Bioactivity ON123300 is a potent inhibitor of CDK4 with an IC50 of 38nM with little inhibitory activity against CDKs 125 and 8
Bioactivity Palbociclib (PD 0332991) is a selective and CDK4 CDK6inhibitor with s of 11 and 16 nM respectivelyIC50Palbociclib is a drug for the treatment of ER-positive andHER2-negative breast cancer
Bioactivity Palbociclib hydrochloride is a highly selective CDK46inhibitor with s of 11 nM and 16 nM respectivelyIC50
Bioactivity Palbociclib isethionate is a highly selective inhibitorof with s of 11 nM16 nMCDK46 IC50respectively
Bioactivity PF-06873600 is a selective and orally bioavailable inhibitorof cyclin-dependent kinase with values of 009 nM(CDK) Ki013 nM and 016 nM for CDK2 CDK4 and CDK6 respectivelyPF-06873600 has potential antineoplastic activity [1] [2]
Bioactivity PHA-767491 is a dual inhibitor with s of 10 nMCdc7Cdk9 IC50and 34 nM respectively
Bioactivity PHA-767491 hydrochloride is a dual inhibitor withCdc7Cdk9s of 10 nM and 34 nM respectivelyIC50
Bioactivity PHA-793887 is a potent ATP-competitive inhibitor canCDKinhibit Cdk2 Cdk1 Cdk4 and Cdk9 with s of 8 nM 60 nMIC5062 nM and 138 nM respectively and also inhibits glycogensynthase kinase 3β with an of 79 nMIC50
Bioactivity PROTAC CDK9 Degrader-1 is a selective degraderCDK9 Bioactivity Purvalanol A is a potent inhibitor which inhibitsCDKcdc2-cyclin B cdk2-cyclin A cdk2-cyclin E cdk4-cyclin D1and cdk5-p35 with s of 4 70 35 850 75 nMIC50resepctively
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9900Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg 500 mg
Purity 9983Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9955Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg
Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Bioactivity Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitorwith IC50 values of 6 6 9 gt 10000 and 6 nM forcdc2cyclin B cdk2cyclin A cdk2cyclin E cdk4cyclin D1and cdk5-p35 respectively
Bioactivity R547 is a potent ATP-competitive inhibitor of CDK124 with Kiof 2 nM3 nM1 nM
Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2
and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip
Bioactivity RGB-286638 is a inhibitor that inhibits the kinaseCDKactivity of cyclin T1-CDK9 cyclin B1-CDK1 cyclin E-CDK2
and with s of 1cyclin D1-CDK4 cyclin E-CDK3 p35-CDK5 IC502 3 4 5 and 5 nM respectively also inhibits GSK-3β TAhellip
Bioactivity Ribociclib (LEE011) is a highly specific inhibitorCDK46with s of 10 nM and 39 nM respectivelyIC50
Bioactivity Ribociclib hydrochloride (LEE011 hydrochloride) is a highlyspecific inhibitor with values of 10 nM and 39CDK46 IC50nM respectively and is over 1000-fold less potent againstthe cyclin BCDK1 complex
Bioactivity Ribociclib succinate (LEE011 succinate) is a highly specific inhibitor with values of 10 nM and 39 nMCDK46 IC50
respectively and is over 1000-fold less potent against thecyclin BCDK1 complex
Bioactivity Ribociclib succinate hydrate (LEE011 succinate hydrate) is ahighly specific inhibitor with values of 10 nMCDK46 IC50and 39 nM respectively and is over 1000-fold less potentagainst the cyclin BCDK1 complex
Bioactivity Riviciclib (P276-00 free base) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1
and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50
and 79 nM respectively Riviciclib shows antituhellip[1] [2]
Bioactivity Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent inhibitor which inhibits kinase (CDK) CDK9-cyclinT1
and with s of 20 nM 63 nMCDK4-cyclin D1 CDK1-cyclinB IC50
and 79 nM respectively Riviciclib hydrochlorhellip[1] [2]
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Purvalanol B (NG 95) Cat No HY-18299
R547 Cat No HY-10014
RGB-286638 Cat No HY-15504
RGB-286638 free base Cat No HY-15504A
Ribociclib (LEE011) Cat No HY-15777
Ribociclib hydrochloride (LEE011 (hydrochloride)) Cat No HY-15777A
Ribociclib succinate (LEE011 (succinate)) Cat No HY-15777B
Ribociclib succinate hydrate (LEE011 (succinate hydrate)) Cat No HY-15777C
Riviciclib (P276-00 (free base)) Cat No HY-16559A
Riviciclib hydrochloride (P276-00) Cat No HY-16559
wwwMedChemExpresscom 31
Purity 9850Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9907Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg
Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg 100 mg
Purity 9994Clinical Data Phase 2Size 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 200 mg
Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9980Clinical Data No Development ReportedSize 5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg
Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9677Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity Ro-3306 is a potent and selective inhibitor of with sCDK1 Kiof 20 nM 35 nM and 340 nM for CDK1 CDK1cyclin B1 andCDK2cyclin E respectively
Bioactivity Roniciclib is an orally bioavailable pan-cyclin dependentkinase inhibitor with of 5-25 nM for CDK1 CDK2(CDK) IC s50CDK3 CDK4 CDK7 and CDK9
Bioactivity SB1317 is a potent inhibitor of and forCDK2 JAK2 FLT3the treatment of cancer with of 13 73 and 56 nM forIC50CDK2 JAK2 and FLT3 respectively
Bioactivity SEL120-34A is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity
Bioactivity SEL120-34A HCl is a potent selective orally availableATP-competitive inhibitor with s of 44 nM and 104CDK8 IC50nM for CDK8CycC and CDK19CycC respectively with antitumoractivity
Bioactivity SEL120-34A monohydrochloride is an ATP-competitive andselective inhibitor inhibits kinase activities ofCDK8CDK8CycC and CDK19CycC complexes with s of 44 nM andIC50104 nM respectively with a of 3 nM for CDhellipKd
Bioactivity Seliciclib (Roscovitine) is a potent and selective CDKsinhibitor with s of 02 μM 065 μM and 07 μM for IC50 CDK5
and respectivelyCdc2 CDK2
Bioactivity Senexin A is a inhibitor with an of 280 nMCDK8 IC50
Bioactivity Simurosertib (TAK-931) is a selective cycle 7 kinase(CDC7)inhibitor with an lt03 nMIC50
Bioactivity SNS-032 (BMS-387032) is a selective inhibitor of CDK2 and with s of 38 nM 62 nM and 4CDK7 CDK9 IC50
nM respectively
Ro-3306 Cat No HY-12529
Roniciclib (BAY 1000394) Cat No HY-13914
SB1317 (TG02) Cat No HY-15166
SEL120-34A Cat No HY-111388
SEL120-34A HCl Cat No HY-111388B
SEL120-34A monohydrochloride Cat No HY-111388A
Seliciclib (Roscovitine CYC202 R-roscovitine) Cat No HY-30237
Senexin A Cat No HY-15681
Simurosertib (TAK-931) Cat No HY-100888
SNS-032 (BMS-387032) Cat No HY-10008
Purity 9846Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9796Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9870Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9882Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg
Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Bioactivity SU9516 is a potent inhibitor with an of 22 nM andCDK2 IC50also shows inhibitory effects on CDK1 and CDK4 with s ofIC5040 200 nM respectively
Bioactivity SY-1365 is a highly selective covalent inhibitor of CDK7SY-1365 possesses therapeutic potential in both hematologicaland solid tumors [1]
Bioactivity T025 is an orally available and highly potent Cdc2-like kinase inhibitor with s of 48 0096 65 and 061 nM(CLK) Kd
for CLK1 CLK2 CLK3 and CLK4 respectively
Bioactivity THAL-SNS-032 is a selective degrader PROTAC consistingCDK9of a CDK-binding SNS-032 ligand linked to a thalidomidederivative that binds the E3 ubiquitin ligase Cereblon (CRBN)
[1]
Bioactivity THZ1 is a selective and potent covalent inhibitor withCDK7an of 32 nMIC50
Bioactivity THZ1 Hydrochloride is a selective and potent inhibitorCDK7with an of 32 nMIC50
Bioactivity THZ1-R is a non-cysteine reactive analog of THZ1 whichdisplays diminished activity for inhibition THZ1-RCDK7binds to with a of 142 nMCDK7 Kd
Bioactivity THZ2 is a potent and selective inhibitor with an ofCDK7 IC50139 nM
Bioactivity THZ531 is a covalent inhibitor of both and withCDK12 CDK13s of 158 nM and 69 nM respectivelyIC50
Bioactivity Trilaciclib is a inhibitor with s of 1 nM and 4 nMCDK46 IC50for CDK4 and CDK6 respectively
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
SU9516 Cat No HY-18629
SY-1365 Cat No HY-128587
T025 Cat No HY-112296
THAL-SNS-032 Cat No HY-123937
THZ1 Cat No HY-80013
THZ1 Hydrochloride Cat No HY-80013A
THZ1-R Cat No HY-19988
THZ2 Cat No HY-12280
THZ531 Cat No HY-103618
Trilaciclib (G1T28) Cat No HY-101467
wwwMedChemExpresscom 33
Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9924Clinical Data Phase 2Size 10mM x 1mL in Water
5 mg 10 mg 50 mg 100 mg
Bioactivity Trilaciclib hydrochloride is a inhibitor with s ofCDK46 IC501 nM and 4 nM for CDK4 and CDK6 respectively
Bioactivity Voruciclib hydrochloride is a clinical stage oral CDK9inhibitor Voruciclib hydrochloride represses expression ofMCL-1 in multiple models of diffuse large B-cell lymphoma(DLBCL) [1]
Bioactivity Wogonin is a naturally occurring mono-flavonoid can inhibitthe activity of and and exhibitsCDK8 Wntanti-inflammatory and anti-tumor effects
Bioactivity XL413 is a potent selective and ATP competitive inhibitor of with an of 34 nM and also shows potent effectCdc7 IC50
with s of 215 42 nM on CK2 PIM1 respectively and anIC50 of 118 nM on pMCMEC50
Bioactivity XL413 hydrochloride is a potent selective and ATP competitiveinhibitor of with an of 34 nM and also showsCdc7 IC50potent effect with s of 215 42 nM on CK2 PIM1IC50respectively and an of 118 nM on pMCMEC50
Trilaciclib hydrochloride (G1T28 hydrochloride) Cat No HY-101467A
Voruciclib hydrochloride Cat No HY-12422A
Wogonin Cat No HY-N0400
XL413 Cat No HY-15260
XL413 hydrochloride Cat No HY-15260A
Checkpoint Kinase (Chk)
Checkpoint Kinases (Chk) are protein kinases that are involved in cellcycle control Two checkpoint kinase subtypes have been identifiedChk1 and Chk2 Chk1 is a central component of genome surveillancepathways and is a key regulator of the cell cycle and cell survivalChk1 is required for the initiation of DNA damage checkpoints andhas recently been shown to play a role in the normal (unperturbed)cell cycle Chk1 impacts various stages of the cell cycle including the Sphase G2M transition and M phase In addition to mediating cellcycle checkpoints Chk1 also contributes to DNA repair processesgene transcription embryo development cellular responses to HIVinfection and somatic cell viability Chk2 is a protein kinase that is
activated in response to DNA damage and is involved in cell cycle arrest In response to DNA damage and replicationblocks cell cycle progression is halted through the control of cell cycle regulators The protein encoded by this gene isa cell cycle checkpoint regulator and putative tumor suppressor
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
wwwMedChemExpresscom 35
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9877Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg
Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9990Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Checkpoint Kinase (Chk) Inhibitors amp Modulators
Bioactivity AZD-7762 is a potent ATP-competitive checkpoint kinase ( )Chkinhibitor in with an of 5 nM for Chk1IC50
Bioactivity BML-277 is a selective checkpoint kinase 2 ( ) inhibitorChk2with an of 15 nMIC50
Bioactivity CCT241533 is a potent and selective ATP competitive inhibitorof with an of 3 nM and of 116 nMCHK2 IC50 Ki
Bioactivity CCT241533 hydrochloride is a potent and selective CHK2inhibitor with an of 3 nM and a of 116 nMIC50 Ki
Bioactivity CCT244747 is a potent orally bioavailable and highlyselective inhibitor with an of 77 nM CCT244747CHK1 IC50also abrogates G2 checkpoint with an of 29 nMIC50
Bioactivity CCT245737 is a orally active and seletive inhibitorChk1with an of 13 nMIC50
Bioactivity CHIR-124 is a potent and selective inhibitor with Chk1 IC50of 03 nM and also potently targets and withPDGFR FLT3
s of 66 nM and 58 nMIC50
Bioactivity CHK-IN-1 is an inhibitor of and withCHK1 CHK2anti-proliferative activities
Bioactivity CHK1 inhibitor is an inhibitor of CHK1 Bioactivity CHK1-IN-2 is a checkpoint kinase 1 inhibitor with an(CHK1) of 6 nMIC50
AZD-7762 Cat No HY-10992
BML-277 (Chk2 Inhibitor II) Cat No HY-13946
CCT241533 Cat No HY-14715
CCT241533 hydrochloride Cat No HY-14715B
CCT244747 Cat No HY-18175
CCT245737 Cat No HY-18958
CHIR-124 Cat No HY-13263
CHK-IN-1 Cat No HY-U00345
CHK1 inhibitor Cat No HY-104022
CHK1-IN-2 Cat No HY-111369
Purity 9965Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9969Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9941Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9791Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9807Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg
Bioactivity CHK1-IN-3 is a inhibitor with anCheckpoint Kinase 1 (CHK1) of 04 nM IC50
[1]Bioactivity GDC-0575 (ARRY-575 RG7741) is a highly-selective oral
small-molecule inhibitor with an of 12nMChk1 IC50
Bioactivity GDC-0575 dihydrochloride is an orally bioavailable CHK1inhibitor with an of 12 nM and has antitumor activityIC50
Bioactivity PF 477736 is a potent selective ATP-competitive inhibitor of with a of 049 nM 100-fold selectivity versus Chk1 Ki Chk2
( 47 nM)Ki
Bioactivity Prexasertib (LY2606368) is a potent selective andATP-competitive inhibitor with ancheckpoint kinase 1 (Chk1)
and a of lt1 nM and 09 nM respectivelyIC50 Ki
Bioactivity Prexasertib dihydrochloride (LY2606368 dihydrochloride) is apotent and selective ATP competitive inhibitor of the Chk1protein kinase with s of lt1 nM and 8 nM for CHK1 andIC50CHK2 respectively and a of 09 nM against purified CHK1Ki
Bioactivity Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is apotent selective ATP competitive and inhibitorCHK1 CHK2with a of 09 nM for CHK1 and s of lt1 nM 8 nM forKi IC50CHK1 and CHK2 respectively Prexasertib Mesylate Hydrateinhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2hellip
Bioactivity Rabusertib (LY2603618) is a potent and selective inhibitor of with an of 7 nMChk1 IC50
Bioactivity SCH900776 is a potent selective and oral inhibitor ofcheckpoint kinase1 ( ) with an of 3 nM It shows 50-Chk1 IC50and 500-fold selectivity over CDK2 andChk2 respectively
36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
CHK1-IN-3 Cat No HY-128601
GDC-0575 (ARRY-575 RG7741) Cat No HY-112167
GDC-0575 dihydrochloride (ARRY-575 dihydrochloride RG7741 dihydrochloride) Cat No HY-112167A
PF 477736 (PF 00477736) Cat No HY-10032
Prexasertib (LY2606368) Cat No HY-18174
Prexasertib dihydrochloride (LY2606368 (dihydrochloride)) Cat No HY-18174A
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate LY2940930) Cat No HY-18174B
Rabusertib (LY2603618 IC-83) Cat No HY-14720
SCH900776 (MK-8776) Cat No HY-15532
wwwMedChemExpresscom 37
CRISPRCas9
CRISPRCas9 (Clustered Regularly-Interspaced Short PalindromicRepeatsCas9) is a bacterial immune system that has been adaptedfor genome editing in mammalian cells Cas9 is a programmablenuclease that generates double-stranded breaks (DSB) in DNAdictated by binding of a ~20 nucleotide recombinant ldquoguide RNArdquo(gRNA) to the target site DSBrsquos produced by Cas9 are most oftenrepaired through the cellrsquos error-prone non-homologous end joining(NHEJ) pathway resulting in small insertions or deletions (indels) Thevast majority of indels shift the reading frame introducing apremature stop codon or resulting in nonsense mediated decay ofthe mRNA-effectively ldquoknocking outrdquo a gene
The CRISPRCas9 system has substantially advanced efforts in specific gene editing and has been successfully appliedto modify the episomal genomes of human and other organisms The CRISPRCas9 system utilizes a prokaryoticRNA-guided programmable nuclease that can make a double-strand DNA break (DSB) at a specific site under theguidance of a leading RNA This DSB process depends on the co-expression of two basic components a guide RNA(gRNA) and Cas9 nuclease Making a specific DSB can trigger DNA repair via either error-prone non-homologous endjoining (NHEJ) or homology-directed repair (HDR) In the presence of the CRISPRCas9 system the NHEJ inhibitorSCR7 is proven to increase the efficiency of Cas9-mediated HDR by at least by 7-fold in mammalian cells Genomeediting via CRISPRCas9 has become an efficient and reliable way to make precise targeted changes to the genome ofliving cells
Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9979Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
CRISPRCas9 Inhibitors amp Modulators
Bioactivity Brefeldin A is a specific inhibitor of whichprotein traffickingblocks the protein transport from the endoplasmic reticulum tothe Golgi complex
Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR
Bioactivity L755507 is a potent selective agonist of with an β -AR3 IC50of 35 nM
Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule
microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9
Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9
Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]
Bioactivity Zidovudine is a nucleoside reverse transcriptase inhibitor () widely used to treat HIV infection Zidovudine increasesNRTI
CRISPRCas9-mediated editing frequency
38 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Brefeldin A (BFA Cyanein Decumbin) Cat No HY-16592
KU-57788 (NU7441) Cat No HY-11006
L755507 Cat No HY-19334
Nocodazole (Oncodazole R17934) Cat No HY-13520
RS-1 Cat No HY-19793
SCR7 Cat No HY-12742
Zidovudine (Azidothymidine AZT ZDV) Cat No HY-17413
wwwMedChemExpresscom 39
DeubiquitinaseDUBs
Deubiquitinases (DUBs) are a large group of proteases that cleaveubiquitin from proteins and other molecules Ubiquitin is attached toproteins in order to regulate the degradation of proteins via theproteasome and lysosome coordinate thecellular localisation ofproteins activate and inactivate proteins and modulateprotein-protein interactions DUBs can reverse these effects bycleaving the peptide or isopeptide bond between ubiquitin and itssubstrate protein In humans there are nearly 100 DUB genes whichcan be classified into two main classes cysteine proteases andmetalloproteases The cysteine proteases comprise ubiquitin-specificproteases (USPs) ubiquitin C-terminal hydrolases (UCHs)
Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU) The metalloprotease groupcontains only the Jab1Mov34Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases DUBs play several roles inthe ubiquitin pathway One of the best characterised functions of DUBs is the removal of monoubiqutin andpolyubiquitin chainsfrom proteins
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9940Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9892Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9893Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 25 mg 50 mg 100 mg 200 mg 500 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Deubiquitinase Inhibitors amp Modulators
Bioactivity 6-Thioguanine (Thioguanine) is an anti-leukemia andimmunosuppressant agent acts as an inhibitor of SARS and MERScoronavirus papain-like proteases ( ) and also potentlyPLprosinhibits activity with s of 25 μM and 40 μM forUSP2 IC50Plpros and recombinant human USP2 respectively
Bioactivity b-AP15 is a specific inhibitor of the enzymesdeubiquitinating and UCHL5 Usp14
Bioactivity BAY 11-7082 is a inhibitor which decreases NF-κB byNF-κBinhibiting TNF-α-induced phosphorylation of IκB-α BAY 11-7082inhibits ubiquitin-specific protease and withUSP7 USP21
s of 019 μM and 096 μM respectivelyIC50
Bioactivity C527 is a is a pan inhibitor with a highDUB enzymepotency for the complex ( =088 μM)USP1UAF1 IC50
Bioactivity Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB)inhibitor directly inhibiting DUB activity of USP9x USP5USP14 and UCH37 Degrasyn has been shown to downregulate theantiapoptotic proteins and Bcr-Abl JAK2
Bioactivity DUBs-IN-1 is an active inhibitor of ubiquitin-specific with an of 024 μM for USP8proteases (USPs) IC50
Bioactivity DUBs-IN-2 is a potent inhibitor with an ofdeubiquitinase IC50028 μM for USP8
Bioactivity DUBs-IN-3 is a potent enzyme inhibitordeubiquitinase (USP)extracted from reference compound 22c with an of 056 μMIC50for USP8
Bioactivity EOAI3402143 is a ( ) inhibitor whichdeubiquitinase DUBinhibits dose-dependently inhibits and Usp9x Usp24 Usp5
Bioactivity FT671 is a potent non-covalent and selective inhibitorUSP7with an of 52 nM and binds to the USP7 catalytic domainIC50with a of 65 nMKd
40 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
6-Thioguanine (Thioguanine2-Amino-6-purinethiol) Cat No HY-13765
b-AP15 (NSC 687852) Cat No HY-13989
BAY 11-7082 (BAY 11-7821) Cat No HY-13453
C527 Cat No HY-12988
Degrasyn (WP1130) Cat No HY-13264
DUBs-IN-1 Cat No HY-50736
DUBs-IN-2 Cat No HY-50737A
DUBs-IN-3 Cat No HY-50737
EOAI3402143 Cat No HY-111408
FT671 Cat No HY-107985
wwwMedChemExpresscom 41
Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9773Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9684Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Bioactivity FT827 is a selective and covalent ubiquitin-specific protease7 ( ) inhibitor with an of 52 nMUSP7 IC50
Bioactivity GNE-6640 is a selective and non-covalent inhibitor ofubiquitin epecific peptidase 7 with values of(USP7) IC50075 μM 043 μM 203 μM and 023 μM for full length USP7USP7 catalytic domain full length USP43 and Ub-MDM2respectively
Bioactivity GNE-6776 is a selective inhibitorUSP7 Bioactivity HBX 19818 is a specific inhibitor of ubiquitin-specific with an of 281 μMprotease 7 (USP7) IC50
Bioactivity IU1 is a special inhibitor with of 4-5 μMUsp14 IC50 Bioactivity IU1-47 is a potent inhibitor with an of 06 μMUSP14 IC50
IU1-47 induces tau elimination in cultured neurons [1]
Bioactivity LDN-57444 is a reversible competitive and site-directedinhibitor of withubiquitin C-terminal hydrolase L1 (UCH-L1)an of 088 μM and a of 040 μM LDN-57444 alsoIC50 Kisuppresses UCH-L3 activity with an of 25 μMIC50
Bioactivity MF-094 is a potent and selective inhibitor with an USP30 IC50of 120 nM
Bioactivity ML-323 is a reversible potent inhibitor with USP1-UAF1 IC50of 76 nM in a Ub-Rho assay The measured inhibition constantsof ML-323 for the free enzyme ( ) is 68 nMKi
Bioactivity ML364 is an inhibitor of ubiquitin specific peptidase 2 and can be used for the research of breast cancer(USP2)
extracted from patent WO 2016134026 A1 compound Figure 10G
FT827 Cat No HY-111350
GNE-6640 Cat No HY-112937
GNE-6776 Cat No HY-107986
HBX 19818 Cat No HY-17540
IU1 Cat No HY-13817
IU1-47 Cat No HY-122243
LDN-57444 Cat No HY-18637
MF-094 Cat No HY-112438
ML-323 Cat No HY-17543
ML364 Cat No HY-100900
Purity 9800Clinical Data Phase 2Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9737Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9881Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9843Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Bioactivity NSC632839 is a nonselective isopeptidase inhibitor whichinhibits and with s of 45plusmn4 μMUSP2 USP7 SENP2 EC5037plusmn1 μM and 98plusmn18 μM respectively
Bioactivity P 22077 is a cell-permeable ubiquitin-specific protease 7 inhibitor with an of 801 μM It also inhibits(USP7) EC50
USP47 with an of 874 μMEC50
Bioactivity P005091 is a selective and potent inhibitor of with anubiquitin-specific protease 7 (USP7)
of 42 μMEC50
Bioactivity PR-619 is a broad-range inhibitor with of 393DUB EC5049 686 72 and 861 μM for USP4 USP8 USP7 USP2and respectivelyUSP5
Bioactivity SJB2-043 is an inhibitor of the native complex withUSP1UAF1 of 544 nMIC50
Bioactivity SJB3-019A is a potent and novel inhibitor 5 times moreUSP1potent than SJB2-043 in promoting ID1 degradation andcytoxicity in K562 cells with of 00781 μMIC50
Bioactivity USP7-IN-1 is a selective and reversible inhibitor of with an of 77 μMubiquitin-specific protease 7 (USP7) IC50
and can be used for the research of cancer
Bioactivity USP7-IN-3 (Compound 5) is a potent and selective allostericubiquitin-specific protease 7 ( ) inhibitor USP7 [1]
Bioactivity USP7USP47 inhibitor is a selective ubiquitin-specific protease inhibitor with s of 042 μM and 10747 (USP7USP47) EC50
μM respectively
Bioactivity VLX1570 is a competitive inhibitor of proteasomedeubiquitinases ( ) with an of approximate 10 μMDUBs IC50
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NSC632839 Cat No HY-100708
P 22077 Cat No HY-13865
P005091 (P5091) Cat No HY-15667
PR-619 Cat No HY-13814
SJB2-043 Cat No HY-15757
SJB3-019A Cat No HY-80012
USP7-IN-1 Cat No HY-16709
USP7-IN-3 Cat No HY-112128
USP7USP47 inhibitor Cat No HY-13487
VLX1570 Cat No HY-12471
wwwMedChemExpresscom 43
DNA AlkylatorCrosslinker
DNA alkylatorcrosslinker is a molecule that alkylates DNA or cancross link with DNA DNA alkylatorcrosslinker can have mutagenicpharmaceutical or other effects Alkylation is the transfer of an alkylgroup from one molecule to another The alkyl group may betransferred as an alkyl carbocation a free radical a carbanion or acarbene Alkylating agents are widely used in chemistry because thealkyl group is probably the most common group encountered inorganic molecules Selective alkylation or adding parts to the chainwith the desired functional groups is used especially if there is nocommonly available biological precursor Alkylation with only onecarbon is termed methylation In medicine alkylation of DNA is used
in chemotherapy to damage the DNA of cancer cells Alkylation is accomplished with the class of drugs calledalkylating antineoplastic agents Crosslinking of DNA occurs when various exogenous or endogenous agents reactwith two different positions in the DNA This can either occur in the same strand (intrastrand crosslink) or in theopposite strands of the DNA (interstrand crosslink) Crosslinks also occur between DNA and protein DNA replicationis blocked by crosslinks which causes replication arrest and cell death if the crosslink is not repaired The RAD51family plays a role in repair
Purity 990Clinical Data LaunchedSize 100 mg 500 mg
Purity 9879Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9985Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg
Purity 9844Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
25 mg 100 mg 200 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity gt98Clinical Data LaunchedSize 100 mg 500 mg
Purity 9961Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
DNA AlkylatorCrosslinker Inhibitors amp Modulators
Bioactivity Altretamine is an antineoplastic agentalkylating Bioactivity Altretamine hydrochloride is an antineoplasticalkylatingagent
Bioactivity Bendamustine D4 is the deuterium labeled BendamustineBendamustine is a agent that causes DNADNA cross-linkingbreaks with alkylating and antimetabolite properties
Bioactivity Bendamustine hydrochloride is a agent thatDNA cross-linkingcauses DNA breaks with alkylating and antimetaboliteproperties
Bioactivity Busulfan is a potent with selective immunosuppressivealkylatoreffect on bone marrow
Bioactivity Calicheamicin is a cytotoxic agent that causes double-strandDNA breaks
Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent
Bioactivity Carmustine is an antitumor chemotherapeutic agent which worksby akylating DNA and RNA
Bioactivity Chlorambucil is an agent with antitumor activityalkylating Bioactivity Cisplatin is a antineoplastic chemotherapy drug which works bycross-linking with and causing DNA damage in cancerDNAcells
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Altretamine (ENT-50852 RB-1515 WR-95704) Cat No HY-B0181
Altretamine hydrochloride (ENT-50852 hydrochloride RB-1515
hydrochloride WR-95704 hydrochloride) Cat No HY-B0181A
Bendamustine D4 (SDX-105 D4) Cat No HY-13567S
Bendamustine hydrochloride (SDX-105 EP-3101) Cat No HY-B0077
Busulfan Cat No HY-B0245
Calicheamicin (Calicheamicin γ1) Cat No HY-19609
Carboplatin (NSC 241240) Cat No HY-17393
Carmustine Cat No HY-13585
Chlorambucil (CB-1348 WR-139013) Cat No HY-13593
Cisplatin (CDDP cis-Diaminodichloroplatinum) Cat No HY-17394
wwwMedChemExpresscom 45
Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg 500 mg
Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
50 mg 100 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 100 mg 500 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
200 mg 500 mg
Purity 980Clinical Data LaunchedSize 200 mg 500 mg
Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg
Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg
Purity 980Clinical Data LaunchedSize 100 mg 200 mg 500 mg
Bioactivity Cyclophosphamide is a synthetic agent chemicallyalkylatingrelated to the nitrogen mustards with antineoplastic andimmunosuppressive activities
Bioactivity Cyclophosphamide hydrate is a synthetic agentalkylatingchemically related to the nitrogen mustards withantineoplastic and immunosuppressive activities
Bioactivity Fotemustine is a agent with antitumor activityDNA-alkylating Bioactivity Ifosfamide is an chemotherapeutic agent withalkylatingactivity against a wide range of tumors
Bioactivity Lomustine (CCNU) is a agent with antitumorDNA alkylatingactivity
Bioactivity Melphalan is an effective agent with potentDNA alkylatingantitumor activity
Bioactivity Methylnitronitrosoguanidine (MNNG) is an agent withalkylatingtoxic and mutagenic effects [1]
Bioactivity Miriplatin is a chemotherapy agent which belongs to the classof agentsalkylating
Bioactivity Miriplatin hydrate is a chemotherapy agent which belongs tothe class of agentsalkylating
Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging
Cyclophosphamide Cat No HY-17420
Cyclophosphamide hydrate (Cyclophosphamide monohydrate) Cat No HY-17420A
Fotemustine (S10036) Cat No HY-B0733
Ifosfamide Cat No HY-17419
Lomustine (CCNU NSC 79037) Cat No HY-13669
Melphalan (L-PAM) Cat No HY-17575
Methylnitronitrosoguanidine (MNNG) Cat No HY-128612
Miriplatin (SM-11355) Cat No HY-16325A
Miriplatin hydrate (SM-11355 (hydrate)) Cat No HY-16325
Mitomycin C (Ametycine) Cat No HY-13316
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg
Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 200 mg 500 mg 1 g
Purity 9958Clinical Data LaunchedSize 100 mg 500 mg
Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity 9926Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 950Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9986Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg
Bioactivity Oxaliplatin is a inhibitor It causes DNADNA synthesiscrosslinking damage prevents DNA replication andtranscription and causes cell death
Bioactivity Palifosfamide is a novel DNA alkylator and the activemetabolite of ifosfamide with antitumor activity
Bioactivity Procarbazine Hydrochloride is an agent withalkylatinganticancer activity
Bioactivity RITA is an inhibitor of binds top53-HDM-2 interactionp53dN with a of 15 nM and also induces Kd DNA-DNA
cross-links
Bioactivity Satraplatin is an agent with potent antitumoralkylatingeffect
Bioactivity SJG-136 is a agent with an of 45 nMDNA cross-linking XL50for pBR322 DNA SJG-136 has potent antitumor activity
Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively
Bioactivity Temozolomide (NSC 362856 CCRG 81045) is an oral DNA agent used to treat some brain cancersalkylating
Bioactivity Thio-TEPA is a agent with antitumor activityDNA alkylating Bioactivity Treosulfan (NSC 39069Treosulphan) is an agent withalkylatingactivity in ovarian cancer and other solid tumor types
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Oxaliplatin Cat No HY-17371
Palifosfamide (Isophosphoramide mustard IPM ZIO-201) Cat No HY-14798
Procarbazine Hydrochloride Cat No HY-13733
RITA (NSC 652287) Cat No HY-13424
Satraplatin (BMS182751 BMY45594 JM216) Cat No HY-17576
SJG-136 (NSC-694501) Cat No HY-14573
Streptozocin (Streptozotocin U 9889) Cat No HY-13753
Temozolomide (NSC 362856 CCRG 81045 TMZ) Cat No HY-17364
Thio-TEPA Cat No HY-17574
Treosulfan (NSC 39069 Treosulphan) Cat No HY-16503
wwwMedChemExpresscom 47
Purity 980Clinical Data Phase 3Size 10mM x 1mL in Water
5 mg 10 mg 50 mg
Purity 9848Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity Uramustine is an oral agent effective in thealkylatingtreatment of lymphosarcoma chronic lymphatic leukaemia andthrombocythemia
Bioactivity VAL-083 is an agent that creates N7 methylation onalkylatingDNA with antitumor activity
Uramustine (Uracil mustard) Cat No HY-13544
VAL-083 (Dianhydrodulcitol Dianhydrogalactitol) Cat No HY-16513
DNA-PKDNA-dependent protein kinase
DNA-PKcs (DNA-dependent protein kinase catalytic subunit) is anenzyme that in humans is encoded by the PRKDC gene DNA-PKcsbelongs to the phosphatidylinositol 3-kinase-related kinase proteinfamily DNA-PKcs is the catalytic subunit of a nuclear DNA-dependentserinethreonine protein kinase called DNA-PK The secondcomponent is the autoimmune antigen Ku On its own DNA-PKcs isinactive and relies on Ku to direct it to DNA ends and trigger itskinase activity DNA-PKcs is required for the non-homologous endjoining (NHEJ) pathway of DNA repair Many proteins have beenidentified as substrates for the kinase activity of DNA-PKAutophosphorylation of DNA-PKcs appears to play a key role in NHEJ
