chain fatty acid is a product ofbacterial metabolism and are associated with allergic skindisorders Pentanoic acid activates signaling pathwayROCK

Bioactivity Ripasudil (K-115) is a specific inhibitor of with sROCK IC50of 19 and 51 nM for and respectivelyROCK2 ROCK1

Bioactivity Ripasudil free base (K-115 free base) is a specific inhibitorof with s of 19 and 51 nM for and ROCK IC50 ROCK2 ROCK1

respectively

Bioactivity RKI-1447 is a potent small molecule inhibitor of andROCK1 with values of 145 nM and 62 nM respectivelyROCK2 IC50

Bioactivity ROCK inhibitor-2 is a selective dual and ROCK1 ROCK2inhibitor with s of 17 nM and 2 nM respectively IC50

[1]

H-1152 dihydrochloride Cat No HY-15720A

Hydroxyfasudil (HA-1100) Cat No HY-13911

Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100

hydrochloride HA1100 hydrochloride) Cat No HY-13911A

LX7101 Cat No HY-12659

Narciclasine (Lycoricidinol) Cat No HY-16563

Pentanoic acid Cat No HY-N6056

Ripasudil (K-115) Cat No HY-15685

Ripasudil free base (K-115 (free base)) Cat No HY-15685A

RKI-1447 Cat No HY-15755

ROCK inhibitor-2 Cat No HY-119937

Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2g

Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9932Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg

Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9843Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Bioactivity ROCK-IN-1 is a potent inhibitor of with an of 12ROCK IC50nM for ROCK2

Bioactivity ROCK2-IN-2 is a selective inhibitor extracted fromROCK2patent US20180093978A1 Compound A-30 has an of lt1IC50μM

Bioactivity SAR407899 is a selective potent and ATP-competitive ROCKinhibitor with an of 135 nM for and s of 36IC50 ROCK-2 KinM and 41 nM for human and rat respectivelyROCK-2

Bioactivity SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an of 135 nM forROCK IC50

and s of 36 nM and 41 nM for human and rat ROCK-2 Ki ROCK-2

respectively

Bioactivity SB-772077B dihydrochloride is an aminofurazan-based Rho inhibitor with s of 56 nM and 6 nM towardkinase( ROCK) IC50

ROCK1 and ROCK2 respevtively [1]

Bioactivity SLx-2119 (KD-025) is a selective inhibitor of with anROCK2 of 105 nMIC50

Bioactivity SR-3677 is a potent and selective inhibitor with anROCK-II of ~3 nMIC50

Bioactivity Thiazovivin is a potent inhibitor which can protectROCKhuman embryonic stem cells

Bioactivity Y-27632 is an ATP-competitive inhibitor of and ROCK-I ROCK-IIwith of 220 nM and 300 nM for and Ki ROCK-I ROCK-II

respectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

Bioactivity Y-27632 dihydrochloride is a cell-permeable ATP-competitiveinhibitor of and with s of 220 and 300 nMROCK-I ROCK-II Kirespectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip

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ROCK-IN-1 Cat No HY-U00351

ROCK2-IN-2 Cat No HY-103620

SAR407899 Cat No HY-15687A

SAR407899 hydrochloride Cat No HY-15687

SB-772077B dihydrochloride Cat No HY-108518

SLx-2119 (KD-025) Cat No HY-15307

SR-3677 Cat No HY-13300

Thiazovivin Cat No HY-13257

Y-27632 Cat No HY-10071

Y-27632 dihydrochloride Cat No HY-10583

wwwMedChemExpresscom 143

Purity 9923Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Bioactivity Y-33075 is a selective inhibitor derived from Y-27632ROCKand is more potent than Y-27632 with an of 36 nMIC50

Bioactivity Y-33075 dihydrochloride is a selective inhibitor with anROCK of 36 nMIC50

Bioactivity ZINC00881524 is a inhibitorROCK

Y-33075 (Y 39983) Cat No HY-10067

Y-33075 dihydrochloride Cat No HY-10069

ZINC00881524 Cat No HY-101244

Sirtuin

Sirtuin (Sir2 proteins) are a class of proteins that possess eithermono-ADP-ribosyltransferase or deacylase activity includingdeacetylase desuccinylase demalonylase demyristoylase anddepalmitoylase activity Sirtuins regulate important biologicalpathways in bacteria archaeaand eukaryotes Sirtuins have beenimplicated in influencing a wide range of cellular processes like agingtranscription apoptosis inflammation and stress resistance as well asenergy efficiency and alertness during low-calorie situations Sirtuinscan also control circadian clocks and mitochondrial biogenesis

