Cell Cycle/DNA Damage - MedchemExpress.com · Antifolates are compounds that antagonise the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor

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Inhibitors, Agonists, Screening Librarieswww.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 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 checkpoint,specialized 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. TheG2/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 checkpointsare 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 DNAreplication, 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 adouble-strand DNA break (DSB). To prevent cells with damaged DNA from entering mitosis, ATR inhibits cyclin B/Cdk1activation by stimulating the Cdk1 inhibitory kinase Wee1 and inhibiting Cdc25C via Chk1, besides, ATM and ATR alsoinitiate 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 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 14;16(1):60.

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2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]


• Mps1 82

• Nucleoside Antimetabolite/Analog 84

• p97 89

• PAK 91

• PARP 93

• PERK 97

• Polo-like Kinase (PLK) 99

• PPAR 102

• RAD51 108

• ROCK 110

• Sirtuin 114

• SRPK 117

• Telomerase 119

• Topoisomerase 121

• Wee1 127

• Antifolate 3

• APC 7

• ATM/ATR 9

• Aurora Kinase 12

• Casein Kinase 16

• CDK 19

• Checkpoint Kinase (Chk) 27

• CRISPR/Cas9 30

• Deubiquitinase 32

• DNA Alkylator/Crosslinker 35

• DNA Stain 39

• DNA-PK 43

• DNA/RNA Synthesis 45

• Eukaryotic Initiation Factor (eIF) 50

• G-quadruplex 52

• Haspin Kinase 54

• HDAC 56

• HSP 63

• IRE1 67

• Kinesin 69

• LIM Kinase (LIMK) 72

• Microtubule/Tubulin 74

Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Target List in Cell Cycle/DNA Damage

http://www.MedChemExpress.com

Antifolate

Antifolates are compounds that antagonise the actions of folic acid(vitamin B9). Folic acid's primary function in the body is as a cofactorto various methyltransferases involved in serine, methionine,thymidine and purine biosynthesis. Consequently antifolates inhibitcell division, DNA/RNA synthesis and repair and protein synthesis.Some such as Proguanil, Pyrimethamine and Trimethoprim selectivelyinhibit folate's actions in microbial organisms such as bacteria,protozoa and fungi. The majority of antifolates work by inhibitingdihydrofolate reductase (DHFR). Many are primarily DHFR inhibitors,but 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.


http://www.medchemexpress.com/Targets/Antifolate.html


Purity: 99.69%Clinical Data: Phase 4Size: 10mM x 1mL in DMSO,

100 mg, 500 mg

Purity: >98.0%Clinical Data:Size: 5 mg, 10 mg, 50 mg

Purity: 98.06%Clinical Data:Size: 10mM x 1mL in Water,

10 mg, 50 mg

Purity: 98.23%Clinical Data:Size: 10mM x 1mL in DMSO,

100 mg, 500 mg, 1 g, 2 g


100 mg, 200 mg, 500 mg

Purity: 99.97%Clinical Data: Phase 3, Phase 4Size: 10mM x 1mL in Water,

100 mg, 500 mg

Purity: >98%Clinical Data:Size: 100 mg


Purity: >98%Clinical Data:Size: 1 mg, 5 mg, 10 mg

Purity: >98%Clinical Data:Size: 5 mg, 10 mg, 50 mg, 100 mg

Antifolate Inhibitors & Modulators

Bioactivity: Calcium N5-methyltetrahydrofolate(NSC173328) is the calcium salt oflevomefolic acid, which has been proposed for treatment ofcardiovascular disease and advanced cancers such as breast andcolorectal cancers.

Bioactivity: Cycloguanil D6 is the deuterium labeled Cycloguanil, which is adihydrofolate reductase inhibitor.

Bioactivity: Cycloguanil D6 Nitrate is the deuterium labeled Cycloguanil, which isa dihydrofolate reductase inhibitor.

Bioactivity: Folinic acid is an adjuvant used in cancer chemotherapy involving thedrug methotrexate.

Bioactivity: Leucovorin Calcium is a reduced folic acid. Bioactivity: Folinic Acid is a reduced folic acid, which is used in combination withother chemotherapy drugs.

Bioactivity: Levoleucovorin calcium is the calcium salt of Levoleucovorin, which isthe enantiomerically active form of folinic acid.

Bioactivity: Levomefolate is an artificial form of folate.

Bioactivity: Levomefolic acid (5-MTHF) is the natural, active form of folic acidused at the cellular level for DNA reproduction, the cysteine cycleand the regulation of homocysteine among other functions.

Bioactivity: Methotrexate is a traditional antagonist, with median offolate IC5078 nM for a 120 h drug exposure in a panel of six pediatric leukemiaand lymphoma cell lines using the sulforhodamine B assay.

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

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 calciumCat. No.: HY-17383

Levomefolic acid(5-MTHF) Cat. No.: HY-14781

Methotrexate(Amethopterin; CL14377; WR19039) Cat. No.: HY-14519

http://www.medchemexpress.com/Targets/Antifolate.html

http://www.medchemexpress.com/calcium-n5-methyltetrahydrofolate.html

http://www.medchemexpress.com/Cycloguanil-D6.html

http://www.medchemexpress.com/Cycloguanil-D6-Nitrate.html

http://www.medchemexpress.com/folinic-acid.html

http://www.medchemexpress.com/Folinic-acid-Calcium.html

http://www.medchemexpress.com/Folinic-acid-calcium-salt-pentahydrate.html

http://www.medchemexpress.com/Levoleucovorin-Calcium.html

http://www.medchemexpress.com/Levomefolate-calcium.html

http://www.medchemexpress.com/Levomefolic-acid.html

http://www.medchemexpress.com/Methotrexate.html


5 g, 10 g


100 mg, 500 mg

Purity: >95.0%Clinical Data: Phase 2, Phase 3Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg

Purity: 99.78%Clinical Data: Phase 3Size: 10mM x 1mL in Water,

100 mg, 500 mg


50 mg, 100 mg

Purity: >98%Clinical Data: Phase 4Size: 50 mg, 100 mg

Bioactivity: Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR andGARFT with Ki of 1

Bioactivity: Pemetrexed disodium is a novel , the values of theantifolate Kipentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibitsthymidylate synthase ( ), dihydrofolate reductase ( ), andTS DHFRglycinamide ribonucleotide formyltransferase ( ), respectively.GARFT

Bioactivity: Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR andGARFT with Ki of 1

Bioactivity: Pralatrexate(Folotyn) is an antifolate, and structurally a folate analog.Its IC50 is < 300 nM in some cell lines.

Bioactivity: Pyrimethamine(RP4753) is a medication used for protozoalinfections; interferes with tetrahydrofolic acid synthesis from folicacid by inhibiting the enzyme dihydrofolate reductase (DHFR).

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


Pemetrexed(LY231514; LY 231514; LY-231514) Cat. No.: HY-10820

Pemetrexed disodium (LY231514 disodium; LY 231514 disodium;

LY-231514 disodium) Cat. No.: HY-10820A

Pemetrexed disodium hemipenta hydrate(Pemetrexed sodium hydrate) Cat. No.: HY-13781

PralatrexateCat. No.: HY-10446

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

TrimethoprimCat. No.: HY-B0510

http://www.medchemexpress.com/pemetrexed.html

http://www.medchemexpress.com/Pemetrexed-disodium.html

http://www.medchemexpress.com/Pemetrexed-disodium-hemipenta-hydrate_-1:2:2.5.html

http://www.medchemexpress.com/Pralatrexate.html

http://www.medchemexpress.com/pyrimethamine.html

http://www.medchemexpress.com/Trimethoprim.html


APC

APC (Anaphase-Promoting Complex) is an E3 ubiquitin ligase thatmarks target cell cycle proteins for degradation by the 26Sproteasome. The APC/C is a large complex of 11–13 subunit proteins,including a cullin (Apc2) and RING (Apc11) subunit much like SCF. TheAPC/C's 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 APC/C 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 APC/C and releases separase, whichdegrades cohesin, sister chromatids become free to move to opposite poles for anaphase. The APC/C also targets themitotic cyclins for degradation, resulting in the inactivation of M-CdK (mitotic cyclin-dependent kinase) complexes,promoting exit from mitosis and cytokinesis.

http://www.medchemexpress.com/Targets/APC.html

Purity: >98%Clinical Data:Size: 10mM x 1mL in DMSO,

50 mg, 100 mg

APC Inhibitors & Modulators

Bioactivity: TAME is a small molecule anaphase-promoting complex/cyclosome(APC) inhibitor.


TAMECat. No.: HY-13255

http://www.medchemexpress.com/Targets/APC.html

http://www.medchemexpress.com/tame.html


ATM/ATR

ATM/ATR 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.

http://www.medchemexpress.com/Targets/ATM_ATR.html


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg

Purity: 98.04%Clinical Data:Size: 5 mg, 10 mg, 50 mg


10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg

Purity: 98%Clinical Data:Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg

ATM/ATR Inhibitors & Modulators

Bioactivity: AZ20 is a potent and selective inhibitor of with an of 5 nM,ATR IC50and has 8-fold selectivity against (IC =38 nM).mTOR 50

Bioactivity: AZD0156 is an orally active, potent and selective ATM kinaseinhibitor, used for cancer treatment.

Bioactivity: AZD6738 is a potent inhibitor of ATR kinase activity with an IC50 of 1nM against the isolated enzyme and 74 nM against ATRkinase-dependent CHK1 phosphorylation in cells.

Bioactivity: CGK 733 is a small molecule inhibitor reportedly targeting the kinaseactivities of ATM and ATR

Bioactivity: CP-466722 is rapidly reversible potential ATM kinase inhibitor Bioactivity: ETP-46464 is a cell-permeable quinoline-containing heterotricycliccompound that acts as a potent inhibitor against mTOR, ATR,DNA-PK, PI 3-Kα, and ATM (IC50= 0.6, 14, 36, 170, and 545 nM,respectively).

Bioactivity: HLM006474 is a potent inhibitor of melanocytes proliferation andsubsequent invasion in a three-dimensional tissue culture modelsystem; interferes with E2F activity.

Bioactivity: KU-55933 is a potent inhibitor with an and of 12.9 andATM IC50 Ki2.2 nM, respectively, and highly selective for ATM as compared toDNA-PK, PI3K/PI4K, ATR and mTOR.

Bioactivity: KU-60019 is an improved kinase-specific inhibitor with ofATM IC506.3 nM.

Bioactivity: VE-821 is a potent ATP-competitive inhibitor of with / ofATR Ki IC5013 nM/26 nM.


AZ20(AZ-20; AZ 20) Cat. No.: HY-15557

AZD0156(AZD-0156; AZD 0156) Cat. No.: HY-100016

AZD6738(AZD-6738) Cat. No.: HY-19323

CGK733(CGK-733; CGK 733) Cat. No.: HY-15520

CP-466722(CP466722; CP 466722) Cat. No.: HY-11002

ETP-46464(ETP 46464; ETP46464) Cat. No.: HY-15521

HLM006474(HLM 006474; HLM-006474) Cat. No.: HY-16667

KU-55933(KU 55933; KU55933) Cat. No.: HY-12016

KU-60019(KU60019; KU 60019) Cat. No.: HY-12061

VE-821(VE821; VE 821) Cat. No.: HY-14731

http://www.medchemexpress.com/Targets/ATM_ATR.html

http://www.medchemexpress.com/AZ20.html

http://www.medchemexpress.com/AZD0156.html


http://www.medchemexpress.com/cgk733.html

http://www.medchemexpress.com/CP-466722.html

http://www.medchemexpress.com/etp-46464.html

http://www.medchemexpress.com/hlm006474.html

http://www.medchemexpress.com/KU-55933.html


http://www.medchemexpress.com/VE-821.html



5 mg, 10 mg, 25 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: VE-822 is an inhibitor with value of <0.2 nM, also inhibits ATR Ki with of 34 nM.ATM Ki

Bioactivity: Wortmannin is a multi-target inhibitor of and with sPI3K MLCK IC50of 3 nM and 170 nM, respectively.

VE-822(VE822; VE 822; VX970; VX-970; VX 970) Cat. No.: HY-13902

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

http://www.medchemexpress.com/VE-822.html

http://www.medchemexpress.com/Wortmannin.html

Aurora Kinase

Aurora kinases are serine/threonine 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 segregation.Defects 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 B,Aurora 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.


http://www.medchemexpress.com/Targets/Aurora Kinase.html


Purity: >98%Clinical Data: Phase 1Size: 10mM x 1mL in DMSO,

10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Purity: 99.59%Clinical Data: Phase 1, Phase 2, Phase 3Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg

Purity: 95.56%Clinical Data: Phase 1, Phase 2Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Aurora Kinase Inhibitors & Modulators

Bioactivity: Alisertib is a selective inhibitor with of 1.2 nM, and isAurora A IC50more selective for Aurora A than Aurora B.

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

respectively.

Bioactivity: AT9283 is a multi-targeted inhibitor with s of 1.2 nM, 1.1 nM for IC50 and , respectively, and is also potent to Aurora A, AuroraJAK2 JAK3

B and Abl(T315I).

Bioactivity: Aurora A inhibitor I is a selective Aurora A inhibitor (Aurora A: IC50=0

Bioactivity: AZD1152 is a pro-drug of barasertib-hQPA, which is a highlyselective inhibitor with of 0.37 nM in a cell-free assay.Aurora B IC50

Bioactivity: AZD1152-HQPA is a highly selective inhibitor with ofAurora B IC500.37 nM in a cell-free assay, and appr 3700 fold more selective forAurora B over Aurora A.

Bioactivity: BI-847325 is an ATP competitive dual inhibitor of and auroraMEKkinases ( ) with values of 4 and 15 nM for human MEK2 andAK IC50AK-C, respectively.

Bioactivity: CCT 137690 is a potent inhibitor of Aurora kinases (IC50 values are0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora Brespectively).

Bioactivity: CCT129202 is a Aurora kinase inhibitor with IC50 of 0.042 ± 0.022,0.198 ± 0.05, and 0.227 ± 0.064 uM for Aurora A, Aurora B, andAurora C, respectively.

Bioactivity: CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM.

Alisertib(MLN 8237; MLN8237; MLN-8237) Cat. No.: HY-10971

AMG 900(AMG-900; AMG900) Cat. No.: HY-13253

AT9283(AT-9283; AT 9283) Cat. No.: HY-50514

Aurora A inhibitor I (Benzamide, N-(2-chlorophenyl)-4-[[2-[[

4-[2-(4-ethyl-1-piperazinyl)-2-oxoethyl]phenyl]a…) Cat. No.: HY-70061

AZD1152(Barasertib; AZD-1152; AZD 1152) Cat. No.: HY-10127

AZD1152-HQPA(Barasertib; AZD1152; AZD 1152) Cat. No.: HY-10126

BI-847325(BI847325; BI 847325) Cat. No.: HY-18955

CCT 137690(CCT-137690; CCT137690) Cat. No.: HY-10804

CCT129202(CCT-129202; CCT 129202) Cat. No.: HY-12049

CYC-116(CYC 116; CYC116) Cat. No.: HY-10558

http://www.medchemexpress.com/Targets/Aurora Kinase.html

http://www.medchemexpress.com/Alisertib.html

http://www.medchemexpress.com/amg-900.html

http://www.medchemexpress.com/at9283.html

http://www.medchemexpress.com/aurora-a-inhibitor-i.html


http://www.medchemexpress.com/AZD1152-HQPA.html

http://www.medchemexpress.com/BI-847325.html

http://www.medchemexpress.com/CCT-137690.html

http://www.medchemexpress.com/CCT129202.html

http://www.medchemexpress.com/CYC-116.html


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg

Purity: >98.0%Clinical Data: Phase 1Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: Danusertib is a pyrrolo-pyrazole and aurora with kinase inhibitor IC of 13, 79, and 61 nM for Aurora A, B, and C, respectively.50

Bioactivity: ENMD-2076 has selective activity against Aurora A and Flt3 with IC50of 14 nM and 1.86 nM, 25-fold selective for Aurora A than overAurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 andFGFR2 and PDGFRα.

Bioactivity: ENMD-2076 tartrate has selective activity against Aurora A and Flt3with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A thanover Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1and FGFR2 and PDGFRα.

Bioactivity: GSK1070916 is a reversible and ATP-competitive inhibitor of AuroraB/C with IC50 of 3

Bioactivity: Hesperadin is a ATP-competitive inhibitor of Aurora B kinase withIC50 of 250 nM

Bioactivity: JNJ-7706621 is pan-CDK inhibitor with the highest potency onCDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity forCDK1/2 than CDK3/4/6; also potently inhibits Aurora A/B and has noactivity on Plk1 and Wee1.

Bioactivity: MK-5108 is a highly potent and specific inhibitor of kinaseAurora-Awith an value of 0.064 nM.IC50

Bioactivity: MK-8745 is a potent and selective Aurora A inhibitor with IC50 of 0.6nM, more than 450-fold selectivity for Aurora A over Aurora B.

Bioactivity: MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of4 nM; exhibits more than 40-fold selective for Aurora A than AuroraB

Bioactivity: PF-03814735 is a novel, potent, orally bioavailable, reversiblesmall-molecule Aurora kinase inhibitor with IC50 of 0.8, 5, 10 and 22nM for Aurora A, Aurora B, Flt 1 and FAk, respectively.


Danusertib(PHA-739358; PHA739358; PHA 739358) Cat. No.: HY-10179

ENMD-2076(ENMD 2076; ENMD2076) Cat. No.: HY-10987A

ENMD-2076 Tartrate(ENMD 2076; ENMD2076) Cat. No.: HY-10987

GSK-1070916(GSK1070916; GSK 1070916) Cat. No.: HY-70044

HesperadinCat. No.: HY-12054

JNJ-7706621(JNJ7706621; JNJ 7706621) Cat. No.: HY-10329

MK-5108(MK 5108; VX-689; VX 689; MK5108; VX689) Cat. No.: HY-13252

MK-8745(MK8745; MK 8745) Cat. No.: HY-13819

MLN8054(MLN-8054; MLN 8054) Cat. No.: HY-10180

PF-03814735(PF 03814735; PF03814735) Cat. No.: HY-14574

http://www.medchemexpress.com/Danusertib.html

http://www.medchemexpress.com/enmd-2076.html

http://www.medchemexpress.com/enmd-2076-tartrate.html

http://www.medchemexpress.com/GSK-1070916.html

http://www.medchemexpress.com/Hesperadin.html

http://www.medchemexpress.com/JNJ-7706621.html

http://www.medchemexpress.com/MK-5108.html


http://www.medchemexpress.com/MLN8054.html

http://www.medchemexpress.com/PF-03814735.html



10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


50 mg, 100 mg, 250 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


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


2 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora Cwith IC50 of 27 nM, 135 nM and 120 nM, respectively.

Bioactivity: Reversine is a novel class of ATP-competitive inhibitorAurora kinasewith s of 400, 500 and 400 nM for , and ,IC50 Aurora A B C

respectively.

Bioactivity: SCH 1473759 is a novel sub-nanomolar Aurora A/B inhibitor withIC50 of 4 nM and 13 nM, respectively.

Bioactivity: SCH 1473759 Hcl is a novel sub-nanomolar Aurora A/B inhibitor withIC50 of 4 nM and 13 nM, respectively.

Bioactivity: SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B andAurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively.

Bioactivity: TAK-632 is a potent inhibitor with of 1.4, 2.4 and 8.3pan-RAF IC50

nM for , , , respectively.CRAF BRAFV600E BRAFWT

Bioactivity: TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. Bioactivity: Tozasertib is the inhibitor of with valuesAurora-A, -B, -C kinases Kiof 0.6, 18, 4.6 nM, respectively.

Bioactivity: XL228 is a protein kinase inhibitor targeting IGF1R, the Aurorakinases, FGFR1-3, ABL and SRC family kinases.

Bioactivity: ZM 447439 is a selective and ATP-competitive inhibitor for Aurora Aand Aurora B with IC50 of 110 nM, 130 nM respectively, > 8 foldselectivity than Aurora C, MEK1, Src

PHA-680632(PHA680632; PHA 680632) Cat. No.: HY-10178

ReversineCat. No.: HY-14711

SCH-1473759(SCH1473759; SCH 1473759) Cat. No.: HY-10482

SCH-1473759 hydrochlorideCat. No.: HY-10483

SNS-314(SNS-314 Mesylate; SNS314; SNS 314) Cat. No.: HY-12003

TAK-632(TAK 632; TAK632) Cat. No.: HY-15767

TAK-901(TAK901; TAK 901) Cat. No.: HY-12201

Tozasertib(MK-0457; VX-680; MK0457; VX680; VX 680; MK 0457) Cat. No.: HY-10161

XL228(XL-228; XL 228) Cat. No.: HY-15749

ZM-447439(ZM447439; ZM 447439) Cat. No.: HY-10128

http://www.medchemexpress.com/PHA-680632.html

http://www.medchemexpress.com/reversine.html

http://www.medchemexpress.com/SCH-1473759.html

http://www.medchemexpress.com/SCH-1473759-hydrochloride.html

http://www.medchemexpress.com/SNS-314.html

http://www.medchemexpress.com/TAK-632.html


http://www.medchemexpress.com/Tozasertib.html

http://www.medchemexpress.com/XL228.html

http://www.medchemexpress.com/ZM-447439.html

Casein Kinase

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


http://www.medchemexpress.com/Targets/Casein Kinase.html



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Purity: 99.92%Clinical Data:Size: 1 g, 5 g


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Casein Kinase Inhibitors & Modulators

Bioactivity: CX-4945 is an orally bioavailable, highly selective and potent CK2inhibitor, with values of 1 nM against CK2α and CK2α'.IC50

Bioactivity: CX-4945 (Silmitasertib) sodium salt is a potent and selectiveATP-competitive small molecule protein kinase CK2 inhibitor with aKi and an IC50 of 0

Bioactivity: D4476 is a potent, selective and cell-permeable inhibitor of caseinkinase 1( ) with an value of 0.3 μM .CK1 IC50 in vitro

Bioactivity: DMAT is a potent and specific inhibitor with an value ofCK2 IC50130 nM.

Bioactivity: Ellagic Acid is a cell permeable and strong casein kinase 2 (CK2)inhibitor (Ki = 20 nM) which acts as a potent antioxidant andanti-mutagenic

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

Bioactivity: IC261 is a novel inhibitor of CK1, triggers the mitotic checkpointcontrol. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5mM.

Bioactivity: LH846 is a selective inhibitor of CK1δ (IC50 values are 290 nM, 1.3uM and 2.5 uM for CK1δ, ε and α); displays no inhibitory activity atCK2.

Bioactivity: LY294002 is a broad-spectrum inhibitor of , with ofPI3K IC500.5/0.57/0.97 μM for , respectively, also potently inhibits PI3Kα/δ/β

with of 98 nM.CK2 IC50

Bioactivity: PF-670462 is a potent (IC50 = 7.7 ± 2.2 nM) and selective (>30-foldwith respect to 42 additional kinases) inhibitor of CK1ε in isolatedenzyme preparations.

CX-4945(Silmitasertib; CX 4945; CX4945) Cat. No.: HY-50855

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

D4476(Casein Kinase I Inhibitor; D 4476; D-4476) Cat. No.: HY-10324

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

Ellagic acidCat. No.: HY-B0183

Emodin(Frangula emodin) Cat. No.: HY-14393

IC261(IC-261; SU-5607) Cat. No.: HY-12774

LH846(LH 846; LH-846) Cat. No.: HY-15704

LY294002(NSC 697286; SF 1101; LY 294002; LY-294002) Cat. No.: HY-10108

PF-670462(PF 670462; PF670462) Cat. No.: HY-15490

http://www.medchemexpress.com/Targets/Casein Kinase.html

http://www.medchemexpress.com/CX-4945.html

http://www.medchemexpress.com/CX-4945-sodium-salt.html

http://www.medchemexpress.com/D4476.html

http://www.medchemexpress.com/DMAT.html

http://www.medchemexpress.com/Ellagic-acid.html

http://www.medchemexpress.com/Emodin.html

http://www.medchemexpress.com/IC261.html

http://www.medchemexpress.com/LH846.html

http://www.medchemexpress.com/LY294002.html



10 mg, 50 mg


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5 mg, 10 mg, 50 mg

Purity: >98.0%Clinical Data:Size: 10mM x 1mL in DMSO,

2 mg, 5 mg, 10 mg, 25 mg, 50 mg

Bioactivity: SR 3029 is a potent and highly specific CK1δ/CK1ε inhibitor with theIC50 of 97 nM.

Bioactivity: TA-01 potently inhibits CK1ε, CK1δ,and p38α (IC50values are 6.4, 6.8,and 6.7 nM respectively).

Bioactivity: TBB is a selective inhibitor for the protein kinase with of 1.6CK2 IC50μM.

Bioactivity: TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2)inhibitor with IC50/Ki of 0.1 uM/40 nM; shows selectivity for CK2 overJNK3, ROCK1, and MET(IC50> 10 uM).


SR-3029(SR 3029; SR3029) Cat. No.: HY-100011

TA-01(TA01; TA 01) Cat. No.: HY-100114

TBB (NSC 231634; TBB (enzyme inhibitor); 1H-Benzotriazole, 4,5,6,7-tet

rabromo-) Cat. No.: HY-14394

TTP 22(TTP22; TTP-22) Cat. No.: HY-15479

http://www.medchemexpress.com/SR-3029.html

http://www.medchemexpress.com/TA-01.html

http://www.medchemexpress.com/TBB.html

http://www.medchemexpress.com/TTP-22.html


CDK

CDKs (Cyclin-dependent kinases) are a family of protein kinases firstdiscovered for their role in regulating the cell cycle. Types: Cdk1,Cdk2, Cdk3, Cdk4, Cdk5, Cdk6, Cdk7, Cdk8, Cdk9, Cdk11. They arealso involved in regulating transcription, mRNA processing, and thedifferentiation of nerve cells. They are present in all knowneukaryotes,and their regulatory function in the cell cycle has been evolutionarilyconserved. CDKs are relatively small proteins, with molecular weightsranging from 34 to 40 kDa, and contain little more than the kinasedomain. By definition, a CDK binds a regulatory protein called a cyclin.Without cyclin, CDK has little kinase activity; only the cyclin-CDKcomplex is an active kinase. CDKs phosphorylate their substrates on

serines and threonines, so they are serine-threonine kinases. CDK levels remains relatively constant throughout thecell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKsof S. pombe (Cdc2), S. cerevisiae (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDKregulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDKinhibitory subunits (CKIs).

http://www.medchemexpress.com/Targets/CDK.html


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Purity: >98%Clinical Data: Phase 1Size: 1 mg, 5 mg, 10 mg, 25 mg


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Purity: >98%Clinical Data: Phase 1, Phase 2Size: 10mM x 1mL in DMSO,

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Purity: >98%Clinical Data: Phase 1, Phase 2Size: 5 mg, 10 mg, 50 mg, 100 mg

Purity: 99.26%Clinical Data:Size: 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg

CDK Inhibitors & Modulators

Bioactivity: 1-NM-PP1 inhibits recovered from the mutant, but not theCdk7wild-type cells with an IC of ~50 nM with either substrate.50

Bioactivity: AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 withIC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; withIC50 of 19 nM in MOLM-13 cell.

Bioactivity: AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of10-210 nM; less potent to CDK3 and little active to CDK7

Bioactivity: AT7519 hydrochloride is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9with IC50 of 10-210 nM; is less potent to CDK3 and little active toCDK7

Bioactivity: AT7519 trifluoroacetate is a multi-CDK inhibitor for CDK1, 2, 4, 6 and9 with IC50 of 10-210 nM; less potent to CDK3 and little active toCDK7.

Bioactivity: AZD-5438 is a potent inhibitor of with of 16 nM/6CDK1/2/9 IC50nM/20 nM in cell-free assays. It also inhibits GSK3β, but is less potentto CDK5/6.

Bioactivity: BAY 1143572 is a highly selective, potent and orally availableinhibitor of ; inhibits the proliferation of AML cell linesPTEFb/CDK9with a median of 385 nM.IC50

Bioactivity: BIO is a potent and selective inhibitor of and GSK-3 CDK1-cyclinBcomplex with s of 5 nM/320 nM/83 nM forIC50GSK-3αβ/CDK1/CDK5, respectively.

Bioactivity: BMS-265246 is a potent and selective CDK1/2 inhibitor forCDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM,respectively.

Bioactivity: Briciclib is a small molecule that suppresses cyclin D1 accumulationin cancer cells.