and is thought to induce a conformational change that allows end processing enzymes to access the ends of thedouble-strand break DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNAdamage checkpoint
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Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9943Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9977Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9722Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9664Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9239Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg
DNA-PK Inhibitors amp Modulators
Bioactivity (R)-Nedisertib ((R)-M3814) is a less active R-enantiomer ofNedisertib with an in the range of 7-30 nM for IC50 DNA-PK
[1]
Bioactivity AZD-7648 is a potent and selective inhibitorDNA-PKAnti-tumor activity [1]
Bioactivity CC-115 is a potent and dual and kinaseDNA-PK mTORinhibitor with s of 13 nM and 21 nM respectively CC-115IC50blocks both and signalingmTORC1 mTORC2
Bioactivity CC-115 hydrochloride is a potent and dual and DNA-PK mTORkinase inhibitor with s of 13 nM and 21 nM respectivelyIC50CC-115 blocks both and signalingmTORC1 mTORC2
Bioactivity Compound 401 is a synthetic inhibitor of ( = 028DNA-PK IC50μM) that also targets mTOR but not PI3K in vitro
Bioactivity KU-57788 is a potent and selective inhibitor of withDNA-PKan of 13 nM with selectivity over a range of kinasesIC50including mTOR PI 3-K ATM and ATR
Bioactivity LTURM34 is a specific inhibitor with an of 0034DNA-PK IC50μM
Bioactivity LY3023414 potently and selectively inhibits class I PI3Kisoforms and with s of 607 nM 776DNA-PK mTORC12 IC50nM 38 nM 238 nM 424 nM and 165 nM for PI3Kα PI3KβPI3Kδ PI3Kγ DNA-PK and mTOR respectively LY3023414potently inhibits at low nanomolarhellipmTORC1 2
Bioactivity Nedisertib (M3814) is a potent and selective inhibitor of ( ) with an of lt3DNA-dependent Protein Kinase DNA-PK IC50
nM
Bioactivity NU 7026 is a novel specific inhibitor with ofDNA-PK IC50023plusmn001 μM also inhibits with of 13plusmn3 μMPI3K IC50
(R)-Nedisertib ((R)-M3814) Cat No HY-101570A
AZD-7648 Cat No HY-111783
CC-115 Cat No HY-16962
CC-115 hydrochloride Cat No HY-16962A
Compound 401 Cat No HY-19341
KU-57788 (NU7441) Cat No HY-11006
LTURM34 Cat No HY-101667
LY3023414 Cat No HY-12513
Nedisertib (M3814) Cat No HY-101570
NU 7026 (DNA-PK Inhibitor II LY293646) Cat No HY-15719
Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9937Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9145Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9906Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity PI-103 is a potent and inhibitor with s of 8PI3K mTOR IC50nM 88 nM 48 nM 150 nM 20 nM and 83 nM for p110α p110β
and PI-103 also inhibitsp110δ p110γ mTORC1 mTORC2 with an of 2 nMDNA-PK IC50
Bioactivity PI-103 Hydrochloride is a dual and inhibitor withPI3K mTORs of 8 nM 88 nM 48 nM 150 nM 20 nM and 83 nM forIC50
and p110α p110β p110δ p110γ mTORC1 mTORC2PI-103 also inhibits with an of 2 nMDNA-PK IC50
Bioactivity PIK-75 is a and inhibitor which inhibits DNA-PKDNA-PK PI3K and p110γ with s of 2 58 and 76 nM respectivelyp110α IC50
PIK-75 inhibits p110α gt200-fold more potently than p110β(IC =13 μM)50
Bioactivity PIK-90 is a and inhibitor which inhibits DNA-PK PI3K p110α and with s of 11 18 and 13 nMp110γ DNA-PK IC50
respectively
Bioactivity Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib apotent inhibitor with an of lt3 nM DNA-PK IC50
[1]Bioactivity SF2523 is a highly selective and potent inhibitor of withPI3K
s of 34 nM 158 nM 9 nM 241 nM and 280 nM for IC50 PI3Kα
BRD4 and mTOR respectivelyPI3Kγ DNA-PK
Bioactivity STL127705 (Compound L) is a Ku 7080 heterodimer proteininhibitor inhibits Ku7080-DNA interaction with an ofIC5035 μM STL127705 also inhibits Ku-dependent activation ofDNA-PKCS kinase ( 25 μM) IC50
[1]
Bioactivity Torin 2 is an inhibitor with of 025 nM formTOR EC50inhibiting cellular mTOR activity and exhibits 800-foldselectivity over PI3K (EC 200 nM) Torin 2 also inhibits50
with an of 05 nM in the cell free assay TorihellipDNA-PK IC50
Bioactivity VX-984 is a potent inhibitorDNA-PK Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]
and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively
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PI-103 Cat No HY-10115
PI-103 Hydrochloride Cat No HY-10115A
PIK-75 (PIK-75 Hydrochloride) Cat No HY-13281
PIK-90 Cat No HY-12030
Rac-Nedisertib (Rac-M3814) Cat No HY-101570B
SF2523 Cat No HY-101146
STL127705 Cat No HY-122727
Torin 2 Cat No HY-13002
VX-984 (M9831) Cat No HY-19939S
Wortmannin (SL-2052 KY-12420) Cat No HY-10197
wwwMedChemExpresscom 51
Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Bioactivity YU238259 is an inhibitor of homology-dependent DNA repair () used for cancer researchHDR
YU238259 Cat No HY-19977
DNARNA Synthesis
RNA synthesis which is also called DNA transcription is a highlyselective process Transcription by RNA polymerase II extends beyondRNA synthesis towards a more active role in mRNA maturationsurveillance and export to the cytoplasmSingle-strand breaks are repaired by DNA ligase using thecomplementary strand of the double helix as a template with DNAligase creating the final phosphodiester bond to fully repair theDNADNA ligases discriminate against substrates containing RNAstrands or mismatched base pairs at positions near the ends of thenickedDNA Bleomycin (BLM) exerts its genotoxicity by generatingfree radicals whichattack C-4prime in the deoxyribose backbone of DNA
leading to opening of the ribose ring and strand breakage it is an S-independentradiomimetic agent that causesdouble-strand breaks in DNAFirst strand cDNA is synthesized using random hexamer primers and M-MuLV Reverse Transcriptase (RNase H)Second strand cDNA synthesis is subsequently performed using DNA Polymerase I and RNase H The remainingoverhangs are converted into blunt ends using exonucleasepolymerase activity After adenylation of the 3prime ends ofDNA fragments NEBNext Adaptor with hairpin loop structure is ligated to prepare the samples for hybridization Cellcycle and DNA replication are the top two pathways regulated by BET bromodomain inhibition Cycloheximide blocksthe translation of mRNA to protein
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Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
250 mg 1 g
Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9979Clinical Data No Development ReportedSize 1 mg 2 mg 5 mg
Purity 9876Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity 9989Clinical Data LaunchedSize 5 mg 10 mg 50 mg
Purity 9968Clinical Data Phase 2Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg
Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
25 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg
Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
DNARNA Synthesis Inhibitors amp Modulators
Bioactivity 2-(Methylamino)-1H-purin-6(7H)-one (N2-Methylguanine) is amodified nucleoside 2-(Methylamino)-1H-purin-6(7H)-one is anendogenous methylated nucleoside found in human fluids
Bioactivity 374-Trihydroxyflavone isolated from Rhus javanica var is a flavonoid with DNA strand-scission activityroxburghiana
[1]
Bioactivity 5-Methoxyflavone belonged to Flavonoid family is a DNApolymerase-beta inhibitor and neuroprotective agent againstbeta-amyloid toxicity possess central nervous system (CNS)depressant effect mediated through the ionotropic GABA Areceptors
Bioactivity 6-Thio-2-Deoxyguanosine is a nucleoside analogue that can beincorporated into de novo-synthesized telomeres by telomerase
Bioactivity Acelarin (NUC-1031) is a ProTide transformation andenhancement of the widely-used nucleoside analoguegemcitabine
Bioactivity Actinomycin D inhibits with an of 042 μMDNA repair IC50
Bioactivity Adenine is a purine derivative and a nucleobase with a varietyof roles in biochemistry Target Nucleosideantimetaboliteanalog Adenine is a nucleobase with a varietyof roles in biochemistry including cellular respiration inthe form of both the energy-rich adenosine triphosphate (ATP)hellip
Bioactivity alpha-Amanitin is the principal toxin of several deadlypoisonous mushrooms exerting its toxic function by inhibiting
RNA-polymerase II
Bioactivity Anisomycin is a potent inhibitor whichprotein synthesisinterferes with protein and by inhibitingDNA synthesispeptidyl transferase or the 80S ribosome system Anisomycin isa JNK activator which increases phospho-JNK
Bioactivity Beaucage reagent is found to be potent in causing DNAcleavage
2-(Methylamino)-1H-purin-6(7H)-one (N2-methylguanine) Cat No HY-101412
374-Trihydroxyflavone (5-Deoxykampferol) Cat No HY-111806
5-Methoxyflavone Cat No HY-107790
6-Thio-2-Deoxyguanosine (6-thio-dG β-TGdR) Cat No HY-18762
Acelarin (NUC-1031) Cat No HY-100885
Actinomycin D (Dactinomycin Actinomycin IV) Cat No HY-17559
Adenine (6-Aminopurine Vitamin B4) Cat No HY-B0152
alpha-Amanitin (α-Amanitin α-Amatoxin) Cat No HY-19610
Anisomycin (Flagecidin Wuningmeisu C) Cat No HY-18982
Beaucage reagent Cat No HY-100951
Purity 9847Clinical Data Phase 2Size 5 mg 10 mg 50 mg
Purity 9804Clinical Data Phase 1Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9803Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9993Clinical Data LaunchedSize 100 mg 200 mg 500 mg
Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity 9967Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9896Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water
10 mg 50 mg
Bioactivity Bleomycin sulfate is a inhibitor with potentDNA synthesisantitumor activity
Bioactivity BMH-21 is a small molecule DNA intercalator that bindsribosomal DNA and inhibits RNA polymerase I (Pol I)transcription does not cause phosphorylation of H2AX
Bioactivity Branaplam (LMI070) is a highly potent selective and orallyactive small molecule modulatorSMN2 splicing
Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase
Bioactivity Carboplatin (NSC 241240) is a inhibitor whichDNA synthesisbinds to DNA inhibits replication and transcription andinduces cell death Carboplatin (NSC 241240) is a derivativeof CDDP and a potent anti-cancer agent
Bioactivity CeMMEC1 is an inhibitor of and also has high affinityBRD4for with an of 09 μM for TAF1 and a of 18TAF1 IC50 KdμM for TAF1 (2)
Bioactivity CeMMEC13 is a potent inhibitor of bromodomain withTAF1 (2)an of 21 μMIC50
Bioactivity Chebulinic acid is a potent natural inhibitor of Mtuberculosis DNA gyrase also can inhibit SMAD-3phosphorylation inhibit H+ K+-ATPase activity
Bioactivity COH29 is a potent ribonucleotide reductase ( ) inhibitorRNRwith anticancer activity COH29 inhibits α and β subunit ofRNR with s of 16 μMIC50
Bioactivity CX-5461 is a potent and oral inhibitor ItrRNA synthesisinhibits RNA polymerase I-driven transcription of rRNA with
s of 142 113 and 54 nM in HCT-116 A375 and MIA PaCa-2IC50cells respectively
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Bleomycin sulfate Cat No HY-17565
BMH-21 Cat No HY-12484
Branaplam (LMI070 NVS-SM1) Cat No HY-19620
Capecitabine Cat No HY-B0016
Carboplatin (NSC 241240) Cat No HY-17393
CeMMEC1 Cat No HY-111445
CeMMEC13 Cat No HY-101088
Chebulinic acid Cat No HY-N2033
COH29 (RNR Inhibitor COH29) Cat No HY-19931
CX-5461 Cat No HY-13323
wwwMedChemExpresscom 55
Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9872Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water
10 mg 50 mg
Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water
10 mg 50 mg 100 mg 200 mg 500 mg
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Purity 9963Clinical Data No Development ReportedSize 10mM x 1mL in Water
1 mg 5 mg 10 mg 20 mg
Purity gt98Clinical Data LaunchedSize 100 mg 500 mg
Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg 1 g
Purity 9945Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
200 mg 500 mg
Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in Water
5 mg 10 mg 50 mg
Bioactivity CX-5461 dihydrochloride is a potent and orally bioavailableinhibitor of Pol I-mediated with s of 142rRNA synthesis IC50nM in HCT-116 113 nM in A375 and 54 nM in MIA PaCa-2 cellsand shows little or no effect on Pol II ( ge25 μM)IC50
Bioactivity Cycloheximide (Naramycin A) is an eukaryote protein synthesisinhibitor with s of 5325 nM and 2880 nM for proteinIC50synthesis and RNA synthesis respectivelyin vivo
Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase
with an of 16 nMDNA synthesis IC50
Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50
Bioactivity Datelliptium chloride is a DNA-intercalating agent derivedfrom ellipticine with anti-tumor activities
Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II
activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells
Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells
Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing
Bioactivity Didox (NSC-324360) is a synthetic (ribonucleotide reductase) inhibitorRR
Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1
CX-5461 dihydrochloride Cat No HY-13323A
Cycloheximide (Naramycin A Actidione CHX) Cat No HY-12320
Cytarabine (Cytosine β-D-arabinofuranoside Cytosine
Arabinoside Ara-C) Cat No HY-13605
Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside
hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A
Datelliptium chloride Cat No HY-U00337
Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A
Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)
Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062
Deoxycytidine triphosphate (dCTP) Cat No HY-101400
Didox (NSC-324360) Cat No HY-19387
Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity 9994Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 5 g
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water
100 mg 200 mg 500 mg 1 g
Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 200 mg 500 mg 1 g
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water
1 mg 5 mg
Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 g 10 g
Bioactivity Folic acid(Vitamin M Vitamin B9) is a B vitamin is necessaryfor the production and maintenance of new cells for DNAsynthesis and RNA synthesis
Bioactivity GC7 Sulfate is a ( ) inhibitordeoxyhypusine synthase DHPS
Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively
Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50
Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively
Bioactivity GNE-371 is a potent and selective chemical probe for thesecond bromodomains of human transcription-initiation-factor
subunit 1 and transcription-initiation-factor TFIID TFIIDsubunit 1-like with an of 10 nM for TAF1(2)IC50
Bioactivity Guanine is one of the fundamental components of nucleic acids( and ) Guanine is a purine derivative consistingDNA RNAof a fused pyrimidine-imidazole ring system with conjugateddouble bonds
Bioactivity Halofuginone (RU-19110) is a less-toxic form of Febrifuginewhich is isolated from the plant Dichroa febrifuga [1]
Halofuginone inhibits in anprolyl-tRNA synthetaseATP-dependent manner with a of 183 nM HalofuginhellipKi
[2]
Bioactivity Halofuginone hydrobromide (RU-19110 hydrobromide) is aless-toxic form of Febrifugine which is isolated from theplant Halofuginone inhibits Dichroa febrifuga [1] prolyl-tRNA
in an ATP-dependent manner with a of 183hellipsynthetase Ki
Bioactivity Hydroxyurea is a cell apoptosis inducer that inhibit DNAsynthesis through inhibition of ribonucleotide reductase
Bioactivity L189 is a novel human DNA ligase inhibitor inhibitshLigIIIIIV with IC50 of 595 μM
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Folic acid (Vitamin B9 Vitamin M) Cat No HY-16637
GC7 Sulfate Cat No HY-108314A
Gemcitabine (NSC 613327 LY188011) Cat No HY-17026
Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003
GNE-371 Cat No HY-112803
Guanine Cat No HY-Y1055
Halofuginone (RU-19110) Cat No HY-N1584
Halofuginone hydrobromide (RU-19110 (hydrobromide)) Cat No HY-N1584A
Hydroxyurea (Hydroxycarbamide) Cat No HY-B0313
L189 Cat No HY-15588
wwwMedChemExpresscom 57
Purity 990Clinical Data No Development ReportedSize 1 mg 5 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9839Clinical Data No Development ReportedSize 1 g
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water
10 mg 50 mg
Purity 9977Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