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wwwMedChemExpresscom 145

Purity 9891Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 500 mg 1 g

Purity 9909Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

100 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Sirtuin Inhibitors amp Modulators

Bioactivity 3-TYP is a selective inhibitor with an of 16 nMSIRT3 IC50more potent over SIRT1 ( =88 nM) SIRT2 ( =92 nM)IC50 IC50

Bioactivity AGK2 is a selective inhibitor with of 35 μM AGK2SIRT2 IC50can also inhibit and with of 30 and 91 μMSIRT1 SIRT3 IC50respectively

Bioactivity AK-1 is a potent specific and cell-permeable inhibitorSIRT2with an of 125 μMIC50

Bioactivity AK-7 is a selective cell- and brain-permeable inhibitorSIRT2with an of 155 μMIC50

Bioactivity Cambinol is a and inhibitor with values of 56SIRT1 SIRT2 IC50and 59 μM respectively

Bioactivity CAY10602 is a activatorSIRT1

Bioactivity Dihydrocoumarin is a compound found in Melilotus Dihydrocoumarin is a inhibitorofficinalis yeast Sir2p

Dihydrocoumarin also inhibits and withhuman SIRT1 SIRT2s of 208 μM and 295 μM respectively IC50

[1]

Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects

Bioactivity Ginkgolide C is a flavone isolated from leavesGinkgo bilobapossessing multiple biological functions such as decreasingplatelet aggregation and ameliorating Alzheimer disease

Bioactivity Inauhzin is a dual inhibitor and acts as anSirT1IMPDH2activator used in the research of cancerp53

3-TYP Cat No HY-108331

AGK2 Cat No HY-100578

AK-1 Cat No HY-101465

AK-7 Cat No HY-16691

Cambinol Cat No HY-100732

CAY10602 Cat No HY-104073

Dihydrocoumarin (Hydrocoumarin Chroman-2-one) Cat No HY-N1926

Fisetin Cat No HY-N0182

Ginkgolide C (BN-52022 Ginkgolide-C) Cat No HY-N0785

Inauhzin (INZ) Cat No HY-15869

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg

Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9876Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

1 g 5 g

Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg

Bioactivity MC3482 is a specific sirtuin5 ( ) inhibitorSIRT5 Bioactivity Nicotinamide is a form of vitamin B3 that plays essentialroles in cell physiology through facilitating NAD+ redoxhomeostasis and providing NAD+ as a substrate to a class ofenzymes that catalyze non-redox reactions Nicotinamide is aninhibitor of SIRT1

Bioactivity OSS_128167 is a selective inhibitor with s of 89SIRT6 IC501578 and 751 μM for and respectivelySIRT6 SIRT1 SIRT2

Bioactivity PROTAC Sirt2 Degrader-1 is a SirReal-based acts as aPROTAC degrader composed of a highly potent andSirt2

isotype-selective inhibitor a linker and a bona fideSirt2cereblon ligand for E3 ubiquitin ligase PROTAC Sirt2Degrader-1 shows an of 025 μM for Sirt2 with no effecthellipIC50

Bioactivity Salermide is an inhibitor of and can cause strongSirt1 Sirt2cancer-specific apoptotic cell death

Bioactivity Selisistat (EX-527) is a potent and selective inhibitorSIRT1with of 98 nMIC50

Bioactivity Selisistat S-enantiomer (EX-527 S-enantiomer) is theS-enantiomer of Selisistat with an of 123 nM for SIRT1IC50Selisistat S-enantiomer is much more potent than SelisistatR-enantiomer

Bioactivity SIRT-IN-1 is a potent inhibitor of with of 15SIRT123 IC s5010 33 μM respectively

Bioactivity SIRT-IN-2 is a potent inhibitor of with of 4SIRT123 IC s504 7 μM respectively

Bioactivity Sirt2-IN-1 (Compound 9) is a ( ) inhibitor withsirtuin 2 Sirt2an of 163 nM IC50

[1]

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MC3482 Cat No HY-112587

Nicotinamide (Niacinamide Nicotinic acid amide Vitamin B3) Cat No HY-B0150

OSS_128167 Cat No HY-107454

PROTAC Sirt2 Degrader-1 Cat No HY-103636

Salermide Cat No HY-101073

Selisistat (EX-527) Cat No HY-15452

Selisistat S-enantiomer (EX-527 (S-enantiomer)) Cat No HY-15452A

SIRT-IN-1 Cat No HY-16615

SIRT-IN-2 Cat No HY-16616

Sirt2-IN-1 Cat No HY-112427

wwwMedChemExpresscom 147

Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Purity 9939Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize

Purity 9887Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g

Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg

Purity 9944Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Bioactivity SIRT5 inhibitor 1 is a potent Human deacylaseSirtuin 5inhibitor with an of 011 μMIC50

Bioactivity Sirtinol is a inhibitor with s of 48 μM 577 μMsirtuin IC50and 131 μM for ySir2 hSIRT2 and hSIRT2 respectively

Bioactivity Sirtuin modulator 1 is a modulator of a homolog of SIRTl SIRT3with EC of lt 1 μM extracted from patent WO 201007185315A1 Compound No4

Bioactivity SRT 1460 a potent activator with an Sirtuin-1 (SIRT1) EC15value of 29 μM shows good selectivity for activation ofSIRT1 versus SIRT2 and SIRT3 (EC15 gt 300 μM) and is morepotent than Resveratrol and the closest sirtuin homologhellip

Bioactivity SRT 1720 is a selective activator of human with anSIRT1 of 016 μM and shows less potent activities agaiinstEC15

SIRT2 and SIRT3 with EC s of 37 μM and gt 300 μM15respectively

Bioactivity SRT 1720 Hydrochloride is a selective activator of withSIRT1an of 016 μM and shows less potent activities onEC15SIRT2 and SIRT3 with EC s of 37 μM and 300 μM15respectively

Bioactivity SRT 2104 is a first-in-class highly selective andbrain-permeable activator of the NAD dependent deacetylase+

increases Sirt1 protein but shows no effect on Sirt1Sirt1mRNA Used in the research of diabetes mellitus hellip

Bioactivity SRT 2183 is a selective activator with anSirtuin-1 (SIRT1) value of 036 μM SRT 2183 induces growth arrestEC15

[1]

and apoptosis concomitant with deacetylation of STAT3 andNF-κB and reduction of c-Myc protein levels [2]

Bioactivity Tenovin-1 is an inhibitor of and ansirtuin 1 sirtuin 2activator of and may have potential in the management ofp53cancer

Bioactivity Tenovin-6 is an inhibitor of and slightly inhibitsSIRT1 SIRT2 and is also a potent activator of with s ofHDAC8 p53 IC50

21 μM 10 μM and 67 μM for SirT1 SirT2 and SirT3respectively

SIRT5 inhibitor 1 Cat No HY-112634

Sirtinol Cat No HY-13515

Sirtuin modulator 1 Cat No HY-19758A

SRT 1460 Cat No HY-124037

SRT 1720 Cat No HY-10532

SRT 1720 Hydrochloride Cat No HY-15145

SRT 2104 Cat No HY-15262

SRT 2183 Cat No HY-19759

Tenovin-1 Cat No HY-13423

Tenovin-6 Cat No HY-15510

Purity 9855Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 50 mg 100 mg

Bioactivity Tenovin-6 Hydrochloride is an inhibitor of and SIRT1 SIRT2slightly inhibits and is also a potent activator ofHDAC8

with s of 21 μM 10 μM and 67 μM for SirT1 SirT2p53 IC50and SirT3 respectively

Bioactivity Thiomyristoyl is a potent and specific inhibitor with anSIRT2 of 28 nMIC50

Bioactivity UBCS039 is the first synthetic specific Sirtuin 6 (SIRT6)activator inducing autophagy in human tumor cells with an

of 38 μM EC50[1]

148 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Tenovin-6 Hydrochloride Cat No HY-15510B

Thiomyristoyl Cat No HY-101278

UBCS039 Cat No HY-115453

wwwMedChemExpresscom 149

SRPKSerine-arginine protein kinases

SRPKs is a critical enzyme family that regulates splicing activity in thecell The first serine-arginine (SR) protein kinase identified is SRPK1which is isolated from mitotic cells and it is described tophosphorylate SR proteins and to promote their release from nuclearspeckles during the G2M phase of the cell cycle SRPK1 is theprototype of the SRPK family which also includes the twohomologous SRPK2 and SRPK3 proteins SRPKs are characterized by abipartite catalytic domain separated by a unique spacer sequence andare mainly localized in the cytoplasm of mammalian cellsSRPKs can translocate into the nucleus of cells under severalconditions such as during the G2M phase of the cell cycle or after

osmotic stress or as a consequence of activation of the epidermal growth factor (EGF) signal transduction pathway

Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg

Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9917Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

SRPK Inhibitors amp Modulators

Bioactivity SPHINX31 is a potent and selective inhibitor of with an ofserinearginine-rich protein kinase 1 (SRPK1) IC50

59 nM SPHINX31 inhibits phosphorylation ofserinearginine-rich splicing factor 1 (SRSF1) SPHINX31 is apotential topical therapeutic for neovascular eye diseasehellip