1-NM-PP1(PP1 Analog II; 1-NM-PP 1) Cat. No.: HY-13942

AMG 925(AMG-925; AMG925) Cat. No.: HY-15889

AT7519(AT 7519; AT-7519) Cat. No.: HY-50940

AT7519 Hydrochloride(AT 7519 Hydrochloride; AT-7519 Hydrochloride) Cat. No.: HY-50943

AT7519 trifluoroacetate (AT 7519 trifluoroacetate; AT-7519 trif

luoroacetate) Cat. No.: HY-50940A

AZD-5438(AZD 5438; AZD5438) Cat. No.: HY-10012

BAY-1143572(BAY1143572; BAY 1143572) Cat. No.: HY-12871

BIO (6BIO; 6-BIO; GSK 3 IX; GS

K 3 Inhibitor IX; MLS 2052; MLS2052) Cat. No.: HY-10580

BMS-265246(BMS265246; BMS 265246) Cat. No.: HY-15275

Briciclib(ON-014185; ON014185; ON 014185) Cat. No.: HY-16366

http://www.medchemexpress.com/Targets/CDK.html

http://www.medchemexpress.com/1-NM-PP1.html

http://www.medchemexpress.com/AMG-925.html

http://www.medchemexpress.com/at7519.html

http://www.medchemexpress.com/AT7519-Hydrochloride.html

http://www.medchemexpress.com/AT7519-trifluoroacetate.html

http://www.medchemexpress.com/AZD-5438.html

http://www.medchemexpress.com/BAY-1143572.html

http://www.medchemexpress.com/BIO.html

http://www.medchemexpress.com/bms-265246.html

http://www.medchemexpress.com/Briciclib.html



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Bioactivity: BS-181 is a highly selective inhibitor with of 21 nM, and >CDK7 IC5040-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

Bioactivity: BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM

Bioactivity: Ca2+ channel agonist 1 is a N-type Ca2+ channel activity agonist,with EC50 of 14.23 uM, also inhibits cdk2 kinase activity with EC50 of3.34 uM.

Bioactivity: CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM.

Bioactivity: CDK9-IN-1 is a novel, selective inhibitor for the treatment ofCDK9HIV infection.

Bioactivity: CDK9-IN-2 is a special cyclin-dependent kinase 9 ( ) inhibitor,CDK9extracted from patent WO/2012131594A1, compound CDKI(8), hasan of 5 nM and 7 nM in H929 multiple myeloma(MM) cell lineIC50(72 hours) and A2058 skin cell line (72 hours), respectively.

Bioactivity: CDK9-IN-6 is a CDK9 inhibitor, refers to Example 399 in WO2012101062 A1

Bioactivity: CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selectivetoxicity to CLL cells(LD50=80 nM) versus normal B cell and normalCD34+ cell(LD50>20 uM).

Bioactivity: CVT-313 is a potent, selective, reversible, and ATP-competitiveinhibitor of wirh of 0.5 μM.CDK2 IC50

Bioactivity: Dinaciclib is a potent and selective inhibitor of s, with s of ofCDK IC901, 1, 3, and 4 nM for , , , and activity,CDK2 CDK5 CDK1 CDK9respectively.

BS-181(BS 181; BS181) Cat. No.: HY-13266

BS-181 hydrochlorideCat. No.: HY-13266A

Ca2+ channel agonist 1Cat. No.: HY-41076

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

CDK9-IN-1Cat. No.: HY-13231



CDKI-73Cat. No.: HY-12445

CVT-313(CVT 313; NG 26; CVT313; NG26; NG-26) Cat. No.: HY-15339

Dinaciclib(SCH 727965; SCH727965; SCH-727965) Cat. No.: HY-10492

http://www.medchemexpress.com/BS-181.html

http://www.medchemexpress.com/BS-181-hydrochloride.html

http://www.medchemexpress.com/Ca2_addition_-channel-agonist-1.html

http://www.medchemexpress.com/CDK-IN-2.html

http://www.medchemexpress.com/cdk9-in-1.html

http://www.medchemexpress.com/cdk9-in-2.html

http://www.medchemexpress.com/CDK9-IN-6.html

http://www.medchemexpress.com/CDKI-73.html

http://www.medchemexpress.com/cvt-313.html

http://www.medchemexpress.com/Dinaciclib.html


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Bioactivity: Flavopiridol is a broad inhibitor of , competing with ATP toCDKinhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with ofIC50around 40 nM.

Bioactivity: Flavopiridol hydrochloride competes with ATP to inhibit CDKsincluding CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM

Bioactivity: JNJ-7706621 is pan-CDK inhibitor with the highest potency onCDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity forCDK1/2 than CDK3/4/6; also potently inhibits Aurora A/B and has noactivity on Plk1 and Wee1.

Bioactivity: K03861 is a type II CDK2 inhibitor with Kd of 8.2 nM.

Bioactivity: Kenpaullone is an ATP-competitive inhibitor of several CDKs as wellas GSK-3β, with an IC50 value of 0.23 μM for GSK-3β and 0.4, 0.68,0.85, and 0.47 μM for CDK1/cyclin B, CDK2/cyclin A, CDK5/p25, andlymphocyte kinase., respectively.

Bioactivity: KH-CB19 is a potent and highly specific inhibitor of the CDC2-likekinase isoforms 1 and 4 (CLK1/CLK4).

Bioactivity: LDC000067 is a highly specific inhibitor with an value ofCDK9 IC5044±10 nM .in vitro

Bioactivity: LEE011 is a highly specific inhibitor with values of 10CDK4/6 IC50nM and 39 nM, respectively, and is over 1,000-fold less potentagainst the cyclin B/CDK1 complex.

Bioactivity: LEE011 Hcl is an orally available cyclin-dependent kinase (CDK)inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cyclepathway, with potential antineoplastic activity

Bioactivity: LEE011 succinate is an orally available cyclin-dependent kinase (CDK)inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cyclepathway, with potential antineoplastic activity


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

Flavopiridol Hydrochloride (HL 275; NSC 649890; MDL 10

7826A; FLAVOPIRIDOL HCL; Alvocidib Hydrochloride) Cat. No.: HY-10006

JNJ-7706621(JNJ7706621; JNJ 7706621) Cat. No.: HY-10329

K03861(K 03861; K-03861) Cat. No.: HY-15004

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

KH-CB19(KH-CB-19) Cat. No.: HY-12828

LDC000067(LDC067; LDC 000067; LDC-000067; LDC 067; LDC-067) Cat. No.: HY-15878

LEE011(Ribociclib; LEE 011; LEE-011) Cat. No.: HY-15777

LEE011 hydrochloride (Ribociclib hydrochloride; LEE 011 hydr

ochloride; LEE-011 hydrochloride) Cat. No.: HY-15777A

LEE011 succinate (Ribociclib succinate; LEE 011 succinat

e; LEE-011 succinate) Cat. No.: HY-15777B

http://www.medchemexpress.com/Flavopiridol.html

http://www.medchemexpress.com/Flavopiridol-Hydrochloride.html

http://www.medchemexpress.com/JNJ-7706621.html

http://www.medchemexpress.com/K03861.html

http://www.medchemexpress.com/Kenpaullone.html

http://www.medchemexpress.com/KH-CB19.html

http://www.medchemexpress.com/LDC000067.html

http://www.medchemexpress.com/LEE011.html

http://www.medchemexpress.com/lee011-hydrochloride.html

http://www.medchemexpress.com/lee011-succinate.html



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Bioactivity: LEE011 succinate hydrate is an orally available cyclin-dependentkinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6cell cycle pathway, with potential antineoplastic activity

Bioactivity: LY2835219 a selective inhibitor with values of 2 nM andCDK4/6 IC5010 nM for CDK4 and CDK6, respectively.

Bioactivity: LY2835219 is a potent and selective inhibitor of CDK4 and CDK6 withIC50 of 2 nM and 10 nM, respectively

Bioactivity: LY2857785 is a type I reversible and competitive ATP kinaseinhibitor against, b>CDK9 ( 11 nM) and other transcriptionIC50kinases ( 16 nM), and ( 246 nM).CDK8 IC50 CDK7 IC50

Bioactivity: LY3177833 is an and inhibitor extracted from patentCDC7 pMCM2US 20140275131and patent WO 2014143601 A1 compound example4; has values of 3.3 nM and 290 nM, respectivelyIC50

Bioactivity: M2I-1 a small Mad2 inhibitor-1. the first small molecule inhibitortargeting the binding of Mad2 to Cdc20, an essential proteinproteininteraction (PPI) within the SAC.

Bioactivity: NG 52 (Compound 52 ) is a potent, cell-permeable, reversible,selective, and ATP-compatible inhibitor of the cell cycle-regulatingkinase, Cdc28p (IC50 = 7 μM), and the related Pho85p kinase (IC50 =2 μM).

Bioactivity: NSC23005 sodium is a novel and effective inhibitor ( =5.21p18 ED50nM) in promoting Hematopoietic stem cells (HSCs) expansion in bothmurine and human models.

Bioactivity: NU2058 is a guanine-based CDK inhibitor with IC50 of 17 μM and 26μM for CDK2 and CDK1.

Bioactivity: NU6300 is a non-covalent ATP-competitive CDK2 inhibitor (IC50 =0.16 mM).

LEE011 succinate hydrate (Ribociclib succinate hydrate; LEE 011

succinate hydrate; LEE-011 succinate hydrate) Cat. No.: HY-15777C

LY2835219 (ABEMACICLIB; CDK4/6 dual inhibitor; LY 2835219; LY-28

35219) Cat. No.: HY-16297

LY2835219 free base (Abemaciclib; CDK4/6 dual inhibitor; LY

-2835219 free base) Cat. No.: HY-16297A

LY2857785(LY 2857785; LY-2857785) Cat. No.: HY-12293

LY3177833(LY-3177833; LY 3177833) Cat. No.: HY-100023

M2I-1Cat. No.: HY-100341

NG 52(Compound 52; NG-52; NG52) Cat. No.: HY-15154

NSC23005 sodium(NSC 23005 sodium; NSC-23005 sodium) Cat. No.: HY-100791

NU2058(NU-2058; O6-(Cyclohexylmethyl)guanine) Cat. No.: HY-19316

NU6300(NU-6300) Cat. No.: HY-18930

http://www.medchemexpress.com/LEE011-succinate-hydrate.html


http://www.medchemexpress.com/LY2835219-free-base.html



http://www.medchemexpress.com/M2I-1.html

http://www.medchemexpress.com/NG-52.html

http://www.medchemexpress.com/NSC23005-sodium.html

http://www.medchemexpress.com/NU2058.html

http://www.medchemexpress.com/NU6300.html


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10 mg, 50 mg

Purity: >98%Clinical Data:Size: 10 mg, 50 mg


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

Purity: 99.99%Clinical Data: Phase 2, Phase 3Size: 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg

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

Bioactivity: ON123300 is a potent inhibitor of CDK4, with an IC50 of 3.8 nM, withlittle inhibitory activity against CDKs 1,2,5 and 8.

Bioactivity: Palbociclib is a highly specific inhibitor of ( =11 nM) and Cdk4 IC50 ( =16 nM), having no activity against a panel of 36Cdk6 IC50

additional protein kinases.

Bioactivity: Palbociclib hydrochloride is a highly specific inhibitor of (Cdk4 IC50=11 nM) and ( =16 nM), having no activity against a panelCdk6 IC50of 36 additional protein kinases.

Bioactivity: Palbociclib (isethionate) is a highly selective inhibitor of CDK4/6 with s of 11 nM/16 nM, and shows no activity against CDK1/2/5,IC50EGFR, FGFR, PDGFR, InsR, etc.

Bioactivity: PHA-767491 (CAY10572) is a potent, ATP-competitive dualCdc7/Cdk9 inhibitor with IC50 values of 10/34 nM.

Bioactivity: PHA-767491 (CAY10572) Hcl is a potent, ATP-competitive dualCdc7/Cdk9 inhibitor with IC50 values of 10/34 nM.

Bioactivity: PHA-793887 is a novel pan-cdk inhibitor, including cdk1, cdk2, cdk4,cdk5, cdk7, and cdk9 with IC50 in the 5 to 140 nM range

Bioactivity: PHA-848125(Milciclib) is a potent, ATP-competitive CDK inhibitor forCDK2 with IC50 of 45 nM; >3-fold more selective for CDK2 thanCDK1, 2, 4, 5, and 7

Bioactivity: Purvalanol A(NG-60) is a potent, cell-permeable, and selectiveinhibitor of cyclin-dependent kinases (CDKs) with IC50 values of 4,70, 35, 850, and 75 nM for cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclinE, Cdk4/cyclin D1 and Cdk5-p35, respectively


NVP-LCQ195 (LCQ-195; AT-9311; NVP LCQ

195; LCQ 195; AT9311; AT 9311) Cat. No.: HY-15241

ON123300(ON-123300; ON 123300) Cat. No.: HY-12624

Palbociclib(PD0332991; PD-0332991; PD 0332991) Cat. No.: HY-50767

Palbociclib hydrochloride (PD-0332991 hydrochloride;

PD0332991 hydrochloride; PD 0332991 hydrochloride) Cat. No.: HY-50767A

Palbociclib isethionate (PD0332991 isethionate; PD-0332991 iset

hionate; PD 0332991 isethionate) Cat. No.: HY-A0065

PHA-767491 (CAY10572; PHA767491; PHA

767491; CAY-10572; CAY 10572) Cat. No.: HY-13461

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

PHA-793887(PHA 793887; PHA793887) Cat. No.: HY-11001

PHA-848125(Milciclib; PHA 848125) Cat. No.: HY-10424

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

http://www.medchemexpress.com/NVP-LCQ195.html

http://www.medchemexpress.com/ON123300.html

http://www.medchemexpress.com/Palbociclib.html

http://www.medchemexpress.com/Palbociclib-hydrochloride.html

http://www.medchemexpress.com/Palbociclib-isethionate.html

http://www.medchemexpress.com/pha-767491.html

http://www.medchemexpress.com/PHA-767491-hydrochloride.html



http://www.medchemexpress.com/Purvalanol-A.html



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Bioactivity: Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A,cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.

Bioactivity: R547 is a potent ATP-competitive inhibitor of CDK1/2/4 with Ki of 2nM/3 nM/1 nM.

Bioactivity: RGB-286638 is a novel CDK inhibitor with IC50s of 1 nM/2 nM/3nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclinE-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; lesspotent against cyclin H-CDK7 and cyclin D3-CDK6.

Bioactivity: RGB-286638 free base is a novel CDK inhibitor with IC50s of 1 nM/2nM/3 nM/4 nM/5 nM for cyclin T1-CDK9/cyclin B1-CDK1/cyclinE-CDK2/cyclin D1-CDK4/cyclin E-CDK3/p35-CDK5 respectively; lesspotent against cyclin H-CDK7 and cyclin D3-CDK6.

Bioactivity: Ro-3306 is a potent and selective inhibitor of CDK1 with Ki value of35 nM for CDK1/cyclin B1, 10-fold selectivity relative to CDK2/cyclin Eand >50-fold relative to CDK4/cyclin D.

Bioactivity: Roscovitine is a potent and selective inhibitor with of 0.2CDK IC50μM, 0.65 μM, and 0.7 μM for , , and , respectively.CDK5 Cdc2 CDK2

Bioactivity: SB1317 is a potent inhibitor of , , and for theCDK2 JAK2 FLT3treatment of cancer, with of 13, 73, and 56 nM for CDK2, JAK2IC50and FLT3, respectively.

Bioactivity: SNS-032 is a selective inhibitor of cyclin-dependent kinase (CDK), with s of 48 nM/62 nM/4 nM.inhibiting CDK2/7/9 IC50

Bioactivity: SU-9516 is a selective CDK2 inhibtor with IC50 of 22 nM; less potentfor CDK1/CDK4(IC50=40/200 nM), no inhibition on PKC, EGFR,p38MAPK etc

Bioactivity: TG003 is a potent inhibitor of ; inhibits Clk1 and Clk4 with Clk1/Sty IC values of 20 and 15 nM, respectively.50

Purvalanol B(NG 95; NG95; NG-95) Cat. No.: HY-18299

R547(R 547; R-547) Cat. No.: HY-10014

RGB-286638(RGB286638) Cat. No.: HY-15504

RGB-286638 free base(RGB286638 free base) Cat. No.: HY-15504A

Ro-3306Cat. No.: HY-12529

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

SB1317(TG02; SB 1317; TG 02; SB-1317; TG-02) Cat. No.: HY-15166

SNS-032 (BMS-387032; SNS 032; SNS0

32; BMS 387032; BMS387032) Cat. No.: HY-10008

SU9516(SU-9516) Cat. No.: HY-18629

TG003(TG 003; TG-003) Cat. No.: HY-15338

http://www.medchemexpress.com/Purvalanol-B.html

http://www.medchemexpress.com/R547.html

http://www.medchemexpress.com/RGB-286638.html

http://www.medchemexpress.com/RGB-286638-free-base.html

http://www.medchemexpress.com/Ro-3306.html

http://www.medchemexpress.com/Roscovitine.html

http://www.medchemexpress.com/SB1317.html

http://www.medchemexpress.com/SNS-032.html

http://www.medchemexpress.com/SU9516.html

http://www.medchemexpress.com/TG003.html


5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg



2 mg, 5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: THZ1 is a selective and potent covalent inhibitor with ofCDK7 IC503.2 nM.

Bioactivity: THZ1 Hydrochloride is a selective and potent covalent CDK7inhibitor with of 3.2 nM.IC50

Bioactivity: THZ1-R is a non-cysteine reactive analog, which displays diminishedactivity for CDK7and reduces anti proliferative potency.

Bioactivity: THZ2 is a potent and selective inhibitor with of 13.9 nM.CDK7 IC50

Bioactivity: WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and1.0 uM, respectively.

Bioactivity: WHI-P180 hydrochloride is a potent EGFR and Cdk2 inhibitors withIC50 of 4.0 and 1.0 uM, respectively.

Bioactivity: Wogonin is a cell-permeable and orally available flavonoid thatdisplays anti-inflammatory and anticancer properties

Bioactivity: XL413 is a potent and selective Cdc7 inhibitor with an IC50 of 3.7 nM,>60-fold selectivity against CK2, >10-fold selectivity against PIM, and>300-fold selectivity against a panel of over 100 protein kinases.

Bioactivity: XL413 is a potent and selective Cdc7 inhibitor with an IC50 of 3


THZ1(CDK7 inhibitor) Cat. No.: HY-80013

THZ1 Hydrochloride(CDK7 inhibitor) Cat. No.: HY-80013A

THZ1-R(THZ 1-R) Cat. No.: HY-19988

THZ2Cat. No.: HY-12280

WHI-P180(Janex 3; WHI-P 180) Cat. No.: HY-15769

WHI-P180 hydrochloride(Janex 3 hydrochloride; WHI-P 180 hydrochloride) Cat. No.: HY-15769A

WogoninCat. No.: HY-N0400

XL413(XL-413; XL 413) Cat. No.: HY-15260

XL413 hydrochloride(XL-413 hydrochloride; XL 413 hydrochloride) Cat. No.: HY-15260A

http://www.medchemexpress.com/THZ1.html

http://www.medchemexpress.com/THZ1-Hydrochloride.html

http://www.medchemexpress.com/THZ1-R.html

http://www.medchemexpress.com/THZ2.html

http://www.medchemexpress.com/whi-p180.html

http://www.medchemexpress.com/whi-p180-hydrochloride.html

http://www.medchemexpress.com/Wogonin.html

http://www.medchemexpress.com/xl413.html

http://www.medchemexpress.com/XL413-hydrochloride.html


Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) are protein kinases that are involved in cellcycle control. Two checkpoint kinase subtypes have been identified,Chk1 and Chk2. Chk1 is a central component of genome surveillancepathways and is a key regulator of the cell cycle and cell survival.Chk1 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, G2/M transition and M phase. In addition to mediating cellcycle checkpoints, Chk1 also contributes to DNA repair processes,gene 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.

http://www.medchemexpress.com/Targets/Checkpoint Kinase (Chk).html


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


2 mg, 5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg



10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg

Checkpoint Kinase (Chk) Inhibitors & Modulators

Bioactivity: AZD-7762 is a potent ATP-competitive checkpoint kinase ( )Chkinhibitor in with of 5 nM for Chk1.IC50

Bioactivity: BML-277 is a selective checkpoint kinase 2 ( ) inhibitor with an Chk2 of 15 nM.IC50

Bioactivity: CCT241533 is a potent serine/threonine checkpoint kinase (Chk2)inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against apanel of kinases at 1 uM.

Bioactivity: CCT241533 hydrochloride is a potent and selective ATP competitiveinhibitor of with an of 3 nM and of 1.16 nM.CHK2 IC50 Ki

Bioactivity: CCT244747 is potent, highly selective, orally active, ATP competitiveCHK1 inhibitor with IC50 of 29-170nM.

Bioactivity: CCT245737 is a potent, ATP-competitive CHK1 inhibitor with an IC50of 30-220 nM.

Bioactivity: CHIR-124 is a potent and selective inhibitor with of 0.3Chk1 IC50nM, and also potently targets and with s of 6.6 nMPDGFR FLT3 IC50and 5.8 nM.

Bioactivity: LY2603618 is a potent and selective inhibitor of protein kinaseChk1activity in vitro with of 7 nM.IC50

Bioactivity: LY2606368 is a potent and selective ATP competitive inhibitor of the protein kinase, with a of 0.9 nM against purified CHK1.Chk1 Ki

Bioactivity: LY2606368 dihydrochloride is a potent and selective ATP competitiveinhibitor of the protein kinase, with a of 0.9 nM againstChk1 Kipurified CHK1.


AZD-7762(AZD7762; AZD 7762) Cat. No.: HY-10992

BML-277(Chk2 Inhibitor II; C 3742; BML277; BML 277) Cat. No.: HY-13946

CCT241533(CCT 241533; CCT-241533) Cat. No.: HY-14715

CCT241533 hydrochloride (CCT-241533 hydrochloride; CCT 241533 h

ydrochloride) Cat. No.: HY-14715B



CHIR-124(CHIR124; CHIR 124) Cat. No.: HY-13263

LY2603618(IC-83; LY 2603618; LY-2603618) Cat. No.: HY-14720

LY2606368(LY 2606368; LY-2606368; Prexasertib) Cat. No.: HY-18174

LY2606368 dihydrochloride (LY-2606368 dihydrochloride

; Prexasertib dihydrochloride) Cat. No.: HY-18174A

http://www.medchemexpress.com/Targets/Checkpoint Kinase (Chk).html

http://www.medchemexpress.com/AZD-7762.html

http://www.medchemexpress.com/BML-277.html

http://www.medchemexpress.com/cct241533.html

http://www.medchemexpress.com/CCT241533-hydrochloride.html



http://www.medchemexpress.com/CHIR-124.html



http://www.medchemexpress.com/LY2606368-dihydrochloride.html



5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


Bioactivity: PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitorwith Ki of 0

Bioactivity: SCH900776 is a potent, selective and orally bioavailable inhibitor ofcheckpoint kinase1 ( ) with of 3 nM, and has much greaterChk1 IC50selectivity against Chk2 (IC =1500 nM) and cyclin-dependent kinase50CDK2 (IC =160 nM).50

Bioactivity: SCH900776 (S-isomer) is the S-isomer form ofSCH900776(HY-15532), which is a potent, selective and orallybioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highlyselective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinaseCDK2 (IC50 = 160 nM)

PF 477736(PF-0044736; PF0044736; PF477736; PF-477736) Cat. No.: HY-10032

SCH900776(SCH 900776; SCH-900776) Cat. No.: HY-15532

SCH900776 S-isomer(SCH 900776 S-isomer; SCH-900776 S-isomer) Cat. No.: HY-15532B


http://www.medchemexpress.com/SCH900776.html

http://www.medchemexpress.com/sch900776-s-isomer.html

CRISPR/Cas9

CRISPR/Cas9 (Clustered Regularly-Interspaced Short PalindromicRepeats/Cas9) 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 “guide RNA”(gRNA) to the target site. DSB’s produced by Cas9 are most oftenrepaired through the cell’s 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 “knocking out” a gene.

The CRISPR/Cas9 system has substantially advanced efforts in specific gene editing and has been successfully appliedto modify the episomal genomes of human and other organisms. The CRISPR/Cas9 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 CRISPR/Cas9 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 CRISPR/Cas9 has become an efficient and reliable way to make precise, targeted changes to the genome ofliving cells.


http://www.medchemexpress.com/Targets/CRISPR_Cas9.html



5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


2 mg, 5 mg, 10 mg, 25 mg, 50 mg

CRISPR/Cas9 Inhibitors & Modulators

Bioactivity: 4-hydroxytamoxifen (OHT), an active metabolite of tamoxifen, is aselective estrogen receptor modulator, which increasesCRISPR/Cas9-mediated editing frequency

Bioactivity: Brefeldin A is a fungal metabolite that induces the Golgi proteins toredistribute into the ER, blocks the secretion from the Golgiapparatus and increases -mediated editing frequencies.CRISPR/Cas9

Bioactivity: KU-57788 is a potent and selective inhibitor of , a modestDNA-PKinhibitor of and , with s of 13 nM, 1 μM and 3.5 μM,BRD4 BRDT IC50respectively, and also increases -mediated editingCRISPR/Cas9frequencies.

Bioactivity: Nocodazole is a rapidly-reversible inhibitor of microtubulepolymerization, which exhibits good potency against ABL,ABL(E255K), and ABL(T315I) with values of 0.21 μM, 0.53 μM,IC50and 0.64 μM, respectively, and increases -mediatedCRISPR/Cas9editing frequencies.

Bioactivity: RS-1 is a RAD51-stimulatory compound, which increases the DNAbinding activity of RAD51.

Bioactivity: SCR7 is a inhibitor, blocks nonhomologousDNA Ligase IVend-joining (NHEJ). SCR7 increases -mediated editingCRISPR/Cas9frequency.

4-Hydroxytamoxifen((Z)-4-Hydroxytamoxifen; trans-4-Hydroxytamoxifen) Cat. No.: HY-16950

Brefeldin A (Ascotoxin; Cyanein; Decumbin; Nectrolide; BFA; Synerg

isidin) Cat. No.: HY-16592

KU-57788(KU 57788; NU-7441; KU57788; NU7441; NU 7441) Cat. No.: HY-11006

Nocodazole(Oncodazole; R17934) Cat. No.: HY-13520

RS-1(RS1; RS 1) Cat. No.: HY-19793

SCR7(SCR-7) Cat. No.: HY-12742

http://www.medchemexpress.com/Targets/CRISPR_Cas9.html

http://www.medchemexpress.com/4-Hydroxytamoxifen.html

http://www.medchemexpress.com/Brefeldin-A.html


http://www.medchemexpress.com/Nocodazole.html

http://www.medchemexpress.com/RS-1.html

http://www.medchemexpress.com/SCR7.html

Deubiquitinase

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 Jab1/Mov34/Mpr1 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.


http://www.medchemexpress.com/Targets/Deubiquitinase.html



5 mg, 10 mg, 25 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg

Deubiquitinase Inhibitors & Modulators

Bioactivity: b-AP15 is a specific inhibitor of the enzymes deubiquitinating and .UCHL5 Usp14

Bioactivity: BAY 11-7082 is a inhibitor. BAY 11-7082 inhibitsNF-κBubiquitin-specific protease ( )7 and 21 with an of 0.19μMUSP IC50and 0.96μM, respectively.

Bioactivity: DUBs-IN-1 is a potent deubiquitinase enzyme inhibitor with IC50s of18 uM/0.71 uM for USP7/USP8 respectively.

Bioactivity: DUBs-IN-2 is a potent inhibitor with s of 7.2deubiquitinase IC50μM/0.93 μM for USP7/USP8, respectively.

Bioactivity: DUBs-IN-3 is a potent enzyme inhibitor, extracteddeubiquitinasefrom the reference, compound 5c, has s of 3.1 μM and > 100 μMIC50for and USP7, respectively.USP8

Bioactivity: HBX 19818 is a selective USP7 inhibitor with IC50 of 28.1 uM .

Bioactivity: LDN-57444 is a potent, reversible, competitive and activesite-directed inhibitor of UCHL1 with Ki of 0

Bioactivity: ML-323 is a reversible, potent inhibitor with of 76USP1-UAF1 IC50nM in a Ub-Rho assay. The measured inhibition constants of ML-323for the free enzyme ( ) is 68 nM.Ki

Bioactivity: ML364 is an inhibitor extracted from patent WO 2016134026USP2A1, compound example 10G.

Bioactivity: NSC632839 is a nonselective isopeptidase inhibitor, which inhibits , , and with s of 45±4 μM, 37±1 μM, andUSP2 USP7 SENP2 EC50

9.8±1.8 μM, respectively.

b-AP15(NSC687852; NSC 687852; NSC-687852) Cat. No.: HY-13989

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

DUBs-IN-1Cat. No.: HY-50736

DUBs-IN-2Cat. No.: HY-50737A

DUBs-IN-3Cat. No.: HY-50737

HBX 19818(HBX19818; HBX-19818) Cat. No.: HY-17540

LDN-57444Cat. No.: HY-18637

ML-323(ML323; ML 323) Cat. No.: HY-17543

ML364(ML 364; ML-364) Cat. No.: HY-100900

NSC632839(NSC-632839; NSC 632839) Cat. No.: HY-100708

http://www.medchemexpress.com/Targets/Deubiquitinase.html

http://www.medchemexpress.com/b-AP15.html

http://www.medchemexpress.com/BAY-11-7082.html

http://www.medchemexpress.com/DUBs-IN-1.html



http://www.medchemexpress.com/HBX-19818.html

http://www.medchemexpress.com/LDN-57444.html

http://www.medchemexpress.com/ML-323.html

http://www.medchemexpress.com/ML364.html

http://www.medchemexpress.com/NSC632839.html


5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg


10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg

Bioactivity: P22077 is a potent inhibitor of ubiquitin-specific protease (USP) 7(EC50=8.6 uM), P22077 also inhibits the closely relateddeubiquitinase (DUB) USP47.