Purity 9945Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9988Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity L67 is a novel competitive human DNA ligase inhibitorinhibits DNA ligases I and III with IC50 of 10 μM and 10 μM
Bioactivity Madrasin is a potent and cell penetrant splicing inhibitorthat interferes with the early stages of spliceosome assemblyMadrasin is cytotoxic at higher concentrations although atlower concentrations it induces cell cycle arrest promotes aspecific reorganization of subnuclear protein localizationhellip
Bioactivity MB-7133 is a inhibitorDNA synthesis Bioactivity Mitomycin C is an antitumor drug and antibiotic that showsextraordinary ability to inhibit Mitomycin C isDNA synthesisa DNA cross-linking agent which induces DNA damaging
Bioactivity ML216(CID-49852229) is a potent inhibitor of the DNA unwindingactivity of BLM helicase showing similar IC50s of 30 and097 μM for full length BLM and BLM636ndash1298 respectively IC50value 30097 uM(Full length636ndash1298 BLM) Target BLMhelicase inhibitor ML216 shows cell-based activity and canhellip
Bioactivity Nedaplatin (NSC 375101D) is a derivative of cisplatin and DNAdamage agent
Bioactivity NITD008 is a potent and selective inhibitor whichflavivirusecan inhibit with an ofDengue Virus Type 2 (DENV-2) EC50064 μM
Bioactivity Oxolinic acid is a potent inhibitor of DNA gyrase and DNAsynthesis lead to DNA cleavage when extracted chromosomes areincubated with sodium dodecyl sulfate
Bioactivity Phen-DC3 is a (G4) specific ligand which canG-quadruplexinhibit and helicases with s of 65plusmn6 and 50plusmn10FANCJ DinG IC50nM respectively
Bioactivity Plicamycin is a selective specificity protein 1 ( )Sp1inhibitor Plicamycin inhibits the growth of various cancersby decreasing Sp1 protein
L67 (DNA Ligase Inhibitor) Cat No HY-15586
Madrasin (DDD00107587) Cat No HY-100236
MB-7133 Cat No HY-16311
Mitomycin C (Ametycine) Cat No HY-13316
ML216 (CID-49852229) Cat No HY-12342
Nedaplatin (NSC 375101D) Cat No HY-13700
NITD008 (7-Deaza-2-C-acetylene-adenosine) Cat No HY-12957
Oxolinic acid Cat No HY-B1002
Phen-DC3 Cat No HY-15594
Plicamycin (Mithramycin A) Cat No HY-A0122
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9762Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9958Clinical Data LaunchedSize 100 mg 500 mg
Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9931Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Bioactivity Quarfloxin (CX 3543) a fluoroquinolone derivative withantineoplastic activity targets and inhibits RNA pol Iactivity with IC values in the nanomolar range in50neuroblastoma cells Quarfloxin disrupts the interactionbetween the nucleolin protein and a G-quadruplex DNA structurehellip
Bioactivity RG7800 a small molecule splicing modifier to enterSMN2human clinical trials to treat spinal muscular atrophy
Bioactivity RG7800 hydrochloride is an orally active splicingSMN2modulator with s of 23 nM and 87 nM for EC15x SMN2
splicing and RG7800 hydrochloride has theSMN proteinpotential to treat spinal muscular atrophy
Bioactivity Risdiplam (RG7916 RO7034067) is an orally administeredcentrally and peripherally distributed pre-mRNASMN2splicing modifier that increases survival motor neuron (SMN)protein levels
Bioactivity Saccharin 1-methylimidazole is an activator for DNARNASynthesis
Bioactivity SCR7 is a inhibitor with anticancer activity andDNA Ligase IVis also a enhancer which increases the efficiencyCRISPR HDRof Cas9-mediated HDR [1] [2]
Bioactivity SMN-C3 is an orally active splicing modulator and hasSMN2the potential to treat spinal muscular atrophy (SMA)
Bioactivity Streptozocin is a potent agent with sDNA-methylating IC50of 117 904 and 1024 μgmL in HL60 K562 and C1498 cellsrespectively
Bioactivity TH287 is a potent inhibitor of MTH1 (NUDT1) with an IC50 valueof 08 nM less potent for MTH2 NUDT5 NUDT12 NUDT14 andNUDT16
Bioactivity TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) withan IC50 value of 08 nM less potent for MTH2 NUDT5 NUDT12NUDT14 and NUDT16
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Quarfloxin (CX 3543) Cat No HY-14776
RG7800 (RO6885247) Cat No HY-101792
RG7800 hydrochloride (RO6885247 hydrochloride) Cat No HY-101792A
Risdiplam (RG7916 RO7034067) Cat No HY-109101
Saccharin 1-methylimidazole Cat No HY-112060
SCR7 Cat No HY-12742
SMN-C3 Cat No HY-112633
Streptozocin (Streptozotocin U 9889) Cat No HY-13753
TH287 Cat No HY-16965
TH287 hydrochloride Cat No HY-16965A
wwwMedChemExpresscom 59
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9920Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9832Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 25 mg 50 mg 100 mg
Purity 9906Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 25 mg 50 mg 100 mg
Bioactivity TH588 is first-in-class nudix hydrolase family inhibitor thatpotently and selectively engage and inhibit the (MTH1
= 5 nM)IC50
Bioactivity TH588 hydrochloride is first-in-class nudix hydrolase familyinhibitor that potently and selectively engage and inhibit the
( = 5 nM)MTH1 IC50
Bioactivity Thiarabine (OSI-7836) shows potent anti-tumor activity andinhibition of synthesisDNA
Bioactivity Triapine is a novel inhibitor of the M2 subunit of ( ) and is a potentribonucleotide reductase RR
radiosensitizer
Bioactivity Triciribine is a inhibitor also inhibits DNA synthesis Aktand with of 130 nM and 002-046 μMHIV-12 IC50respectively
Bioactivity YK 4-279 is an inhibitor of RNA Helicase A (RHA) binding tothe oncogenic transciption factor EWS-FLI1 YK-4-279 inhibitsEwings sarcoma family tumor (ESFT) cell growth YK-4-279induces apoptosis
Bioactivity Zoliflodacin (ETX0914AZD0914) is a novelspiropyrimidinetrione bacterial DNA gyrasetopoisomeraseinhibitor Zoliflodacin has potent antibacterialin vitroactivity against Gram-positive and Gram-negative organismsincluding with the of 025 μgmLS aureus MIC90
TH588 Cat No HY-12814
TH588 hydrochloride Cat No HY-12814A
Thiarabine (OSI-7836) Cat No HY-16496
Triapine (3-AP PAN-811 OCX191 NSC663249) Cat No HY-10082
Triciribine (API-2 NSC 154020 TCN) Cat No HY-15457
YK-4-279 Cat No HY-14507
Zoliflodacin (ETX0914 AZD0914) Cat No HY-17647
Eukaryotic Initiation Factor (eIF)
Eukaryotic initiation factors (eIFs) are proteins involved in theinitiation phase of eukaryotic translation These proteins help stabilizethe formation of the functional ribosome around the start codon andalso provide regulatory mechanisms in translation initiationEukaryotic initiation factor 2B (eIF2B) is a guaninenucleotide-exchange factor which mediates the exchange of GDP(bound to initiation factor eIF2) for GTP thus regenerating the active[eIF2GTP] complex that is required for peptide-chain initiation Theactivity of eIF2B is a key control point for eukaryotic protein synthesisand is altered in response to viral infection hormones nutrientsgrowth factors and certain stresses
Eukaryotic translation initiation factor 4E (eIF4E) is best known for its function in the initiation of protein synthesis oncapped mRNAs in the cytoplasm Eukaryotic initiation factor (elF) 4A functions as a subunit of the initiation factorcomplex elF4F which mediates the binding of mRNA to the ribosome
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Purity 9800Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 2 mg
Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg
Purity 9981Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg
Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9958Clinical Data Phase 1Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Eukaryotic Initiation Factor (eIF) Inhibitors amp Modulators
Bioactivity 4E1RCat is an inhibitor of cap-dependent translation andinhibits interaction with an an of 4 μMeIF4EeIF4GI IC50
Bioactivity 4E2RCat is an inhibitor of interaction with an eIF4E-eIF4G IC50of 135 μM
Bioactivity 4EGI-1 is an inhibitor of interaction with a eIF4EeIF4G Kdof 25 μM against eIF4E binding
Bioactivity Briciclib is a water soluble derivative of ON 013100 and hasthe potential in targeting for solid cancerseIF4E
Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)
Bioactivity eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic inhibitor with an of 110initiation factor 4A-3 (eIF4A3) IC50
nM
Bioactivity Episilvestrol is a derivative of silvestrol isolated from thefruits and twigs of and is a specificAglaia silvestris
-targeting translation inhibitor with antitumor activityeIF4A
Bioactivity GCN2iB is an ATP-competitive inhibitor of aserinethreonine-protein kinase general control
with an of 24 nMnonderepressible 2 (GCN2) IC50
Bioactivity SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1and disrupts the eIF4F complex
Bioactivity Silvestrol is a eukaryotic translation initiation factor 4A () inhibitor isolated from the fruits and twigs of eIF4A Aglaia
foveolata
4E1RCat Cat No HY-14427
4E2RCat Cat No HY-100733
4EGI-1 Cat No HY-19831
Briciclib (ON 014185) Cat No HY-16366
CCT020312 Cat No HY-119240
eIF4A3-IN-2 Cat No HY-101785
Episilvestrol Cat No HY-15359
GCN2iB Cat No HY-112654
SBI-0640756 (SBI-756) Cat No HY-19560
Silvestrol ((-)-Silvestrol) Cat No HY-13251
G-quadruplex
G-quadruplexes (G-tetrads or G4-DNA) are nucleic acid sequencesthat are rich in guanine and are capable of forming a four-strandedstructure Four guanine bases can associate through Hoogsteenhydrogen bonding to form a square planar structure called a guaninetetrad and two or more guanine tetrads can stack on top of eachother to form a G-quadruplex The quadruplex structure is furtherstabilized by the presence of a cation especially potassium which sitsin a central channel between each pair of tetradsThey can be formedof DNA RNA LNA and PNA and may be intramolecular bimolecularor tetramolecular Depending on the direction of the strands or partsof a strand that form the tetrads structures may be described as
parallel or antiparallel
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Purity 980Clinical Data No Development ReportedSize 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in Water
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg
Purity 9680Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
G-quadruplex Inhibitors amp Modulators
Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay
Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay
Bioactivity APTO-253 is an inducer of andKruppel-like factor 4 (KLF4)also stabilizes with anti-proliferative activityGquadruplex
Bioactivity Phen-DC3 Trifluoromethanesulfonate is a (G4)G-quadruplexspecific ligand which can inhibit and helicasesFANCJ DinGwith s of 65plusmn6 and 50plusmn10 nM respectivelyIC50
Bioactivity Pyridostatin is a stabilizer with a of 490G-quadruplexe KdnM
Bioactivity Pyridostatin hydrochloride is a stabilizer withG-quadruplexea of 490 nMKd
Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip
360A Cat No HY-15595
360A iodide (360 A iodide) Cat No HY-15595A
APTO-253 (LOR-253 LT-253) Cat No HY-16291
Phen-DC3 Trifluoromethanesulfonate (Phen-DC3 Triflate) Cat No HY-15594A
Pyridostatin (RR82) Cat No HY-15176
Pyridostatin hydrochloride (RR-82 hydrochloride) Cat No HY-15176A
TMPyP4 tosylate (TMP 1363) Cat No HY-108477
Haspin Kinase
Haspin is a protein kinase that regulates chromosome and spindlefunction during mitosis and meiosis Haspin expression is detected infetal liver skin kidney small intestine and in all proliferating cellsHaspin phosphorylates H3 thr3 (H3T3ph) in human cell lines anddepletion of Haspin by RNA interference reveals that Haspin isrequired for H3 thr3 phosphorylation in mitotic cells Phosphorylationof H3T3ph by Haspin is necessary for chromosomal passengercomplex (CPC) accumulation at centromeres H3T3ph then positionsthe CPC at centromeres to regulate selected targets of Aurora Bduring mitosis
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Purity 9956Clinical Data No Development ReportedSize 5 mg
Purity 9812Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Haspin Kinase Inhibitors amp Modulators
Bioactivity CHR-6494 is a potent inhibitor of inhibiting histonehaspinH3T3 phosphorylation with an of 2 nMIC50
Bioactivity LDN-192960 is a potent ( Haspin Haploid Germ Cell-Specific) inhibitor with an of 0010 microMNuclear Protein Kinase IC50
CHR-6494 Cat No HY-15217
LDN-192960 Cat No HY-13455
HDACHistone deacetylases
HDAC (Histone deacetylases) are a class of enzymes that removeacetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid onahistone allowing the histones to wrap the DNA more tightly This isimportant because DNA is wrapped around histones and DNAexpression is regulated by acetylation and de-acetylation Its action isopposite to that of histone acetyltransferase HDAC proteins are nowalso called lysine deacetylases (KDAC) to describe their functionrather than their target which also includes non-histone proteinsTogether with the acetylpolyamine amidohydrolases and the acetoinutilization proteins the histone deacetylases form an ancient proteinsuperfamily known as the histone deacetylase superfamily
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Purity 9600Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9971 Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 g
Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 200 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg
Purity 9896Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9861Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
HDAC Inhibitors amp Modulators
Bioactivity Abexinostat (CRA 024781) is a novel pan- inhibitorHDACmostly targeting HDAC1 with of 7 nMKi
Bioactivity ACY-1083 is a selective and brain-penetrating inhibitorHDAC6with an of 3 nM and is 260-fold more selective for HDAC6IC50than all other classes of HDAC isoforms ACY-1083 effectivelyreverses chemotherapy-induced peripheral neuropathy [1]
Bioactivity ACY-738 is a potent selective and orally-bioavailable HDAC6inhibitor with an of 17 nM ACY-738 also inhibitsIC50HDAC1 HDAC2 and HDAC3 with s of 94 128 and 218 nMIC50
Bioactivity ACY-775 is a potent and selective inhibitor of the of histonedeacetylase 6 ( ) with an of 75nMHDAC6 IC50
Bioactivity ACY-957 is a selective inhibitor of and withHDAC1 HDAC2s of 7 nM 18 nM and 1300 nM against HDAC123IC50
respectively and shows no inhibition on HDAC456789
Bioactivity AES-135 is a potent inhibitor inhibits HDAC HDAC3 HDAC6 with s of 654 190 and 636 nM respectivelyHDAC11 IC50
Anti-tumor activity [1]
Bioactivity Belinostat is a potent inhibitor with an of 27 nMHDAC IC50in HeLa cell extracts
Bioactivity Benzenebutyric acid is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)
Bioactivity BG45 is an HDAC class I inhibitor with selectivity for HDAC3(IC50 = 289 nM) It inhibits HDAC1 HDAC2 and HDAC6 withgreatly reduced potency (IC50s = 2 22 and gt20 μMrespectively) IC50 value 289 nM (HDAC3) 2 μM (HDAC1) 22μM (HDAC2) gt20 μM (HDAC6) Target HDAC At concentrationshellip
Bioactivity BML-210 is a novel HDAC inhibitor and its mechanism of actionhas not been characterized IC50 value 5 μM[1] Target HDAC4In vitro Cell cycle analysis indicated that HeLa celltreatment with 20 and 30 μM concentration of BML-210 increasedthe proportion of cells in G0G1 phase and causedhellip
Abexinostat (CRA 024781 PCI-24781) Cat No HY-10990
ACY-1083 Cat No HY-111791
ACY-738 Cat No HY-19327
ACY-775 Cat No HY-19328
ACY-957 Cat No HY-104008
AES-135 Cat No HY-114483
Belinostat (PXD101 PX105684) Cat No HY-10225
Benzenebutyric acid (4-Phenylbutyric acid) Cat No HY-A0281
BG45 Cat No HY-18712
BML-210 Cat No HY-19350
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9875Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg
Purity 9906Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg
Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg
Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Bioactivity BRD 4354 is a moderately potent inhibitor of andHDAC5 with of 085 and 188 μM respectivelyHDAC9 IC s50
Bioactivity BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitorof and with of 085 and 188 μMHDAC5 HDAC9 IC s50
respectively [1]
Bioactivity BRD73954 ia a potent and selective HDAC inhibitor with IC50 of36 nM and 120 nM for HDAC6 and HDAC8 respectively
Bioactivity Bufexamac is a class IIB histone deacetylases (HDAC6 andHDAC10) inhibitor used as an anti-inflammatory agent
Bioactivity CAY10603 (BML-281) is a potent and selective inhibitorHDAC6with an of 2 pM CAY10603 (BML-281) also inhibits HDAC1IC50HDAC2 HDAC3 HDAC8 HDAC10 with s of 271 252 042IC506851 907 nM