Bioactivity SRPIN340 is an ATP-competitive serine-arginine-rich proteinkinase ( ) inhibitor with a of 089 μM for SRPK1SRPK Ki

Bioactivity SRPKIN-1 is a covalent and irreversible inhibitorSRPK12with s of 356 and 98 nM respectively Anti-angiogenesisIC50

effect [1]

150 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

SPHINX31 Cat No HY-117661

SRPIN340 (SRPK inhibitor) Cat No HY-13949

SRPKIN-1 Cat No HY-116856

wwwMedChemExpresscom 151

Telomerase

Telomerase is a ribonucleoprotein that is an enzyme that adds DNAsequence repeats (TTAGGG in all vertebrates) to the 3 end of DNAstrands in the telomere regions which are found at the ends ofeukaryotic chromosomes This region of repeated nucleotide calledtelomeres contains noncoding DNA and hinders the loss of importantDNA from chromosome ends As a result every time the chromosomeis copied only 100ndash200 nucleotides are lost which causes no damageto the organisms DNA Telomerase is a reverse transcriptase thatcarries its own RNA molecule which is used as a template when itelongates telomeres which are shortened after each replication cycleTelomerase a eukaryotic ribonucleoprotein (RNP) complex contains

both an essential RNA and a protein reverse transcriptase subunit By reverse transcription the telomerase RNPmaintains telomere length stability in almost all cancer cells

Purity 980Clinical Data No Development ReportedSize 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Telomerase Inhibitors amp Modulators

Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay

Bioactivity BIBR 1532 is a potent selective and non-competitive inhibitor with of 100 nM intelomerase IC50

a cell-free assay

Bioactivity Telomerase-IN-1 is a inhibitor with an ofTelomerase IC50019 μM

Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip

152 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

360A Cat No HY-15595

360A iodide (360 A iodide) Cat No HY-15595A

BIBR 1532 Cat No HY-17353

Telomerase-IN-1 Cat No HY-U00268

TMPyP4 tosylate (TMP 1363) Cat No HY-108477

wwwMedChemExpresscom 153

TOPKT-LAK cell-originated protein kinase

TOPK (T-lymphokine-activated killer cellndashoriginated protein kinasealso known as PBK or PDZ-binding kinase) is a SerThr protein kinasethat is highly expressed in many types of human cancer includingbreast and lung cancers TOPK is included in the ldquoconsensus stemnessranking signaturerdquo gene list that is up-regulated in cancer stemcell-enriched tumors and is associated with poor prognosis inmultiple types of cancerTOPKPBK is an oncogenic kinase upregulated in most humancancers TOPK is important for mitotic cell division and thatphosphorylation by Cdk1 is needed for its activationTOPK a member of the MEK36-related MAPKK family is expressed in

a wide range of proliferating cells and tissues including cancer cells and testis TOPK negatively regulates the activityof p38α by phosphorylating the p38α-specific phosphatase MKP1 and enhancing the stability of MKP1 The MAPKphosphatase MKP1 an archetypal member of the MKP family plays a pivotal role in the deactivation of p38 through adephosphorylation reaction

Purity 9563Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

TOPK Inhibitors amp Modulators

Bioactivity HI-TOPK-032 is a potent and specific inhibitorTOPK Bioactivity OTS-964 is a potent T-lymphokine-activated killer inhibitor ( =28cell-originated protein kinase (TOPK) IC50

nM) which inhibits TOPK kinase activity with high affinityand selectivity

Bioactivity OTS514 is a highly potent inhibitor which inhibits TOPKTOPKkinase activity with a median inhibitory concentration ( )IC50value of 26 nM

154 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

HI-TOPK-032 Cat No HY-101550

OTS-964 Cat No HY-12467

OTS514 Cat No HY-18621

wwwMedChemExpresscom 155

Topoisomerase

Topoisomerases are enzymes that regulate the overwinding orunderwinding of DNA The winding problem of DNA arises due to theintertwined nature of its double-helical structure Topoisomerases areisomerase enzymes that act on the topology of DNA Type Itopoisomerase cuts one strand of a DNA double helix relaxationoccurs and then the cut strand is reannealed Type I topoisomerasesare subdivided into two subclasses type IA topoisomerases whichshare many structural and mechanistic features with the type IItopoisomerases and type IB topoisomerases which utilize acontrolled rotary mechanism Type II topoisomerase cuts both strandsof one DNA double helix pass another unbroken DNA helix through

it and then reanneal the cut strands This class is also split into two subclasses type IIA and type IIB topoisomeraseswhich possess similar structure and mechanisms

Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg 500 mg

Purity gt98Clinical Data LaunchedSize 1 mg 5 mg

Purity 980Clinical Data LaunchedSize 1 mg 5 mg

Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9243Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity 9808Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg

Purity 9889Clinical Data Phase 2Size 10mM x 1mL in DMSO

2 mg 5 mg 10 mg 25 mg

Topoisomerase Inhibitors amp Modulators

Bioactivity 9-Aminocamptothecin is a inhibitor withtopoisomerase Ipotent anticancer activity

Bioactivity Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) afluorescent molecule and the first described non-peptidicinhibitor showing discrete specificity for the CTRL(chymotrypsin-like) activity of the 20S proteasome [1]

Aclacinomycin A hydrochloride is also a dual inhibitor ofhellip

Bioactivity Aldoxorubicin (INNO-206) is an albumin-binding prodrug ofdoxorubicin which is released from albumin under acidicconditions Aldoxorubicin (INNO-206) has potent antitumoractivities in various cancer cell lines and in murine tumormodels

Bioactivity Amonafide is a inhibitor and DNAtopoisomerase IIintercalator that induces apoptotic signaling by blocking thebinding of Topo II to DNA

Bioactivity Amrubicin (SM-5887) is a DNA inhibitortopoisomerase IIused for the research of cancer

Bioactivity Amrubicin (hydrochloride) (SM-5887 (hydrochloride)) is a DNA inhibitor used for the research of cancertopoisomerase II

Bioactivity Amsacrine (m-AMSA) is an inhibitor of andtopoisomerase IIacts as an antineoplastic agent which can intercalates intothe DNA of tumor cells

Bioactivity Amsacrine hydrochloride (mAMSA hydrochloride) is an inhibitorof and acts as an antineoplastic agenttopoisomerase IIwhich can intercalates into the DNA of tumor cells

Bioactivity Banoxantrone D12 (AQ4N D12) is the deuterium labeledbanoxantrone Banoxantrone is a novel bioreductive agent thatcan be reduced to a stable DNA-affinic compound AQ4 which isa potent inhibitortopoisomerase II

Bioactivity Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) isthe deuterium labeled banoxantrone dihydrochlorideBanoxantrone is a novel bioreductive agent that can be reducedto a stable DNA-affinic compound AQ4 which is a potent

inhibitortopoisomerase II

156 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

9-amino-CPT (9-amino-20(S)-camptothecin) Cat No HY-100309

Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) Cat No HY-N2306A

Aldoxorubicin (INNO-206 DOXO-EMCH) Cat No HY-16261

Amonafide (AS1413) Cat No HY-10982

Amrubicin (SM-5887 AMR) Cat No HY-B0067

Amrubicin hydrochloride (SM-5887 (hydrochloride) AMR (hydrochloride)) Cat No HY-B0067A

Amsacrine (m-AMSA acridinyl anisidide) Cat No HY-13551

Amsacrine hydrochloride (m-AMSA hydrochloride acridinyl anisidide hydrochloride) Cat No HY-13551A

Banoxantrone D12 (AQ4N D12) Cat No HY-13562S

Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) Cat No HY-13562AS

wwwMedChemExpresscom 157

Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water

10 mg 50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

2 mg 5 mg 10 mg

Purity 9826Clinical Data Phase 4Size 10mM x 1mL in DMSO

100 mg 500 mg

Purity 9635Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg

Purity 9818Clinical Data Phase 2Size 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 g

Purity gt98Clinical Data LaunchedSize 100 mg 500 mg

Purity 9880Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 25 mg

Bioactivity Banoxantrone dihydrochloride is a novel bioreductive agentthat can be reduced to a stable DNA-affinic compound AQ4which is a potent inhibitortopoisomerase II

Bioactivity Belotecan hydrochloride (CKD-602 hydrochloride) a inhibitor is a synthetic and water-solubleTopoisomerase I

camptothecin derivative

Bioactivity Berberine chloride is an alkaloid isolated from the Chineseherbal medicine Huanglian as an Berberine chlorideantibioticinduces reactive oxygen species ( ) generation andROSinhibits Antineoplastic propertiesDNA topoisomerase

[1]

Bioactivity Berberine chloride hydrate is an alkaloid isolated from theChinese herbal medicine Huanglian as an Berberineantibioticchloride hydrate induces reactive oxygen species ( )ROSgeneration and inhibits AntineoplasticDNA topoisomeraseproperties [1]

Bioactivity Betulinic acid is a natural pentacyclic triterpenoid acts asa eukaryotic inhibitor with an of 5topoisomerase I IC50μM and possesses anti-HIV anti-malarial anti-inflammatoryand anti-tumor properties

Bioactivity Bisantrene is a highly effective antitumor drug targetseukaryotic type II topoisomerases