Bioactivity: P005091 is a selective and potent inhibitor of ubiquitin-specific with of 4.2 μM and the closely relatedprotease 7 (USP7) EC50

USP47.

Bioactivity: PR-619 is a broad-range inhibitor with of 3.93, 4.9, 6.86,DUB EC507.2, and 8.61 μM for , , , , and , respectively.USP4 8 7 2 5

Bioactivity: SJB2-043 is an inhibitor of the native complex with USP1/UAF1 IC50of 544 nM.

Bioactivity: SJB3-019A is a potent and novel inhibitor, 5 times more potentUSP1than SJB2-043 in promoting ID1 degradation and cytoxicity in K562cells with of 0.0781 μM.IC50

Bioactivity: USP7-IN-1 is a novel selective and reversible inhibitor of USP7 withIC50 of 33 uM; less or no inhibition on USP5, USP8, Uch-L1, Uch-L3and Caspase(IC50>200 uM); HCT116 cell viability GI50 is 67 uM.

Bioactivity: USP7/USP47 inhibitor is a potent and dual inhibitor of USP7/USP47with IC50s of 0.42 uM(USP7) and 1.0 uM(USP47).

Bioactivity: VLX1570 is a competitive inhibitor of proteasome DUB activity withIC50 ranging from 4.2 uM to 8.6 uM.

Bioactivity: WP1130 inhibits the autoactivation of by inducing its rapidBcr-Abldown-regulation with of 1.8 μM. WP1130 also in aIC50deubiquitinase inhibitor.


P 22077(P22077; P-22077) Cat. No.: HY-13865

P005091(P5091; P-005091; P 005091; P 5091; P-5091) Cat. No.: HY-15667

PR-619 (2,6-Diamino-3,5-dithiocya

nopyridine; PR 619; PR619) Cat. No.: HY-13814

SJB2-043Cat. No.: HY-15757

SJB3-019ACat. No.: HY-80012

USP7-IN-1Cat. No.: HY-16709

USP7/USP47 inhibitor (2-Thiophenecarboxamide, 4-cyano-5-[(3,

5-dichloro-4-pyridinyl)thio]-N-[4-(methylsulfony…) Cat. No.: HY-13487

VLX1570(VLX 1570; VLX-1570) Cat. No.: HY-12471

WP1130(Degrasyn; WP 1130; WP-1130) Cat. No.: HY-13264

http://www.medchemexpress.com/p-22077.html

http://www.medchemexpress.com/P005091.html

http://www.medchemexpress.com/PR-619.html

http://www.medchemexpress.com/SJB2-043.html

http://www.medchemexpress.com/SJB3-019A.html

http://www.medchemexpress.com/USP7-IN-1.html

http://www.medchemexpress.com/USP7-USP47-inhibitor.html

http://www.medchemexpress.com/VLX1570.html

http://www.medchemexpress.com/WP1130.html


DNA Alkylator/Crosslinker

DNA alkylator/crosslinker is a molecule that alkylates DNA or cancross link with DNA. DNA alkylator/crosslinker can have mutagenic,pharmaceutical, 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.

http://www.medchemexpress.com/Targets/DNA Alkylator_Crosslinker.html


100 mg, 200 mg, 500 mg


100 mg, 500 mg


10 mg, 50 mg

Purity: >98.0%Clinical Data: Phase 3Size: 10mM x 1mL in Water,

100 mg, 200 mg, 500 mg


1 mg, 5 mg, 10 mg


1 g, 5 g


100 mg, 200 mg, 500 mg




100 mg, 500 mg

DNA Alkylator/Crosslinker Inhibitors & Modulators

Bioactivity: Altretamine is an alkylating agent proposed as an antineoplastic Bioactivity: Altretamine is an alkylating agent proposed as an antineoplastic

Bioactivity: Bendamustine D4 is the deuterium labeled Bendamustine(SDX-105),which is an alkylating agent

Bioactivity: Bendamustine Hcl(SDX105; EP-3101) is a DNA-damaging agent withIC50 of 50 μM

Bioactivity: Busulfan is a bifunctional alkylating agent Bioactivity: Calicheamicin is a potent DNA-damaging cytotoxic agent.

Bioactivity: Carboplatin is a chemotherapy drug by binding to DNA andinterfering with the cell's repair mechanism

Bioactivity: Carmustine is a cell-cycle phase nonspecific alkylating antineoplasticagent

Bioactivity: Chlorambucil(WR-139013; CB-1348) is a chemotherapy drug that hasbeen mainly used in the treatment of chronic lymphocytic leukemia

Bioactivity: Cyclophosphamide is a synthetic alkylating agent chemically relatedto the nitrogen mustards with antineoplastic and immunosuppressiveactivities.


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

Altretamine hydrochloride (ENT-50852 hydrochloride; R

B-1515 hydrochloride; WR-95704 hydrochloride) Cat. No.: HY-B0181A

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

Bendamustine hydrochloride(SDX105; SDX 105; SDX-105; EP-3101 ) Cat. No.: HY-B0077

BusulfanCat. No.: HY-B0245

Calicheamicin(Calicheamicin γ1) Cat. No.: HY-19609

Carboplatin (cis-Diammine(1,1-cyclobut

anedicarboxylato)platinum) Cat. No.: HY-17393

CarmustineCat. No.: HY-13585

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

CyclophosphamideCat. No.: HY-17420

http://www.medchemexpress.com/Targets/DNA Alkylator_Crosslinker.html

http://www.medchemexpress.com/Altretamine.html

http://www.medchemexpress.com/altretamine-hydrochloride.html

http://www.medchemexpress.com/Bendamustine-D4.html

http://www.medchemexpress.com/bendamustine-hydrochloride.html

http://www.medchemexpress.com/busulfan.html

http://www.medchemexpress.com/Calicheamicin.html

http://www.medchemexpress.com/Carboplatin.html

http://www.medchemexpress.com/Carmustine.html

http://www.medchemexpress.com/Chlorambucil.html

http://www.medchemexpress.com/Cyclophosphamide.html



5 mg, 10 mg, 50 mg


50 mg, 100 mg, 200 mg, 500 mg


5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg


50 mg, 100 mg, 500 mg


200 mg, 500 mg


200 mg, 500 mg


10 mg, 50 mg


100 mg, 200 mg

Bioactivity: Cyclophosphamide is a nitrogen mustard alkylating agent used in thetreatment of cancers and autoimmune disorders.

Bioactivity: Fotemustine (S 10036) is a nitrosourea alkylating agent approved foruse in the treatment of metastasising melanoma

Bioactivity: Ifosfamide is a nitrogen mustard alkylating agent used in thetreatment of cancer

Bioactivity: Lomustine (CCNU) is an alkylating nitrosourea compound used inchemotherapy

Bioactivity: Melphalan(Sarcolysin; L-PAM) is a chemotherapy drug belonging tothe class of nitrogen mustard alkylating agents; attaches the alkylgroup to the guanine base of DNA.

Bioactivity: Miriplatin (SM-11355) is a novel platinum complex used in TACE thatshows promise for the treatment of hepatocellular carcinoma (HCC)

Bioactivity: Miriplatin hydrate was approved for lipiodolization for the treatmentof hepatocellular carcinoma in 2009; it is a lipophilic platinumcomplex containing myristates as leaving groups, and can be easilysuspended in ethyl esters of iodized fatty acids obtained from poppyseed oil

Bioactivity: Mitomycin C is a DNA-damaging agent and small-molecule inhibitoreffectively sensitize cancer cells to tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL).

Bioactivity: Oxaliplatin inhibits DNA synthesis by conforming DNA adducts. Bioactivity: Palifosfamide is a novel DNA alkylator and the active metabolite ofifosfamide, with antitumor activity.

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

Fotemustine(S10036; S 10036; S-10036) Cat. No.: HY-B0733

IfosfamideCat. No.: HY-17419

LomustineCat. No.: HY-13669

Melphalan(L-PAM) Cat. No.: HY-17575

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

Miriplatin hydrate(Miriplatin) Cat. No.: HY-16325

Mitomycin C(Ametycine) Cat. No.: HY-13316

OxaliplatinCat. No.: HY-17371

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

http://www.medchemexpress.com/Cyclophosphamide-hydrate.html

http://www.medchemexpress.com/Fotemustine.html

http://www.medchemexpress.com/ifosfamide.html

http://www.medchemexpress.com/Lomustine.html

http://www.medchemexpress.com/Melphalan.html

http://www.medchemexpress.com/Miriplatin.html

http://www.medchemexpress.com/miriplatin-hydrate.html

http://www.medchemexpress.com/Mitomycin-C.html

http://www.medchemexpress.com/Oxaliplatin.html

http://www.medchemexpress.com/Palifosfamide.html


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


100 mg


10 mg, 50 mg, 100 mg


100 mg, 500 mg


5 mg, 10 mg, 25 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


100 mg, 500 mg

Bioactivity: Procarbazine Hcl, an antineoplastic chemotherapy drug, is analkylating agent for the treatment of Hodgkin's lymphoma andcertain brain cancers; also inhibits MAO thus increasing the effects ofsympathomimetics, TCAs, and tyramine

Bioactivity: RITA(NSC 652287) induced both DNA-protein and DNA-DNAcross-links with no detectable DNA single-strand breaks

Bioactivity: Satraplatin(BMS182751; BMY45594; JM216) is a platinum-basedantineoplastic agent that is under investigation as one treatment ofpatients with advanced prostate cancer who have failed previouschemotherapy.

Bioactivity: SJG-136 is a novel rationally designed DNA minor groove interstrandcross-linking agent with potent and broad spectrum antitumoractivity

Bioactivity: Streptozocin is a potent agent, with valuesDNA-methylating IC50of 11.7, 904 and 1024 μg/mL for HL60, K562 and C1498 cellsrespectively.

Bioactivity: Temozolomide is a agent. Temozolomide is anDNA-methylatingalkylating cytostatic drug.

Bioactivity: Thio-TEPA(Thioplex; Tiofosfamid) is an alkylating agent used to treatcancer, this molecule features tetrahedral phosphorus and isstructurally akin to phosphate

Bioactivity: Treosulfan is an alkylating agent used for conventional, as well ashigh-dose chemotherapy regimens, whereby plasma concentrationsover 500 μg/ml can be achieved

Bioactivity: Uramustine is an antineoplastic agent with of 5 Bioactivity: VAL-083 is a bi-functional alkylating agent; inhibit U251 and SF188cell growth in monolayer better than TMZ and caused apoptosis


Procarbazine HydrochlorideCat. No.: HY-13733

RITA(NSC 652287; NSC-652287; NSC652287) 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; TZM) Cat. No.: HY-17364

Thio-TEPACat. No.: HY-17574

Treosulfan(Treosulphan) Cat. No.: HY-16503

Uramustine(Uracil mustard) Cat. No.: HY-13544

VAL-083 (Dianhydrodulcitol; Dianhydrogalactitol; VAL083; VAL 0

83) Cat. No.: HY-16513

http://www.medchemexpress.com/Procarbazine-Hydrochloride.html

http://www.medchemexpress.com/rita.html

http://www.medchemexpress.com/Satraplatin.html

http://www.medchemexpress.com/SJG-136.html

http://www.medchemexpress.com/Streptozocin.html

http://www.medchemexpress.com/Temozolomide.html

http://www.medchemexpress.com/Thio-TEPA.html

http://www.medchemexpress.com/Treosulfan.html

http://www.medchemexpress.com/Uramustine.html

http://www.medchemexpress.com/val-083.html


DNA Stain

http://www.medchemexpress.com/Targets/DNA Stain.html


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg




50 mg, 100 mg

DNA Stain Inhibitors & Modulators

Bioactivity: DMA is a DNA dye Bioactivity: Dye 937, substituted unsymmetrical cyanine dyes with selectedpermeability, useful in the detection of DNA in electrophoretic gels.

Bioactivity: Dye 993, substituted unsymmetrical cyanine dyes with selectedpermeability, useful in the detection of DNA in electrophoretic gels.

Bioactivity: HOE 32020 is a Hoechst stain, which is a blue fluorescent dyes usedto stain DNA

Bioactivity: Hoechst stains are part of a family of blue fluorescent dyes used tostain DNA



Bioactivity: Hoechst 33258 is a fluorescent acid dye, used to stain DNA.

Bioactivity: Hoechst stains are part of a family of blue fluorescent dyes used tostain DNA.



DMACat. No.: HY-15621

Dye 937(Dye937; Dye-937) Cat. No.: HY-15422

Dye 993(Dye993; Dye-993) Cat. No.: HY-15423

HOE 32020(HOE32020; HOE-32020) Cat. No.: HY-15629



HOE-S 785026(meta-Hoechst) Cat. No.: HY-15561

Hoechst 33258 (bisBenzimide H 33258; H 33258; Hoechst33258; Hoechst-

33258) Cat. No.: HY-15558

Hoechst 33258 analogCat. No.: HY-15623

Hoechst 33258 analog 2Cat. No.: HY-15624

http://www.medchemexpress.com/Targets/DNA Stain.html

http://www.medchemexpress.com/dma.html

http://www.medchemexpress.com/dye-937.html

http://www.medchemexpress.com/dye-993.html

http://www.medchemexpress.com/HOE-32020.html

http://www.medchemexpress.com/hoe-32021.html

http://www.medchemexpress.com/hoe-33187.html

http://www.medchemexpress.com/HOE-S-785026.html

http://www.medchemexpress.com/Hoechst-33258.html

http://www.medchemexpress.com/Hoechst-33258-analog.html

http://www.medchemexpress.com/hoechst-33258-analog-2.html



50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Purity: 99.79%Clinical Data:Size: 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg



10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


Bioactivity: Hoechst 33258 analog 5 is a analog of Hoechst stains, which are partof a family of blue fluorescent dyes used to stain DNA

Bioactivity: Hoechst 33258 analog 6 is a anglog of Hoechst stains(Hoechst33258), which are part of a family of blue fluorescent dyes used tostain DNA


Bioactivity: Hoechst 33342 analog is a nalog of Hoechst stains, which are part ofa family of blue fluorescent dyes used to stain DNA

Bioactivity: Hoechst 33342 analog 2 is a anglog of Hoechst stains, which are partof a family of blue fluorescent dyes used to stain DNA

Bioactivity: Hoechst 33342 trihydrochloride is an AT-specific DNA minor grooveligand used fluorochrome for visualizing cellular .DNA



Bioactivity: Methylproamine is a DNA-binding radioprotector which, on the basisof published pulse radiolysis studies, acts by repair of transientradiation-induced oxidative species on DNA.




Hoechst 33342 (bisBenzimide H 33342; HOE 33342; Hoechst-33342; Hoech

st33342) Cat. No.: HY-15559

Hoechst 33342 analogCat. No.: HY-15627


Hoechst 33342 trihydrochloride (bisBenzimide H 33342 trihy

drochloride; HOE 33342 trihydrochloride; Hoechst…) Cat. No.: HY-15559A

Hoechst 34580(HOE 34580; Proamine; Hoechst-34580; Hoechst34580) Cat. No.: HY-15560

meta-iodoHoechst 33258(iodoHoechst 33258) Cat. No.: HY-15622

MethylproamineCat. No.: HY-15620


http://www.medchemexpress.com/Hoechst-33258-analog-5.html


http://www.medchemexpress.com/hoechst-33342.html

http://www.medchemexpress.com/hoechst-33342-analog.html

http://www.medchemexpress.com/Hoechst-33342-analog-2.html

http://www.medchemexpress.com/Hoechst-33342-trihydrochloride.html

http://www.medchemexpress.com/Hoechst-34580.html

http://www.medchemexpress.com/meta-iodohoechst-33258.html

http://www.medchemexpress.com/Methylproamine.html


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: Nuclear yellow (Hoechst S769121) exhibits excitation/emissionmaxima ~335/495 nm when bound to DNA




Nuclear yellowCat. No.: HY-15619

ortho-iodoHoechst 33258(iodoHoechst 33258) Cat. No.: HY-15626

para-iodoHoechst 33258(iodoHoechst 33258) Cat. No.: HY-15632

http://www.medchemexpress.com/Nuclear-yellow.html

http://www.medchemexpress.com/ortho-iodohoechst-33258.html

http://www.medchemexpress.com/para-iodoHoechst-33258.html


DNA-PK

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-dependentserine/threonine 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-PK.Autophosphorylation 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.

http://www.medchemexpress.com/Targets/DNA-PK.html


5 mg, 10 mg, 25 mg


10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

DNA-PK Inhibitors & Modulators

Bioactivity: CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM). Bioactivity: CC-115 hydrochloride is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13nM).

Bioactivity: Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM)that also targets mTOR but not PI3K.

Bioactivity: KU-57788 is a potent and selective inhibitor of , a modestDNA-PKinhibitor of and , with s of 13 nM, 1 μM and 3.5 μM,BRD4 BRDT IC50respectively, and also increases -mediated editingCRISPR/Cas9frequencies.

Bioactivity: LY3023414 is an oral ATP competitive inhibitor of the class I PI3Kisoforms, mTOR and DNA-PK, extracted from patentWO/2012097039A1, compound example 1, has an IC50 of 64

Bioactivity: NU 7026 is a novel specific inhibitor with of 0.23±0.01DNA-PK IC50μM, also inhibits with of 13±3 μM.PI3K IC50

Bioactivity: PIK-75 is a p110α inhibitor with IC50 of 5.8 nM (200-fold morepotently than p110β), isoform-specific mutants at Ser773, and alsopotently inhibits DNA-PK with IC50 of 2 nM.

Bioactivity: Wortmannin is a multi-target inhibitor of and with sPI3K MLCK IC50of 3 nM and 170 nM, respectively.


CC-115Cat. No.: HY-16962

CC-115 hydrochlorideCat. No.: HY-16962A

Compound 401(Compound-401; Compound401) Cat. No.: HY-19341

KU-57788(KU 57788; NU-7441; KU57788; NU7441; NU 7441) Cat. No.: HY-11006

LY3023414(LY-3023414; LY 3023414) Cat. No.: HY-12513

NU 7026(LY293646; NU7026; NU-7026; LY 293646; LY-293646) Cat. No.: HY-15719

PIK-75(PIK-75 Hydrochloride; PIK 75) Cat. No.: HY-13281

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

http://www.medchemexpress.com/Targets/DNA-PK.html

http://www.medchemexpress.com/CC-115.html

http://www.medchemexpress.com/CC-115-hydrochloride.html

http://www.medchemexpress.com/Compound-401.html



http://www.medchemexpress.com/NU-7026.html

http://www.medchemexpress.com/pik-75.html

http://www.medchemexpress.com/Wortmannin.html


DNA/RNA 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 maturation,surveillance and export to the cytoplasm.Single-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 theDNA.DNA 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-4′ 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 DNA.First 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 exonuclease/polymerase activity. After adenylation of the 3′ 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.

http://www.medchemexpress.com/Targets/DNA_RNA Synthesis.html


1 mg, 5 mg, 10 mg, 50 mg, 100 mg



1 g, 5 g


10 mg, 50 mg

Purity: >98.0%Clinical Data: Phase 2, Phase 3Size: 10 mg, 50 mg


250 mg, 1 g

Purity: 95.14%Clinical Data:Size: 1 mg, 5 mg

Purity: 99.2%Clinical Data:Size: 1 g, 5 g


5 mg, 10 mg, 50 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg

DNA/RNA Synthesis Inhibitors & Modulators

Bioactivity: Acelarin (NUC-1031) is a ProTide transformation and enhancement ofthe widely-used nucleoside analogue, gemcitabine.

Bioactivity: Actinomycin D inhibits with of 0.42 μM.DNA repair IC50

Bioactivity: Adenine is a purine derivative and a nucleobase with a variety ofroles in biochemistry.

Bioactivity: alpha-Amanitin is the principal toxin of several deadly poisonousmushrooms, exerting its toxic function by inhibiting

.RNA-polymerase II

Bioactivity: Beaucage reagent is found to be potent in causing DNA cleavage. Bioactivity: Bleomycin sulfate is a potent agent, as theDNA damagingbest-studied (MN) inducer. Bleomycin also is a naturalmicronucleusantibiotic, toxic to dividing cells (G /M-phase), also proven effective2in squamous cell carcinomas (SCC).

Bioactivity: BMH-21 is a small molecule DNA intercalator that binds ribosomalDNA and inhibits RNA polymerase I (Pol I) transcription; does notcause phosphorylation of H2AX.

Bioactivity: Capecitabine is an oral prodrug that is converted to its only activemetabolite, fluorouracil (FU), by thymidine phosphorylase.

Bioactivity: Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNAgyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+K+-ATPase activity.

Bioactivity: COH29 is a potent ribonucleotide reductase ( ) inhibitor withRNRanticancer activity with an of 8 μM in KB cell.IC50


Acelarin(NUC-1031; NUC1031; 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

Beaucage reagentCat. No.: HY-100951

Bleomycin sulfateCat. No.: HY-17565

BMH-21Cat. No.: HY-12484

CapecitabineCat. No.: HY-B0016

Chebulinic acidCat. No.: HY-N2033

COH29(COH-29; COH 29) Cat. No.: HY-19931

http://www.medchemexpress.com/Targets/DNA_RNA Synthesis.html

http://www.medchemexpress.com/Acelarin.html

http://www.medchemexpress.com/Actinomycin-D.html

http://www.medchemexpress.com/Adenine.html

http://www.medchemexpress.com/alpha-Amanitin.html

http://www.medchemexpress.com/Beaucage-reagent.html

http://www.medchemexpress.com/Bleomycin-sulfate.html

http://www.medchemexpress.com/BMH-21.html

http://www.medchemexpress.com/Capecitabine.html

http://www.medchemexpress.com/Chebulinic-acid.html

http://www.medchemexpress.com/COH29.html



5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg


1 g, 5 g


5 g


100 mg, 200 mg, 500 mg, 1 g


100 mg, 200 mg, 500 mg, 1 g

Purity: >98%Clinical Data:Size: 10mM x 1mL in Water,

10 mg, 50 mg


200 mg, 500 mg, 1 g, 5 g

Purity: 98.47%Clinical Data:Size: 5 mg, 10 mg, 50 mg

Bioactivity: CX-5461 is an inhibitor of , and selectively inhibitsrRNA synthesisPol I-driven transcription of rRNA with of 142 nM in HCT-116,IC50A375, and MIA PaCa-2 cells, with no effect on Pol II, and possesses250- to 300-fold selectivity for inhibition of rRNA transcription versusDNA replication and protein …

Bioactivity: Cycloheximide is an inhibitor of protein biosynthesis in eukaryoticorganisms, with of 532.5 nM and 2880 nM for IC50 protein synthesis

and in vivo, respectively.RNA synthesis

Bioactivity: Deoxycytidine triphosphate (dCTP), a nucleoside triphosphate, is araw material in DNA synthesis. Deoxycytidine triphosphate has manyapplications, such as real-time PCR, cDNA synthesis, and DNAsequencing.

Bioactivity: Gemcitabine is a inhibitor with of 37.6, 42.9,DNA synthesis IC5092.7, 89.3 and 131.4 nM in BxPC-3, Mia Paca-2, PANC-1, PL-45 andAsPC-1 cells, respectively.

Bioactivity: Gemcitabine hydrochloride is a inhibitor with ofDNA synthesis IC5037.6, 42.9, 92.7, 89.3 and 131.4 nM in BxPC-3, Mia Paca-2, PANC-1,PL-45 and AsPC-1 cells, respectively.

Bioactivity: Guanine is one of the fundamental components of nucleic acids ( and ). Guanine is a purine derivative, consisting of a fusedDNA RNA

pyrimidine-imidazole ring system with conjugated double bonds.

Bioactivity: Hydroxyurea is a cell apoptosis inducer that inhibit synthesisDNAthrough inhibition of ribonucleotide reductase.

Bioactivity: L189 is a novel human DNA ligase inhibitor, inhibits hLigI/III/IV withIC50 of 5/9/5 μM.

Bioactivity: L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNAligases I and III with IC50 of 10 μM and 10 μM.

Bioactivity: LMI070 (NVS-SM1) is a highly potent, selective and orally active smallmolecule SMN2 splicing modulator.

CX-5461(CX 5461; CX5461) Cat. No.: HY-13323

Cycloheximide(Naramycin A; Actidione) Cat. No.: HY-12320

Deoxycytidine triphosphate(dCTP) Cat. No.: HY-101400

Gemcitabine(LY 188011; NSC 613327; LY188011; LY-188011) Cat. No.: HY-17026

Gemcitabine Hydrochloride(LY 188011 hydrochloride) Cat. No.: HY-B0003

GuanineCat. No.: HY-Y1055

Hydroxyurea(Hydroxycarbamide) Cat. No.: HY-B0313

L189(L-189) Cat. No.: HY-15588

L67(DNA Ligase Inhibitor; L-67; L 67) Cat. No.: HY-15586

LMI070(NVS-SM1; LMI-070; LMI 070) Cat. No.: HY-19620

http://www.medchemexpress.com/cx-5461.html

http://www.medchemexpress.com/Cycloheximide.html

http://www.medchemexpress.com/Deoxycytidine_triphosphate.html

http://www.medchemexpress.com/Gemcitabine.html

http://www.medchemexpress.com/Gemcitabine-Hydrochloride.html

http://www.medchemexpress.com/Guanine.html

http://www.medchemexpress.com/hydroxyurea.html

http://www.medchemexpress.com/L189.html

http://www.medchemexpress.com/L67.html

http://www.medchemexpress.com/LMI070.html



5 mg, 25 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg


100 mg, 500 mg


5 mg, 10 mg, 50 mg

Purity: 97.08%Clinical Data:Size: 1 g

Purity: >98.0%Clinical Data:Size: 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg

Bioactivity: ML216(CID-49852229) is a potent inhibitor of the DNA unwindingactivity of BLM helicase; showing similar IC50s of 3.0 and 0.97 μM forfull length BLM and BLM636–1298 respectively.

Bioactivity: N2-Methylguanine is a modified nucleoside. N2-Methylguanine is anendogenous methylated nucleoside found in human fluids.

Bioactivity: Nedaplatin is a derivative of cisplatin and DNA damage agent. Bioactivity: Oxolinic acid is a potent inhibitor of DNA gyrase and DNA synthesis,lead to DNA cleavage when extracted chromosomes are incubatedwith sodium dodecyl sulfate.

Bioactivity: SCR7 is a inhibitor, blocks nonhomologousDNA Ligase IVend-joining (NHEJ). SCR7 increases -mediated editingCRISPR/Cas9frequency.

Bioactivity: Streptozocin is a potent agent, with valuesDNA-methylating IC50of 11.7, 904 and 1024 μg/mL for HL60, K562 and C1498 cellsrespectively.

Bioactivity: TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, andNUDT16.

Bioactivity: TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) with anIC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12,NUDT14, and NUDT16.

Bioactivity: TH588 is first-in-class nudix hydrolase family inhibitor that potentlyand selectively engage and inhibit the MTH1(IC50= 5 nM) in cells.

Bioactivity: TH588 hydrochloride is first-in-class nudix hydrolase family inhibitorthat potently and selectively engage and inhibit the MTH1(IC50= 5nM) in cells.


ML216 (ML 216; ML-216; CID-49852229; CID49852229; CID 498522

29) Cat. No.: HY-12342

N2-MethylguanineCat. No.: HY-101412

NedaplatinCat. No.: HY-13700

Oxolinic acidCat. No.: HY-B1002

SCR7(SCR-7) Cat. No.: HY-12742

Streptozocin(Streptozotocin; U 9889) Cat. No.: HY-13753

TH287(TH-287) Cat. No.: HY-16965

TH287 hydrochloride(TH-287 hydrochloride) Cat. No.: HY-16965A

TH588(TH-588) Cat. No.: HY-12814

TH588 hydrochloride(TH-588 hydrochloride) Cat. No.: HY-12814A


http://www.medchemexpress.com/N2-Methylguanine.html

http://www.medchemexpress.com/Nedaplatin.html

http://www.medchemexpress.com/Oxolinic-acid.html

http://www.medchemexpress.com/SCR7.html

http://www.medchemexpress.com/Streptozocin.html

http://www.medchemexpress.com/TH287.html

http://www.medchemexpress.com/TH287-hydrochloride.html

http://www.medchemexpress.com/TH588.html

http://www.medchemexpress.com/TH588-hydrochloride.html



10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg

Bioactivity: Triapine is a novel inhibitor of the M2 subunit of ribonucleotide ( ), and is a potent radiosensitizer.reductase RR

Bioactivity: Triciribine is a inhibitor, also inhibits and DNA synthesis Akt with of 130 nM, and 0.02-0.46 μM, respectively.HIV-1/2 IC50

Bioactivity: YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding to theoncogenic transciption factor EWS-FLI1. YK-4-279 inhibits Ewing'ssarcoma family tumor (ESFT) cell growth; YK-4-279 inducesapoptosis.

Triapine(3-AP; PAN-811; OCX191; NSC663249) Cat. No.: HY-10082

Triciribine(API-2; NSC 154020; TCN) Cat. No.: HY-15457

YK-4-279(YK 4-279) Cat. No.: HY-14507

http://www.medchemexpress.com/Triapine.html

http://www.medchemexpress.com/Triciribine.html

http://www.medchemexpress.com/YK-4-279.html

Eukaryotic Initiation Factor (eIF)


http://www.medchemexpress.com/Targets/Eukaryotic Initiation Factor (eIF).html



2 mg, 5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 50 mg

Eukaryotic Initiation Factor (eIF) Inhibitors & Modulators

Bioactivity: 4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1interaction, and inhibits the binding of eIF4G to eIF4E with IC50 of 3.2μM.