Bioactivity CHDI-390576 a potent cell permeable and CNS penetrant class inhibitor with s of 54 nMIIa histonedeacetylase (HDAC) IC50
60 nM 31 nM 50 nM for class IIa HDAC4 HDAC5 HDAC7 HDAC9respectively shows gt500-fold selectivity over class IHDACs (1 2 3) and ~150-fold selectivity over HDAC8 and thehellip
Bioactivity Citarinostat is a HDAC6 specific inhibitor with IC50 of 4 nMand 76 nM for HDAC6 and HDAC3 respectively IC50 value 4 nM(HDAC6) 76 nM (HDAC3) Target HDAC The detailed informationplease refer to WO2015061684A1 and 2015054197A1
Bioactivity CM-675 is a dual and phosphodiesterase 5 (PDE5) class I histone-selective inhibitor with values of 114 nMdeacetylases IC50
and 673 nM for PDE5 and HDAC1 respectively CM-675 haspotential to treat Alzheimerrsquos disease [1]
Bioactivity Corin is a dual inhibitor of histone lysine specificdemethylase and histone deacetylase with a(LSD1) (HDAC)
of 110 nM for LSD1 and an IC of 147 nM forK (inact)i 50HDAC1
Bioactivity CRA-026440 is a potent broad-spectrum inhibitor The HDAC Kivalues against recombinant HDAC isoenzymes HDAC1 HDAC2
and are 4 14 11 15 7 andHDAC3 HDAC6 HDAC8 HDAC1020 nM respectively
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BRD 4354 Cat No HY-112719
BRD 4354 ditrifluoroacetate Cat No HY-112719B
BRD73954 Cat No HY-18700
Bufexamac (Bufexamic acid) Cat No HY-B0494
CAY10603 (BML-281) Cat No HY-18613
CHDI-390576 Cat No HY-119939
Citarinostat (ACY241) Cat No HY-15994
CM-675 Cat No HY-114303
Corin Cat No HY-111048
CRA-026440 Cat No HY-19754
wwwMedChemExpresscom 69
Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9995Clinical Data Phase 2Size 10mM x 1mL in Ethanol
2 mg 5 mg 10 mg 50 mg
Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 200 mg
Purity 9809Clinical Data Phase 2Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9881Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9899Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9959Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity CUDC-101 is a potent inhibitor of and withHDAC EGFR HER2s of 44 24 and 157 nM respectivelyIC50
Bioactivity Dacinostat is a potent inhibitor with an of 32 nMHDAC IC50Dacinostat also inhibits with an of 9 nM and usedHDAC1 IC50in cancer research
Bioactivity Domatinostat (4SC-202 free base) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1
(LSD1)
Bioactivity Domatinostat tosylate (4SC-202) is a selective class I HDACinhibitor with of 120 μM 112 μM and 057 μM forIC50HDAC1 HDAC2 and HDAC3 respectively It also displaysinhibitory activity against Lysine specific demethylase 1
(LSD1)
Bioactivity Droxinostat(NS41080) is a selective inhibitor of HDAC3 HDAC6and HDAC8 with IC50 of 169 247 and 146 μM respectivelygt 8-fold selective against HDAC3 and no inhibition toHDAC1 2 4 5 7 9 and 10 IC50 Value 169 μM(HDAC3) 247μM(HDAC6) 146 μM(HDAC8) Target HDAC368 in vitrohellip
Bioactivity EDO-S101 is a pan inhibitor inhibits HDAC1 HDAC2 andHDACHDAC3 with values of 9 9 and 25 nM respectivelyIC50
Bioactivity Entinostat is an oral and selective class I inhibitorHDACwith s of 243 nM 453 nM and 248 nM for IC50 HDAC1 HDAC2
and respectivelyHDAC3
Bioactivity Fimepinostat (CUDC-907) potently inhibits class I s as wellPI3Kas classes I and II enzymes with an of 195439 nMHDAC IC50and 17501828 nM for PI3KαPI3KβPI3Kδ andHDAC1HDAC2HDAC3HDAC10 respectively
Bioactivity FT895 is a potent and selective inhibitor with an HDAC11 IC50
of 3 nM [1]
Bioactivity Givinostat (ITF-2357) is a inhibitor with an of 198HDAC IC50and 157 nM for and respectivelyHDAC1 HDAC3
CUDC-101 Cat No HY-10223
Dacinostat (NVP-LAQ824 LAQ824) Cat No HY-13606
Domatinostat (4SC-202 (free base)) Cat No HY-16012A
Domatinostat tosylate (4SC-202) Cat No HY-16012
Droxinostat (NS 41080) Cat No HY-13267
EDO-S101 (Tinostamustine) Cat No HY-101780
Entinostat (MS-275 SNDX-275) Cat No HY-12163
Fimepinostat (CUDC-907) Cat No HY-13522
FT895 Cat No HY-112285
Givinostat (ITF-2357) Cat No HY-14842
Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9849Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9609Clinical Data LaunchedSize 2 mg 5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg
Bioactivity Givinostat hydrochloride (ITF-2357 hydrochloride) is a HDACinhibitor with an of 198 and 157 nM for andIC50 HDAC1
respectivelyHDAC3
Bioactivity Givinostat hydrochloride monohydrate (ITF-2357 hydrochloridemonohydrate) is a inhibitor with an of 198 and 157HDAC IC50nM for and respectivelyHDAC1 HDAC3
Bioactivity HDAC-IN-3 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2008040934 A1
Bioactivity HDAC-IN-4 is a histone deacetylase (HDAC) inhibitor extractedfrom patent WO2007045844 A1 20070426
Bioactivity HDAC-IN-5 is a histone deacetylase inhibitor(HDAC) Bioactivity HDAC-IN-7 (Chidamide impurity) is an impurity of ChidamideChidamide is a potent and orally bioavailable HDAC enzymesclass I (HDAC123) and class IIb (HDAC10) inhibitor
Bioactivity HDAC6-IN-1 is a potent and selective inhibitor for withHDAC6an of 17 nM and shows 25-fold and 200-fold selectivityIC50relative to ( =422 nM) and ( =3398 nM)HDAC1 IC50 HDAC8 IC50respectively
Bioactivity HDAC8-IN-1 is a inhibitor with an of 272 nMHDAC8 IC50
Bioactivity HDACsmTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs)and targetmammalian target of Rapamycin (mTOR)inhibitor for treating hematologic malignancies with ofIC s50019 nM 18 nM 12 nM and gt500 nM for HDAC1 HDAC6 mTORand PI3Kα respectively HDACsmTOR Inhibitor 1 stimulateshellip
Bioactivity HPOB is a highly potent and selective inhibitor of histonedeacetylase 6 (HDAC6) with IC50 of 56 nM gt30 fold lesspotent against other HDACs target HDAC6 [1] IC 50 56nM [1]In vitro HPOB causes growth inhibition of normal andtransformed cells but does not induce cell death HPOBhellip
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Givinostat hydrochloride (ITF-2357 hydrochloride) Cat No HY-14842A
Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) Cat No HY-14842B
HDAC-IN-3 Cat No HY-19772
HDAC-IN-4 (CXD101) Cat No HY-100748
HDAC-IN-5 Cat No HY-18362
HDAC-IN-7 (Chidamide impurity) Cat No HY-13592
HDAC6-IN-1 Cat No HY-18947
HDAC8-IN-1 Cat No HY-111342
HDACsmTOR Inhibitor 1 Cat No HY-114414
HPOB Cat No HY-19747
wwwMedChemExpresscom 71
Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg 100 mg
Bioactivity IDO1 and HDAC1 Inhibitor (Compound 10) is a dual andIDO1 inhibitor with s of 690 nM and 665 nMHDAC1 IC50
respectively [1]
Bioactivity ITSA-1 is membrane permeable and specifically suppresses TSAinhibition of HDAC (histone deacetylase) but not other HDACinhibitors
Bioactivity J22352 is a PROTAC (proteolysis-targeting chimeras)-like andhighly selective inhibitor with an value of 47HDAC6 IC50nM J22352 promotes HDAC6 degradation and induces anticancereffects by inhibiting autophagy and eliciting the antitumorimmune response in glioblastoma cancers and leading to thehellip
Bioactivity JAKHDAC-IN-1 is a potent dual inhibitor exhibitsJAK2HDACantiproliferative and proapoptotic activities in severalhematological cell lines JAKHDAC-IN-1 shows s of 4 and 2IC50
nM for JAK2 and HDAC respectively [1]
Bioactivity LMK-235 is a potent and selective inhibitor inhibitsHDAC45HDAC5 HDAC4 HDAC6 HDAC1 HDAC2 HDAC11 and HDAC8 with
s of 422 nM 119 nM 557 nM 320 nM 881 nM 852 nM andIC501278 nM respectively and is used in cancer research
Bioactivity M344 (D 237) is an inhibitor of ( =100histone deacetylase IC50nM) and an inducer of terminal cell fifferentiation
Bioactivity MC1568 is a selective class II (IIa) histone deacetylas () inhibitor used for cancer researchHDAC II
Bioactivity Mocetinostat (MGCD0103) is a potent orally active andisotype-selective inhibitor with s ofHDAC (Class IIV) IC50015 029 166 and 059 μM for andHDAC1 HDAC2 HDAC3
respectively Mocetinostat shows no inhibition onHDAC11HDAC4 HDAC5 HDAC6 HDAC7 or HDAC8
Bioactivity Nanatinostat (CHR-3996) is a potent class I selective andorally active inhibitor with anhistone deacetylase (HDAC)
of 8 nM IC50[1]
Bioactivity Nexturastat A is a potent and selective HDAC6 inhibitor withIC50 of 5 nM no inhibition on other HDAC forms
IDO1 and HDAC1 Inhibitor Cat No HY-112147
ITSA-1 Cat No HY-100508
J22352 Cat No HY-126147
JAKHDAC-IN-1 Cat No HY-126141
LMK-235 Cat No HY-18998
M344 (D 237 MS 344) Cat No HY-13506
MC1568 Cat No HY-16914
Mocetinostat (MGCD0103) Cat No HY-12164
Nanatinostat (CHR-3996) Cat No HY-13432
Nexturastat A Cat No HY-16699
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9907Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg
Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9842Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 200 mg 500 mg
Purity 9867Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg
Purity 9797Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Bioactivity NKL 22 is a HDAC inhibitor The value of IC 50 is 78 uM NKL 22increase frataxin protein concentrations NKL 22 inhibitorsincrease FXN mRNA in FRDA lymphocytes HDAC inhibitors actdirectly on FXN [1]
Bioactivity Oxamflatin (Metacept-3) is a potent inhibitor with anHDAC of 157 nMIC50
Bioactivity Panobinostat is a non-selective histone deacetylase ( )HDACinhibitor
Bioactivity PCI-34051 is a potent and selective inhibitor with HDAC8 IC50of 10 nM with gt200-fold selectivity over the other HDACisoforms
Bioactivity PI3KHDAC-IN-1 is a potent dual inhibitor of PI3KHDACpotently inhibits PI3Kδ and HDAC1 with s of 81 nM and 14IC50
nM respectively [1]
Bioactivity Pimelic diphenylamide 106 is a slow tight-binding inhibitorof class I HDAC (HDAC 1 2 and 3 with IC50 values of 150 nM 760nM and 370 nM respectively) demonstrating no activityagainst class II HDACs
Bioactivity Pracinostat is a potent inhibitorhistone deacetylase (HDAC)with s of 40-140 nM used for cancer researchIC50
Bioactivity PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDACPTACH exerts potent growth inhibition against various humancancer cells with EC50 values ranging from 1 to 10 μM
Bioactivity Quisinostat (JNJ-26481585) is an orally available potent inhibitor with an of 011 nM for HDAC1HDAC IC50
Bioactivity Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of which is under developmenthistone deacetylase enzymes (HDAC)
for the treatment of cutaneous T-cell lymphoma [1]
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NKL 22 Cat No HY-100384
Oxamflatin (Metacept-3) Cat No HY-102033
Panobinostat (LBH589 NVP-LBH589) Cat No HY-10224
PCI-34051 Cat No HY-15224
PI3KHDAC-IN-1 Cat No HY-128582
Pimelic Diphenylamide 106 (RGFA-8 TC-H 106 Histone Deacetylase Inhibitor VII) Cat No HY-19348
Pracinostat (SB939) Cat No HY-13322
PTACH (NCH-51) Cat No HY-12954
Quisinostat (JNJ-26481585) Cat No HY-15433
Remetinostat (SHP-141) Cat No HY-100365
wwwMedChemExpresscom 73
Purity 9961Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
100 mg
Purity 9912Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 9970Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9899Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg
Bioactivity Resminostat is a potent inhibitor of andHDAC1 HDAC3 with mean values of 425 501 718 nMHDAC6 IC50
respectively and shows less potent activities against HDAC8with an of 877 nMIC50
Bioactivity Resminostat hydrochloride is a potent inhibitor of HDAC1 and with mean values of 425 501 718HDAC3 HDAC6 IC50
nM respectively and shows less potent activities againstHDAC8 with an of 877 nMIC50
Bioactivity RG2833 is a brain-penetrant inhibitor with of 60 nMHDAC IC50and 50 nM for HDAC1 and HDAC3 respectively
Bioactivity RGFP966 is a highly selective inhibitor with an ofHDAC3 IC5080 nM and shows no inhibition to other HDACs at concentrationsup to 15 μM
Bioactivity Ricolinostat (ACY-1215) is a potent and selective HDAC6inhibitor with an of 5 nM ACY-1215 also inhibitsIC50
and with s of 58 48 and 51 nMHDAC1 HDAC2 HDAC3 IC50respectively
Bioactivity Romidepsin is a potent and inhibitor with sHDAC1 HDAC2 IC50of 36 and 47 nM respectively
Bioactivity RTS-V5 is a dual inhibitor with s ofHDACproteasome IC5069 18 15 027 053 μM for HDAC1 HDAC2 HDAC3 HDAC6HDAC8 respectively
Bioactivity Santacruzamate A (CAY-10683) is a potent and selective HDAC2inhibitor with an of 119 pM IC50
[1]
Bioactivity Scriptaid is a potent inhibitorhistone deacetylase (HDAC)used in cancer research
Bioactivity Sinapinic acid (Sinapic acid) is a phenolic compound isolatedfrom Jack Rhizome acts as anHydnophytum formicaruminhibitor of with an of 227 mM and alsoHDAC IC50
[1]
inhibits activity Sinapinic acid posssess pothellipACE-I [2]
Resminostat (RAS2410 4SC-201) Cat No HY-14718
Resminostat hydrochloride (RAS2410 hydrochloride 4SC-201 hydrochloride) Cat No HY-14718A
RG2833 (RGFP109) Cat No HY-16425
RGFP966 Cat No HY-13909
Ricolinostat (ACY-1215 Rocilinostat) Cat No HY-16026
Romidepsin (FK 228 FR 901228 NSC 630176) Cat No HY-15149
RTS-V5 Cat No HY-112908
Santacruzamate A (CAY-10683) Cat No HY-N0931
Scriptaid (Scriptide GCK1026) Cat No HY-15489
Sinapinic acid (Sinapic acid) Cat No HY-W009732
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9985Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9932Clinical Data Phase 3Size 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 200 mg 500 mg
Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO
10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg
Purity 9833Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water
100 mg 200 mg
Purity 9800Clinical Data Phase 3Size 10mM x 1mL in Water
1 g 5 g 500 g
Bioactivity Butyric acid is a inhibitor withhistone deacetylase (HDAC)anti-tumor effects in several cancers
Bioactivity Sodium phenylbutyrate is an inhibitor of and endoplasmicHDACreticulum stress used in cancer and infection research(ER)
Bioactivity SR-4370 is an inhibitor of with s of 013 μM 058HDAC IC50μM 0006 μM 23 μM and 34 μM for HDAC1 HDAC2 HDAC3HDAC8 and HDAC6 respectively
Bioactivity ST8154AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]
Bioactivity ST8155AA1 is a part of antibody drug conjugates ( )ADCscharged with inhibitor by a linker shows antitumorHDACactivity [1]
Bioactivity Sulforaphane is an isothiocyanate present naturally in widelyconsumed vegetables has shown anticancer and cardioprotectiveactivities
Bioactivity SW-100 a selective inhibitorhistone deacetylase 6 (HDAC6)with an of 23 nM shows at least 1000-fold selectivityIC50for HDAC6 relative to all other HDAC isozymes SW-100 displaysa significantly improved ability to cross hellip
Bioactivity Tacedinaline (N-acetyldinaline) is an inhibitor of the histonedeacetylase ( ) with s of 09 09 12 μM forHDAC IC50recombinant HDAC 1 2 and 3 respectively
Bioactivity Tasquinimod is an oral antiangiogenic agent in clinical trialsfor the treatment of castration-resistant prostate cancerTasquinimod binds to the regulatory Zn binding domain of2+
with of 10-30 nMHDAC4 Kd
Bioactivity TH34 an inhibitor with s of 46 μM 19HDAC6 8 10 IC50μM and 77 μM respectively shows high selectivity overHDAC123 [1]
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Sodium Butyrate (Butanoic acid sodium salt) Cat No HY-B0350A
Sodium phenylbutyrate (Sodium 4-phenylbutyrate TriButyrate) Cat No HY-15654
SR-4370 Cat No HY-111400
ST8154AA1 Cat No HY-112805
ST8155AA1 Cat No HY-112806
Sulforaphane Cat No HY-13755
SW-100 Cat No HY-115475
Tacedinaline (N-acetyldinaline CI-994 Goe-5549) Cat No HY-50934
Tasquinimod (ABR-215050) Cat No HY-10528
TH34 Cat No HY-111818
wwwMedChemExpresscom 75
Purity 980Clinical Data LaunchedSize 10mM x 1mL in Water
1 g 5 g 25 g
Purity 9867Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g 25 g
Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 200 mg
Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9887Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 20 mg
Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg
Purity 9842Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg 200 mg
Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity TMP195 is a selective class IIa histone deacetylase ( )HDACinhibitor with s of 59 60 26 15 nM for HDAC4 HDAC5KiHDAC7 and HDAC9 respectively
Bioactivity TMP269 is a novel and selective class IIa histone deacetylase inhibitor with s of 157 nM 97 nM 43 nM and 23 nM(HDAC) IC50
for HDAC4 HDAC5 HDAC7 and HDAC9 respectively
Bioactivity Trichostatin A is a potent and specific inhibitor of HDAC with an value of 18 nM for HDACclass III IC50
Bioactivity Tubacin is a potent and selective inhibitor of with anHDAC6 value of 4 nM and approximately 350-fold selectivity overIC50
HDAC1
Bioactivity Tubastatin A (Hydrochloride) is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50
cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)
Bioactivity Tubastatin-A is a potent and selective inhibitor with of 15 nM in aHDAC6 IC50
cell-free assay and is selective (1000-fold more) against allother isozymes except HDAC8 (57-fold more)
Bioactivity Tucidinostat is a potent and orally bioavailable enzymesHDACclass I ( ) and class IIb ( ) inhibitor withHDAC123 HDAC10
s of 95 160 67 and 78 nM less active on HDAC8 andIC50HDAC11 ( s 733 nM 432 nM respectively) and showshellipIC50
Bioactivity UF010 is a potent and selective HDAC inhibitor with IC50 ~006μM 01 μM 05 μM and 15 μM for HDACs 3 2 1 and 8respectively It has gt 6-fold selectivity over other HDACsIC50 value 006 μM (HDAC3) 01 μM (HDAC2) 05 μM (HDAC1)15 μM(HDAC 8) Target HDAC in vitro UF010 is a competitivehellip
Bioactivity Valproic acid is an inhibitor with in the range ofHDAC IC5005 and 2 mM also inhibits ( 400 μM) andHDAC1 IC50induces proteasomal degradation of Valproic acidHDAC2sodium salt is used in the treatment of epilepsy bipohellip
Bioactivity Valproic acid sodium salt is an anticonvulsants used to treatepilepsy bipolar disorder and migraines Valproic acidinhibits with an of 04 mMhistone deacetylase 1 (HDAC1) IC50
TMP195 Cat No HY-18361
TMP269 Cat No HY-18360
Trichostatin A (TSA) Cat No HY-15144
Tubacin Cat No HY-13428
Tubastatin A Hydrochloride (Tubastatin A HCl TSA HCl) Cat No HY-13271
Tubastatin-A Cat No HY-13271A
Tucidinostat (Chidamide HBI-8000 CS 055) Cat No HY-109015
UF010 Cat No HY-18976
Valproic acid (VPA 2-Propylpentanoic Acid) Cat No HY-10585
Valproic acid sodium salt (Sodium Valproate) Cat No HY-10585A
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9990Clinical Data LaunchedSize 10mM x 1mL in DMSO
250 mg 500 mg 1 g 5 g
Bioactivity Vorinostat is a potent and orally available inhibitor of and andHDAC1 HDAC2 HDAC3 (Class I) HDAC7 (Class II)
with values of 10 nM and 20 nM forHDAC11 (Class IV ) ID50HDAC1 and HDAC3 respectively
Bioactivity WT-161 is a potent and selective inhibitor with an HDAC6 IC50of 040 nM
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Vorinostat (SAHA) Cat No HY-10221
WT-161 Cat No HY-100871
wwwMedChemExpresscom 77
HSPHeat shock proteins
HSP (Heat shock proteins) are a group of proteins induced by heatshock the most prominent members of this group are a class offunctionally related proteins involved in the folding and unfolding ofother proteins HSP expression is increased when cells are exposed toelevated temperatures or other stress This increase in expression istranscriptionally regulated The dramatic upregulation of the heatshock proteins is a key part of the heat shock response and is inducedprimarily by heat shock factor (HSF) HSPs are found in virtually allliving organisms from bacteria to humans Heat shock proteinsappear to serve a significant cardiovascular role Hsp90 Hsp84Hsp70 Hsp27 Hsp20 and alpha B crystallin all have been reported as
having roles in the cardiovasculature
Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 g
Purity 9997Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg
Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Purity 9957Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9932Clinical Data Phase 2Size 10mM x 1mL in DMSO
10 mg 25 mg 100 mg 200 mg
Purity gt98Clinical Data Phase 2Size 1 mg
HSP Inhibitors amp Modulators
Bioactivity Alvespimycin is a potent inhibitor of binding to Hsp90Hsp90with an of 62 plusmn 29 nMEC50
Bioactivity Alvespimycin hydrochloride is a potent inhibitor of Hsp90binding to Hsp90 with of 62plusmn29 nMEC50
Bioactivity Apoptozole is an inhibitor of the ATPase domain of andHsc70 with s of 021 and 014 μM respectively and canHsp70 Kd
induce apoptosis
Bioactivity Arimoclomol maleate (BRX-220) is a co-inducer of heat shockproteins ( )HSP
Bioactivity BIIB021 is an orally available fully synthetic inhibitor of with and of 17 nM and 38 nM respectivelyHSP90 Ki EC50
Bioactivity Bimoclomol is a coinducer used forheat shock protein (HSP)treatment of cardiovascular diseases
Bioactivity CCT251236 is an orally available pirin ligand from a heatshock transcription factor 1 (hsf1) phenotypic screen with an
of 19 nM for inhibition of HSF1-mediated IC50 HSP72
induction
Bioactivity Col003 is a potent inhibitor of competitively binds toHsp47the collagen binding site on Hsp47 ( 18 μM) andIC50inhibits collagen secretion by destabilizing the collagentriple helix [1]
Bioactivity Debio 0932 is an orally active inhibitor with s ofHSP90 IC50100 and 103 nM for HSP90α and HSP90β respectively
Bioactivity Ethoxyquin is an antioxidant which has been used in animalfeed for many years and also an inhibitor of heat shock
( )protein 90 Hsp90
78 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Alvespimycin (17-DMAG NSC 707545) Cat No HY-10389
Alvespimycin hydrochloride (17-DMAG hydrochloride KOS-1022 BMS 826476) Cat No HY-12024
Apoptozole (Apoptosis Activator VII) Cat No HY-15098
Arimoclomol maleate (BRX-220) Cat No HY-106443A
BIIB021 (CNF2024) Cat No HY-10212
Bimoclomol Cat No HY-U00398
CCT251236 Cat No HY-101026
Col003 Cat No HY-124817
Debio 0932 (CUDC-305) Cat No HY-13469
Ethoxyquin Cat No HY-B1425
wwwMedChemExpresscom 79
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg 200 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9933Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg
Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg
Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity 9994Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg
Bioactivity Feretoside a phenolic compound extracted from the barks of E is a which act as cytoprotectiveulmoides HSP inducer
agent
Bioactivity Ganetespib is a heat shock protein 90 ( ) inhibitorHSP90which exhibits potent cytotoxicity in a wide variety ofhematological and solid tumor cell lines
Bioactivity Geldanamycin is a inhibitor with antimicrobial activityHsp90against many Gram-positive and some Gram-negative bacteria
Bioactivity Grp94 Inhibitor-1 is a potent selective inhibitor withGrp94an value of 2 nM and over 1000-fold selectivity to Grp94IC50
against Hsp90α [1]
Bioactivity HA15 a molecule that targets specifically BiP GRP78 HSPA5inhibits the ATPase activity of BiP HA15 strongly increasesBiP protein expression in A375 melanoma cells [1]
Bioactivity HSF1A is a cell-permeable activator of heat shocktranscription factor 1 ( )HSF1
Bioactivity HSP70-IN-1 is a heat shock protein ( ) inhibitor inhibitsHSPthe growth of Kasumi-1 cells with an of 23 μMIC50
Bioactivity JG-98 is an allosteric heat shock protein 70 (Hsp70)inhibitor with anti-cancer activities which disrupts Hsp70
and affects signalinginteraction with a co-chaperone Bag3pathways important for cancer development [1] [2] [3]
Bioactivity KNK437 is a inhibitor and inhibits the induction ofHSPHSP105 HSP70 and HSP40
Bioactivity KRIBB11 is an inhibitor of withHeat shock factor 1 (HSF1) of 12 μMIC50
Feretoside Cat No HY-N6249
Ganetespib (STA-9090) Cat No HY-15205
Geldanamycin Cat No HY-15230
Grp94 Inhibitor-1 Cat No HY-112910
HA15 Cat No HY-100437
HSF1A Cat No HY-103000
HSP70-IN-1 Cat No HY-12622
JG-98 Cat No HY-117282
KNK437 (Heat Shock Protein Inhibitor I) Cat No HY-100110
KRIBB11 Cat No HY-100872
Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 100 mg
Purity 9569Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9831Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg
Purity gt98Clinical Data No Development ReportedSize
Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 980Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity 9914Clinical Data Phase 2Size 5 mg 10 mg 25 mg 100 mg 200 mg 500 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Bioactivity KU-32 is a novel novobiocin-based inhibitor that canHsp90protect against neuronal cell death
Bioactivity KW-2478 is an inhibitor of with an of 38 nMHsp90α IC50and has antitumor activity against various human hematologicaltumor cells
Bioactivity Luminespib (NVP-AUY922) is a potent inhibitor withHSP90s of 78 and 21 nM for HSP90α and HSP90β respectivelyIC50
Bioactivity MKT-077 is a rhodacyanine dye and also a heat shock protein 70( ) inhibitor which exhibits significant antitumorHsp70activity
Bioactivity NVP-HSP990 is a potent and selective inhibitor withHsp90 values of 06 08 and 85 nM for Hsp90α Hsp90β andIC50
Grp94 respectively
Bioactivity Onalespib (AT13387) is a potent inhibitor of with aHsp90 of 071 nMKd
Bioactivity p5 Ligand for Dnak and DnaJ is a nonapeptide whichcorresponds to the main binding site for the 23-residue partof the presequence of mitochondrial aspartateaminotransferase p5 Ligand for Dnak and DnaJ is ahigh-affinity ligand for DnaK and DnaJ [1]
Bioactivity Pifithrin-μ is an inhibitor of and with antitumorp53 HSP70and neuroprotective activity
Bioactivity PU-WS13 is a selective inhibitor with an ofGrp94 EC50022 μM
Bioactivity Retaspimycin is a potent and water-soluble inhibitor of with s of 119 nM for both Hsp90 and Grp9Hsp90 EC50
80 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
KU-32 Cat No HY-108248
KW-2478 Cat No HY-13468
Luminespib (NVP-AUY922 AUY922 VER-52296) Cat No HY-10215
MKT-077 (FJ-776) Cat No HY-15096
NVP-HSP990 (HSP-990) Cat No HY-15190
Onalespib (AT13387) Cat No HY-14463
p5 Ligand for Dnak and DnaJ Cat No HY-P1887
Pifithrin-μ (PFTμ 2-Phenylethynesulfonamide) Cat No HY-10940
PU-WS13 Cat No HY-18680
Retaspimycin Cat No HY-15263
wwwMedChemExpresscom 81
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 9926Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg 100 mg
Purity 9964Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9740Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9982Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9903Clinical Data Phase 3Size 10mM x 1mL in DMSO
10 mg 25 mg 100 mg 200 mg
Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize
Purity 950Clinical Data Phase 3Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Bioactivity Retaspimycin Hydrochloride is a potent and water-solubleinhibitor of with s of 119 nM for both Hsp90 andHsp90 EC50Grp9
Bioactivity Shepherdin (79-87) is amino acids 79 to 87 fragment ofShepherdin Shepherdin is a peptidomimetic antagonist of thecomplex between Hsp90 and Survivin Anticancer activity [1]
Bioactivity SNX-5422 Mesylate (PF-04929113 Mesylate) a prodrug ofSNX-2112 is an orally active inhibitor with a ofHsp90 Kd41 nM and also induces Her-2 degradation with an ofIC5037nM
Bioactivity Tanespimycin (17-AAG) is a potent inhibitor with anHSP90 of 5 nM having a 100-fold higher binding affinity forIC50
tumour cell derived HSP90 than normal cell derived HSP90
Bioactivity TAS-116 is an oral bioavailable ATP-competitive highlyspecific inhibitor ( s of 347 nM and 213HSP90αHSP90β KinM respectively) without inhibiting other HSP90 familyproteins such as GRP94 TAS-116 demonstrates less ocuhellip[1]
Bioactivity Teprenone is a anti-ulcer drug and works as an inducer ofheat shock proteins ( )HSPs
Bioactivity TRC051384 is a heat shock protein 70 ( ) inducerHSP70 Bioactivity VER-155008 is an inhibitor of with s of 05 μMHsp70 IC5026 μM and 26 μM for Hsc70 and Grp7 respectivelyHsp70and with a of 03 μM for Kd Hsp70
Bioactivity VER-49009 is a inhibitor with an of 25 nM and aHsp90 IC50 of 78 nMKd
Bioactivity VER-50589 is a inhibitor with an of 21 nM and aHsp90 IC50 of 45 nMKd
Retaspimycin Hydrochloride (IPI-504) Cat No HY-10210
Shepherdin 79-87 Cat No HY-P1750
SNX-5422 Mesylate (PF-04929113 (Mesylate)) Cat No HY-10213A
Tanespimycin (17-AAG NSC 330507 CP 127374) Cat No HY-10211
TAS-116 Cat No HY-15785
Teprenone (Geranylgeranylacetone) Cat No HY-B0779
TRC051384 Cat No HY-101712
VER-155008 Cat No HY-10941
VER-49009 (CCT 129397) Cat No HY-15986
VER-50589 Cat No HY-15984
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg
Purity 9924Clinical Data Phase 1Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg
Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity VER-82576 (NVP-BEP800) is a potent orally available andselective inhibitor with an of 58 nM for Hsp90βHsp90 IC50VER-82576 also slightly blocks Grp94 and Trap-1 with s ofIC5041 and 55 μM respectively
Bioactivity XL888 is a heat shock protein-90 ( ) inhibitor with anHSP90 of 24 nMIC50
Bioactivity YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathwayagainst glioblastoma directly binding to heat shock protein
with an of 820 nM on NFAT nuclear90 (HSP90) IC50translocation YZ129-induced GBM cell-cycle arrest at the G2Mphase promotes apoptosis and inhibited tumor cellhellip
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VER-82576 (NVP-BEP800) Cat No HY-10942
XL888 Cat No HY-13313
YZ129 Cat No HY-114413
wwwMedChemExpresscom 83
IRE1Inositol requiring enzyme 1
The serinethreonine-protein kinaseendoribonucleaseinositol-requiring enzyme 1 (IRE1) is an enzyme that in humans isencoded by the gene IRE1 is an endoplasmic reticulum (ER)ERN1transmembrane sensor that activates UPR to maintain ER and cellularfunction While mammalian IRE1 promotes cell survive it can initiateapoptosis via decay of anti-apoptotic microRNAsIRE1 activation is initiated by homotypic interactions of thestress-sensing lumenal domain favoring transautophosphorylation ofthe kinase-extension nuclease (KEN) domain on the cytoplasmic sideof the ER membraneIRE1XBP-1 has been shown to regulate a variety of genes in various
cell types in response to ER stress mostly related to ER function and the secretory pathway although the target genesvary depending on the cell type and nature of the stress stimuli
Purity 9977Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9875Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9954Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
50 mg
Purity 9852Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 5 mg
IRE1 Inhibitors amp Modulators
Bioactivity 36-DMAD hydrochloride is a inhibitor of the pathwayIRE1α-XBP1of the unfolded protein response
Bioactivity 4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor ofIRE1α
Bioactivity 6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1αinhibitor with an of 008 μM extracted from patent WOIC502008154484 A1 IRE-lα inhibitor compound 3-5
Bioactivity APY29 is an allosteric modulator of which inhibits IRE1αIRE1αautophosphorylation with of 280 nM and activates IRE1αIC50RNase activity
Bioactivity B I09 is an RNase inhibitor with an of 1230 nMIRE-1 IC50 Bioactivity GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1alpha ( ) which can inhibit and IRE1α IRE1α kinase activity RNase
with s of 20 and 200 nM respectivelyactivity IC50
Bioactivity GSK2850163 hydrochloride is a novel inhibitor ofinositol-requiring enzyme-1 alpha ( ) which can inhibitIRE1α
and with s of 20 andIRE1α kinase activity RNase activity IC50200 nM respectively
Bioactivity KIRA6 allosterically inhibits activity withIRE1α RNase kinasean of 06 microMIC50
Bioactivity Kira8 is a mono-selective inhibitor that allostericallyIRE1αattenuates with an of 59 nM IRE1α RNase activity IC50
[1]Bioactivity MKC3946 is a potent and soluble inhibitor used forIRE1α
cancer research
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36-DMAD hydrochloride Cat No HY-U00460
4μ8C (IRE1 Inhibitor III) Cat No HY-19707
6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) Cat No HY-107371
APY29 Cat No HY-17537
B I09 Cat No HY-107400
GSK2850163 Cat No HY-U00459
GSK2850163 hydrochloride Cat No HY-U00459B
KIRA6 Cat No HY-19708
Kira8 Cat No HY-114368
MKC3946 Cat No HY-19710
wwwMedChemExpresscom 85
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Bioactivity MKC8866 is an inhibitor with an of less thanIRE1 RNase IC5001 μM for IRE1α RNase
Bioactivity MKC9989 is a ( ) inhibitor and alsoHydroxy aryl aldehydes HAAinhibits with an of 023 to 44 μMIRE1α IC50
Bioactivity STF-083010 is an inhibitor STF-083010 inhibits Ire1Ire1endonuclease activity without affecting its kinase activityafter endoplasmic reticulum stress
MKC8866 Cat No HY-104040
MKC9989 Cat No HY-12399
STF-083010 Cat No HY-15845
Kinesin
Kinesin is a protein belonging to a class of motor proteins found ineukaryotic cells Kinesins move along microtubule filaments and arepowered by the hydrolysis of ATP (thus kinesins are ATPases) Theactive movement of kinesins supports several cellular functionsincluding mitosis meiosis and transport of cellular cargo Mostkinesins walk towards the plus end of a microtubule entailstransporting cargo from the centre of the cell towards the peripheryKinesins were discovered as microtubule (MT)-based anterogradeintracellular transport motors The founding member of thissuperfamily the genomes of mammals encode more than 40 kinesinproteins organized into at least 14 families named kinesin-1 through