Bioactivity Campathecin is a potent DNA enzyme topoisomerase Iinhibitor with an of 679 nMIC50

Bioactivity Daun02 is a prodrug of the inhibitortopoisomeraseDaunorubicin

Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II

activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells

Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells

Banoxantrone dihydrochloride (AQ4N dihydrochloride) Cat No HY-13562A

Belotecan hydrochloride (CKD-602) Cat No HY-13566A

Berberine chloride (Natural Yellow 18 (chloride)) Cat No HY-18258

Berberine chloride hydrate (Natural Yellow 18 (chloride hydrate)) Cat No HY-17577

Betulinic acid (Lupatic acid Betulic acid) Cat No HY-10529

Bisantrene (CL216942) Cat No HY-100875

Campathecin (Camptothecin (S)-(+)-Camptothecin CPT) Cat No HY-16560

Daun02 Cat No HY-13061

Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A

Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)

Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062

Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9965Clinical Data LaunchedSize 10mM x 1mL in DMSO

100 mg 200 mg 500 mg

Purity 9888Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 5 mg 10 mg

Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9839Clinical Data Phase 3Size 1 mg 5 mg 10 mg

Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg

Purity 9947Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg 1 g

Purity gt98Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg

Bioactivity Doxorubicin is a cytotoxic anthracycline antibiotic for thetreatment of multiple cancers The possible mechanisms bywhich doxorubicin acts in the cancer cell are intercalationinto DNA and disruption of -mediated DNAtopoisomerase-IIrepair

Bioactivity Doxorubicin hydrochloride is a cytotoxic anthracyclineantibiotic for the treatment of multiple cancers The possiblemechanisms by which doxorubicin acts in the cancer cell areintercalation into DNA and disruption of

-mediated DNA repairtopoisomerase-II

Bioactivity Dxd is a potent inhibitor with an ofDNA topoisomerase I IC50031 μM used as a conjugated drug of HER2-targeting ADC(DS-8201a)

Bioactivity Edotecarin is a potent inhibitor of that cantopoisomerase Iinduces single-strand DNA cleavage with of 50 nMIC50

Bioactivity Ellipticine (NSC 71795) is a potent antineoplastic agentinhibits activitiesDNA topoisomerase II

Bioactivity Ellipticine (NSC 71795) hydrochloride is a potentantineoplastic agent inhibits DNA topoisomerase IIactivities

Bioactivity Epirubicin is a semisynthetic L-arabino derivative ofdoxorubicin and an antineoplastic agent by inhibiting

Topoisomerase

Bioactivity Epirubicin (hydrochloride) is a semisynthetic L-arabinoderivative of doxorubicin and an antineoplastic agent byinhibiting Topoisomerase

Bioactivity Etoposide (VP-16 VP-16-213) a chemotherapy medication usedfor the treatments of a number of types of cancer inhibits

by forming a complex with topoisomerase II andDNA synthesisDNA Etoposide arrests cell cycle in G2 and induces apoptoshellip

Bioactivity Exatecan is a water soluble inhibitor withtopoisomerase Ian of 22 μM (0975 μgmL) and can be used in cancerIC50research

158 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Doxorubicin (Hydroxydaunorubicin) Cat No HY-15142A

Doxorubicin hydrochloride (Hydroxydaunorubicin (hydrochloride)) Cat No HY-15142

Dxd (Exatecan derivative for ADC) Cat No HY-13631D

Edotecarin (J 107088 PF 804950) Cat No HY-13618

Ellipticine (NSC 71795) Cat No HY-15753

Ellipticine hydrochloride (NSC 71795 (hydrochloride)) Cat No HY-15753A

Epirubicin Cat No HY-13624

Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride) Cat No HY-13624A

Etoposide (VP-16 VP-16-213) Cat No HY-13629

Exatecan (DX-8951) Cat No HY-13631

wwwMedChemExpresscom 159

Purity 9830Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9978Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg

Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg

Purity 9803Clinical Data Phase 1Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg

Purity 9912Clinical Data Phase 3Size 10mM x 1mL in DMSO

50 mg 100 mg 250 mg 500 mg

Bioactivity Exatecan Mesylate is a water soluble topoisomerase Iinhibitor with an of 22 μM (0975 μgmL) and can beIC50used in cancer research

Bioactivity Flumequine (R-802) is a quinolone antibiotic and acts as a inhibitor with an of 15 μM (392topoisomerase II IC50

μgmL)

Bioactivity Genz-644282 is a non-camptothecin inhibitortopoisomerase Iused for cancer research