Bioactivity: SBI-0640756SBI-756 is a first-in-class inhibitor that targets eIF4G1and disrupts the eIF4F complex. SBI-756 also suppressed AKT andNF-κB signaling.

4E1RCatCat. No.: HY-14427

SBI-0640756(SBI0640756; SBI 0640756) Cat. No.: HY-19560

http://www.medchemexpress.com/Targets/Eukaryotic Initiation Factor (eIF).html

http://www.medchemexpress.com/4E1RCat.html

http://www.medchemexpress.com/SBI-0640756.html

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 tetrads.They 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.


http://www.medchemexpress.com/Targets/G-quadruplex.html


Purity: >98.0%Clinical Data:Size: 10mM x 1mL in Water,

5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg


G-quadruplex Inhibitors & Modulators

Bioactivity: 360A is a strong affinity and selectivity inhibitor of G-quadruplexstructures.

Bioactivity: 360A is a strong affinity and selectivity inhibitor of G-quadruplexstructures.

Bioactivity: Pyridostatin(RR-82) is a G-quadruplex-interacting drug which canpromote growth arrest in human cancer cells by inducing replication-and transcription-dependent DNA damage.

Bioactivity: Pyridostatin(RR-82) Hcl is a G-quadruplex-interacting drug which canpromote growth arrest in human cancer cells by inducing replication-and transcription-dependent DNA damage.

360A(360 A) Cat. No.: HY-15595

360A iodide(360 A iodide) Cat. No.: HY-15595A

Pyridostatin(RR-82; RR82; RR 82) Cat. No.: HY-15176

Pyridostatin hydrochloride(RR-82 hydrochloride) Cat. No.: HY-15176A

http://www.medchemexpress.com/Targets/G-quadruplex.html

http://www.medchemexpress.com/360a.html

http://www.medchemexpress.com/360a-iodide.html

http://www.medchemexpress.com/Pyridostatin.html

http://www.medchemexpress.com/Pyridostatin-hydrochloride.html

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 cells.Haspin 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.


http://www.medchemexpress.com/Targets/Haspin Kinase.html



5 mg, 10 mg, 50 mg, 100 mg

Haspin Kinase Inhibitors & Modulators

Bioactivity: CHR-6494 is a potent and selective Haspin (Haploid GermCell-Specific Nuclear Protein Kinase) inhibitor that blocks H3T3phphosphorylation.

CHR-6494(CHR 6494; CHR6494) Cat. No.: HY-15217

http://www.medchemexpress.com/Targets/Haspin Kinase.html

http://www.medchemexpress.com/CHR-6494.html

HDAC

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 proteins.Together with the acetylpolyamine amidohydrolases and the acetoinutilization proteins, the histone deacetylases form an ancient proteinsuperfamily known as the histone deacetylase superfamily.


http://www.medchemexpress.com/Targets/HDAC.html



2 mg, 5 mg, 10 mg, 50 mg


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


5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

HDAC Inhibitors & Modulators

Bioactivity: 4SC-202 is an orally available potent HDACi specific for class I HDACisoenzymes(NO HDAC8) with IC50s of 1

Bioactivity: 4SC-202 (free base) is a selective class I inhibitor with ofHDAC IC501.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3,respectively. It also displays inhibitory activity against Lysine specific

.demethylase 1 (LSD1)

Bioactivity: ACY-1215 is a potent and selective inhibitor, with anHDAC6enzymatic value of 5 nM. ACY-1215 also inhibits , IC50 HDAC1

, and with of 58, 48, and 51 nM, respectively.HDAC2 HDAC3 IC50

Bioactivity: ACY-738 demonstrates inhibitory activity against recombinantHDAC6 with IC50 values of 1.7 nM, with respective average selectivityover class I HDACs being 100-fold.

Bioactivity: Belinostat is a potent inhibitor with an of 27 nM in HeLaHDAC IC50cell extracts.

Bioactivity: BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 =289 nM). It inhibits HDAC1, HDAC2, and HDAC6 with greatly reducedpotency (IC50s = 2, 2.2, and >20 μM, respectively).

Bioactivity: BML-210 is the novel HDAC inhibitor, and its mechanism of actionhas not been characterized.

Bioactivity: BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36nM and 120 nM for HDAC6 and HDAC8, respectively.

Bioactivity: CAY10603 is a potent and selective inhibitor of HDAC6 with IC50 of 2pM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1,2, 3, 8, and 10, respectively.

Bioactivity: Chidamide is a synthetic benzamide-type which mainly actsHDACias a class I HDACi (inhibiting , , and with of 95, 160,HDAC1 2 3 8 IC5067 and 733 nM, respectively).

4SC-202(4SC 202; 4SC202) Cat. No.: HY-16012

4SC-202 free base(4SC 202 free base; 4SC202 free base) Cat. No.: HY-16012A

ACY-1215(Ricolinostat; Rocilinostat; ACY1215; ACY 1215) Cat. No.: HY-16026

ACY-738Cat. No.: HY-19327

Belinostat(PXD101; PX105684; PXD-101; PXD 101; PX-105684) Cat. No.: HY-10225

BG45(BG-45) Cat. No.: HY-18712

BML-210(BML210; BML 210) Cat. No.: HY-19350

BRD73954(BRD-73954) Cat. No.: HY-18700

CAY10603(CAY-10603) Cat. No.: HY-18613

Chidamide(CS055; HBI-8000) Cat. No.: HY-13592

http://www.medchemexpress.com/Targets/HDAC.html

http://www.medchemexpress.com/4SC-202.html

http://www.medchemexpress.com/4SC-202-free-base.html

http://www.medchemexpress.com/ACY-1215.html

http://www.medchemexpress.com/ACY-738.html

http://www.medchemexpress.com/Belinostat.html

http://www.medchemexpress.com/BG45.html

http://www.medchemexpress.com/BML-210.html

http://www.medchemexpress.com/BRD73954.html

http://www.medchemexpress.com/CAY10603.html

http://www.medchemexpress.com/Chidamide.html


10 mg, 50 mg




10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg


2 mg, 5 mg, 10 mg, 50 mg


10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


10 mg, 50 mg, 100 mg

Bioactivity: CI-994 (Tacedinaline) is an inhibitor of the histone deacetylase () with an of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2HDAC IC50

and 3 respectively.

Bioactivity: Citarinostat is a HDAC6 specific inhibitor, with IC50 of 4 nM and 76nM for HDAC6 and HDAC3, respectively.

Bioactivity: CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitorwith IC50 of 4.4, 2.4, and 15.7 nM, respectively.

Bioactivity: CUDC-907 potently inhibits class I s as well as classes I and II PI3K enzymes with of 1.7/5.0/1.8/2.8 nM and 19/54/39 nM forHDAC IC50

HDAC1/2/3/10 and PI3Kα/β/δ, respectively.

Bioactivity: Dacinostat (NVP-LAQ824, LAQ824) is a highly potent HDAC inhibitorwith IC50 of 32 nM

Bioactivity: Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, andHDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; > 8-foldselective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and10.

Bioactivity: Entinostat is the class I-selective inhibitor, with of 243HDAC IC50nM, 453 nM, and 248 nM for , , and .HDAC1 HDAC2 HDAC3

Bioactivity: Givinostat (ITF-2357) is a potent HDAC inhibitor for Maize HD2,HD1-B and HD1-A with IC50 of 10 nM, 7.5 nM and 16nM,respectively.

Bioactivity: Givinostat (ITF-2357) hydrochloride is a potent HDAC inhibitor forMaize HD2, HD1-B and HD1-A with IC50 of 10 nM, 7.5 nM and 16nM, respectively.

Bioactivity: HDAC-IN-1 is a chemical analog of MC 1568, which is a potent andselective class IIa HDACs inhibitor


CI-994 (Acetyldinaline; Tacedinaline; PD 123654; Goe 5549; CI

994; CI994) Cat. No.: HY-50934

CitarinostatCat. No.: HY-15994

CUDC-101(CUDC101; CUDC 101) Cat. No.: HY-10223

CUDC-907(CUDC907; CUDC 907) Cat. No.: HY-13522

Dacinostat(NVP-LAQ824; LAQ824; LAQ 824; LAQ-824) Cat. No.: HY-13606

Droxinostat(NS 41080; NS-41080; NS41080) Cat. No.: HY-13267

Entinostat(MS-275; SNDX-275; MS 275; SNDX 275) Cat. No.: HY-12163

Givinostat(Gavinostat; ITF-2357) Cat. No.: HY-14842

Givinostat hydrochloride(Gavinostat hydrochloride; ITF-2357 hydrochloride) Cat. No.: HY-14842A

HDAC-IN-1Cat. No.: HY-15140

http://www.medchemexpress.com/CI-994.html

http://www.medchemexpress.com/Citarinostat.html

http://www.medchemexpress.com/CUDC-101.html

http://www.medchemexpress.com/CUDC-907.html

http://www.medchemexpress.com/Dacinostat.html

http://www.medchemexpress.com/Droxinostat.html

http://www.medchemexpress.com/Entinostat.html

http://www.medchemexpress.com/Givinostat.html

http://www.medchemexpress.com/Givinostat-hydrochloride.html

http://www.medchemexpress.com/HDAC-IN-1.html



5 mg, 10 mg, 25 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor, extracted frompatent WO/2008040934 A1.

Bioactivity: HDAC-IN-4 is a histone deacetylase (HDAC) inhibitor, extracted frompatent WO/2007045844 A1 20070426.

Bioactivity: HPOB is a highly potent and selective inhibitor of histone deacetylase6 (HDAC6) with IC50 of 56 nM, >30 fold less potent against otherHDACs.

Bioactivity: ITSA-1 is membrane permeable and specifically suppresses TSAinhibition of HDAC (histone deacetylase), but not other HDACinhibitors.

Bioactivity: LMK235 is a HDAC inhibitor, previously shown to be a novel andspecific inhibitor of human HDAC4 and 5, with IC50 values of 0.49μM (A2780) and 0.32 μM (A2780 CisR).

Bioactivity: M344 is an inhibitor of ( =100 nM) and anhistone deacetylase IC50inducer of terminal cell fifferentiation.

Bioactivity: MC1568 is a selective class II (IIa) histone deacetylas ( )HDAC IIinhibitor with an of 220 nM.IC50

Bioactivity: Mocetinostat is a potent isotype-selective inhibitor with HDAC IC50of 0.15, 0.29, 1.66 and 0.59 μM for , , and HDAC1 HDAC2 HDAC3

, respectively.HDAC11

Bioactivity: Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of5 nM; no inhibition on other HDAC forms.

Bioactivity: NKL 22 is a HDAC inhibitor. The value of IC 50 is 78 uM.

HDAC-IN-3 (Cyclohexaneacetic acid, α-[[[6-[3-(hydroxyamino)-3-ox

opropyl]-3-pyridinyl]methyl]amino]-, cyclopentyl…) Cat. No.: HY-19772

HDAC-IN-4Cat. No.: HY-100748

HPOBCat. No.: HY-19747

ITSA-1(ITSA1; ITSA 1) Cat. No.: HY-100508

LMK-235(LMK 235; LMK 235) Cat. No.: HY-18998

M344(M 344; M-344; D 237; MS 344) Cat. No.: HY-13506

MC1568(MC-1568) Cat. No.: HY-16914

Mocetinostat(MGCD0103; MGCD 0103; MGCD-0103) Cat. No.: HY-12164

Nexturastat ACat. No.: HY-16699

NKL 22(NKL22; NKL-22) Cat. No.: HY-100384



http://www.medchemexpress.com/HPOB.html

http://www.medchemexpress.com/ITSA-1.html

http://www.medchemexpress.com/LMK-235.html

http://www.medchemexpress.com/M344.html

http://www.medchemexpress.com/MC1568.html

http://www.medchemexpress.com/Mocetinostat.html

http://www.medchemexpress.com/Nexturastat-A.html

http://www.medchemexpress.com/NKL-22.html



5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


50 mg, 100 mg, 200 mg


10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Bioactivity: Panobinostat is a novel histone deacetylase ( ) inhibitor with aHDACmulti-targeted profile.

Bioactivity: Parthenolide is an inhibitor, reduces histone deacetylase 1NF-κB(HDAC-1) and DNA methyltransferase 1 independent of NF-κBinhibition.

Bioactivity: PCI-24781 (Abexinostat; CRA 24781) is a novel pan- inhibitorHDACmostly targeting HDAC1 with of 7 nM.Ki

Bioactivity: PCI-34051 is a potent and selective inhibitor with of 10HDAC8 IC50nM, with >200-fold selectivity over the other HDAC isoforms.

Bioactivity: Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class IHDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and370 nM, respectively), demonstrating no activity against class IIHDACs.

Bioactivity: Pimelic Diphenylamide 106 analog is an analog of PimelicDiphenylamide 106 with unknown biological activity.

Bioactivity: Pracinostat(SB939) is a potent pan-HDAC inhibitor with IC50 of40-140 nM with exception for HDAC6; has no activity against theclass III isoenzyme SIRT I

Bioactivity: PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDAC.PTACH exerts potent growth inhibition against various human cancercells, with EC50 values ranging from 1 to 10 μM.

Bioactivity: Quisinostat (JNJ-26481585) is an orally available, potent HDACinhibitor with values of 0.11 nM for HDAC1.IC50

Bioactivity: Remodelin is a novel potent and selective inhibitor of theacetyl-transferase protein NAT10.


Panobinostat(LBH-589; LBH589; NVP-LBH589) Cat. No.: HY-10224

Parthenolide((-)-Parthenolide) Cat. No.: HY-N0141

PCI-24781(CRA 024781; CRA 24781; PCI 24781; Abexinostat) Cat. No.: HY-10990

PCI-34051(PCI 34051; PCI34051) Cat. No.: HY-15224

Pimelic Diphenylamide 106 (RGFA-8; TC-H 106; Histone

Deacetylase Inhibitor VII) Cat. No.: HY-19348

Pimelic Diphenylamide 106 analog(RGFA-8 analog; TC-H 106 analog) Cat. No.: HY-19430

Pracinostat(SB939; SB-939; SB 939) Cat. No.: HY-13322

PTACH(NCH-51) Cat. No.: HY-12954

Quisinostat(JNJ-26481585) Cat. No.: HY-15433

RemodelinCat. No.: HY-16706

http://www.medchemexpress.com/Panobinostat.html

http://www.medchemexpress.com/Parthenolide.html

http://www.medchemexpress.com/PCI-24781.html

http://www.medchemexpress.com/PCI-34051.html

http://www.medchemexpress.com/Pimelic-Diphenylamide-106.html

http://www.medchemexpress.com/Pimelic-Diphenylamide-106-analog.html

http://www.medchemexpress.com/pracinostat.html

http://www.medchemexpress.com/PTACH.html

http://www.medchemexpress.com/Quisinostat.html

http://www.medchemexpress.com/Remodelin.html



100 mg, 200 mg


1 g, 5 g


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg


1 mg, 5 mg, 10 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: Phase 2Size: 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg

Bioactivity: Remodelin HBr salt is a novel potent and selective inhibitor of theacetyl-transferase protein NAT10.

Bioactivity: Resminostat(RAS2410; 4SC-201) is a potent inhibitor ofHDAC1/3/6(IC50=43-72 nM); less potent to HDAC8 with IC50 of 877nM.

Bioactivity: Resminostat Hcl(RAS2410; 4SC-201) is a potent inhibitor ofHDAC1/3/6(IC50=43-72 nM); less potent to HDAC8 with IC50 of 877nM.

Bioactivity: RG2833 is a brain-penetrant inhibitor with of 60 nM andHDAC IC5050 nM for HDAC1 and HDAC3, respectively.

Bioactivity: RGFP966 is a selective inhibitor with an of 80 nM andHDAC3 IC50no effective inhibition of any other HDAC at concentrations up to 15μM.

Bioactivity: Romidepsin is a potent and inhibitor with of 36HDAC1 HDAC2 IC50nM and 47 nM, respectively.

Bioactivity: Scriptaid(Scriptide; GCK-1026) is an inhibitor of HDAC; shows agreater effect on acetylated H4 than H3

Bioactivity: Sirtinol is a inhibitor; inhibit the growth of MCF-7 cells with ansirtuin of 48.6 μM at 24 h.IC50

Bioactivity: Sodium Butyrate is a inhibitor, hashistone deacetylase (HDAC)anti-tumor effects in several cancers.

Bioactivity: Sodium 4-phenylbutyrate(TriButyrate), a Histone deacetylaseinhibitor, is terminal aromatic substituted fatty acid that has beenused for the treatment of urea cycle disorders.

Remodelin hydrobromideCat. No.: HY-16706A

Resminostat(RAS2410; 4SC-201; RAS 2410; RAS-2410) Cat. No.: HY-14718

Resminostat hydrochloride (RAS2410 hydrochloride; 4SC

-201 hydrochloride; RAS 2410 hydrochloride; RAS-…) Cat. No.: HY-14718A

RG2833(RG 2833; RG-2833; RGFP-109; RGFP109; RGFP 109) Cat. No.: HY-16425

RGFP966(RGFP 966; RGFP-966) Cat. No.: HY-13909

Romidepsin(FK 228; FR 901228; NSC 630176) Cat. No.: HY-15149

Scriptaid(GCK 1026; Scriptide; GCK1026; GCK-1026) Cat. No.: HY-15489

SirtinolCat. No.: HY-13515

Sodium Butyrate(Butanoic acid sodium salt) Cat. No.: HY-B0350A

Sodium phenylbutyrate(Sodium 4-phenylbutyrate; TriButyrate) Cat. No.: HY-15654

http://www.medchemexpress.com/Remodelin-hydrobromide.html

http://www.medchemexpress.com/resminostat.html

http://www.medchemexpress.com/Resminostat-hydrochloride.html

http://www.medchemexpress.com/rg2833.html

http://www.medchemexpress.com/RGFP966.html

http://www.medchemexpress.com/Romidepsin.html

http://www.medchemexpress.com/Scriptaid.html

http://www.medchemexpress.com/Sirtinol.html

http://www.medchemexpress.com/Sodium-Butyrate.html

http://www.medchemexpress.com/Sodium-phenylbutyrate.html


250 mg, 500 mg, 1 g, 5 g


1 g, 5 g

Purity: >98%Clinical Data:Size: 1 g, 5 g


10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


1 mg, 5 mg, 10 mg, 20 mg


2 mg, 5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: Tasquinimod is an allosteric modulator of with of 0.5HDAC4 IC50μM in 3D-HUVEC sprouting assay.

Bioactivity: TMP269 is a novel and selective class IIa histone deacetylase inhibitor with s of 126/80/36/9 nM for HDAC 4/5/7/9,(HDAC) IC50

respectively, and 20-400 fold selectivity over class1 HDACs.

Bioactivity: Trichostatin A is a potent and specific inhibitor of histone deacetylase( ) activity with value of 1.8 nM.HDAC IC50

Bioactivity: Tubacin is a histone deacetylase 6 (HDAC6) inhibitor, blockssphingolipid synthesis.

Bioactivity: Tubastatin A (Hydrochloride) is a potent and selective HDAC6 inhibitor with of 15 nM in a cell-free assay, and is selectiveIC50(1000-fold more) against all other isozymes except HDAC8 (57-foldmore).

Bioactivity: Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of15 nM; is selective (1000-fold more) against all other isozymes exceptHDAC8 (57-fold more)

Bioactivity: UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM,0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively. Ithas > 6-fold selectivity over other HDACs.

Bioactivity: Valproic acid, a histone deacetylase (HDAC) inhibitor (IC50=10 uM inHela cell, 24h) has an anticancer effect

Bioactivity: Valproic acid (sodium salt) is an inhibitor by selectivelyHDACinducing proteasomal degradation of HDAC2, used in the treatmentof epilepsy, bipolar disorder and prevention of migraine headaches.

Bioactivity: Vorinostat is an inhibitor of with values of 10 nM andHDAC1/3 IC5020 nM, respectively.


Tasquinimod(ABR-215050; ABR215050; ABR 215050) Cat. No.: HY-10528

TMP269(TMP 269; TMP-269) Cat. No.: HY-18360

Trichostatin A(TSA) Cat. No.: HY-15144

TubacinCat. No.: HY-13428

Tubastatin A Hydrochloride(Tubastatin A HCl; TSA HCl) Cat. No.: HY-13271

Tubastatin-A(Tubastatin A) Cat. No.: HY-13271A

UF010(UF-010; UF 010) Cat. No.: HY-18976

Valproic acid(VPA; 2-Propylpentanoic Acid) Cat. No.: HY-10585

Valproic acid sodium salt(Sodium Valproate) Cat. No.: HY-10585A

Vorinostat(SAHA) Cat. No.: HY-10221

http://www.medchemexpress.com/Tasquinimod.html

http://www.medchemexpress.com/TMP269.html

http://www.medchemexpress.com/Trichostatin-A.html

http://www.medchemexpress.com/Tubacin.html

http://www.medchemexpress.com/Tubastatin-A-Hydrochloride.html

http://www.medchemexpress.com/Tubastatin-A.html

http://www.medchemexpress.com/UF010.html

http://www.medchemexpress.com/valproic-acid.html

http://www.medchemexpress.com/Valproic-acid-sodium-salt.html

http://www.medchemexpress.com/Vorinostat.html


HSP

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, Hsp84,Hsp70, Hsp27, Hsp20 and alpha B crystallin all have been reported as

having roles in the cardiovasculature.

http://www.medchemexpress.com/Targets/HSP.html


5 mg, 10 mg


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


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


10 mg, 25 mg, 100 mg, 200 mg, 500 mg

Purity: >98%Clinical Data: Phase 1, Phase 2Size: 10 mg, 25 mg, 100 mg, 200 mg, 500 mg


10 mg, 25 mg, 100 mg, 200 mg


10 mg, 25 mg, 100 mg, 200 mg

HSP Inhibitors & Modulators

Bioactivity: 17-AAG is a potent inhibitor with of 5 nM, having aHSP90 IC50100-fold higher binding affinity for HSP90 derived from tumour cellsthan HSP90 from normal cells.

Bioactivity: 17-AAG Hcl is a potent HSP90 inhibitor with IC50 of 5 nM, having a100-fold higher binding affinity for HSP90 derived from tumour cellsthan HSP90 from normal cells

Bioactivity: Alvespimycin (17-DMAG; KOS-1022; NSC 707545) is a potent,water-soluble HSP90 inhibitor with IC50 of 62 nM.

Bioactivity: Alvespimycin hydrochloride is a potent inhibitor of , binding toHsp90Hsp90with of 62±29 nM.EC50

Bioactivity: Apoptozole is an inhibitor of heat shock protein 70 (Hsp70; 65%inhibition at 200 μM) that acts by blocking its ATPase activity.

Bioactivity: AT13387 is a selective potent Hsp90 inhibitor with IC50 of 18 nM inA375 cells, displays a long duration of anti-tumor activity

Bioactivity: BIIB021 is an orally available, fully synthetic inhibitor of with HSP90 K and of 1.7 nM and 38 nM, respectively.i EC50

Bioactivity: Debio 0932 ( CUDC-305 ) is a novel heat shock protein 90 (HSP90)inhibitor trong affinity for HSP90 alpha/beta, high oral bioavailabilityand potent anti-proliferative activity against a broad range of cancercell lines (with a mean IC50 of 220 nmol/L).

Bioactivity: Ganetespib is a unique non-geldanamycin heat shock protein 90 () inhibitor, with of 4 nM in OSA 8 cells.HSP90 IC50

Bioactivity: Geldanamycin is a specific inhibitor of interferon regulatory factor 3 () (by inhibiting of the IRF3 phosphorylation chaperone).IRF3 Hsp90


17-AAG (Tanespimycin; NSC 330507;

CP 127374; 17AAG; 17 AAG) Cat. No.: HY-10211

17-AAG Hydrochloride (Tanespimycin Hydrochloride; NSC 330507

Hydrochloride; CP 127374 Hydrochloride; 17AAG H…) Cat. No.: HY-10211A

Alvespimycin(17-DMAG; KOS-1022; NSC 707545) Cat. No.: HY-10389

Alvespimycin hydrochloride(17-DMAG; KOS-1022; NSC 707545) Cat. No.: HY-12024

ApoptozoleCat. No.: HY-15098

AT13387(Onalespib; AT 13387; AT-13387) Cat. No.: HY-14463

BIIB021(CNF2024; BIIB-021; BIIB 021; CNF 2024; CNF-2024) Cat. No.: HY-10212

Debio 0932 (CUDC-305; Debio-0932; Deb

io0932; CUDC305; CUDC 305) Cat. No.: HY-13469

Ganetespib(STA-9090; STA 9090; STA9090) Cat. No.: HY-15205

GeldanamycinCat. No.: HY-15230

http://www.medchemexpress.com/Targets/HSP.html

http://www.medchemexpress.com/17-AAG.html

http://www.medchemexpress.com/17-AAG-Hydrochloride.html

http://www.medchemexpress.com/alvespimycin.html

http://www.medchemexpress.com/Alvespimycin-hydrochloride.html

http://www.medchemexpress.com/Apoptozole.html

http://www.medchemexpress.com/AT13387.html

http://www.medchemexpress.com/BIIB021.html

http://www.medchemexpress.com/Debio-0932.html

http://www.medchemexpress.com/Ganetespib.html

http://www.medchemexpress.com/Geldanamycin.html




5 mg, 10 mg, 50 mg


Purity: 99.59%Clinical Data: Phase 1, SuspendedSize: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 25 mg, 100 mg, 200 mg, 500 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: HSP70-IN-1 is a heat shock protein ( ) inhibitor; inhibits theHSPgrowth of Kasumi-1 cells with an of 2.3 μM.IC50

Bioactivity: KNK437, dose-dependently inhibited the acquisition ofthermotolerance and the induction of various HSPs includingHSP105, HSP70, and HSP40 in COLO 320DM (human coloncarcinoma) cells. It also inhibit mRNA levels with IC 50: 17 umol/L.

Bioactivity: KRIBB11 is an inhibitor of , with of 1.2Heat shock factor (HSF) IC50μM.

Bioactivity: ML346 is a novel activator of Hsp70 with EC50 of 4600 nM in HeLacell toxicity assay.

Bioactivity: NVP-AUY922 is a highly potent inhibitor with of 13HSP90 IC50nM/21 nM for for HSP90α/β, respectively, and has weaker potencyagainst the HSP90 family members GRP94 and TRAP-1.

Bioactivity: NVP-BEP800(VER82576) is a novel, fully synthetic, oral Hsp90inhibitor with an IC50 of 0.058 ± 0.006 μM.

Bioactivity: NVP-HSP990(HSP990) is an orally bioavailable inhibitor ofHsp90(IC50=13 nM; Hsp90α) with potential antineoplastic activity.

Bioactivity: PF-04929113 Mesylate is a potent and selective Hsp90 inhibitor withan IC50 of median 50 nM.

Bioactivity: PU-WS13 is a potent, Grp94-specific Hsp90 inhibitor of the purinescaffold class.

Bioactivity: Retaspimycin(IPI 504) is a small-molecule inhibitor of heat shockprotein 90 (HSP90) with antiproliferative and antineoplastic activities.

HSP70-IN-1Cat. No.: HY-12622

KNK437(KNK-437; KNK 437) Cat. No.: HY-100110

KRIBB11(KRIBB-11; KRIBB 11) Cat. No.: HY-100872

ML346(ML-346) Cat. No.: HY-18669

NVP-AUY922 (Luminespib; AUY922; VER-52296; NVP-AUY 922; AUY-922;

VER 52296; VER52296) Cat. No.: HY-10215

NVP-BEP800(VER-82576; VER82576) Cat. No.: HY-10942

NVP-HSP990(HSP-990) Cat. No.: HY-15190

PF-04929113 Mesylate (PF04929113 Mesylate; SNX-5422 Mesylate

; PF04929113 Mesylate; SNX5422 Mesylate) Cat. No.: HY-10213A

PU-WS13(PU-WS-13) Cat. No.: HY-18680

Retaspimycin(IPI-504; IPI504; IPI 504) Cat. No.: HY-15263

http://www.medchemexpress.com/HSP70-IN-1.html

http://www.medchemexpress.com/KNK437.html

http://www.medchemexpress.com/KRIBB11.html


http://www.medchemexpress.com/NVP-AUY922.html

http://www.medchemexpress.com/NVP-BEP800.html

http://www.medchemexpress.com/NVP-HSP990.html

http://www.medchemexpress.com/PF-04929113-Mesylate.html

http://www.medchemexpress.com/PU-WS13.html

http://www.medchemexpress.com/retaspimycin.html


1 mg, 5 mg, 10 mg


2 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


2 mg, 5 mg, 10 mg, 25 mg, 100 mg


100 mg, 500 mg


200u g, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: Retaspimycin hydrochloride is a novel and highly soluble inhibitor ofthe ATPase activity.Hsp90

Bioactivity: Rocaglamide is potent and selective for ( ofheat shock reporter IC5050 nM) and for the control reporter (IC >1000 nM).50

Bioactivity: Teprenone(Geranylgeranylacetone; GGA)is commonly utilized toprotect the gastric mucosa in peptic ulcer disease; has been shown toprotect the myocardium from ischemia/reperfusion by activatingheat shock proteins.