kinesin-14
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wwwMedChemExpresscom 87
Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9871Clinical Data Phase 2Size 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9973Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg
Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg
Purity 9886Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Kinesin Inhibitors amp Modulators
Bioactivity (R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of ARRY-520(R)-Filanesib ((R)-ARRY-520) is a synthetic kinesin spindle
inhibitor with of 6 nMprotein (KSP) IC50
Bioactivity AZ82 is a selective kinesin-like protein KIFC1 (HSETKIFC1)inhibitor with a of 43 nM and an of 300 nM for KIFC1Ki IC50
Bioactivity CW-069 is an allosteric inhibitor of microtubule motor with an of 75 μMprotein HSET IC50
Bioactivity Dimethylenastron is a potent inhibitor with ankinesin Eg5 of 200 nMIC50
Bioactivity Eg5 Inhibitor V trans-24 is a potent and specific kinesin Eg5inhibitor with an of 065 μM and can be used in theIC50research of cancer
Bioactivity EMD534085 is a potent and selective inhibitor of the mitotic with an of 8 nMkinesin-5 IC50
Bioactivity Filanesib (ARRY-520) is a synthetic kinesin spindle protein inhibitor with of 6 nM(KSP) IC50
Bioactivity Ispinesib is a specific inhibitor of kinesin spindle protein with a of 17 nM(KSP) Ki app
Bioactivity K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5with an of 13 μMIC50
Bioactivity Kif15-IN-1 is an inhibitor of the mitotic Kinesin family member and is used for the research of cellular15 (Kif15)
proliferative diseases
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
AZ82 Cat No HY-12241
CW-069 Cat No HY-15857
Dimethylenastron Cat No HY-19944
Eg5 Inhibitor V trans-24 Cat No HY-112915
EMD534085 Cat No HY-15000
Filanesib (ARRY-520) Cat No HY-15187
Ispinesib (SB-715992) Cat No HY-50759
K858 Racemic Cat No HY-19966
Kif15-IN-1 Cat No HY-15948
Purity 9731Clinical Data Phase 2Size 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9705Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg
Purity 9900Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg
Purity 9959Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9651Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity Kif15-IN-2 is an inhibitor of the mitotic and iskinesin Kif15used for the research of cellular proliferative diseases
Bioactivity Litronesib is a selective mitosis-specific kinesin Eg5inhibitor with antitumor activity
Bioactivity Litronesib (Racemate) is the racemate of litronesibLitronesib is a selective allosteric inhibitor of kinesin
Eg5
Bioactivity Monastrol is a potent and cell-permeable inhibitor of themitotic with an value of 14 μMkinesin Eg5 IC50
Bioactivity Paprotrain is a cell-permeable inhibitor of the kinesin inhibits the ATPase activity of MKLP-2 with an MKLP-2 IC50
of 135 μM and a of 336 μM and shows a moderate inhibitionKiactivity on with an of 55 μMDYRK1A IC50
Bioactivity PF-2771 is a potent and selective centromere protein E inhibitor inhibiting CENP-E motor activity with an(CENP-E)
of 161 nM PF-2771 is used as an anticancer agentIC50
Bioactivity SB-743921 is a potent inhibitor of the mitotic kinesin KSP with a of 01 nM(Eg5) Ki
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Kif15-IN-2 Cat No HY-15949
Litronesib (LY-2523355 KF-89617) Cat No HY-14846
Litronesib Racemate (LY-2523355 Racemate KF-89617 Racemate) Cat No HY-14846A
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Paprotrain Cat No HY-101298
PF-2771 Cat No HY-19530
SB-743921 Cat No HY-12069
wwwMedChemExpresscom 89
LIM Kinase (LIMK)LIMKs
LIM kinases (LIMKs) are important cell cytoskeleton regulators thatplay a prominent role in cancer manifestation and neuronal diseasesThe LIMK family consists of two homologues LIMK1 and LIMK2which differ from one another in expression profile intercellularlocalization and function The main substrate of LIMK is cofilin amember of the actin-depolymerizing factor (ADF) protein familyWhen phosphorylated by LIMK cofilin is inactive LIMKs play acontributory role in several neurodevelopmental disorders and incancer growth and metastasisLIM domain kinases (LIMK1 and 2) are substrate for Cdc42Rac-PAKand modulate actin dynamics by phosphorylating cofilin at serine-3
This modification inactivates cofilinrsquos actin severing and depolymerizing activity LIMKs also translocate into thenucleus and regulate cell cycle progression LIMKs are potential therapeutic targets for NF2 and other merlin-deficienttumors
Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize
Purity 9935Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
LIM Kinase (LIMK) Inhibitors amp Modulators
Bioactivity BMS-3 is a potent inhibitor with s of 5 nM and 6LIMK IC50nM for and respectivelyLIMK1 LIMK2
Bioactivity BMS-5 (LIMKi 3) is a potent inhibitor with s of 7LIMK IC50nM and 8 nM for and respectivelyLIMK1 LIMK2
Bioactivity R-10015 a broad-spectrum antiviral compound for HIVinfection acts as a potent and selective inhibitor of LIM
and binds to the ATP-binding pocketdomain kinase (LIMK)with an of 38 nM for human LIMK1 IC50
[1]
Bioactivity T56-LIMKi is a selective inhibitor of inhibits theLIMK2growth of Panc-1 cells with an of 352 μMIC50
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BMS-3 Cat No HY-18304
BMS-5 (LIMKi 3) Cat No HY-18305
R-10015 Cat No HY-120097
T56-LIMKi (T5601640) Cat No HY-19352
wwwMedChemExpresscom 91
MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughoutthe cytoplasm These tubular polymers of tubulin can grow as long as50 micrometres with an average length of 25 microm and are highlydynamic The outer diameter of a microtubule is about 24 nm whilethe inner diameter is about 12 nm Microtubules are found ineukaryotic cells and are formed by the polymerization of a dimer oftwo globular proteins alpha and beta tubulin Tubulin is one ofseveral members of a small family of globular proteins The tubulinsuperfamily includes five distinct families the alpha- beta- gamma-delta- and epsilon-tubulins and a sixth family which is present only inkinetoplastid protozoa The most common members of the tubulin
family are α-tubulin and β-tubulin the proteins that make up microtubules Microtubules are very important in anumber of cellular processes They are involved in maintaining the structure of the cell
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity 9987Clinical Data Phase 2Size 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Purity 9920Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
50 mg 100 mg
Purity 9982Clinical Data Phase 2Size 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
MicrotubuleTubulin Inhibitors amp Modulators
Bioactivity 10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel derivativewith improved pharmacological features and higher watersolubility IC50 value Target Microtubule inhibitor10-Deacetyl-7-xylosyl paclitaxel induced mitotic cell cyclearrest and apoptosis as measured by flow cytometry DNAhellip
Bioactivity 10-Oxo Docetaxel (Docetaxel Impurity) is a novel taxoid havingremarkable anti-tumor properties and a Docetaxel intermediate
Bioactivity 2-Methoxyestradiol is an inhibitor and angiogenesis apoptosisinducer with potent antineoplastic activity2-Methoxyestradiol also destablize microtubules
Bioactivity 4-Demethylepipodophyllotoxin(4-DMEP) is a key intermediatecompound for the preparation of podophyllotoxin-typeanti-cancer drugs a potent inhibitor of microtubule assembly
Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity ofdocetaxel detected by high performance liquid chromatography(HPLC)
Bioactivity 7-Epi-10-oxo-docetaxel (Docetaxel Impurity C 7-Epitaxotere)is a impurity of docetaxel
Bioactivity 7-epi-Taxol is an active metabolite of taxol with activitycomparable to that of taxol against cell replicationpromoting bundle formation and againstmicrotubulemicrotubule depolymerization
Bioactivity 7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel)derivative Paclitaxel binds to tubulin and inhibits thedisassembly of microtubules
Bioactivity ABT-751(E 7010) is a novel bioavailable tubulin-binding andantimitotic sulfonamide agent with IC50 of about 15 and 34μM in neuroblastoma and non-neuroblastoma cell linesrespectively IC50 Value 15 μM(neuroblastoma) 34μM(non-neuroblastoma) Target MicrotubuleTubulin in vitrohellip
Bioactivity Amphethinile is an agent The affinity constantanti-tubulinfor the association ( ) of Amphethinile with tubulin isKa13 μM
92 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
ABT-751 (E7010) Cat No HY-13270
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
wwwMedChemExpresscom 93
Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9903Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9929Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9996Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9949Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9751Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity Ansamitocin P-3 is a inhibitor Ansamitocin P-3microtubuleis a macrocyclic antitumor antibiotic
Bioactivity Auristatin E is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAE analog and cytotoxin inAntibody-drug conjugates
Bioactivity Auristatin F is a cytotoxic tubulin modifier with potent andselective antitumor activity MMAF analog and cytotoxin inAntibody-drug conjugates
Bioactivity BNC105 is a tubulin polymerization inhibitor with potentantiproliferative and tumor vascular disrupting properties
Bioactivity BTB-1 is a potent selective and reversible mitotic motorprotein inhibitor with an of 169 μMKif18A IC50
Bioactivity Cabazitaxel is a semi-synthetic derivative of the naturaltaxoid 10-deacetylbaccatin III with potential antineoplasticactivity
Bioactivity CCB02 is a selective inhibitor bindingCPAP-tubulin interactionto tubulin and competing for the CPAP binding site ofβ-tubulin with an of 689 nM and shows potent anti-tumorIC50activity CCB02 shows no inhibition on the cell cycle- andcentrosome-related kinases or the phosphorylation status ofhellip
Bioactivity Cephalomannine is a taxol derivative with antitumorantiproliferative properties
Bioactivity Cevipabulin (TTI-237) is an oral microtubule-active antitumorcompound and inhibits the binding of [ H] vinblastine to3
tubulin with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line [1] [2]
Bioactivity Cevipabulin fumarate (TTI-237 fumarate) is an oralmicrotubule-active antitumor compound and inhibits thebinding of [ H] vinblastine to tubulin with an of3 IC50
18-40 nM for cytotoxicity in human tumor cell line [1] [2]
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Auristatin E Cat No HY-15582
Auristatin F Cat No HY-15583
BNC105 Cat No HY-16114
BTB-1 Cat No HY-101770
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
CCB02 Cat No HY-114302
Cephalomannine Cat No HY-77554
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Purity 9828Clinical Data Phase 2Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9956Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity 9831Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 9942Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg
Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9941Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO
200 mg 500 mg
Bioactivity Colchicine is a inhibitor and a tubulin microtubuledisrupting agent Colchicine inhibits microtubulepolymerization with an of 3 nMIC50
Bioactivity Combretastatin A4 is a -targeting agent thatmicrotubulebinds with of 04 μMβ-tubulin Kd
Bioactivity Crolibulin is a small molecule tubulin polymerizationinhibitor
Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate IC50 Value NATarget tubulin ADCs For comparison purposes the ADC A1-mc-MMAD andor A1 -vc-MMAD were used The linker payloadmc-MMAD (6-maleimidocaproyl-monomethylauristatin-D) washellip
Bioactivity D-64131 is a novel inhibitor of Tubulin polymerization thatcompetitively binds with [(3)H]colchicine to αβ-Tubulin
Bioactivity D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Bioactivity D8-MMAE is a deuterated labeled MMAE a potent mitoticinhibitor
Bioactivity D8-MMAF is a deuterated form of MMAF which is a disrupting agentmicrotubule
Bioactivity D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a disrupting agentmicrotubule
Bioactivity DM4 is is an agent that inhibit cell division DM4antitubulincan be used in the preparation of antibody drug conjugate
94 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Colchicine Cat No HY-16569
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Crolibulin (EPC2407) Cat No HY-13603
Cys-mcMMAD Cat No HY-15750
D-64131 Cat No HY-15482
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride Cat No HY-15579AS
DM4 Cat No HY-12454
wwwMedChemExpresscom 95
Purity 9897Clinical Data LaunchedSize 500u g 1 mg
Purity gt98Clinical Data LaunchedSize 1 mg
Purity 9993Clinical Data Phase 2Size 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg
Purity 9988Clinical Data Phase 3Size 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg
Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg
Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 20 mg
Purity 9555Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9983Clinical Data Phase 2Size 1 mg 5 mg
Purity gt98Clinical Data LaunchedSize 100 mg 200 mg
Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 200 mg
Bioactivity Docetaxel is an antineoplastic drug by inhibiting depolymerization and attenuating of themicrotubule
effects of and gene expressionbcl-2 bcl-xL
Bioactivity Docetaxel Trihydrate is a semi-synthetic taxane analogue actsas a stabilizermicrotubule
Bioactivity Angiotensin II human is a vasoconstrictor that acts on the and the receptorAT1 AT2
Bioactivity ELR510444 is a novel microtubule disruptor inhibitsMDA-MB-231 cell proliferation with IC50 of 309 nM not asubstrate for the P-glycoprotein drug transporter and retainsactivity in βIII-tubulin-overexpressing cell lines
Bioactivity Entasobulin is a polymerization inhibitor withβ-tubulinpotential anticancer activity
Bioactivity Epothilone A is a competitive inhibitor of the binding of [H] paclitaxel to polymers with a of 06-14 μM3 tubulin Ki
Bioactivity Epothilone B is a stabilizer with a ofmicrotubule Ki071μM It acts by binding to the αβ-tubulin heterodimersubunit which causes decreasing of αβ-tubulin dissociation
Bioactivity Epothilone D (KOS 862) is a potent stabilizermicrotubule
Bioactivity Eribulin (E7389) is a targeting agent that ismicrotubuleused in the treatment of metastatic breast cancer Eribulin(E7389) inhibits the proliferation of cancer cells by bindingmicrotubule proteins and microtubules
Bioactivity Eribulin mesylate (E7389 mesylate) is a microtubuletargeting agent that is used in the treatment of metastaticbreast cancer Eribulin mesylate (E7389 mesylate) inhibits theproliferation of cancer cells by binding microtubule proteinsand microtubules
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel Trihydrate (RP-56976 (Trihydrate)) Cat No HY-B0011A
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
ELR510444 Cat No HY-16191
Entasobulin Cat No HY-16777
Epothilone A (Epo A) Cat No HY-13503
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone D (KOS 862) Cat No HY-15278
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Purity 9874Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9958Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 9723Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 9903Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9947Clinical Data Phase 3Size 10mM x 1mL in Water
5 mg 10 mg 50 mg
Purity 9801Clinical Data LaunchedSize 10mM x 1mL in Water
10 mg 50 mg 100 mg
Bioactivity Estramustine phosphate sodium is an antimicrotubulechemotherapy agent arrests prostate cancer cells in the G2Mphase of the cell cycle
Bioactivity Fosbretabulin disodium(CA 4DP CA 4P) is a microtubuledestabilizing drug a type of vascular-targeting agent a drugdesigned to damage the vasculature (blood vessels) of cancertumors causing central necrosis IC50 Value 4 nM [1] Targetmicrotubule in vitro Cytotoxic IC(50) values of CA-4 in humanhellip