Bioactivity Idarubicin hydrochloride is an anthracycline antileukemicdrug It inhibits the interfering with thetopoisomerase IIreplication of DNA and RNA transcription

Bioactivity Indotecan (LMP-400) is a potent topoisomerase 1(Top1)inhibitor with values of 300 1200 560 nM for P388IC50HCT116 MCF-7 cell lines respectively

Bioactivity Intoplicine is a and inhibitorDNA topoisomerase I II

Bioactivity Irinotecan is a water soluble inhibitortopoisomerase Ipreventing religation of the DNA strand by binding totopoisomerase I-DNA complex

Bioactivity Irinotecan hydrochloride is a water soluble topoisomerase Iinhibitor mainly used to treat colon cancer and rectal cancer

Bioactivity Irinotecan hydrochloride trihydrate is a water soluble inhibitor with antitumor activitytopoisomerase I

Bioactivity Karenitecin (Cositecan) is a inhibitor withtopoisomerase Ipotent anti-cancer activity

Exatecan Mesylate (DX8951f) Cat No HY-13631A

Flumequine (R-802) Cat No HY-B0526

Genz-644282 Cat No HY-16228

Idarubicin hydrochloride (4-Demethoxydaunorubicin hydrochloride) Cat No HY-17381

Indotecan (LMP-400 NSC-724998) Cat No HY-18351

Intoplicine Cat No HY-101647

Irinotecan ((+)-Irinotecan CPT-11) Cat No HY-16562

Irinotecan hydrochloride (CPT-11 hydrochloride Camptothecin 11 hydrochloride) Cat No HY-16562A

Irinotecan hydrochloride trihydrate Cat No HY-16568

Karenitecin (Cositecan BNP 1350) Cat No HY-14812

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity 9690Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9902Clinical Data LaunchedSize 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg

Purity 9702Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO

50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

1 mg 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg

Bioactivity LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I inhibitor with antitumor activity (Top1) [1]

Bioactivity LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNAintercalator and inhibitor withTopoisomerase I (Top1)antitumor activity [1]

Bioactivity MC-DOXHZN is an albumin-binding prodrug of Doxorubicin withacid-sensitive properties [1]

Bioactivity MC-DOXHZN hydrochloride is an albumin-binding prodrug ofDoxorubicin with acid-sensitive properties [1]

Bioactivity Mitoxantrone is a inhibitor also inhibitstopoisomerase IIprotein kinase C ( ) activity with an of 85 μMPKC IC50

Bioactivity Mitoxantrone dihydrochloride is a topoisomerase IIinhibitor also inhibits protein kinase C ( ) activityPKCwith an of 85 μMIC50

Bioactivity Namitecan is a potent inhibitor withtopoisomerase Iantitumor property

Bioactivity Pirarubicin is an anthracycline antibiotics acts as a inhibitor and is a widely used fortopoisomerase II

treatment of various cancers in particular solid tumors

Bioactivity Pirarubicin Hydrochloride is an anthracycline antibioticsacts as a inhibitor and is a widely usedtopoisomerase IIfor treatment of various cancers in particular solid tumors

Bioactivity Pixantrone is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

160 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

LMP744 (MJ-III65 NSC706744) Cat No HY-U00248

LMP744 hydrochloride (MJ-III65 hydrochloride NSC706744 hydrochloride) Cat No HY-U00248A

MC-DOXHZN (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat No HY-16261A

MC-DOXHZN hydrochloride (Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat No HY-16261B

Mitoxantrone (mitozantrone) Cat No HY-13502

Mitoxantrone dihydrochloride (mitozantrone dihydrochloride) Cat No HY-13502A

Namitecan (ST-1968) Cat No HY-14821

Pirarubicin (THP) Cat No HY-13725

Pirarubicin Hydrochloride (THP Hydrochloride) Cat No HY-13725A

Pixantrone (BBR 2778) Cat No HY-13727

wwwMedChemExpresscom 161

Purity 9920Clinical Data LaunchedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity gt98Clinical Data LaunchedSize 10 mg 50 mg

Purity gt98Clinical Data No Development ReportedSize 250 mg 100 mg 500 mg

Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO

25 mg 50 mg 100 mg 200 mg

Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg

Purity 9960Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO

50 mg 100 mg 200 mg 500 mg

Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg

Purity 950Clinical Data LaunchedSize 10mM x 1mL in Water

5 mg 10 mg 50 mg 100 mg

Bioactivity Pixantrone dimaleate is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity

Bioactivity Podocarpusflavone A is a DNA topoisomerase I inhibitor havemoderated anti-proliferative activity induce cell apoptosis inMCF-7 is developing anti-tumor drugs target DNAtopoisomerase I In vitro podocarpusflavone-A show significantinhibitions against DLD KB MCF-7 HEp-2 tumor cell lineshellip