Bioactivity: Triptolide is an inhibitor of heat shock factor ( ), inhibitsHSF1HSP90-CDC37 binding and induces acetylation of HSP90, and alsoinhibits expression in a dose-dependent manner with MDM2 IC50values range from 47 to 73 nM.

Bioactivity: VER-155008 is a novel, small molecule inhibitor of Hsc70/Hsp70 withGI50 of 5

Bioactivity: VER-49009 is a pyrazole compound that inhibits Hsp90 with an IC50value of 47 nM.

Bioactivity: VER-50589 is an isoxazole compound that inhibits Hsp90 with anIC50 value of 21 nM.


Retaspimycin Hydrochloride(IPI-504; IPI504; IPI 504) Cat. No.: HY-10210

Rocaglamide(Rocaglamide A; Roc-A) Cat. No.: HY-19356

Teprenone(Geranylgeranylacetone) Cat. No.: HY-B0779

Triptolide(PG490; PG 490; PG-490) Cat. No.: HY-32735

VER-155008Cat. No.: HY-10941

VER-49009 (VER49009; VER 49009; CCT1

29397; CCT 129397; CCT-129397) Cat. No.: HY-15986

VER-50589(VER 50589; VER50589) Cat. No.: HY-15984

http://www.medchemexpress.com/Retaspimycin-Hydrochloride.html

http://www.medchemexpress.com/Rocaglamide.html

http://www.medchemexpress.com/Teprenone.html

http://www.medchemexpress.com/Triptolide.html

http://www.medchemexpress.com/VER-155008.html

http://www.medchemexpress.com/ver-49009.html

http://www.medchemexpress.com/VER-50589.html


IRE1

http://www.medchemexpress.com/Targets/IRE1.html


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg

IRE1 Inhibitors & Modulators

Bioactivity: APY29 is an allosteric modulator of which inhibits IRE1αIRE1αautophosphorylation with of 280 nM and activates IRE1α RNaseIC50activity.

Bioactivity: MKC3946 is a potent and soluble inhibitor, used for cancerIRE1αresearch.

Bioactivity: STF-083010 is an inhibitor. STF-083010 inhibits Ire1Ire1endonuclease activity, without affecting its kinase activity, afterendoplasmic reticulum stress.


APY29(APY 29; APY-29) Cat. No.: HY-17537

MKC3946(MKC-3946; MKC 3946) Cat. No.: HY-19710

STF-083010Cat. No.: HY-15845

http://www.medchemexpress.com/Targets/IRE1.html

http://www.medchemexpress.com/APY29.html

http://www.medchemexpress.com/MKC3946.html

http://www.medchemexpress.com/STF-083010.html


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 periphery.Kinesins 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.

http://www.medchemexpress.com/Targets/Kinesin.html


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Kinesin Inhibitors & Modulators

Bioactivity: ARRY-520 is a synthetic kinesin spindle protein ( ) inhibitor with KSP of 6 nM.IC50

Bioactivity: ARRY-520 R enantiomer is the R form of ARRY-520, which is asynthetic, small molecule kinesin spindle protein (KSP) inhibitor withIC50 of 6 nM

Bioactivity: CW-069 is a novel and allosteric inhibitor of the microtubule motorprotein HSET with IC50 value of 75 ± 20 μM; shows statisticallysignificant selectivity over KSP.

Bioactivity: Dimethylenastron is an Eg5 inhibitor, which arrests cells withmonopolar spindles to which all chromosomes attach in a syntelicmanner.

Bioactivity: EMD534085 is a potent and selective inhibitor of the mitotic with an of 8 nM.kinesin-5 IC50

Bioactivity: GSK-923295 is a special, allosteric inhibitor of kinesin motorCENP-EATPase activity, with of 3.2±0.2 nM and 1.6± 0.1 nM for humanKiand canine, respectively.

Bioactivity: Ispinesib (SB-715992) is a potent, specific and reversible inhibitor ofKSP (HsEg5) with Ki of 1.7 nM.

Bioactivity: K858 selectively inhibits Eg5 ATPase activity with an IC50 of 1.3 μM.

Bioactivity: Kif15-IN-1 is a potent Kif15 kinesin inhibitor; inhibits cellularproliferation in tumor cell lines.

Bioactivity: Kif15-IN-2 is a potent Kif15 kinesin inhibitor; inhibits cellularproliferation in tumor cell lines.


ARRY-520(Filanesib; ARRY520; ARRY 520) Cat. No.: HY-15187

ARRY-520 R enantiomer (1,3,4-Thiadiazole-3(2H)-carboxamide, 2

-(3-aminopropyl)-5-(2,5-difluorophenyl)-N-methox…) Cat. No.: HY-15187A

CW-069(CW069; CW 069) Cat. No.: HY-15857

DimethylenastronCat. No.: HY-19944

EMD534085(EMD 534085; EMD-534085) Cat. No.: HY-15000

GSK-923295(GSK 923295; GSK923295) Cat. No.: HY-10299

Ispinesib(SB-715992; SB 715992; SB715992) Cat. No.: HY-50759

K858(K-858; K 858) Cat. No.: HY-19966

Kif15-IN-1Cat. No.: HY-15948

Kif15-IN-2Cat. No.: HY-15949

http://www.medchemexpress.com/Targets/Kinesin.html

http://www.medchemexpress.com/ARRY-520.html

http://www.medchemexpress.com/arry-520-r-enantiomer.html

http://www.medchemexpress.com/CW-069.html

http://www.medchemexpress.com/Dimethylenastron.html

http://www.medchemexpress.com/EMD534085.html

http://www.medchemexpress.com/GSK-923295.html

http://www.medchemexpress.com/Ispinesib.html

http://www.medchemexpress.com/K858.html

http://www.medchemexpress.com/kif15-in-1.html

http://www.medchemexpress.com/kif15-in-2.html



10 mg, 50 mg, 100 mg


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


5 mg, 10 mg, 50 mg, 100 mg


2 mg, 5 mg, 10 mg, 50 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg


2 mg, 5 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: Litronesib is a selective, allosteric inhibitor of Eg5, which may result inmitotic disruption, apoptosis and consequently cell death in tumorcells that are actively dividing.

Bioactivity: Litronesib (Racemate) is the racemate of litronesib. Litronesib is aselective, allosteric inhibitor of Eg5.

Bioactivity: Monastrol is a potent and cell-permeable inhibitor of the mitotickinesin with an value of 14 μM.Eg5 IC50

Bioactivity: MPI-0479605 is a potent, ATP competitive and selective inhibitor ofmitotic kinase Mps1 with IC50 of 1.8 nM, > 40-fold selectivity overother kinases.

Bioactivity: PF-2771 is a potent, selective CENP-E inhibitor, PF-2771 inhibitsCENP-E motor activity with an IC50 of 16.1 ± 1.2 nM.

Bioactivity: Rbin-1 is a potent, reversible, and specific chemical inhibitor ofeukaryotic ribosome biogenesis. Rbin-1 inhibits the with ATPase GI

of 136±7 nM.50

Bioactivity: SB-743921 is a second generation, highly potent and active KSPinhibitor with Ki of 0.1 nM; no affinity to MKLP1, Kin2, Kif1A, Kif15,KHC, Kif4 and CENP-E.

Litronesib(LY-2523355; KF-89617) Cat. No.: HY-14846

Litronesib Racemate(LY-2523355 Racemate; KF-89617 Racemate) Cat. No.: HY-14846A

Monastrol((±)-Monastrol) Cat. No.: HY-101071A

MPI-0479605Cat. No.: HY-12660

PF-2771(PF2771; PF 2771) Cat. No.: HY-19530

Rbin-1(Ribozinoindole-1) Cat. No.: HY-100816

SB-743921(SB743921; SB 743921) Cat. No.: HY-12069

http://www.medchemexpress.com/Litronesib.html

http://www.medchemexpress.com/Litronesib-Racemate.html

http://www.medchemexpress.com/Monastrol.html

http://www.medchemexpress.com/MPI-0479605.html


http://www.medchemexpress.com/Rbin-1.html

http://www.medchemexpress.com/SB-743921.html

LIM Kinase (LIMK)


http://www.medchemexpress.com/Targets/LIM Kinase (LIMK).html



5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

LIM Kinase (LIMK) Inhibitors & Modulators

Bioactivity: BMS-3 is a potent inhibitor of LIMK1.LIM kinase 1 (LIMK1) activity isessential for cell migration and cell cycle progression.

Bioactivity: BMS-5 is a Potent LIM kinase inhibitor (IC50 values are 7 and 8 nMfor LIMK1 and LIMK2 respectively).Inhibits cofilin phosphorylation inMDA-MB-231 breast cancer cells. Reduces MDA-MB-231 tumor cellinvasion in a 3D matrigel invasion assay.

Bioactivity: T56-LIMKi is a selective inhibitor of ; inhibits the growth ofLIMK2Panc-1 cells with an of 35.2 μM.IC50


BMS-5(LIMKI-3; BMS5; BMS 5; LIMKI3; LIMKI 3) Cat. No.: HY-18305

T56-LIMKi(T5601640) Cat. No.: HY-19352

http://www.medchemexpress.com/Targets/LIM Kinase (LIMK).html

http://www.medchemexpress.com/BMS-3.html


http://www.medchemexpress.com/T56-LIMKi.html

Microtubule/Tubulin


http://www.medchemexpress.com/Targets/Microtubule_Tubulin.html



1 mg, 5 mg, 10 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg



1 mg, 10 mg



50 mg, 100 mg


10 mg, 50 mg, 100 mg



10 mg, 50 mg

Microtubule/Tubulin Inhibitors & Modulators

Bioactivity: 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivative withimproved pharmacological features and higher water solubility.

Bioactivity: 10-Oxo Docetaxel(Docetaxel Impurity) is a novel taxoid havingremarkable anti-tumor properties and a Docetaxel intermediate.

Bioactivity: 2-Methoxyestradiol is a and inhibitor, binds to microtubule HIF-1 at or near the colchicine site and inhibits the polymerizationtubulin

of tubulin in vitro, works by interfering with normal microtubulefunction.

Bioactivity: 4'-Demethylepipodophyllotoxin(4'-DMEP) is a key intermediatecompound for the preparation of podophyllotoxin-type anti-cancerdrugs; 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 aimpurity of docetaxel.

Bioactivity: 7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel) derivative;Paclitaxel binds to tubulin and inhibits the disassembly ofmicrotubules.

Bioactivity: ABT-751(E 7010) is a novel bioavailable tubulin-binding andantimitotic sulfonamide agent with IC50 of about 1

Bioactivity: Ansamitocin P-3 is a inhibitor. Ansamitocin P-3 is amicrotubulemacrocyclic antitumor antibiotic.

Bioactivity: Auristatin E is a cytotoxic tubulin modifier with potent and selectiveantitumor activity; MMAE analog and cytotoxin in Antibody-drugconjugates.

10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol

; 10-Deacetylpaclitaxel 7-Xyloside; 10-Deacetylt…) Cat. No.: HY-20584

10-Oxo Docetaxel(Docetaxel Impurity) 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) Cat. No.: HY-16675

7-Epi-docetaxel(4-epi-Docetaxel; 7-Epidocetaxel; 7-Epitaxotere) Cat. No.: HY-16676

7-xylosyltaxol(7-Xylosylpaclitaxel; Taxol-7-xyloside) Cat. No.: HY-77574

ABT-751(ABT751; ABT 751; E7010; E-7010; E 7010) Cat. No.: HY-13270

Ansamitocin P-3 (Antibiotic C 15003P3; Maytansinol buty

rate; C15003P3) Cat. No.: HY-15739

Auristatin ECat. No.: HY-15582

http://www.medchemexpress.com/Targets/Microtubule_Tubulin.html

http://www.medchemexpress.com/10-deacetyl-7-xylosyl-paclitaxel.html

http://www.medchemexpress.com/10-oxo-docetaxel.html

http://www.medchemexpress.com/2-Methoxyestradiol.html

http://www.medchemexpress.com/4_acute_-demethylepipodophyllotoxin.html

http://www.medchemexpress.com/7-epi-10-oxo-docetaxel.html

http://www.medchemexpress.com/7-Epi-docetaxel.html

http://www.medchemexpress.com/7-xylosyltaxol.html

http://www.medchemexpress.com/ABT-751.html

http://www.medchemexpress.com/Ansamitocin-P-3.html

http://www.medchemexpress.com/Auristatin-E.html


10 mg, 50 mg




200 mg, 500 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg


1 mg, 5 mg, 10 mg

Bioactivity: Auristatin F is a cytotoxic tubulin modifier with potent and selectiveantitumor activity; MMAF analog and cytotoxin in Antibody-drugconjugates.

Bioactivity: Auristatin PE is a novel synthetic Dolastatin 10 derivative andinhibitor of polymerization.tubulin

Bioactivity: BNC105 is a tubulin polymerization inhibitor with potentantiproliferative and tumor vascular disrupting properties.

Bioactivity: Cabazitaxel is a semi-synthetic derivative of the natural taxoid10-deacetylbaccatin III with potential antineoplastic activity.

Bioactivity: Cephalomannine is a taxol derivative with antitumor, antiproliferativeproperties.

Bioactivity: Cevipabulin(TTI-237) is a novel, potent, synthetic small molecule,inhibits binding of vinblastine at the Vinca alkaloid site of theαβ-tubulin heterodimer.

Bioactivity: Colchicine is a inhibitor and a disrupting agent.tubulin microtubuleColchicine triggers apoptosis.

Bioactivity: Combretastatin A4 is a -targeting agent that binds microtubule with of 0.4 μM.β-tubulin Kd

Bioactivity: Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, is atoxin payload in antibody drug conjugate.

Bioactivity: D-64131 is a novel inhibitor of Tubulin polymerization thatcompetitively binds with [(3)H]colchicine to αβ-Tubulin.


Auristatin FCat. No.: HY-15583

Auristatin PE(Soblidotin; TZT 1027; TZT-1027; TZT1027) Cat. No.: HY-14672

BNC105(BNC-105) Cat. No.: HY-16114

Cabazitaxel(XRP6258; RPR-116258A; taxoid XRP6258) Cat. No.: HY-15459

CephalomannineCat. No.: HY-77554

Cevipabulin(TTI-237) Cat. No.: HY-14949

ColchicineCat. No.: HY-16569

Combretastatin A4(CRC 87-09) Cat. No.: HY-N2146

Cys-mcMMADCat. No.: HY-15750

D-64131(D 64131; D64131) Cat. No.: HY-15482

http://www.medchemexpress.com/Auristatin-F.html

http://www.medchemexpress.com/Auristatin-PE.html

http://www.medchemexpress.com/BNC105.html

http://www.medchemexpress.com/Cabazitaxel.html

http://www.medchemexpress.com/cephalomannine.html

http://www.medchemexpress.com/Cevipabulin.html

http://www.medchemexpress.com/Colchicine.html

http://www.medchemexpress.com/Combretastatin-A4.html

http://www.medchemexpress.com/cys-mcmmad.html

http://www.medchemexpress.com/D-64131.html



10 mg, 50 mg, 100 mg

Purity: 95.82%Clinical Data:Size: 500u g, 1 mg



5 mg, 10 mg


2 mg, 5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg



100 mg, 200 mg


1 mg, 5 mg, 10 mg

Bioactivity: D8-MMAE is a deuterated form of MMAE, which is a microtubule-disrupting agent.

Bioactivity: Docetaxel is a semi-synthetic taxane analogue, acts as a microtubulestabilizer.

Bioactivity: Docetaxel trihydrate(Taxotere trihydrate), an analog of taxol, is aninhibitor of depolymerisation of microtubules through binding tostabilized microtubules

Bioactivity: Dolastatin 10 is a potent antimitotic peptide, isolated from themarine mollusk , that inhibits Dolabela auricularia tubulinpolymerization.

Bioactivity: ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231cell proliferation with IC50 of 30.9 nM; not a substrate for theP-glycoprotein drug transporter and retains activity inβIII-tubulin-overexpressing cell lines.

Bioactivity: Epothilone B is a (MT) targeting agent with ofmicrotubule EC0.011.8 μM.

Bioactivity: Epothilone D is a potent stabilizer.microtubule Bioactivity: Eribulin (E7389; ER-086526), a synthetic analogue of halichondrin B inphase III clinical trials for breast cancer, binds to tubulin andmicrotubules.

Bioactivity: Eribulin Mesylate (E7389 Mesylate), a synthetic analogue ofhalichondrin B in phase III clinical trials for breast cancer, binds totubulin and microtubules.

Bioactivity: Estramustine phosphate sodium is an antimicrotubule chemotherapyagent; arrests prostate cancer cells in the G2/M phase of the cellcycle.

D8-MMAE(D8-Monomethyl auristatin E; D8-Vedotin; D8 MMAE) Cat. No.: HY-15162A

DocetaxelCat. No.: HY-B0011

Docetaxel TrihydrateCat. No.: HY-B0011A

Dolastatin 10(DLS 10; NSC 376128; Dolastatin-10) Cat. No.: HY-15580

ELR510444(ELR-510444) Cat. No.: HY-16191

Epothilone B(EPO 906; Patupilone) Cat. No.: HY-17029

Epothilone D (12,13-Desoxyepothilone B;

Desoxyepothilone B; KOS 862) Cat. No.: HY-15278

Eribulin(B1939; E7389; ER-086526) Cat. No.: HY-13442

Eribulin mesylate (B1939 mesylate; E7389 mesylate; ER-086

526 mesylate) Cat. No.: HY-13442A

Estramustine phosphate sodium(Estramustine phosphate disodium) Cat. No.: HY-13627

http://www.medchemexpress.com/d8-mmae.html

http://www.medchemexpress.com/Docetaxel.html

http://www.medchemexpress.com/docetaxel-trihydrate.html

http://www.medchemexpress.com/Dolastatin-10.html

http://www.medchemexpress.com/ELR510444.html

http://www.medchemexpress.com/Epothilone-B.html

http://www.medchemexpress.com/Epothilone-D.html

http://www.medchemexpress.com/eribulin.html

http://www.medchemexpress.com/eribulin-mesylate.html

http://www.medchemexpress.com/Estramustine-phosphate-sodium.html


1 mg, 5 mg, 10 mg


1 mg, 5 mg, 10 mg


5 mg, 10 mg, 50 mg



5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg

Bioactivity: Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizingdrug, a type of vascular-targeting agent, a drug designed to damagethe vasculature (blood vessels) of cancer tumors causing centralnecrosis.

Bioactivity: Ixabepilone is an orally bioavailable inhibitor, whichmicrotubulebinds to tubulin and promotes tubulin polymerization andmicrotubule stabilization, thereby arrests cells in the G2-M phase ofthe cell cycle and induces tumor cell apoptosis.

Bioactivity: KX2-391 is an inhibitor of that targets the peptide substrate siteSrcof Src, with of 9-60 nM in cancer cell lines.GI50

Bioactivity: KX2-391 (dihydrochloride) is an inhibitor of that targets theSrcpeptide substrate site of Src, with of 9-60 nM in cancer cellGI50lines.

Bioactivity: KX2-391 Mesylate is a synthetic, orally bioavailable inhibitor of Src and .kinase tubulin polymerization

Bioactivity: Lexibulin(CYT-997) is a potent tubulin polymerisation inhibitor withIC50 of 10-100 nM in cancer cell lines; with potent cytotoxic andvascular disrupting activity in vitro and in vivo.

Bioactivity: Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulin polymerisationinhibitor with IC50 of 10-100 nM in cancer cell lines; with potentcytotoxic and vascular disrupting activity in vitro and in vivo.

Bioactivity: Maytansinol inhibits microtubule assembly and induces microtubuledisassembly in vitro.

Bioactivity: Monomethyl auristatin D (MMAD), a potent tubulin inhibitor, is atoxin payload in antibody drug conjugate; Mc-MMAD is a protectivegroup (maleimidocaproyl) -conjugated MMAD.

Bioactivity: Mc-MMAE is a protective group (maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE), which is a potent inhibitor,tubulinis a toxin payload in antibody drug conjugate ( ).ADC


Fosbretabulin disodium (Fosbretabulin disodium salt; CA 4DP; C

A 4P; Combretastatin A4 disodium phosphate) Cat. No.: HY-17449

Ixabepilone(Azaepothilone B; BMS 247550; BMS 247550-1) Cat. No.: HY-10222

KX2-391(KX 01; KX 2-391; KX01; KX-01) Cat. No.: HY-10340

KX2-391 dihydrochloride(KX2-391 2HCl; KX2-391) Cat. No.: HY-10340A

KX2-391 Mesylate(KX01 Mesylate) Cat. No.: HY-10340B

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(Mc MMAD; McMMAD) Cat. No.: HY-15740

Mc-MMAE (Maleimidocaproyl-monomethylauristatin E; Mc MMAE; McM

MAE) Cat. No.: HY-15741

http://www.medchemexpress.com/fosbretabulin-disodium.html

http://www.medchemexpress.com/Ixabepilone.html

http://www.medchemexpress.com/kx2-391.html

http://www.medchemexpress.com/KX2-391-dihydrochloride.html

http://www.medchemexpress.com/KX2-391-Mesylate.html

http://www.medchemexpress.com/Lexibulin.html

http://www.medchemexpress.com/Lexibulin-dihydrochloride.html

http://www.medchemexpress.com/Maytansinol.html

http://www.medchemexpress.com/Mc-MMAD.html

http://www.medchemexpress.com/Mc-MMAE.html



1 mg, 5 mg, 10 mg


50 mg, 100 mg, 500 mg


10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


2 mg, 5 mg, 10 mg



10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


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


1 mg, 5 mg, 10 mg

Bioactivity: Mc-MMAF is a protective group-conjugated MMAF. MMAF is a morepotent drug than Monomethyl auristatin E (MMAE), but is chargedand relatively membrane-impermeable, is a potent tubulin inhibitor,is a toxin payload in antibody drug conjugate.

Bioactivity: Mertansine is a tubulin inhibitorinhibits the assemblyof microtubulesby binding to tubulin, with a linker structure can create anantibody-drug conjugate (ADC).

Bioactivity: MMAD is a potent inhibitor, is a toxin payload in antibodytubulindrug conjugates ( ).ADCs

Bioactivity: Monomethyl auristatin D Hcl (MMAD Hcl), a potent tubulin inhibitor,is a toxin payload in antibody drug conjugate.

Bioactivity: MMAF is an antitubulin agent that inhibit cell division; inhibits H3397cell growth with an of 105 nM.IC50

Bioactivity: MMAF hydrochloride is an antitubulin agent that inhibit cell division;inhibits H3397 cell growth with an of 105 nM.IC50

Bioactivity: Monomethyl auristatin E (MMAE) is an antimitotic agent whichinhibits cell division by blocking the polymerisation of , andtubulinalso shows inhibition of antibody-drug conjugates ( ) activity.ADCs

Bioactivity: Nocodazole is a rapidly-reversible inhibitor of microtubulepolymerization, which exhibits good potency against ABL,ABL(E255K), and ABL(T315I) with values of 0.21 μM, 0.53 μM,IC50and 0.64 μM, respectively, and increases -mediatedCRISPR/Cas9editing frequencies.

Bioactivity: Paclitaxel is a potent anticancer agent known to promote assembly, inhibit MT depolymerization, andmicrotubule (MT)

change MT dynamics required for mitosis and cell proliferation.

Bioactivity: PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; withexcellent potencies in tumor cell proliferation assays and differentialADME properties when compared to other synthetic auristatinanalogues that are used in the preparation of ADCs.

McMMAF(mc-MMAF; Maleimidocaproyl monomethylauristatin F) Cat. No.: HY-15578

Mertansine (DM1; Maytansinoid DM1; DM-1; Maytansinoid DM-1; DM 1;

Maytansinoid DM 1) Cat. No.: HY-19792

MMAD (Demethyldolastatin 10; Monomethylauristatin D; Monomethyl Dolasta

tin 10) Cat. No.: HY-15581

MMAD hydrochloride (Demethyldolastatin 10 hydrochloride; M

onomethylauristatin D hydrochloride; Monomethyl …) Cat. No.: HY-79105

MMAF(Monomethylauristatin F) Cat. No.: HY-15579

MMAF Hydrochloride(Monomethylauristatin F Hydrochloride) Cat. No.: HY-15579A

Monomethyl auristatin E(Vedotin; MMAE) Cat. No.: HY-15162

Nocodazole(Oncodazole; R17934) Cat. No.: HY-13520

PaclitaxelCat. No.: HY-B0015

PF-06380101Cat. No.: HY-12522

http://www.medchemexpress.com/McMMAF.html

http://www.medchemexpress.com/Mertansine.html

http://www.medchemexpress.com/MMAD.html

http://www.medchemexpress.com/MMAD-hydrochloride.html

http://www.medchemexpress.com/mmaf.html

http://www.medchemexpress.com/MMAF-Hydrochloride.html

http://www.medchemexpress.com/Monomethyl-auristatin-E.html

http://www.medchemexpress.com/Nocodazole.html

http://www.medchemexpress.com/Paclitaxel.html



5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg


1 mg, 5 mg, 10 mg

Purity: >98%Clinical Data: Phase 1Size: 1 mg


100 mg, 500 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg


100 mg, 500 mg

Bioactivity: Podophyllotoxin is a potent inhibitor of microtubule assembly andDNA topoisomerase II.

Bioactivity: Taltobulin (HTI-286; SPA-110) is an analogue of Hemiasterlin; potenttubulin inhibitor; ADCs cytotoxin.

Bioactivity: Taltobulin hydrochloride is an analogue of Hemiasterlin; potenttubulin inhibitor; ADCs cytotoxin.

Bioactivity: Taltobulin trifluoroacetate (HTI-286; SPA-110) is an analogue ofHemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.

Bioactivity: Triclabendazole(CGA89317) is a benzimidazole, it binds to tubulinimpairing intracellular transport mechanisms and interferes withprotein synthesis.

Bioactivity: Tubulysin A(TubA) is a myxobacterial product that can function as anantiangiogenic agent in many in vitro assays; anti-microtubule,anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, andantiproliferative.

Bioactivity: Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulininhibitor (MMAD), Vc-MMAD is an antibody drug conjugate

Bioactivity: VcMMAE is a with potent antitumordrug-linker conjugate for ADCactivity by using the anti-mitotic agent, monomethyl auristatin E(MMAE), linked via the lysosomally cleavable dipeptide,valine-citrulline (vc).

Bioactivity: Vinblastine is a cytotoxic alkaloid used against various cancer types.Vinblastine inhibits the formation of microtubule and suppressesnAChR with an of 8.9 μM.IC50

Bioactivity: Vinblastine sulfate is a cytotoxic alkaloid used against various cancertypes. Vinblastine sulfate inhibits the formation of microtubule andsuppresses nAChR with an of 8.9 μM.IC50


Podophyllotoxin(Podofilox; PPT) Cat. No.: HY-15552

Taltobulin (HTI-286; SPA-110; HTI286;

SPA110; HTI 286; SPA 110) Cat. No.: HY-15584

Taltobulin hydrochloride(HTI-286 hydrochloride; SPA-110 hydrochloride) Cat. No.: HY-15584B

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate;

SPA-110 trifluoroacetate) Cat. No.: HY-15584A

Triclabendazole(CGA89317) Cat. No.: HY-B0621

Tubulysin A(TubA) Cat. No.: HY-15995

Vc-MMAD(Vc MMAD; VcMMAD) Cat. No.: HY-15742

VcMMAECat. No.: HY-15575

VinblastineCat. No.: HY-17418

Vinblastine sulfate(Vincaleukoblastine sulfate salt) Cat. No.: HY-13780

http://www.medchemexpress.com/Podophyllotoxin.html

http://www.medchemexpress.com/taltobulin.html

http://www.medchemexpress.com/Taltobulin-hydrochloride.html

http://www.medchemexpress.com/Taltobulin-trifluoroacetate.html

http://www.medchemexpress.com/triclabendazole.html

http://www.medchemexpress.com/Tubulysin-A.html

http://www.medchemexpress.com/Vc-MMAD.html

http://www.medchemexpress.com/VcMMAE.html

http://www.medchemexpress.com/Vinblastine.html

http://www.medchemexpress.com/Vinblastine-sulfate.html



10 mg, 50 mg

Purity: >98%Clinical Data: Phase 3Size: 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg



10 mg, 50 mg, 100 mg, 200 mg

Bioactivity: Vincristine (sulfate) is an inhibitor of polymerizationof microtubules by binding to tubulin with IC of 32 μM in a50cell-free assay.

Bioactivity: Vinflunine is a new vinca alkaloid uniquely fluorinated with theproperties of mitotic-arresting and tubulin-interacting activity.

Bioactivity: Vinflunine Tartrat is a new vinca alkaloid uniquely fluorinated withthe properties of mitotic-arresting and tubulin-interacting activity.

Bioactivity: Vinorelbine(KW-2307 base) is an anti-mitotic agent which inhibits theproliferation of Hela cells with IC50 of 1

Bioactivity: Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits theproliferation of Hela cells with IC of 1.25 nM.50

Vincristine sulfate (Leurocristine sulfate; 22-Oxovincaleuk

oblastine sulfate) Cat. No.: HY-N0488

VinflunineCat. No.: HY-B0628

Vinflunine TartrateCat. No.: HY-B0628A

Vinorelbine(KW-2307 base) Cat. No.: HY-12053

Vinorelbine ditartrate(KW-2307; Nor-5'-anhydrovinblastine ditartrate) Cat. No.: HY-12053A

http://www.medchemexpress.com/vincristine-sulfate.html

http://www.medchemexpress.com/vinflunine.html

http://www.medchemexpress.com/Vinflunine-Tartrate.html

http://www.medchemexpress.com/vinorelbine.html

http://www.medchemexpress.com/Vinorelbine-ditartrate.html

Mps1


http://www.medchemexpress.com/Targets/Mps1.html






5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


2 mg, 5 mg, 10 mg, 50 mg


1 mg, 5 mg, 10 mg, 25 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg

Mps1 Inhibitors & Modulators

Bioactivity: AZ3146 is a reasonably potent and selective inhibitor with Mps1 IC50

of 35 nM for Mps1 .Cat

Bioactivity: BAY 1161909 inhibits Mps1 kinase activity with IC50 of < 1 nM whenassay with 10 μM ATP, with IC50 of < 1.9 nM when assay with 2 mMATP.

Bioactivity: BAY 1217389 is a potent, and selective inhibitor of the monopolarspindle 1 ( ) kinase with an value less than 10 nM.MPS1 IC50

Bioactivity: MPI-0479605 is a potent, ATP competitive and selective inhibitor ofmitotic kinase Mps1 with IC50 of 1.8 nM, > 40-fold selectivity overother kinases.

Bioactivity: Mps1-IN-1 is a highly potent and selectibe Mpsl inhibitor with IC50of 367 nM; >1000-fold selectivity relative to the 352 member kinasepanel with the major exceptions of Alk and Ltk.

Bioactivity: Mps1-IN-2 is a potent Mps1 kianse inhibitor with IC50 value of 145nM.

Bioactivity: Mps1-IN-3 is a selective and highly potent MPS1 kinase inhibitorwith an IC50 of 50 nM.

Bioactivity: NMS-P715 is the first selective, ATP-competitive and orallybioavailable MPS1 small-molecule inhibitor(IC50=8 nM); selectivelyreduces cancer cell proliferation, leaving normal cells almostunaffected.

Bioactivity: NMS-P715 analog is the analog of NMS-P715, which is the firstselective, ATP-competitive and orally bioavailable MPS1small-molecule inhibitor(IC50=8 nM); selectively reduces cancer cellproliferation, leaving normal cells almost unaffected.

AZ3146(AZ 3146; AZ-3146) Cat. No.: HY-14710

BAY 1161909 (Benzeneacetamide, 4-fluoro-N-[4-[2-[[2-methoxy-4-(met

hylsulfonyl)phenyl]amino][1,2,4]triazolo[1,5-a]p…) Cat. No.: HY-12858

BAY1217389(BAY 1217389; BAY-1217389) Cat. No.: HY-12859

MPI-0479605Cat. No.: HY-12660

Mps1-IN-1Cat. No.: HY-13298

Mps1-IN-2Cat. No.: HY-13994

Mps1-IN-3(MPS1-IN-3) Cat. No.: HY-12401

NMS-P715(NMS P715; NMS-P 715) Cat. No.: HY-12382

NMS-P715 analog(NMS P715 analog; NMS-P 715 analog) Cat. No.: HY-14712

http://www.medchemexpress.com/Targets/Mps1.html


http://www.medchemexpress.com/BAY-1161909.html

http://www.medchemexpress.com/BAY1217389.html

http://www.medchemexpress.com/MPI-0479605.html

http://www.medchemexpress.com/Mps1-IN-1.html

http://www.medchemexpress.com/Mps1-IN-2.html

http://www.medchemexpress.com/mps1-in-3.html

http://www.medchemexpress.com/NMS-P715.html

http://www.medchemexpress.com/nms-p715-analog.html

Nucleoside Antimetabolite/Analog

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 HIV.Once 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-FU.Antimetabolite is a chemical that inhibits the use of a metabolite,which 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.


http://www.medchemexpress.com/Targets/Nucleoside Antimetabolite_Analog.html




100 mg, 500 mg, 1 g


10 mg, 50 mg


100 mg, 500 mg


1 g, 5 g


1 g, 5 g


50 mg, 100 mg


1 g, 5 g


100 mg, 500 mg

Purity: 99%Clinical Data: Phase 3, Phase 4Size: 10mM x 1mL in DMSO,

100 mg, 200 mg, 500 mg

Nucleoside Antimetabolite/Analog Inhibitors & Modulators

Bioactivity: 5-Azacytidine is a nucleoside analogue of cytidine that specificallyinhibits DNA methylation by trapping DNA methyltransferases.

Bioactivity: 5-BrdU is a nucleoside analog, and competes with thymidine forincorporation into DNA, and is used in the detection of proliferatingcells.

Bioactivity: 5-Fluorouracil is a potent antitumor agent that affects pyrimidinesynthesis by inhibiting thymidylate synthetase thus depletingintracellular dTTP pools.

Bioactivity: Mercaptopurine (6-mercaptopurine; 6-MP) is an immunosuppressivedrug; is a thiopurine

Bioactivity: Adenosine is a nucleoside composed of a molecule of adenineattached to a ribose sugar molecule (ribofuranose) moiety via aβ-N9-glycosidic bond

Bioactivity: Capecitabine is an oral prodrug that is converted to its only activemetabolite, fluorouracil (FU), by thymidine phosphorylase.

Bioactivity: Carmofur is a derivative of fluorouracil, an antimetabolite used as anantineoplastic agent.

Bioactivity: Clofarabine(Clolar; Clofarex) inhibits the enzymatic activities ofribonucleotide reductase (IC50 = 65 nM) and DNA polymerase

Bioactivity: Cytarabine is an antimetabolic agent and inhibitorDNA synthesiswith of 16 nM.IC50

Bioactivity: Cytarabine (AraC) is an antimetabolic agent and DNA synthesisinhibitor

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-Mercaptopurine(Mercaptopurine; 6-MP) Cat. No.: HY-13677

Adenosine(Adenine riboside; D-Adenosine) Cat. No.: HY-B0228

CapecitabineCat. No.: HY-B0016

Carmofur(HCFU) Cat. No.: HY-B0182

ClofarabineCat. No.: HY-A0005

Cytarabine (Cytosine β-D-arabinofuranoside; Cytosine Arabinoside;

Ara-C) Cat. No.: HY-13605

Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside hydroch

loride; Cytosine Arabinoside hydrochloride; Ara-…) Cat. No.: HY-13605A

http://www.medchemexpress.com/Targets/Nucleoside Antimetabolite_Analog.html

http://www.medchemexpress.com/5-Azacytidine.html

http://www.medchemexpress.com/5-BrdU.html

http://www.medchemexpress.com/5-Fluorouracil.html

http://www.medchemexpress.com/6-Mercaptopurine.html

http://www.medchemexpress.com/Adenosine.html

http://www.medchemexpress.com/Capecitabine.html

http://www.medchemexpress.com/carmofur.html

http://www.medchemexpress.com/clofarabine.html

http://www.medchemexpress.com/Cytarabine.html

http://www.medchemexpress.com/cytarabine-hydrochloride.html


100 mg, 200 mg, 500 mg, 1 g


1000u g, 2500u g, 5 mg, 10 mg

Purity: >98%Clinical Data: Phase 1, Phase 2Size: 2500u g, 5 mg, 10 mg


10 mg, 50 mg, 100 mg



100 mg, 200 mg, 500 mg


1 g, 5 g

Purity: >98%Clinical Data:Size: 10mM x 1mL in Water,

10 mg, 50 mg


200 mg, 1 g


1 g, 5 g

Bioactivity: Cytidine is a nucleoside molecule that is formed when cytosine isattached to a ribose ring, cytidine is a component of RNA.

Bioactivity: Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It hassignificant activity against melanomas.

Bioactivity: Deoxycytidine triphosphate (dCTP), a nucleoside triphosphate, is araw material in DNA synthesis. Deoxycytidine triphosphate has manyapplications, such as real-time PCR, cDNA synthesis, and DNAsequencing.

Bioactivity: Doxifluridine is a thymidine phosphorylase activator for PC9-DPE2cells with IC50 of 0.62 μM.

Bioactivity: Floxuridine (5-fluorodeoxyuridine) is an oncology drug that belongsto the class known as antimetabolites with an GI50 of 5.1 μM for theinhibition of PEPT1.

Bioactivity: Fludarabine(NSC 118218), a DNA synthesis inhibitor, is achemotherapy drug used in the treatment of hematologicalmalignancies.

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 orally bioavailablePNP inhibitor with picomolar potency; induces apoptosis, mainly in Tcells.

Bioactivity: Forodesine Hcl (BCX-1777 freebase; Immucillin-H) is an orallybioavailable PNP inhibitor with picomolar potency; inducesapoptosis, mainly in T cells.

Bioactivity: Gemcitabine is a inhibitor with of 37.6, 42.9,DNA synthesis IC5092.7, 89.3 and 131.4 nM in BxPC-3, Mia Paca-2, PANC-1, PL-45 andAsPC-1 cells, respectively.


Cytidine (Cytosine β-D-riboside; Cy

tosine-1-β-D-ribofuranoside) Cat. No.: HY-B0158

Dacarbazine(Imidazole Carboxamide) Cat. No.: HY-B0078

Deoxycytidine triphosphate(dCTP) Cat. No.: HY-101400

Doxifluridine(Ro 21-9738; 5-Fluoro-5'-deoxyuridine; 5'-DFUR) Cat. No.: HY-B0021

Floxuridine(5-Fluorouracil 2'-deoxyriboside) Cat. No.: HY-B0097

Fludarabine(F-ara-A; NSC 118218) Cat. No.: HY-B0069

Fludarabine phosphateCat. No.: HY-B0028

Forodesine(BCX-1777 freebase; Immucillin-H) Cat. No.: HY-16210

Forodesine hydrochloride(BCX-1777; Immucillin-H hydrochloride) Cat. No.: HY-16209

Gemcitabine(LY 188011; NSC 613327; LY188011; LY-188011) Cat. No.: HY-17026

http://www.medchemexpress.com/Cytidine.html

http://www.medchemexpress.com/Dacarbazine.html

http://www.medchemexpress.com/Deoxycytidine_triphosphate.html

http://www.medchemexpress.com/Doxifluridine.html

http://www.medchemexpress.com/floxuridine.html

http://www.medchemexpress.com/fludarabine.html

http://www.medchemexpress.com/Fludarabine-phosphate.html

http://www.medchemexpress.com/Forodesine.html

http://www.medchemexpress.com/Forodesine-hydrochloride.html

http://www.medchemexpress.com/Gemcitabine.html




100 mg, 500 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


100 mg, 500 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


100 mg, 200 mg, 500 mg, 1 g


5 mg, 10 mg, 50 mg

Bioactivity: Gemcitabine elaidate(CP-4126; CO-101) is a lipophilic, unsaturatedfatty acid ester derivative of gemcitabine (dFdC), an antimetabolitedeoxynucleoside analogue, with potential antineoplastic activity

Bioactivity: Gemcitabine hydrochloride is a inhibitor with ofDNA synthesis IC5037.6, 42.9, 92.7, 89.3 and 131.4 nM in BxPC-3, Mia Paca-2, PANC-1,PL-45 and AsPC-1 cells, respectively.

Bioactivity: LY2334737 is an orally available prodrug of gemcitabine which is anucleoside analog used as chemotherapy.

Bioactivity: Merimepodib is a novel noncompetitive inhibitor of IMPDH (Inosine.monophosphate dehydrogenase)

Bioactivity: Nelarabine (Arranon, 506U78) is a purine nucleoside analog and DNAsynthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.Nelarabine is a chemotherapy drug used in T-cell acutelymphoblastic leukemia.

Bioactivity: Orotic acid (OA) is an intermediate in pyrimidine metabolism.

Bioactivity: RX-3117(TV-1360; Fluorocyclopentenylcytosine) is novel a cytidineanalog; shows anticancer activity in several cancer cell lines, includinggemcitabine-resistant variants.

Bioactivity: TAS-102 is a novel oral combination drug that consists of anantineoplastic thymidine-based nucleoside analog,trifluorothymidine, and a potent inhibitor,thymidine phosphorylasetipiracil, in a 1:0.5 molar ratio.

Bioactivity: Tegafur (also known as Ftorafur) is a chemotherapeutic 5-FU prodrugused in the treatment of cancers; is a component of tegafur-uracil.

Bioactivity: Tipiracil is a thymidine phosphorylase ( ) inhibitor.TPase

Gemcitabine elaidate(CP-4126; CO-101; Gemcitabine 5'-elaidate) Cat. No.: HY-13538

Gemcitabine Hydrochloride(LY 188011 hydrochloride) Cat. No.: HY-B0003

LY2334737(LY 2334737; LY-2334737) Cat. No.: HY-13672

Merimepodib (VI-21497; VX-497; MMP; VI21497; VI 21497; VX497; VX 4

97) Cat. No.: HY-13986

Nelarabine(506U78; GW 506U78; Nelzarabine) Cat. No.: HY-13701

Orotic acid(6-Carboxyuracil; Vitamin B13) Cat. No.: HY-N0157

RX-3117(TV-1360; fluorocyclopentenylcytosine) Cat. No.: HY-15228

TAS-102(Trifluridine-tipiracil hydrochloride mixture) Cat. No.: HY-16478

TegafurCat. No.: HY-17400

TipiracilCat. No.: HY-A0063A

http://www.medchemexpress.com/Gemcitabine-elaidate.html

http://www.medchemexpress.com/Gemcitabine-Hydrochloride.html

http://www.medchemexpress.com/ly2334737.html

http://www.medchemexpress.com/Merimepodib.html

http://www.medchemexpress.com/Nelarabine.html

http://www.medchemexpress.com/Orotic-acid.html

http://www.medchemexpress.com/RX-3117.html

http://www.medchemexpress.com/TAS-102.html

http://www.medchemexpress.com/Tegafur.html

http://www.medchemexpress.com/Tipiracil.html


100 mg, 200 mg, 500 mg

Purity: >98%Clinical Data: Phase 1Size: 10mM x 1mL in DMSO,

50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Bioactivity: Tipiracil (hydrochloride) is a thymidine phosphorylase inhibitor (TPI),used for cancer research.

Bioactivity: Triciribine is a inhibitor, also inhibits and DNA synthesis Akt with of 130 nM, and 0.02-0.46 μM, respectively.HIV-1/2 IC50

Bioactivity: Trifluorothymidine (TFT) and is an inhibitor of thymidinephosphorylase. TFT also inhibits thymidylate synthase (TS), arate-limiting enzyme of DNA biosynthesis, and is incorporated intoDNA.

Bioactivity: Vidarabine is an antiviral drug which is active against herpes simplexand varicella zoster viruses.


Tipiracil hydrochloride(Tipiracil) Cat. No.: HY-A0063

Triciribine(API-2; NSC 154020; TCN) Cat. No.: HY-15457

Trifluorothymidine (Trifluridine; FTD; 5-Trifluorothymidin

e; NSC 529182; NSC 75520) Cat. No.: HY-A0061

Vidarabine (Ara-A; Arabinosyladenine; Adenine Arabinoside; 9-β-D-

Arabinofuranosyladenine) Cat. No.: HY-B0277

http://www.medchemexpress.com/Tipiracil-hydrochloride.html

http://www.medchemexpress.com/Triciribine.html

http://www.medchemexpress.com/Trifluorothymidine.html

http://www.medchemexpress.com/Vidarabine.html


p97

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 2.9 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.

http://www.medchemexpress.com/Targets/p97.html


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg

p97 Inhibitors & Modulators

Bioactivity: CB-5083 is a potent, selective and orally bioavailable inhibitorp97with an value of 11 nM.IC50

Bioactivity: DBeQ(JRF-12) is a selective, potent, reversible, and ATP-competitivep97 inhibitor with IC50 of 1.5 μM.

Bioactivity: ML240 is a selective, ATP-competitive p97 inhibitor with IC50 valuesof 100 nM.

Bioactivity: ML241 hydrochloride is a potent and selective inhibitors of p97ATPase with IC50 values of 100 nM.

Bioactivity: NMS-859 is a potent and specific small molecule covalent inhibitor ofthe ATPase VCP/p97 (IC50 ~0.37 μM), identified by high-throughputscreening.

Bioactivity: NMS-873 is a potent, selective allosteric inhibitor with VCP/p97 IC50value of 20 nM (Wild Type, 1 mM ATP).


CB-5083(CB5083; CB 5083) Cat. No.: HY-12861

DBeQ(JRF 12; JRF12; JRF-12) Cat. No.: HY-15945

ML240(ML 240; ML-240) Cat. No.: HY-19795

ML241 hydrochloride(ML-241 hydrochloride; ML 241 hydrochloride) Cat. No.: HY-19797A

NMS-859Cat. No.: HY-15714

NMS-873(NMS873; NMS 873) Cat. No.: HY-15713

http://www.medchemexpress.com/Targets/p97.html

http://www.medchemexpress.com/CB-5083.html

http://www.medchemexpress.com/DBeQ.html


http://www.medchemexpress.com/ML241-hydrochloride.html

http://www.medchemexpress.com/NMS-859.html



PAK

PAKs (p21-activated kinases) are key regulators of actin dynamics, cellproliferation and cell survival. PAKs are Ser/Thr kinases that areclassified into two groups on the basis of their structural andfunctional features: group I (PAK1–3) and group II (PAK4–6). 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 GTPases.Because the deregulation of PAKs is closely associated with varioushuman diseases,small-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 pathway.PAKs 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 survival,anchorage-independent growth, angiogenesis, invasion, migration and regulation of cell cycle and mitosis.Consequently, PAKs have also been implicated in a number of pathological conditions including cancer.

http://www.medchemexpress.com/Targets/PAK.html


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

PAK Inhibitors & Modulators

Bioactivity: APTO-253 is a novel small molecule with potent anti-tumor activity incancer cells via induction of the gene that expresses the Krüppel-likefactor 4 (KLF4) master transcription factor, leading to cell cycleinhibition and programmed cell death

Bioactivity: FRAX1036 is a novel ATP-competitive small molecule inhibitor ofgroup I p21-activated Kinases (PAKs)

Bioactivity: FRAX486 is a p21-activated kinase ( ) inhibitor with sPAK IC50between 10-100 nM for PAK1-3.

Bioactivity: FRAX597 is a potent group I p21-activated Kinases ( s) inhibitorPAKwith of 8, 13 and 19 nM for , and .IC50 PAK1 2 3

Bioactivity: G-5555 is a selective PAK1 Inhibitor (Ki=3 Bioactivity: IPA-3 is a selective non-ATP competitive inhibitor with ofPAK1 IC502.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).

Bioactivity: PAK4-IN-1 is an inhibitor of p21-activated kinase ( ) extractedPAKfrom patent WO 2015003166 A1; has an of less than 100 nM inIC50MTT assay.

Bioactivity: PF-3758309 is an inhbitor of with of 1.3 nM for PAK4.PAK IC50


APTO-253(LOR-253; LT-253) Cat. No.: HY-16291

FRAX1036(FRAX-1036; FRAX 1036) Cat. No.: HY-19538

FRAX486(FRAX-486) Cat. No.: HY-15542B

FRAX597(FRAX 597; FRAX-597) Cat. No.: HY-15542A

G-5555(G5555; G 5555) Cat. No.: HY-19635

IPA-3(IPA 3; IPA3) Cat. No.: HY-15663

PAK4-IN-1(KPT-9274) Cat. No.: HY-12793

PF-3758309(PF 3758309; PF3758309) Cat. No.: HY-13007

http://www.medchemexpress.com/Targets/PAK.html

http://www.medchemexpress.com/APTO-253.html

http://www.medchemexpress.com/FRAX1036.html



http://www.medchemexpress.com/G-5555.html

http://www.medchemexpress.com/IPA-3.html

http://www.medchemexpress.com/PAK4-IN-1.html



PARP

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 cell’s nucleus. The main role is to detectand signal single-strand DNA breaks (SSB) to the enzymaticmachinery involved in the SSB repair.

http://www.medchemexpress.com/Targets/PARP.html


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: Phase 1, Phase 2, Phase 3Size: 10mM x 1mL in DMSO,

5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg

PARP Inhibitors & Modulators

Bioactivity: A-966492 is a novel and potent inhibitor of and with PARP1 PARP2 of 1 nM and 1.5 nM, respectively.Ki

Bioactivity: AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM. It is at least1000-fold more potent than the benzamides.

Bioactivity: AZ6102 is a potent TNKS1/2 inhibitor (IC50=3/1 nM) that has100-fold selectivity against other PARP family enzymes (IC50: 0.5-3μM) and shows 5 nM Wnt pathway inhibition in DLD-1 cells.

Bioactivity: AZD2461 is a novel PARP inhibitor, which has the potential to avoidthe olaparib resistence mediated by Pgp.

Bioactivity: BGP-15 is a inhibitor, that can protect against heart failure andPARPatrial fibrillation in mice.

Bioactivity: BMN-673 is a novel inhibitor with of 0.57 nM for PARP1/2 IC50.PARP1

Bioactivity: BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673 Bioactivity: BSI-201 (Iniparib; NSC-746045) is a PARP1 inhibitor withdemonstrated effectiveness in triple-negative breast cancer (TNBC)

Bioactivity: E7449 is an orally bioavailable, potent, small molecule inhibitor ofPARP1 and PARP2; enhances the efficacy of radiotherapy andchemotherapy and has potent single agent anticancer activity inBRCA-deficient tumors.

Bioactivity: G007-LK displays high selectivity toward tankyrases 1 and 2 withbiochemical IC50 values of 46 nM and 25 nM, respectively, and acellular IC50 value of 50 nM combined with an excellentpharmacokinetic profile in mice.


A-966492(A966492; A 966492) Cat. No.: HY-10614

AG14361(AG 14361; AG-14361) Cat. No.: HY-12032

AZ6102(AZ 6102; AZ-6102) Cat. No.: HY-12975

AZD-2461(AZD2461; AZD 2461) Cat. No.: HY-13536

BGP-15(BGP 15; BGP15) Cat. No.: HY-100828

BMN-673(Talazoparib; BMN673; BMN 673) Cat. No.: HY-16106

BMN-673 8R,9S (Talazoparib (8R,9S); (8R,9S)-BMN-673; BMN673 (8R,9S);

BMN 673 (8R,9S)) Cat. No.: HY-16106A

BSI-201(Iniparib; NSC-746045; IND-71677; BSI 201; BSI201) Cat. No.: HY-12015

E7449(E-7449) Cat. No.: HY-12418

G007-LK(G007 LK; G007LK) Cat. No.: HY-12438

http://www.medchemexpress.com/Targets/PARP.html

http://www.medchemexpress.com/A-966492.html

http://www.medchemexpress.com/AG14361.html


http://www.medchemexpress.com/azd-2461.html

http://www.medchemexpress.com/BGP-15.html

http://www.medchemexpress.com/BMN-673.html

http://www.medchemexpress.com/BMN-673-8R,9S.html

http://www.medchemexpress.com/BSI-201.html

http://www.medchemexpress.com/E7449.html

http://www.medchemexpress.com/G007-LK.html



10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g, 2 g


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


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


1 g, 5 g


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


200 mg, 500 mg

Bioactivity: INO-1001 is a potent inhibitor of with of < 50 nM in CHOPARP IC50cells, and acts as a mediator of oxidant-induced myocyte dysfunctionduring reperfusion.

Bioactivity: JW 55 is a potent and selective signaling pathwayβ-catenininhibitor, which functions via inhibition of the PARP domain oftankyrase 1 and tankyrase 2 (TNKS1/2). JW55 decreasesauto-PARsylation of TNKS1/2 in vitro with s of 1.9 μM and 830IC50nM respectively.

Bioactivity: MK-4827 is an excellent and inhibitor with of 3.8 andPARP1 2 IC502.1 nM, respectively.

Bioactivity: MK-4827(Niraparib) Hcl is a selective inhibitor of PARP1/PARP2 withIC50 of 3.8 nM/2.1 nM; with great activity in cancer cells with mutantBRCA-1 and BRCA-2; >330-fold selective against PARP3, V-PARP andTank1.

Bioactivity: MK-4827 tosylate is an excellent and inhibitor with ofPARP1 2 IC503.8 and 2.1 nM, respectively.

Bioactivity: MN-64 is a inhibitor of tankyrases, showed 6 nM potency againsttankyrase 1, isoenzyme selectivity, and Wnt signaling inhibition.

Bioactivity: Nicotinamide is a water-soluble vitamin, an active component ofcoenzymes NAD and NADP, and acts as poly (ADP-ribose)polymerase ( ) inhibitor.PARP

Bioactivity: NMS-P118 is a potent, orally available, and highly selective PARP-1Inhibitor for cancer therapy.

Bioactivity: NVP-TNKS656 is a highly potent, selective, and orally active TNKS2inhibitor with of 6 nM, and is > 300 fold selectivity against IC50

and .PARP1 PARP2

Bioactivity: Olaparib is a potent inhibitor with of 5 and 1 nM for PARP IC50 and , respectively.PARP-1 PARP-2

INO-1001(3-Aminobenzamide; INO1001; INO 1001) Cat. No.: HY-12022

JW 55(JW55; JW-55) Cat. No.: HY-13968

MK-4827(Niraparib; MK 4827; MK4827) Cat. No.: HY-10619

MK-4827 hydrochloride (Niraparib hydrochloride; MK 4827 hydro

chloride; MK4827 hydrochloride) Cat. No.: HY-10619A

MK-4827 tosylate (Niraparib tosylate; MK 4827 tosylate;

MK4827 tosylate) Cat. No.: HY-10619B

MN-64(MN64; MN 64) Cat. No.: HY-19351

Nicotinamide(Niacinamide; Nicotinic acid amide; Vitamin B3) Cat. No.: HY-B0150

NMS-P118Cat. No.: HY-18954

NVP-TNKS656(TNKS656; TNKS-656) Cat. No.: HY-13990

Olaparib (AZD2281; KU-0059436; KU0059436; AZD-2281; KU0059436;

AZD 2281) Cat. No.: HY-10162

http://www.medchemexpress.com/INO-1001.html

http://www.medchemexpress.com/JW-55.html


http://www.medchemexpress.com/mk-4827-hydrochloride.html

http://www.medchemexpress.com/MK-4827-tosylate.html

http://www.medchemexpress.com/MN-64.html

http://www.medchemexpress.com/Nicotinamide.html

http://www.medchemexpress.com/NMS-P118.html

http://www.medchemexpress.com/NVP-TNKS656.html

http://www.medchemexpress.com/Olaparib.html


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg


1 mg, 5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg



10 mg, 50 mg, 100 mg


Bioactivity: PJ34 is a potent specific inhibitor of / with of 110 nMPARPl 2 IC50and 86 nM, respectively.

Bioactivity: PJ34 hydrochloride is a potent specific inhibitor of / with PARPl 2 IC50of 110 nM and 86 nM, respectively.

Bioactivity: Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Kiof 1

Bioactivity: Rucaparib (phosphate) is an inhibitor of with of 1.4 nM forPARP KiPARP1 in a cell-free assay, and also shows binding affinity to eightother PARP domains.

Bioactivity: Saroglitazar magnesium is a novel peroxisome proliferator-activatedreceptor ( ) agonist with predominant PPARα and moderatePPARPPARγ activity with values of 0.65 pM and 3 nM in HepG2 cells,EC50respectively.

Bioactivity: UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM; ~27-foldselective against PARP1.

Bioactivity: Veliparib is a potent inhibitor, inhibiting and PARP PARP1 PARP2with s of 5.2 and 2.9 nM, respectively.Ki

Bioactivity: Veliparib (dihydrochloride) is a potent inhibitor of and PARP1 with of 5.2 nM and 2.9 nM in cell-free assays, respectively.PARP2 Ki

Bioactivity: XAV-939 is a selective Wnt pathway -mediatedβ-catenintranscription inhibitor and axin stabilizing agent with values ofIC5011 and 4 nM for the inhibition of TNKS1 and TNKS2, respectively.


PJ34(PJ-34; PJ 34) Cat. No.: HY-13688A

PJ34 hydrochloride(PJ-34 hydrochloride; PJ 34 hydrochloride) Cat. No.: HY-13688

Rucaparib (AG014699; PF01367338; AG 014699; PF 01367338; AG-0146

99; PF-01367338) Cat. No.: HY-10617A

Rucaparib phosphate (AG014699 phosphate; PF01367338 phospha

te; AG 014699 phosphate; PF 01367338 phosphate; …) Cat. No.: HY-10617

Saroglitazar (Magnesium)Cat. No.: HY-19937A

UPF 1069(UPF-1069; UPF1069) Cat. No.: HY-14478

Veliparib(ABT-888; ABT 888; ABT888) Cat. No.: HY-10129

Veliparib dihydrochloride (ABT-888 dihydrochloride; A

BT888 dihydrochloride; ABT 888 dihydrochloride) Cat. No.: HY-10130

XAV-939(XAV939; NVP-XAV 939) Cat. No.: HY-15147

http://www.medchemexpress.com/pj34.html

http://www.medchemexpress.com/PJ34-hydrochloride.html

http://www.medchemexpress.com/rucaparib.html

http://www.medchemexpress.com/Rucaparib-phosphate.html

http://www.medchemexpress.com/Saroglitazar-Magnesium.html

http://www.medchemexpress.com/UPF-1069.html

http://www.medchemexpress.com/Veliparib.html

http://www.medchemexpress.com/Veliparib-dihydrochloride.html

http://www.medchemexpress.com/XAV-939.html


PERK

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.

http://www.medchemexpress.com/Targets/PERK.html


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg

PERK Inhibitors & Modulators

Bioactivity: GSK2606414 is an orally available and selective inhibitor withPERKan of 0.4 nM.IC50

Bioactivity: GSK2656157 is an ATP-competitive inhibitor of enzyme activityPERKwith an value of 0.9 nM, and highly selective for PERK with ICIC50 50values of > 100 nM against a panel of 300 kinases.