Bioactivity SN-38 (NK012) is an active metabolite of the Topoisomerase Iinhibitor Irinotecan SN-38 (NK012) inhibits and DNA RNA

with s of 0077 and 13 μM respectivelysynthesis IC50

Bioactivity SW044248 is a non-canonical inhibitor andtopoisomerase Iselectively toxic for certain non-small cell lung cancer(NSCLC) cell lines

Bioactivity TAS-103 is a dual inhibitor of DNA usedtopoisomerase IIIfor cancer research

Bioactivity TAS-103 dihydrochloride is a dual inhibitor of DNA used for cancer researchtopoisomerase III

Bioactivity Teniposide is a podophyllotoxin derivative acts as a inhibitor and used as a chemotherapeutictopoisomerase II

agent

Bioactivity Top1 inhibitor 1 (compound 28) is a potent human inhibitor with an value of 29topoisomerase I (Top1) IC50

nM [1]

Bioactivity Topotecan (SKF 104864A NSC 609669) is a Topoisomerase Iinhibitor The values of Topotecan at 24 h are 273plusmn025IC50μM of U251 cells 295plusmn023 μM of U87 cells 546plusmn041 μM ofGSCs-U251 and 595plusmn024 μM of GSCs-U87

Bioactivity Topotecan Hydrochloride (SKF 104864A Hydrochloride NSC 609669Hydrochloride) is a inhibitor with potentTopoisomerase Iantineoplastic activities

Pixantrone dimaleate (BBR 2778 dimaleate) Cat No HY-13727A

Podocarpusflavone A Cat No HY-N2198

SN-38 (NK012) Cat No HY-13704

SW044248 Cat No HY-19637

TAS-103 (BMS-247615) Cat No HY-13758

TAS-103 dihydrochloride (BMS-247615 dihydrochloride) Cat No HY-13758A

Teniposide (VM26) Cat No HY-13761

Top1 inhibitor 1 Cat No HY-126142

Topotecan (SKF 104864A NSC 609669) Cat No HY-13768

Topotecan Hydrochloride (SKF 104864A (Hydrochloride) NSC 609669 (Hydrochloride)) Cat No HY-13768A

Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

10 mg 50 mg 100 mg

Purity 9970Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg

Bioactivity Voreloxin is a first-in-class inhibitortopoisomerase IIthat intercalates DNA and induces site-selective DNA DSB G2arrest and apoptosis

Bioactivity Voreloxin Hydrochloride is a first-in-class topoisomerase IIinhibitor that intercalates DNA and induces site-selective DNADSB G2 arrest and apoptosis

Bioactivity β-Lapachone is a naturally occurring O-naphthoquinone acts asa inhibitor and induces apoptosis bytopoisomerase Iinhibiting cell cycle progression

162 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Voreloxin (SNS-595 Vosaroxin AG 7352) Cat No HY-10534

Voreloxin Hydrochloride (SNS-595 Hydrochloride Vosaroxin

Hydrochloride AG 7352 Hydrochloride) Cat No HY-16518

β-Lapachone (ARQ-501 NSC-26326) Cat No HY-13555

wwwMedChemExpresscom 163

Wee1

Wee1 is a nuclear kinase belonging to the SerThr family of proteinkinases in the fission yeast ( )Schizosaccharomyces pombe S pombeWee1 has amolecular mass of 96 kDa and it is a key regulator of cellcycle progression Wee1 influences cell size by inhibiting the entryinto mitosis through inhibiting Cdk1 Wee1 has homologues in manyother organisms including mammals Wee1 inhibits Cdk1 byphosphorylating it on two different sites Tyr15 and Thr14 Cdk1 iscrucial for the cyclin-dependent passage of the various cell cyclecheckpoints At least three checkpoints exist for which the inhibitionof Cdk1 by Wee1 is important G M checkpoint Cell size checkpoint2DNA damage checkpoint Wee1 is shown to phosphorylate histone

H2B at tyrosine 37 residue which regulates global expression of histones

Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO

5 mg 10 mg 25 mg 50 mg 100 mg

Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO

5 mg 10 mg 50 mg 100 mg

Wee1 Inhibitors amp Modulators

Bioactivity Adavosertib (AZD-1775 MK-1775) is a potent inhibitorWee1with an of 52 nMIC50

Bioactivity PD0166285 is a inhibitor and a weak inhibitorWEE1 Myt1with s of 24 and 72 nM respectivelyIC50

164 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom

Adavosertib (AZD1775 MK-1775) Cat No HY-10993

PD0166285 Cat No HY-13925

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