Bioactivity: ISRIB (trans-isomer) is a potent inhibitor of with an of 5PERK IC50nM.

Bioactivity: Sal003 is a potent cell-permeable analog of the eIF2α phosphataseinhibitor Salubrinal with enhanced aqueous solubility.

Bioactivity: Salubrinal is an inhibitor of phosphatases ( ) that act on thePP1eukaryotic translation initiation factor 2 subunit ( ), with ofeIF2α IC501.7 µM for blocking PP1 activity.


GSK2606414(GSK 2606414; GSK-2606414) Cat. No.: HY-18072


ISRIB trans-isomerCat. No.: HY-12495

Sal003(Sal-003) Cat. No.: HY-15969

SalubrinalCat. No.: HY-15486

http://www.medchemexpress.com/Targets/PERK.html

http://www.medchemexpress.com/GSK2606414.html


http://www.medchemexpress.com/ISRIB-trans-isomer.html

http://www.medchemexpress.com/Sal003.html

http://www.medchemexpress.com/Salubrinal.html


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 CDK/cyclin complexes duringM-phase of the cell cycle.Polo-like kinases (Plks) are a family ofconserved serine/threonine kinases involved in the regulation of cellcycle progression through G2 and mitosis. Mammalian polo-likekinases include Plk1 (Xenopus Plx1), Plk2/Snk (Xenopus Plx2),Plk3/Prk/FnK (Xenopus Plx3), Plk4/Sak 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 and/or mitotic spindle disruption.

http://www.medchemexpress.com/Targets/Polo-like Kinase (PLK).html


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg, 200 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Polo-like Kinase (PLK) Inhibitors & Modulators

Bioactivity: BI 2536 is a potent and selective inhibitor of with of 0.83Plk1 IC50nM, and is also a potent inhibitor of with of 25 nM.BRD4 IC50

Bioactivity: Centrinone is a selective and reversible inhibitor of polo-like kinase 4(Plk4), a serine-threonine protein kinase that initiatescentriole/centrosome assembly.

Bioactivity: Centrinone-B is a high affinity and selective PLK4 inhibitor (Ki = 0.59nM).

Bioactivity: CFI400945 is a potent and selective,orally bioavailable PLK4 inhibitorwith an IC50 value of 2

Bioactivity: GSK461364 is a potent inhibitor with a Polo-like kinase 1 (PLK1) Kivalue of 2.2 nM.

Bioactivity: GW843682X is a selective PLK1 and PLK3 inhibitor with IC50s of 2

Bioactivity: HMN-214(IVX214) is a potent PLK1 inhibitor an average IC50 of 0 Bioactivity: LFM-A13 is a potent and selective inhibitor of Btk with IC50 of 17.2uM; also inhibits PLK3 with IC50 of 7.2 uM.

Bioactivity: MLN0905 is a small-molecule and potent inhibitor of PLK1 with IC50of 2 nM.

Bioactivity: NMS-1286937(NMS-P937) is an orally bioavailable, small-moleculePolo-like kinase 1 (PLK1) inhibitor(IC50=2 nM) with potentialantineoplastic activity; no inhibition on PLK2 and PLK3


BI 2536(BI-2536; BI2536) Cat. No.: HY-50698

CentrinoneCat. No.: HY-18682

Centrinone-B(Centrinone B) Cat. No.: HY-18683

CFI-400945 free base(CFI400945 free base; CFI 400945 free base) Cat. No.: HY-12300

GSK461364 (GSK 461364; GSK-461364; GSK-461364A; GSK461364A; GSK

461364A) Cat. No.: HY-50877

GW843682X(GW 843682X; GW843682; GW-843682X) Cat. No.: HY-11003

HMN-214 (IVX-214; HMN214; HMN 214;

IVX 214; IVX-214; IVX214) Cat. No.: HY-12045

LFM-A13Cat. No.: HY-18009

MLN0905(PLK1 Inhibitor; MLN 0905; MLN-0905) Cat. No.: HY-15155

NMS-1286937(NMS-P937; NMS1286937; NMS 1286937; NMS P937) Cat. No.: HY-15828

http://www.medchemexpress.com/Targets/Polo-like Kinase (PLK).html

http://www.medchemexpress.com/bi-2536.html

http://www.medchemexpress.com/Centrinone.html

http://www.medchemexpress.com/Centrinone-B.html

http://www.medchemexpress.com/CFI-400945-free-base.html

http://www.medchemexpress.com/gsk461364.html

http://www.medchemexpress.com/GW843682X.html

http://www.medchemexpress.com/HMN-214.html

http://www.medchemexpress.com/LFM-A13.html

http://www.medchemexpress.com/MLN0905.html




5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg



2 mg, 5 mg, 10 mg, 50 mg

Purity: 99.49%Clinical Data: Safety; Efficacy, Safety; Efficacy; Pharmacokinetics,

Safety; Efficacy; Pharmacokinetics; PharmacodynamicsSize: 10mM x 1mL in Water,5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data: Safety; Efficacy, Safety; Efficacy; Pharmacokinetics,

Safety; Efficacy; Pharmacokinetics; PharmacodynamicsSize: 5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg, 500 mg, 1 g

Bioactivity: The phosphoserine/phosphothreonine recognition site of thepolo-box domain of polo-like kinase 1 is the binding pocket forthymoquinone and its analogue poloxime. Both small moleculesdisplace phosphopeptides bound with the polo-box domain in aslow but noncovalent binding mode.

Bioactivity: Poloxin is a non-ATP competitive inhibitorPolo-like Kinase 1 (PLK1)that targets the polo-box domain.

Bioactivity: Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1with IC50 of 9 nM; shows 30-fold greater selectivity against PLK2 andno activity to PLK3

Bioactivity: Rigosertib (sodium) is a non-ATP-competitive inhibitor of with PLK1 of 9 nM, and shows 30-fold greater selectivity against PLK2.IC50

Bioactivity: RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1(PLK1) with IC50 of 3 nM.

Bioactivity: SBE13 is a potent and selective PLK1 with IC50 of 0.2 nM; noinhibition om Aurora A kinase, Plk2 and Plk3.

Bioactivity: SBE13 Hcl is a potent and selective PLK1 with IC50 of 0 Bioactivity: TAK-960 is a novel, investigational, orally bioavailable, potent, andselective PLK1 inhibitor(IC50=1.5 nM) that has shown activity inseveral tumor cell lines, including those that expressmultidrug-resistant protein 1 (MDR1).

Bioactivity: TAK-960 hydrochloride is a novel, investigational, orally bioavailable,potent, and selective PLK1 inhibitor(IC50=1.5 nM) that has shownactivity in several tumor cell lines, including those that expressmultidrug-resistant protein 1 (MDR1).

Bioactivity: Volasertib is a highly potent inhibitor with an of 0.87 nM,PLK1 IC50as well as the two closely related kinases and with Plk2 Plk3 IC50values 5 and 56 nM, respectively.

Poloxime (2,5-Cyclohexadiene-1,4-dione, 2-methyl-5-(1-methyleth

yl)-, 1-oxime) Cat. No.: HY-77195

PoloxinCat. No.: HY-12134

Rigosertib(ON-01910; ON01910; ON 01910) Cat. No.: HY-12037A

Rigosertib sodium(ON-01910 sodium; ON01910 sodium; ON01910 sodium) Cat. No.: HY-12037

Ro3280(Ro 3280; Ro-3280) Cat. No.: HY-15161

SBE13(SBE-13) Cat. No.: HY-15158A

SBE13 Hydrochloride(SBE-13 Hydrochloride) Cat. No.: HY-15158

TAK-960Cat. No.: HY-15160

TAK-960 hydrochlorideCat. No.: HY-15160A

Volasertib(BI 6727; BI-6727; BI6727) Cat. No.: HY-12137

http://www.medchemexpress.com/Poloxime.html

http://www.medchemexpress.com/Poloxin.html

http://www.medchemexpress.com/rigosertib.html

http://www.medchemexpress.com/Rigosertib-sodium.html

http://www.medchemexpress.com/Ro3280.html

http://www.medchemexpress.com/SBE13.html

http://www.medchemexpress.com/SBE13-Hydrochloride.html


http://www.medchemexpress.com/TAK-960-hydrochloride.html

http://www.medchemexpress.com/Volasertib.html

PPAR

PPARs (Peroxisome proliferator-activated receptors) areligand-activated transcription factors of nuclear hormone receptorsuperfamily comprising of the following three subtypes: PPARα,PPARγ, and PPARβ/δ. PPARs play essential roles in the regulation ofcellular differentiation, development, and metabolism (carbohydrate,lipid, 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 homeostasis.Activation of PPAR-γ causes insulin sensitization and enhancesglucose metabolism, whereas activation of PPAR-β/δ enhances fatty

acids metabolism.


http://www.medchemexpress.com/Targets/PPAR.html



1 g, 5 g



100 mg, 500 mg


10 mg, 100 mg


5 mg, 10 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


100 mg


5 mg, 10 mg, 50 mg, 100 mg

Purity: 99%Clinical Data: Phase 3Size: 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

PPAR Inhibitors & Modulators

Bioactivity: (20S)-Protopanaxatriol(g-PPT) is a metabolites of ginsenoside,protopanaxatriol (g-PPT), could modulate endothelial cell functionsthrough the glucocorticoid receptor (GR) and oestrogen receptor(ER).

Bioactivity: Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist withIC50 of 2.8 nM/4.6 nM.

Bioactivity: Balaglitazone (DRF-2593; NN-2344) is a novel partial agonist ofPPAR-γ.

Bioactivity: Bezafibrate(BM15075) is the first clinically tested dual and pan-PPARco-agonism.

Bioactivity: BMS-687453 is a potent and selective PPARα agonist, with an EC50of 10 nM for human PPARα and 410-fold selectivity vs human PPARγin PPAR-GAL4 transactivation assays.

Bioactivity: CDDO-Im(RTA-403) is a novel synthetic triterpenoid more potentthan its parent compound CDDO both in vitro and in vivo; PPARγagonist.

Bioactivity: Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acidunder clinical development as a combination therapy withrosuvastatin for the management of dyslipidemia.

Bioactivity: Ciprofibrate is a peroxisome proliferator-activated receptor agonist.

Bioactivity: Ciprofibrate D6 is deuterium labeled Ciprofibrate, which is aperoxisome proliferator-activated receptor agonist.

Bioactivity: Clofibrate (Atromid-S), a fibric acid derivative used in the treatmentof hyperlipoproteinemia type III and severe hypertriglyceridemia.

(20S)-Protopanaxatriol(20(S)-APPT; g-PPT) Cat. No.: HY-N0835

Aleglitazar (R1439; RO0728804; R-1439; RO-0728804; R 1439; RO 0728

804) Cat. No.: HY-14728

Balaglitazone (DRF-2593; NN-2344; DRF259

3; NN2344; DRF 2593; NN 2344) Cat. No.: HY-16086

Bezafibrate(BM15075) Cat. No.: HY-B0637


CDDO-Im(RTA-403; TP-235; CDDO-Imidazolide) Cat. No.: HY-15725

Choline Fenofibrate(ABT-335; ABT 335; ABT335) Cat. No.: HY-14739

Ciprofibrate(Win35833) Cat. No.: HY-B0664

Ciprofibrate D6Cat. No.: HY-B0664S

ClofibrateCat. No.: HY-B0287

http://www.medchemexpress.com/Targets/PPAR.html

http://www.medchemexpress.com/_20S_-Protopanaxatriol.html

http://www.medchemexpress.com/aleglitazar.html

http://www.medchemexpress.com/balaglitazone.html

http://www.medchemexpress.com/Bezafibrate.html


http://www.medchemexpress.com/CDDO-Im.html

http://www.medchemexpress.com/Choline-Fenofibrate.html

http://www.medchemexpress.com/Ciprofibrate.html

http://www.medchemexpress.com/Ciprofibrate-D6.html

http://www.medchemexpress.com/Clofibrate.html


10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


100 mg, 500 mg


10 mg, 50 mg


1 g, 5 g


5 g, 10 g


5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


500 mg, 1 g, 5 g

Bioactivity: Daidzein is a soy isoflavone, which acts as a activator.PPAR Bioactivity: DG172 dihydrochloride is a novel PPARβ/δ-selective ligand showinghigh binding affinity (IC50 = 27 nM) and potent inverse agonisticproperties.

Bioactivity: Elafibranor is an agonist of the peroxisome proliferator-activatedreceptor-α ( ) and peroxisome proliferator-activatedPPAR-αreceptor-δ ( ) with values of 45 and 175 nM,PPAR-δ EC50respectively.

Bioactivity: Eupatilin, a flavone derived from Artemisia princepsPampanini, hasvarious pharmacological activities, including antioxidant, anti-tumor,and anti-inflammatory capacities

Bioactivity: Fenofibrate is a relatively potent inhibitor of ( =0.2 μM)CYP2C19 IC50and ( =0.7 μM). Fenofibrate is also a well-known CYP2B6 IC50 PPARα

agonist ( =30 μM).EC50

Bioactivity: Fenofibric acid is a lipid regulating agent available as delayed releasecapsules for oral administration.

Bioactivity: FH535 is a compound that suppresses both Wnt/beta-catenin andperoxisome proliferator-activated receptor (PPAR) signaling.

Bioactivity: Gemfibrozil (Lopid) is a compound used to lower lipid levels.

Bioactivity: GSK0660 is a specific antagonist of PPARβ/δ, also has inverse agonisteffects when used alone.

Bioactivity: GSK3787 is as a selective and irreversible antagonist of PPARδ withpIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.


Daidzein(Isoflavone) Cat. No.: HY-N0019

DG172 dihydrochloride(DG 172 dihydrochloride; DG-172 dihydrochloride) Cat. No.: HY-19737A

Elafibranor(GFT505; GFT-505; GFT 505) Cat. No.: HY-16737

EupatilinCat. No.: HY-N0783

FenofibrateCat. No.: HY-17356

Fenofibric acid(FNF acid) Cat. No.: HY-B0760

FH535(FH 535; FH-535) Cat. No.: HY-15721

Gemfibrozil(CI-719) Cat. No.: HY-B0258

GSK0660(GSK-0660; GSK 0660) Cat. No.: HY-12377


http://www.medchemexpress.com/Daidzein.html

http://www.medchemexpress.com/DG172-dihydrochloride.html

http://www.medchemexpress.com/Elafibranor.html

http://www.medchemexpress.com/Eupatilin.html

http://www.medchemexpress.com/Fenofibrate.html

http://www.medchemexpress.com/Fenofibric-acid.html

http://www.medchemexpress.com/fh535.html

http://www.medchemexpress.com/Gemfibrozil.html


http://www.medchemexpress.com/gsk3787.html



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


10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg



5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: GW501516(GSK-516; GW1516) is a potent and highly selectivePPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity overhPPARα and hPPARγ

Bioactivity: GW0742 (GW610742) is a potent and highly selective PPARδ agonist.EC50 values are 1nM, 1.1μM and 2 μM for transactivation of humanPPARδ, -α, and -γ receptors respectively.

Bioactivity: GW1929 is a synthetic peroxisome proliferator-activated receptor-γ(PPARγ) agonist with IC50 of 6.2 nM and 13 nM for human andmouse, respectively.

Bioactivity: GW9662 is a selective antagonist for with of 3.3PPAR PPARγ IC50nM, with ~10 and ~1000-fold functional selectivity in cells againstPPARα and PPARδ, respectively.

Bioactivity: Inolitazone(RS5444; CS-7017) is a novel high-affinity PPARγ agonist,which activates PPARγ with an EC50 about 1/50 that of rosiglitazoneand has no effect on RIE cells that do not express PPARγ.

Bioactivity: Inolitazone dihydrochloride a novel high-affinity agonist thatPPARγis dependent upon PPARγ for its biological activity with of 0.8IC50nM for growth inhibition.

Bioactivity: JW74 is an efficient and specific inhibitor of the canonical Wntsignaling. JW74 shows a reduction of canonical Wnt signaling in theST-Luc assay with IC50 values of 790 nM.

Bioactivity: L-165041 is a cell permeable agonist which inducesPPARδadipocyte differentiation in NIH-PPARδ cells.

Bioactivity: Magnolol, the main polyphenol compound of the bark of Magnoliaofficinalis, has a variety of pharmacological activities

Bioactivity: Pemafibrateis a novel selective PPARα modulator ( ) thatSPPARMαhas antihyperlipidaemic activity.

GW 501516(GW 1516; GSK-516; GW-501516) Cat. No.: HY-10838

GW0742(GW610742; GW 0742; GW-0742; GW 610742; GW-610742) Cat. No.: HY-13928

GW1929(GW 1929; GW-1929) Cat. No.: HY-15655

GW9662(GW 9662; GW-9662) Cat. No.: HY-16578

Inolitazone(Efatutazone; CS-7017; RS5444) Cat. No.: HY-14792

Inolitazone dihydrochloride(Efatutazone; CS-7017; RS5444; CS 7017; RS 5444) Cat. No.: HY-14792B

JW74(JW-74; JW 74) Cat. No.: HY-19739

L-165041(L 165041; L165041) Cat. No.: HY-20019

MagnololCat. No.: HY-N0163

Pemafibrate((R)-K13675; (R)-K-13675; (R)-K 13675) Cat. No.: HY-17618

http://www.medchemexpress.com/GW-501516.html

http://www.medchemexpress.com/GW0742.html

http://www.medchemexpress.com/gw1929.html

http://www.medchemexpress.com/GW9662.html

http://www.medchemexpress.com/inolitazone.html

http://www.medchemexpress.com/inolitazone-dihydrochloride.html

http://www.medchemexpress.com/JW74.html

http://www.medchemexpress.com/L-165041.html

http://www.medchemexpress.com/Magnolol.html

http://www.medchemexpress.com/Pemafibrate.html


10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg

Purity: 98.22%Clinical Data:Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


100 mg, 500 mg


50 mg, 200 mg


100 mg, 500 mg, 1 g, 5 g


1 mg, 5 mg, 10 mg, 25 mg


100 mg, 500 mg


Purity: >98%Clinical Data:Size: 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: Pemafibrate (racemate) is a novel selective modulatorPPARα(SPPARMα).

Bioactivity: Pioglitazone (U 72107) is a selective peroxisomeproliferator-activated receptor gamma(PPARγ) stimulator.

Bioactivity: Pioglitazone hydrochloride is a potent and selective agonistPPARγwith high affinity binding to the PPARγ ligand-binding domain with

of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.EC50

Bioactivity: Procyanidin B2 exerts a potent and beneficial role in reducinggranulosa cell apoptosis and inducing autophagy process,and exertsa variety of potent protective pharmacological effects on diabeticcomplications.

Bioactivity: Retinoic acid is a natural agonist of nuclear receptors.RAR/RXRRetinoic acid also bind to , with of 17 nM.PPARβ/δ Kd

Bioactivity: Rosiglitazone is a peroxisome proliferator-activated receptor-gamma( ) agonist, and is a blocker of and channels.PPAR-γ TRPM2 TRPM3

Bioactivity: Rosiglitazone maleate(BRL-49653C) is a high-affinity selective agonistof the peroxisome proliferator-activated receptor-γ(PPARγ)

Bioactivity: Saroglitazar is a novel peroxisome proliferator-activated receptor () agonist with predominant PPARα and moderate PPARγPPAR

activity with values of 0.65 pM and 3 nM in HepG2 cells,EC50respectively.

Bioactivity: T0070907 is a potent a antagonist and a potential PPARγ RAD51inhibitor, with the of 1 nM towards PPARγ.IC50

Bioactivity: Troglitazone is a agonist with anti-inflammatory andPPARγanti-tumor activity.


Pemafibrate racemateCat. No.: HY-17618A

Pioglitazone(U 72107) Cat. No.: HY-13956

Pioglitazone hydrochloride(U 72107A; AD 4833) Cat. No.: HY-14601

Procyanidin B2(Proanthocyanidin B2) Cat. No.: HY-N0796

Retinoic acid (ATRA; Tretinoin; Vitamin A acid; all-trans-Retinoic a

cid) Cat. No.: HY-14649

Rosiglitazone(BRL 49653; BRL49653; BRL-49653) Cat. No.: HY-17386

Rosiglitazone maleate(BRL 49653C) Cat. No.: HY-14600

SaroglitazarCat. No.: HY-19937

T0070907(T-0070907; T 0070907) Cat. No.: HY-13202

Troglitazone(CS-045) Cat. No.: HY-50935

http://www.medchemexpress.com/Pemafibrate-racemate.html

http://www.medchemexpress.com/pioglitazone.html

http://www.medchemexpress.com/pioglitazone-hydrochloride.html

http://www.medchemexpress.com/Procyanidin-B2.html

http://www.medchemexpress.com/Retinoic-acid.html

http://www.medchemexpress.com/Rosiglitazone.html

http://www.medchemexpress.com/rosiglitazone-maleate.html

http://www.medchemexpress.com/Saroglitazar.html

http://www.medchemexpress.com/t0070907.html

http://www.medchemexpress.com/troglitazone.html



10 mg, 50 mg, 100 mg, 250 mg

Bioactivity: Wy-14,643 (Pirinixic acid) is a moderate agonist of PPARα and PPARγwith IC50 of 36.5 μM and 53.7 μM, respectively.

Wy-14643(Pirinixic acid) Cat. No.: HY-16995

http://www.medchemexpress.com/Wy-14643.html

RAD51

RAD51 protein family assist in repair of DNA double strand breaks.RAD51 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.


http://www.medchemexpress.com/Targets/RAD51.html



5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg

RAD51 Inhibitors & Modulators

Bioactivity: RAD51 Inhibitor B02 (B02) is an inhibitor of human with an RAD51 IC of 27.4 μM.50

Bioactivity: RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM.

Bioactivity: RI-2 is an optimized RAD51 inhibitor with an IC50 of 44.17 μM in thestandard DNA binding assay; specifically inhibits HR(Homologousrecombination) repair in human cells.

Bioactivity: T0070907 is a potent a antagonist and a potential PPARγ RAD51inhibitor, with the of 1 nM towards PPARγ.IC50

RAD51 Inhibitor B02(BO2) Cat. No.: HY-101462

RI-1Cat. No.: HY-15317

RI-2Cat. No.: HY-16904

T0070907(T-0070907; T 0070907) Cat. No.: HY-13202

http://www.medchemexpress.com/Targets/RAD51.html

http://www.medchemexpress.com/RAD51_Inhibitor_B02.html

http://www.medchemexpress.com/RI-1.html

http://www.medchemexpress.com/RI-2.html

http://www.medchemexpress.com/t0070907.html

ROCK

ROCK (Rho-associated protein kinase) is a kinase belonging to theAGC (PKA/ PKG/PKC) family of serine-threonine kinases. ROCKs(ROCK1 and ROCK2) occur in mammals, zebrafish, Xenopus,invertebrates 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.


http://www.medchemexpress.com/Targets/ROCK.html



5 mg, 10 mg, 50 mg


5 mg, 10 mg



5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


100 mg, 200 mg, 500 mg



5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg

ROCK Inhibitors & Modulators

Bioactivity: chroman 1 is a highly potent and selective ROCK II inhibitor. Bioactivity: Coptisine (chloride) is a natural product.

Bioactivity: Fasudil Hcl(HA-1077; AT-877) is a potent inhibitor of ROCK-II, PKA,PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and36 μM, respectively.

Bioactivity: Fasudil (Hydrochloride) is a potent inhibitor of , , , ROCK-II PKA PKG, and with of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36PKC MLCK KI

μM, respectively.

Bioactivity: GSK180736A is a G protein-coupled receptor kinase 2 ( )GRK2inhibitor with an of 0.77 μM.IC50

Bioactivity: GSK269962A is a potent inhibitor with s of 1.6 and 4 nMROCK IC50for recombinant human and respectively.ROCK1 ROCK2

Bioactivity: GSK429286A is a selective inhibitor of and with ROCK1 ROCK2 IC50values of 14 nM and 63 nM, respectively.

Bioactivity: H-1152, an isoquinolinesulfonamide derivative, is a more specific,stronger and membrane-permeable inhibitor of Rho-kinase with a Kivalue of 1.6 nM, but poor inhibitor of other serine/threonine kinases.

Bioactivity: H-1152 2Hcl, an isoquinolinesulfonamide derivative, is a morespecific, stronger and membrane-permeable inhibitor of Rho-kinasewith a Ki value of 1.6 nM, but poor inhibitor of other serine/threoninekinases.

Bioactivity: Hydroxyfasudil(HA1100), metabolite of Fasudil, is a potentRho-kinase inhibitor and vasodilator.

chroman 1(ROCK-II inhibitor) Cat. No.: HY-15392

Coptisine chlorideCat. No.: HY-N0736

Fasudil(AT-877; HA-1077; AT877; HA1077; AT 877; HA 1077) Cat. No.: HY-10341A

Fasudil Hydrochloride(HA-1077; AT-877; Fasudil HCl) Cat. No.: HY-10341

GSK180736A(GSK 180736A; GSK-180736A) Cat. No.: HY-18990

GSK269962A (GSK 269962A; GSK-269962A; GSK269962; GSK 269962; GSK-

269962) Cat. No.: HY-15556

GSK429286A(GSK 429286A; GSK-429286A) Cat. No.: HY-11000

H-1152(H 1152; H1152) Cat. No.: HY-15720

H-1152 dihydrochloride(H 1152 dihydrochloride; H1152 dihydrochloride) Cat. No.: HY-15720A

Hydroxyfasudil(HA-1100; HA 1100; HA1100) Cat. No.: HY-13911

http://www.medchemexpress.com/Targets/ROCK.html

http://www.medchemexpress.com/chroman-1.html

http://www.medchemexpress.com/Coptisine-chloride.html

http://www.medchemexpress.com/fasudil.html

http://www.medchemexpress.com/Fasudil-Hydrochloride.html

http://www.medchemexpress.com/GSK180736A.html



http://www.medchemexpress.com/h-1152.html

http://www.medchemexpress.com/H-1152-dihydrochloride.html

http://www.medchemexpress.com/Hydroxyfasudil.html


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg, 100 mg


1 mg


2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Purity: >98%Clinical Data:Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg

Bioactivity: Hydroxyfasudil Hcl(HA1100 Hcl), metabolite of Fasudil, is a potentRho-kinase inhibitor and vasodilator.

Bioactivity: K-115, an isoquinolinesulfonamide compound, is a highly selectiveand potent (IC50 = 31 nM) Rho-kinase inhibitor; is in Phase II clinicaldevelopment in patients with POAG or ocular hypertension.

Bioactivity: K-115, an isoquinolinesulfonamide compound, is a highly selectiveand potent (IC50 = 31 nM) Rho-kinase inhibitor; is in Phase II clinicaldevelopment in patients with POAG or ocular hypertension.

Bioactivity: LX7101 is a potent inhibitor of and with values ofLIMK ROCK2 IC5024, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; alsoinhibits with an less than 1 nM.PKA IC50

Bioactivity: Narciclasine is a plant growth modulator. Narciclasine modulates theRho/Rho kinase/LIM kinase/cofilin signaling pathway, greatlyincreasing GTPase RhoA activity as well as inducing actin stress fiberformation in a RhoA-dependent manner.

Bioactivity: RKI-1447 is a potent small molecule inhibitor of and ROCK1 ROCK2with values of 14.5 nM and 6.2 nM, respectively.IC50

Bioactivity: ROCK inhibitor(azaindole 1) is a highly potent inhibitor of humanROCK-1 and ROCK-2 isoenzymes with IC50 values of 0.6 and 1.1 nM,respectively.

Bioactivity: SAR407899 is a potent, ATP-competitive ROCK inhibitor woth Kivalue of 36 nM/41 nM for human ROCK/Rat ROCK respectively.

Bioactivity: SAR407899 Hcl is a potent, ATP-competitive ROCK inhibitor woth Kivalue of 36 nM/41 nM for human ROCK/Rat ROCK respectively.

Bioactivity: SLx-2119 is a selective inhibitor of with of 105 nM, moreROCK2 IC50than 200 fold selecivity over ROCK1 (IC =24 μM).50


Hydroxyfasudil hydrochloride (HA-1100 hydrochloride; HA

1100 hydrochloride; HA1100 hydrochloride) Cat. No.: HY-13911A

K-115(Ripasudil; K 115; K115) Cat. No.: HY-15685

K-115 free base (Ripasudil free base; K 115 free base;

K115 free base) Cat. No.: HY-15685A

LX7101(LX-7101) Cat. No.: HY-12659

Narciclasine(Lycoricidinol) Cat. No.: HY-16563

RKI-1447(RKI 1447; RKI1447) Cat. No.: HY-15755

ROCK inhibitor(Rho-kinase inhibitor; Rho Kinase Inhibitor; ROCK) Cat. No.: HY-10319

SAR407899(SAR-407899) Cat. No.: HY-15687A

SAR407899 hydrochloride(SAR-407899 hydrochloride) Cat. No.: HY-15687

SLx-2119(SLx 2119; SLx2119; ROCK inhibitor; KD-025) Cat. No.: HY-15307

http://www.medchemexpress.com/Hydroxyfasudil-hydrochloride.html

http://www.medchemexpress.com/K-115.html

http://www.medchemexpress.com/K-115-free-base.html

http://www.medchemexpress.com/LX7101.html

http://www.medchemexpress.com/Narciclasine.html

http://www.medchemexpress.com/rki-1447.html

http://www.medchemexpress.com/ROCK-inhibitor.html

http://www.medchemexpress.com/SAR407899.html

http://www.medchemexpress.com/SAR407899-hydrochloride.html

http://www.medchemexpress.com/SLx-2119.html


Purity: 98.37%Clinical Data: Phase 1, Phase 2Size: 100 mg, 50 mg, 10 mg, 5 mg



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


5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


10 mg, 50 mg, 100 mg

Bioactivity: SR-3677 is a potent and selective inhibitor with an ofROCK-II IC50~3 nM.

Bioactivity: Thiazovivin (Tzv) is a novel ROCK inhibitor with IC50 of 0.5 μM,promotes hESC survival after single-cell dissociation.

Bioactivity: Y-27632 is an ATP-competitive inhibitor of and ,ROCK-I ROCK-IIwith of 220 nM and 300 nM for and , respectively.Ki ROCK-I ROCK-II

Bioactivity: Y-27632 dihydrochloride is an ATP-competitive inhibitor of ROCK-Iand , with of 220 nM and 300 nM for and ROCK-II Ki ROCK-I

, respectively.ROCK-II

Bioactivity: Y-33075 is potent and selective p160ROCK inhibitor with an Ki valueof 0.14 uM, > 200 fold selectivity for p160ROCK than PKC,cAMP-dependent protein kianse and Mypsin light-chain kinase.

Bioactivity: Y-33075 dihydrochloride is a selective inhibitor derived fromROCKY-27632, and is more potent than Y-27632.

SR-3677(SR3677; SR 3677) Cat. No.: HY-13300

ThiazovivinCat. No.: HY-13257

Y-27632(Y 27632; Y27632) Cat. No.: HY-10071

Y-27632 dihydrochloride(Y 27632 dihydrochloride; Y27632 dihydrochloride) Cat. No.: HY-10583

Y-33075(Y 39983) Cat. No.: HY-10067

Y-33075 dihydrochloride(Y39983 hydrochloride) Cat. No.: HY-10069

http://www.medchemexpress.com/SR-3677.html

http://www.medchemexpress.com/Thiazovivin.html

http://www.medchemexpress.com/Y-27632.html

http://www.medchemexpress.com/Y-27632-dihydrochloride.html

http://www.medchemexpress.com/Y-33075.html

http://www.medchemexpress.com/Y-33075-dihydrochloride.html

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 aging,transcription, apoptosis, inflammation and stress resistance, as well asenergy efficiency and alertness during low-calorie situations. Sirtuinscan also control circadian clocks and mitochondrial biogenesis.


http://www.medchemexpress.com/Targets/Sirtuin.html



5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg, 100 mg


1 g, 5 g


5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg


5 mg, 10 mg


5 mg, 10 mg


10 mg, 50 mg, 100 mg


5 mg, 10 mg, 25 mg, 50 mg

Sirtuin Inhibitors & Modulators

Bioactivity: AK-1 is a potent, specific and cell-permeable inhibitor.SIRT2 Bioactivity: AK-7 is a selective and brain-permeable SIRT2 inhibitor; isneuroprotective in Huntington disease mouse models.

Bioactivity: EX-527 is a potent and selective inhibitor with of 38 nM.SIRT1 IC50EX-527 has much lower potency against SIRT2 (IC , 19.6 μM) or50SIRT3 (IC , 48.7 μM).50

Bioactivity: EX-527 R-enantiomer is a negative control of the active form EX-527S-enantiomer(Speculated for reference); IC50 > 100 uM, e1/e2 canbe found in the reference paper

Bioactivity: EX-527 S-enantiomer is a potent and selective SIRT1 inhibitor withIC50 of 123 nM; no inhibition on SIRT3 and SIRT3

Bioactivity: Ginkgolide C, a natural product, can enhance the cardiac function ofrats in the body.

Bioactivity: Inauhzin(INZ) is a novel small molecule that effectively reactivatesp53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosisof human cancer cells without causing apparently genotoxicstress(IC50=3 uM, in A549 cell).

Bioactivity: Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1and also a inhibitor with of 2.4-5.4 μM.PI3K IC50

Bioactivity: Salermide is an inhibitor of and ; can cause strongSirt1 Sirt2cancer-specific apoptotic cell death.

Bioactivity: Sirtinol is a inhibitor; inhibit the growth of MCF-7 cells with ansirtuin of 48.6 μM at 24 h.IC50

AK-1Cat. No.: HY-101465

AK-7(AK 7; AK7) Cat. No.: HY-16691

EX-527(Selisistat) Cat. No.: HY-15452

EX-527 R-enantiomer(Selisistat R-enantiomer) Cat. No.: HY-15452B

EX-527 S-enantiomer(Selisistat S-enantiomer) Cat. No.: HY-15452A

Ginkgolide C(BN-52022; Ginkgolide-C) Cat. No.: HY-N0785

Inauhzin(INZ) Cat. No.: HY-15869

QuercetinCat. No.: HY-18085

SalermideCat. No.: HY-101073

SirtinolCat. No.: HY-13515

http://www.medchemexpress.com/Targets/Sirtuin.html

http://www.medchemexpress.com/AK-1.html

http://www.medchemexpress.com/AK-7.html

http://www.medchemexpress.com/EX-527.html

http://www.medchemexpress.com/EX-527-R-enantiomer.html

http://www.medchemexpress.com/EX-527-S-enantiomer.html

http://www.medchemexpress.com/Ginkgolide-C.html

http://www.medchemexpress.com/Inauhzin.html

http://www.medchemexpress.com/Quercetin.html

http://www.medchemexpress.com/Salermide.html

http://www.medchemexpress.com/Sirtinol.html


1 mg, 5 mg, 10 mg, 50 mg, 100 mg


2 mg, 5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


2 mg, 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg



1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: Sirtuin modulator 1 is a sirtuin modulator extracted from patentWO/2010071853 A1, compound 570, with EC1.5 <1 uM.

Bioactivity: SRT1720 is a selective activator of human SIRT1 (EC1.5 = 0.16 μM)versus the closest sirtuin homologues, SIRT2 and SIRT3 (SIRT2: EC1.5= 37 μMSIRT3: EC1.5 > 300 μM).

Bioactivity: SRT 1720 (Hydrochloride) is a selective activator of human (ECSIRT1=0.16 μM) versus the closest sirtuin homologues, SIRT2 and SIRT31.5

(SIRT2: EC =37 μM; SIRT3: EC > 300 μM).1.5 1.5

Bioactivity: 6-phenylimidazo[2,1-b]thiazole derivatives; SRT 2104.

Bioactivity: Tenovin-6 is the water soluble analog of Tenovin-1 (HY-13423) andacts as a potent SIRT1 (IC50=21 uM) and SIRT2 (IC50= 10 uM)inhibitor as well as p53 activator.

Bioactivity: Tenovin-1 is a inhibitor of SIRT1 and SIRT2; activator of p21 and p53

Bioactivity: Tenovin-6 is the water soluble analog of Tenovin-1 (HY-13423) andacts as a potent SIRT1 (IC50=21 uM) and SIRT2 (IC50= 10 uM)inhibitor as well as p53 activator.

Bioactivity: Thiomyristoyl is a potent and specific inhibitor with an ofSIRT2 IC5028 nM.


Sirtuin modulator 1 (4-Thiazolecarboxamide, 5-(3-methoxypro

pyl)-2-phenyl-N-[2-[6-(1-pyrrolidinylmethyl)thia…) Cat. No.: HY-19758A

SRT 1720(SRT-1720; SRT1720) Cat. No.: HY-10532

SRT 1720 Hydrochloride(SRT-1720; SRT1720) Cat. No.: HY-15145

SRT 2104 (5-Thiazolecarboxamide, 4-methyl-N-[2-[3-(4-morpholiny

lmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-(3-…) Cat. No.: HY-15262

Tenovin 6 Hydrochloride (Tenovin 6 hydrochloride; Tenovin6 hydr

ochloride; Tenovin 2) Cat. No.: HY-15510B

Tenovin-1(Tenovin 1) Cat. No.: HY-13423

Tenovin-6(Tenovin 6; Tenovin6) Cat. No.: HY-15510

ThiomyristoylCat. No.: HY-101278

http://www.medchemexpress.com/Sirtuin-modulator-1.html

http://www.medchemexpress.com/srt-1720.html

http://www.medchemexpress.com/SRT-1720-Hydrochloride.html

http://www.medchemexpress.com/SRT-2104.html

http://www.medchemexpress.com/Tenovin-6-Hydrochloride.html

http://www.medchemexpress.com/Tenovin-1.html

http://www.medchemexpress.com/Tenovin-6.html

http://www.medchemexpress.com/Thiomyristoyl.html


SRPK

http://www.medchemexpress.com/Targets/SRPK.html


5 mg, 10 mg, 50 mg, 100 mg

SRPK Inhibitors & Modulators

Bioactivity: SRPIN340 is a serine/arginine-rich protein kinase (SRPK)-specificinhibitor with an IC50 value of 0.89 uM (SRPK1); no significantinhibitory activity against more than 140 other kinases.


SRPIN340(SRPIN 340; SRPIN-340; SRPK inhibitor) Cat. No.: HY-13949

http://www.medchemexpress.com/Targets/SRPK.html

http://www.medchemexpress.com/SRPIN340.html


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 100–200 nucleotides are lost, which causes no damageto the organism's 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 cycle.Telomerase, 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.

http://www.medchemexpress.com/Targets/Telomerase.html


10 mg, 50 mg, 100 mg


50 mg, 100 mg

Telomerase Inhibitors & Modulators

Bioactivity: (-)-Epigallocatechin Gallate is an antioxidant polyphenol flavonoidthat inhibits and , and blockstelomerase DNA methyltransferasethe activation of EGF receptors and HER-2 receptors.

Bioactivity: BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with of 100 nM in a cell-free assay.IC50


(-)-Epigallocatechin Gallate(EGCG; Epigallocatechol Gallate) Cat. No.: HY-13653

BIBR 1532(BIBR1532; BIBR-1532) Cat. No.: HY-17353

http://www.medchemexpress.com/Targets/Telomerase.html

http://www.medchemexpress.com/_-_-Epigallocatechin-Gallate.html

http://www.medchemexpress.com/BIBR-1532.html


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 topoisomerases,which possess similar structure and mechanisms.

http://www.medchemexpress.com/Targets/Topoisomerase.html



5 mg, 10 mg


100 mg, 500 mg


10 mg, 25 mg, 50 mg


100 mg, 200 mg, 500 mg



10 mg, 50 mg, 100 mg


Purity: >98.0%Clinical Data:Size: 1 mg, 5 mg


5 mg, 10 mg, 50 mg, 100 mg

Topoisomerase Inhibitors & Modulators

Bioactivity: Amonafide(AS1413) produces protein-associated DNA-strand breaksthrough a topoisomerase II-mediated reaction, but does not producetopoisomerase I-mediated DNA cleavage.

Bioactivity: Amrubicin(SM-5887) is a novel anthracycline derivative for treatmentof bladder carcinoma.

Bioactivity: Amrubicin hydrochloride (SM-5887 hydrochloride) is atopoisomerase II inhibitor used in the treatment of lung cancer.

Bioactivity: Amsacrine is an inhibitor of , specifically inhibitingtopoisomerasetopoisomerase II, and acts as an antineoplastic agent which canintercalates into the DNA of tumor cells.

Bioactivity: Amsacrine hydrochloride is a specific inhibitor, actstopoisomerase IIas an antineoplastic agent which can intercalates into the DNA oftumor cells.

Bioactivity: Betulinic acid, a pentacyclic triterpene, selectively induces apoptosisin tumor cells, also is a inhibitor of HIV-1 with EC50 of 1

Bioactivity: Bisantrene is a highly effective antitumor drug, targets eukaryotictype .II topoisomerases

Bioactivity: Campathecin is a potent DNA enzyme topoisomerase I (topo I)inhibitor, with and of 50 nM and 0.225 μM in breast cancerIC50 IC70cell line MDA-MB-231.

Bioactivity: Daun02 is converted by to Daunorubicin, which is a β-galactosidase inhibitor.topoisomerase

Bioactivity: Daunorubicin(RP13057) inhibits both DNA and RNA synthesis andinhibits DNA synthesis with Ki of 0


Amonafide(AS1413) Cat. No.: HY-10982

Amrubicin(AMR) Cat. No.: HY-B0067

Amrubicin hydrochloride(AMR hydrochloride) Cat. No.: HY-B0067A

Amsacrine (AMSA; m-AMSA; CI-880; SN-

11841; acridinyl anisidide) Cat. No.: HY-13551

Amsacrine hydrochloride (AMSA hydrochloride; m-AMSA hydrochlori

de; CI-880 hydrochloride; SN-11841 hydrochloride…) Cat. No.: HY-13551A

Betulinic acid(Lupatic acid; Betulic acid) Cat. No.: HY-10529

Bisantrene(CL216942) Cat. No.: HY-100875

Campathecin((S)-(+)-Camptothecin; CPT) Cat. No.: HY-16560

Daun02(Daun 02; Daun-02) Cat. No.: HY-13061

Daunorubicin(RP13057; Daunomycin; Rubidomycin) Cat. No.: HY-13062A

http://www.medchemexpress.com/Targets/Topoisomerase.html

http://www.medchemexpress.com/amonafide.html

http://www.medchemexpress.com/amrubicin.html

http://www.medchemexpress.com/amrubicin-hydrochloride.html

http://www.medchemexpress.com/Amsacrine.html

http://www.medchemexpress.com/amsacrine-hydrochloride.html

http://www.medchemexpress.com/Betulinic-acid.html

http://www.medchemexpress.com/Bisantrene.html

http://www.medchemexpress.com/Campathecin.html

http://www.medchemexpress.com/daun02.html

http://www.medchemexpress.com/daunorubicin.html




100 mg, 200 mg, 500 mg


5 mg, 10 mg, 50 mg, 100 mg



5 mg, 10 mg, 50 mg, 100 mg



50 mg, 100 mg, 200 mg, 500 mg, 1 g




10 mg, 50 mg, 100 mg, 200 mg, 500 mg

Bioactivity: Daunorubicin hydrochloride is a inhibitor.topoisomerase II Bioactivity: DOXO-EMCH is a 6-maleimidocaproyl hydrazone derivative ofDoxorubicin, is an albumin binding prodrug.

Bioactivity: Doxorubicin(Adriamycin) is an antibiotic agent that inhibits DNAtopoisomerase II and induces DNA damage and apoptosis

Bioactivity: Topoisomerase IIDoxorubicin hydrochloride is a (Top2) catalyticinhibitor, also is a broad spectrum antibiotic used in the treatment ofcancers, with of 374 nM for Hela cells.IC50

Bioactivity: Ellipticine is a potent antineoplastic agent exhibiting multiplemechanisms of action, IC50 of 1.25±0.13, 0.67±0.06, 1.25±0.13,0.67±0.06, 0.27±0.02, 0.44±0.03, 0.49±0.04, and 1.48±0.62 μM forBreast adenocarcinoma MCF-7, Leukemia HL-60, Breastadenocarcinoma MCF-7, Leukemia HL-60, Neuroblastoma IMR-32,Neuroblastoma UKF-NB-3, …

Bioactivity: Ellipticine hydrochloride is a potent antineoplastic agent; inhibits activities.DNA topoisomerase II

Bioactivity: Epirubicin, a semisynthetic L-arabino derivative of doxorubicin, is anantineoplastic agent by inhibiting Topoisomerase

Bioactivity: Epirubicin (hydrochloride) is a semisynthetic L-arabino derivative ofdoxorubicin, and an antineoplastic agent by inhibiting

.Topoisomerase

Bioactivity: Etoposide is a inhibitor, inhibiting DNA synthesis.topoisomerase II Bioactivity: Exatecan (DX-8951) is a totally synthetic analogue of thetopoisomerase I-inhibitor camptothecin, which was synthesised toimpart increased aqueous solubility, greater tumour efficacy, and lesstoxicity than camptothecin itself.

Daunorubicin Hydrochloride (RP 13057 Hydrochloride; Da

unomycin; RP13057 Hydrochloride; RP-13057 Hydroc…) Cat. No.: HY-13062

DOXO-EMCH(Doxorubicin-EMCH) Cat. No.: HY-16261A

Doxorubicin(Adriamycin; Hydroxydaunorubicin) Cat. No.: HY-15142A

Doxorubicin hydrochloride(Adriamycin; Hydroxydaunorubicin hydrochloride) Cat. No.: HY-15142

EllipticineCat. No.: HY-15753

Ellipticine hydrochlorideCat. No.: HY-15753A

EpirubicinCat. No.: HY-13624

Epirubicin hydrochloride(4'-Epidoxorubicin hydrochloride) Cat. No.: HY-13624A

Etoposide(VP-16; VP-16-213) Cat. No.: HY-13629

Exatecan(DX8951; DX 8951; DX-8951) Cat. No.: HY-13631

http://www.medchemexpress.com/Daunorubicin-Hydrochloride.html

http://www.medchemexpress.com/DOXO-EMCH.html

http://www.medchemexpress.com/Doxorubicin.html

http://www.medchemexpress.com/Doxorubicin-hydrochloride.html

http://www.medchemexpress.com/Ellipticine.html

http://www.medchemexpress.com/Ellipticine-hydrochloride.html

http://www.medchemexpress.com/epirubicin.html

http://www.medchemexpress.com/epirubicin-hydrochloride.html

http://www.medchemexpress.com/etoposide.html

http://www.medchemexpress.com/exatecan.html


50 mg, 100 mg



50 mg, 100 mg, 200 mg, 500 mg


50 mg, 100 mg, 200 mg, 500 mg


50 mg, 100 mg, 200 mg

Purity: >95.0%Clinical Data: Phase 1, Phase 2Size: 5 mg, 10 mg, 50 mg, 100 mg


5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg


10 mg, 50 mg


1 mg, 5 mg, 10 mg

Bioactivity: Exatecan Mesylate (DX-8951) is a totally synthetic analogue of thetopoisomerase I-inhibitor camptothecin, which was synthesised toimpart increased aqueous solubility, greater tumour efficacy, and lesstoxicity than camptothecin itself.

Bioactivity: Flumequine is a synthetic chemotherapeutic antibiotic, inhibitingtopoisomerase II with IC50 of 15 μM.

Bioactivity: Genz-644282 is a non-camptothecin inhibitor of topoisomerase Iwith potential antineoplastic activity(IC50=1.2 nM).

Bioactivity: Idarubicin hydrochloride is an anthracycline antibiotic in thetreatment of leukaemia and a inhibitor withDNA topoisomerase IIan of 3.3 ng/mL in MCF-7 cells.IC50

Bioactivity: INNO-206 is a prodrug of the anticancer agent doxorubicin, which isreleased from albumin under acidic conditions.

Bioactivity: Irinotecan(CPT-11) prevents DNA from unwinding by inhibition oftopoisomerase 1

Bioactivity: Irinotecan hydrochloride is an inhibitor of , and is isTopoisomerase Iactivated by hydrolysis to SN-38 (the active metabolite of Irinotecan).

Bioactivity: Irinotecan Hcl-trihydrate prevents DNA from unwinding by inhibitionof topoisomerase 1

Bioactivity: Mitoxantrone is a inhibitor; also inhibits proteintopoisomerase IIkinase C ( ) activity with an of 8.5 μM.PKC IC50

Bioactivity: Mitoxantrone dihydrochloride is a inhibitor; alsotopoisomerase IIinhibits protein kinase C ( ) activity with an of 8.5 μM.PKC IC50


Exatecan Mesylate(DX8951f; DX 8951f; DX-8951f) Cat. No.: HY-13631A

FlumequineCat. No.: HY-B0526

Genz-644282(Genz644282; Genz 644282) Cat. No.: HY-16228

Idarubicin hydrochloride(4-Demethoxydaunorubicin hydrochloride) Cat. No.: HY-17381

INNO-206(Aldoxorubicin; INNO 206; INNO206) Cat. No.: HY-16261

Irinotecan((+)-Irinotecan; CPT-11) Cat. No.: HY-16562

Irinotecan hydrochloride (CPT-11 hydrochloride; CPT 11 hydrochlo

ride; CPT11 hydrochloride; Camptothecin 11 hydro…) Cat. No.: HY-16562A

Irinotecan hydrochloride trihydrateCat. No.: HY-16568

Mitoxantrone(mitozantrone) Cat. No.: HY-13502

Mitoxantrone dihydrochloride(mitozantrone dihydrochloride) Cat. No.: HY-13502A

http://www.medchemexpress.com/Exatecan-Mesylate.html

http://www.medchemexpress.com/flumequine.html

http://www.medchemexpress.com/Genz-644282.html

http://www.medchemexpress.com/Idarubicin-hydrochloride.html

http://www.medchemexpress.com/INNO-206.html

http://www.medchemexpress.com/Irinotecan.html

http://www.medchemexpress.com/Irinotecan-hydrochloride.html

http://www.medchemexpress.com/irinotecan-hydrochloride-trihydrate.html

http://www.medchemexpress.com/mitoxantrone.html

http://www.medchemexpress.com/Mitoxantrone-dihydrochloride.html




5 mg, 10 mg, 50 mg, 100 mg


100 mg, 200 mg, 500 mg



1 mg, 5 mg, 10 mg, 50 mg


5 mg, 10 mg, 50 mg, 100 mg



10 mg, 50 mg, 100 mg


10 mg, 50 mg, 100 mg


1 mg, 5 mg, 10 mg

Bioactivity: Nemorubicin(Methoxymorpholinyl doxorubicin; MMDX; PNU 152243)is a 3'-deamino-3'[2-(S)-methoxy-4-morpholinyl]derivative ofdoxorubicin, Nemorubici has the anticancer activity on humanhepatocellular carcinoma with an IC50 of 80 nM.

Bioactivity: Pirarubicin is an analogue of the anthracycline anti-neoplasticdoxorubicin, which is an inhibitor of Topo II Target: TopoisomerasePirarubicin is an anthracycline drug

Bioactivity: Pirarubicin Hcl is an analogue of the anthracycline anti-neoplasticdoxorubicin, which is an inhibitor of Topo II

Bioactivity: Pixantrone (BBR 2778) is an experimental antineoplastic drug.

Bioactivity: Pixantrone dimaleate (BBR 2778 dimaleate) is an experimentalantineoplastic drug.

Bioactivity: PNU-159682 is a major bioactive metabolite of Nemorubicin inhuman liver microsomes; > 3,000-fold cytotoxic than its parentcompound(MMDX and doxorubicin).

Bioactivity: Podocarpusflavone A is a DNA topoisomerase I inhibitor, havemoderated anti-proliferative activity induce cell apoptosis in MCF-7,is developing anti-tumor drugs.

Bioactivity: SN-38 is an active metabolite of the inhibitorTopoisomerase IIrinotecan.

Bioactivity: SW044248 is a novel noncanonical Top1 inhibitor with a pattern ofselective toxicity for NSCLC cells.

Bioactivity: TAS-103(BMS-247615) is a dual inhibitor of topoisomerase-I (topo-I)and topoisomerase-II (topoII).

Nemorubicin (Methoxymorpholinyldoxorubicin; PNU-152243; PNU 152243

; PNU152243; PNU-152243A) Cat. No.: HY-15794

Pirarubicin(THP) Cat. No.: HY-13725

Pirarubicin Hydrochloride(THP Hydrochloride) Cat. No.: HY-13725A

Pixantrone(BBR-2778; BBR2778; BBR 2778) Cat. No.: HY-13727

Pixantrone dimaleate (BBR2778 dimaleate; BBR 2778 dimaleate;

BBR-2778 dimaleate) Cat. No.: HY-13727A

PNU-159682(PNU159682; PNU 159682) Cat. No.: HY-16700

Podocarpusflavone ACat. No.: HY-N2198

SN-38(SN 38; SN38; NK-012; NK012; NK 012) Cat. No.: HY-13704

SW044248(SW 044248; SW-044248) Cat. No.: HY-19637

TAS-103 (BMS-247615; TAS103; TAS 1

03; BMS247615; BMS 247615) Cat. No.: HY-13758

http://www.medchemexpress.com/Nemorubicin.html

http://www.medchemexpress.com/Pirarubicin.html

http://www.medchemexpress.com/pirarubicin-hydrochloride.html

http://www.medchemexpress.com/pixantrone.html

http://www.medchemexpress.com/pixantrone-dimaleate.html

http://www.medchemexpress.com/pnu-159682.html

http://www.medchemexpress.com/Podocarpusflavone-A.html

http://www.medchemexpress.com/SN-38.html

http://www.medchemexpress.com/SW044248.html

http://www.medchemexpress.com/tas-103.html


10 mg, 50 mg, 100 mg


5 mg, 10 mg

Purity: >98%Clinical Data: Phase 2, Phase 3Size: 5 mg, 10 mg, 50 mg


10 mg, 50 mg, 100 mg



100 mg, 200 mg


50 mg


5 mg, 10 mg, 50 mg, 100 mg

Bioactivity: TAS-103 2Hcl(BMS-247615 2Hcl) is a dual inhibitor oftopoisomerase-I (topo-I) and topoisomerase-II (topoII).

Bioactivity: Teniposide(VM-26) is a semisynthetic derivative of podophyllotoxinand are increasingly used in cancer medicine; causing breaks in DNAvia an interaction with DNA topoisomerase II.

Bioactivity: Tirapazamine(SR259075; Win59075; SR4233) is an experimentalanticancer drug that is activated to a toxic radical only at very lowlevels of oxygen; a phenomenon known as tumor hypoxia.

Bioactivity: Topotecan (SKF104864) is a topoisomerase I inhibitor forchemotherapeutic agent.

Bioactivity: Topotecan hydrochloride is a inhibitor. The Topoisomerase I IC50values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells,2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and5.95±0.24 μM of GSCs-U87.

Bioactivity: Voreloxin(SNS-595; AG 7352) is a small molecule and a naphthyridineanalogue with antineoplastic activity; inhibitor of Topo II.

Bioactivity: Voreloxin (Hydrochloride) is a naphthyridine, which acts as aninhibitor of with antineoplastic activity.Topo II

Bioactivity: β-Lapachone(ARQ-501; beta-lapachone) is a naturally occurringquinone obtained from the bark of the lapacho tree (Tabebuiaavellanedae) with cancer chemopreventive properties; potentinhibitor of IDO1(IC50=0


TAS-103 dihydrochloride (BMS-247615 dihydrochloride; TAS103 dih

ydrochloride; TAS 103 dihydrochloride; BMS247615…) Cat. No.: HY-13758A

Teniposide(VM-26; VM26; VM 26) Cat. No.: HY-13761

Tirapazamine(SR259075; SR4233; Win59075) Cat. No.: HY-13767

Topotecan(SKF104864) Cat. No.: HY-13768

Topotecan Hydrochloride (SK&F 104864-A; SKF 104864A; SKFS 10486

4A; NSC 609669; Nogitecan hydrochloride) Cat. No.: HY-13768A

Voreloxin(SNS-595; Vosaroxin; AG 7352) Cat. No.: HY-10534

Voreloxin Hydrochloride (SNS-595 Hydrochloride; Vosaroxin Hydro

chloride; AG 7352 Hydrochloride) Cat. No.: HY-16518

β-Lapachone (ARQ-501; NSC-26326; NSC-629749; SL-11001; beta-lapach

one) Cat. No.: HY-13555

http://www.medchemexpress.com/TAS-103-dihydrochloride.html

http://www.medchemexpress.com/Teniposide.html

http://www.medchemexpress.com/Tirapazamine.html

http://www.medchemexpress.com/topotecan.html

http://www.medchemexpress.com/Topotecan-Hydrochloride.html

http://www.medchemexpress.com/voreloxin.html

http://www.medchemexpress.com/Voreloxin-Hydrochloride.html

http://www.medchemexpress.com/_beta_-Lapachone.html


Wee1

Wee1 is a nuclear kinase belonging to the Ser/Thr 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 checkpoint,2DNA damage checkpoint. Wee1 is shown to phosphorylate histone

H2B at tyrosine 37 residue which regulates global expression of histones.

http://www.medchemexpress.com/Targets/Wee1.html


5 mg, 10 mg, 50 mg, 100 mg

Wee1 Inhibitors & Modulators

Bioactivity: MK-1775 is a potent inhibitor with of 5.2 nM.Wee1 IC50


MK-1775(AZD-1775; AZD1775; AZD 1775) Cat. No.: HY-10993

http://www.medchemexpress.com/Targets/Wee1.html


Cell Cycle/DNA Damage - MedchemExpress.com · Antifolates are compounds that antagonise the actions of folic acid (vitamin B9). Folic acid's primary function in the body is as a cofactor

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