Bioactivity Ixabepilone is an orally bioavailable inhibitor which binds to tubulin andmicrotubule
promotes tubulin polymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of the cell cycle andinduces tumor cell apoptosis
Bioactivity Lexibulin(CYT-997) is a potent tubulin polymerisationinhibitor with IC50 of 10-100 nM in cancer cell lines withpotent cytotoxic and vascular disrupting activity in vitro andin vivo
Bioactivity Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM in cancer celllines with potent cytotoxic and vascular disrupting activityin vitro and in vivo
Bioactivity Maytansinol inhibits microtubule assembly and inducesmicrotubule disassembly in vitro Target MicrotubuleTubulinin vitro Maytansinol disrupts the mitotic spindle andprevents mitotic exit in Drosophila Maytansinol reduces thegrowth andor survival of HCT116 cells in a dose-dependenthellip
Bioactivity Monomethyl auristatin D (MMAD) a potent tubulin inhibitor isa toxin payload in antibody drug conjugate Mc-MMAD is aprotective group (maleimidocaproyl) -conjugated MMAD IC50Value Target tubulin ADCs For comparison purposes the ADCA1 -mc-MMAD andor A1 -vc-MMAD were used The linkerpayloadhellip
Bioactivity Mc-MMAE is a protective group (maleimidocaproyl)-conjugatedmonomethyl auristatin E (MMAE) which is a potent tubulininhibitor is a toxin payload in antibody drug conjugate (
)ADC
Bioactivity Mc-MMAF is a protective group-conjugated MMAF MMAF is a morepotent drug than Monomethyl auristatin E (MMAE) but ischarged and relatively membrane-impermeable is a potenttubulin inhibitor is a toxin payload in antibody drugconjugate Target MMAF is a new auristatin derivative with ahellip
Bioactivity Mertansine (DM1) is a inhibitor and is anmicrotubulinantibody-conjugatable maytansinoid that is developed toovercome systemic toxicity associated with maytansine and toenhance tumor-specific delivery Mertansine can be attached toa monoclonal antibody with a linker to create an antibody-drughellip
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Estramustine phosphate sodium Cat No HY-13627
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Ixabepilone (Azaepothilone B BMS 247550 BMS 247550-1) Cat No HY-10222
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin dihydrochloride (CYT-997 dihydrochloride) Cat No HY-10498A
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Mc-MMAD Cat No HY-15740
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
wwwMedChemExpresscom 97
Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 100 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9957Clinical Data Phase 3Size 10mM x 1mL in Water
1 mg 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg
Purity 9868Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9994Clinical Data Phase 4Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg 500 mg 1 g
Purity 9989Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg
Bioactivity Microtubule inhibitor 1 is an antitumor agent with inhibitory activity with anmicrotubule polymerization
value of 9-16 nM in cancer cells IC50[1]
Bioactivity MMAD is a potent inhibitor is a toxin payload intubulinantibody drug conjugates ( )ADCs
Bioactivity MMAF (Monomethylauristatin F) is an antitubulin agent thatinhibit cell division inhibits H3397 cell growth with an IC50of 105 nM
Bioactivity MMAF hydrochloride is an antitubulin agent that inhibit celldivision inhibits H3397 cell growth with an of 105 nMIC50
Bioactivity Monomethyl auristatin E (MMAE SGD-1010) is a syntheticderivative of dolastatin 10 and functions as a potent
inhibitor by inhibiting tubulin polymerizationmitoticMMAE is widely used as a cytotoxic component of antibody-drug
to treat several different cancer typesconjugates (ADCs)
Bioactivity Nocodazole is a rapidly-reversible inhibitor of Nocodazole binds to β-tubulin and disruptsmicrotubule
microtubule assemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells Nocodazoleinhibits activates Bcr-Abl CRISPRCas9
Bioactivity Ombrabulin (AVE8062) is a derivative of CA-4 phosphate whichis known to exhibit antivascular effects through selectivedisruption of the cytoskeleton of endothelial cellstubulin
Bioactivity Ombrabulin hydrochloride is a derivative of CA-4 phosphatewhich is known to exhibit antivascular effects throughselective disruption of the cytoskeleton of endothelialtubulincells
Bioactivity OSIP-486823 is a novel -interfering agent withmicrotubuledistinct biological effects on both protein kinase G (PKG) andmicrotubules
Bioactivity Paclitaxel (Taxol) a naturally occurring antineoplasticagent stabilizes resulting intubulin polymerizationarrest at the G2M phase of the cell cycle and apoptotic celldeath [1] [2]
Microtubule inhibitor 1 Cat No HY-114313
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat No HY-15579A
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Nocodazole (Oncodazole R17934) Cat No HY-13520
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin hydrochloride (AVE8062 (hydrochloride) AC7700 (hydrochloride)) Cat No HY-18256
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
Paclitaxel (Taxol) Cat No HY-B0015
Purity 9990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9976Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9979Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9344Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9968Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 25 mg 50 mg 100 mg
Bioactivity Parbendazole is a potent inhibitor of assemblymicrotubuledestabilizes tubulin with an of 879nM and exhibitsEC50a broad-spectrum anthelmintic activity
Bioactivity PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX) compound acts asa -depolymerizing agent and an apoptotic agentmicrotubule
Bioactivity PE859 is a potent inhibitor of both and aggregationtau Aβwith values of 066 and 12 μM respectivelyIC50
Bioactivity PF-06380101 is a novel cytotoxic Dolastatin 10 analogue withexcellent potencies in tumor cell proliferation assays anddifferential ADME properties when compared to other syntheticauristatin analogues that are used in the preparation of ADCsIC50 value ~02 nM(GI50 in BT474 MDA-MB-361-DYT2 and N87hellip
Bioactivity Plinabulin (NPI-2358) is a vascular disrupting agents (VDA)against tubulin-depolymerizing with IC50 of 98~18 nM in tumorcells IC50 Value 98~18 nM Target MicrotubuleTubulin invitro NPI-2358 binds to the colchicine-binding site oftubulin and has potent inhibitory to human tumor cell lineshellip
Bioactivity Podofilox (Podophyllotoxin) is a potent inhibitor ofmicrotubule assembly and DNA topoisomerase II
Bioactivity Rosabulin is a potent inhibitor withmicrotubuleanti-cancer activities
Bioactivity Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10derivative and inhibitor of polymerizationtubulin
Bioactivity SSE15206 is a polymerization inhibitor (GI microtubule 50= 197 nM in HCT116 cells) that overcomes multidrug resistanceCauses aberrant mitosis resulting in G2M arrest due toincomplete spindle formation in cancer cells [1]
Bioactivity Taltobulin (HTI-286 SPA-110) is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibitedproliferation of all three hepatic tumor cell lines (mean IC50= 2 nmolL +- 1 nmolL) in vitro Interestingly no decreasehellip
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Parbendazole (SKF 29044) Cat No HY-115364
PBOX 6 Cat No HY-U00446
PE859 Cat No HY-12662
PF-06380101 Cat No HY-12522
Plinabulin (NPI-2358) Cat No HY-14444
Podofilox (Podophyllotoxin) Cat No HY-15552
Rosabulin (STA 5312) Cat No HY-14934
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
SSE15206 Cat No HY-111425
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
wwwMedChemExpresscom 99
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9838Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9997Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9624Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9996Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Bioactivity Taltobulin hydrochloride is an analogue of Hemiasterlinpotent tubulin inhibitor ADCs cytotoxin IC50 value Targettubulin in vitro HTI-286 significantly inhibits proliferationof all three hepatic tumor cell lines (mean IC50 = 2 nmolL+- 1 nmolL) Interestingly no decrease in viable primaryhellip
Bioactivity Taltobulin trifluoroacetate (HTI-286 SPA-110) is an analogueof Hemiasterlin potent tubulin inhibitor ADCs cytotoxinIC50 value Target tubulin in vitro HTI-286 significantlyinhibited proliferation of all three hepatic tumor cell lines(mean IC50 = 2 nmolL +- 1 nmolL) in vitro Interestinglyhellip
Bioactivity Tasidotin hydrochloride is a peptide analog of the antimitoticdepsipeptide dolastatin 15 as an inhibitor of microtubuleassembly and microtubule dynamics
Bioactivity Tirbanibulin (KX2-391) is an inhibitor of that targetsSrcthe peptide substrate site of Src with of 9-60 nM inGI50cancer cell lines
Bioactivity Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) isan inhibitor of that targets the peptide substrate siteSrcof Src with of 9-60 nM in cancer cell linesGI50
Bioactivity Tirbanibulin (Mesylate) (KX2-391 (Mesylate)) is an inhibitorof that targets the peptide substrate site of Src withSrc
of 9-60 nM in cancer cell linesGI50
Bioactivity Triclabendazole(CGA89317) is a benzimidazole it binds totubulin impairing intracellular transport mechanisms andinterferes with protein synthesis Target MicrotubuleTubulinTriclabendazole treatment produces percentage decreases of thefluke egg output by 153 43 and 366 respectively inhellip
Bioactivity Tubulin inhibitor 1 is a inhibitor occupying thetubulincolchicine binding site inhibits tubulin polymerizationTubulin inhibitor 1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase and inducescellular apoptosis [1]
Bioactivity Tubulysin A(TubA) is a myxobacterial product that can functionas an antiangiogenic agent in many in vitro assaysanti-microtubule anti-mitotic an apoptosis induceranticancer anti-angiogenic and antiproliferative IC50value Target microtubule Tubulysin A is a novel antibiotichellip
Bioactivity Valecobulin (CKD516) a valine prodrug of (S516) and avascular disrupting agent (VDA) is a potent beta-tubulin
inhibitor with marked antitumor activitypolymerizationagainst murine and human solid tumors [1] [2]
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Tasidotin hydrochloride (ILX651) Cat No HY-13760
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin dihydrochloride (KX2-391 (dihydrochloride) KX-01 (dihydrochloride)) Cat No HY-10340A
Tirbanibulin Mesylate (KX2-391 (Mesylate) KX01 (Mesylate)) Cat No HY-10340B
Triclabendazole (CGA89317) Cat No HY-B0621
Tubulin inhibitor 1 Cat No HY-112607
Tubulysin A (TubA) Cat No HY-15995
Valecobulin (CKD-516) Cat No HY-13598
Purity 9958Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Purity 9914Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg
Purity 9966Clinical Data LaunchedSize 10 mg 50 mg 100 mg 200 mg
Purity 9987Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9989Clinical Data Phase 2Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Bioactivity Vc-MMAD consists the ADCs linker(Val-Cit) and potent tubulininhibitor (MMAD) Vc-MMAD is an antibody drug conjugate IC50Valu NA Target tubulin ADCs Monomethyl auristatin D(MMAD) a potent tubulin inhibitor is a toxin payload andantibody drug conjugate For comparison purposes the ADC A1hellip
Bioactivity VcMMAE is a with potentdrug-linker conjugate for ADCantitumor activity by using the anti-mitotic agent monomethylauristatin E (MMAE) linked via the lysosomally cleavabledipeptide valine-citrulline (vc)
Bioactivity Vinblastine sulfate is a cytotoxic alkaloid used againstvarious cancer types Vinblastine sulfate inhibits theformation of microtubule and suppresses nAChR with an ofIC5089 μM
Bioactivity Vincristine sulfate is an antitumor vinca alkaloid whichinhibits formation in mitotic spindlemicrotubuleresulting in an arrest of dividing cells at the metaphasestage It binds to with a of 85 nMmicrotubule Ki
Bioactivity Vinflunine is a new vinca alkaloid uniquely fluorinated withthe properties of mitotic-arresting and tubulin-interactingactivity
Bioactivity Vinflunine Tartrat is a new vinca alkaloid uniquelyfluorinated with the properties of mitotic-arresting andtubulin-interacting activity Target MicrotubuleTubulin Themajor effects of Vinflunine on dynamic instability are aslowing of the microtubule growth rate an increase in growthhellip
Bioactivity Vinorelbine is an anti-mitotic agent which inhibits theproliferation of Hela cells with IC of 125 nM50
Bioactivity Vinorelbine (ditartrate) is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC of 12550nM
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Vc-MMAD Cat No HY-15742
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vincristine sulfate (Leurocristine sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vinflunine Cat No HY-B0628
Vinflunine Tartrate Cat No HY-B0628A
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
wwwMedChemExpresscom 101
Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threoninekinase which ensures proper biorientation of sister chromatids on themitotic spindle by the activation of the spindle assembly checkpoint(SAC) Mps1 has been shown to function as the key kinase thatactivates the spindle assembly checkpoint (SAC) to secure properdistribution of chromosomes to daughter cellsMps1 is a dual specificity protein kinase that is essential for thebipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomesare properly attached Mps1 is expressed at high levels during mitosisand is abundantly expressed in cancer cells Disruption of Mps1
function induces aneuploidy and cell death
Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9952Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9994Clinical Data Phase 1Size 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg
Purity 9992Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Mps1 Inhibitors amp Modulators
Bioactivity AZ3146 is a reasonably potent and selective inhibitorMps1with of 35 nM for Mps1 IC50
CatBioactivity BAY 1217389 is a potent and selective inhibitor of the
monopolar spindle 1 ( ) kinase with an value lessMPS1 IC50than 10 nM
Bioactivity BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1)checkpoint with an of 2 nMIC50
Bioactivity CCT251455 is a potent and selective mitotic kinase monopolarspindle 1 ( ) inhibitor with an of 3 nMMPS1 IC50
Bioactivity CFI-402257 is a highly selective and orally bioavailable inhibitor with an of 17 nM for TTK in vitroTTKMps1 IC50
CFI-402257 has anti-cancer activity [1]
Bioactivity CFI-402257 hydrochloride is a highly selective and orallybioavailable inhibitor with an of 17 nM forTTKMps1 IC50TTK in vitro CFI-402257 hydrochloride has anti-canceractivity [1]
Bioactivity Empesertib (BAY 1161909) is a potent inhibitor withMps1an of lt 1 nMIC50
Bioactivity MPI-0479605 is a potent and selective ATP-competitiveinhibitor of with an of 18 nMMps1 IC50
Bioactivity Mps1-IN-1 is a potent selective and ATP-competitive Mps1kinase inhibitor with an and a of 367 nM and 27 nMIC50 Kd
Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd
12 nM for Mps1 and a of 61 nM for Plk1Kd
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AZ3146 Cat No HY-14710
BAY1217389 Cat No HY-12859
BOS-172722 Cat No HY-112162
CCT251455 Cat No HY-12603
CFI-402257 Cat No HY-101340
CFI-402257 hydrochloride Cat No HY-101340A
Empesertib (BAY 1161909) Cat No HY-12858
MPI-0479605 Cat No HY-12660
Mps1-IN-1 Cat No HY-13298
Mps1-IN-2 Cat No HY-13994
wwwMedChemExpresscom 103
Purity gt98Clinical Data No Development ReportedSize 5 mg
Purity 990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity Mps1-IN-3 is a potent and selective kinase inhibitorMPS1with an of 50 nMIC50
Bioactivity NMS-P715 is a selective ATP-competitive inhibitor of MPS1with an of 182 nMIC50
Bioactivity NMS-P715 analog is an inhibitor of with an of 84MPS1 IC50nM
Mps1-IN-3 Cat No HY-12401
NMS-P715 Cat No HY-12382
NMS-P715 analog Cat No HY-14712
Nucleoside AntimetaboliteAnalog
Nucleoside analogues are molecules that act like nucleosides in DNAsynthesis They include a range of antiviral products used to preventviral replication in infected cells Nucleoside analogues can be usedagainst hepatitis B virus hepatitis C virus herpes simplex and HIVOnce they are phosphorylated they work as antimetabolites by beingsimilar enough to nucleotidesto be incorporated into growing DNAstrands Less selective nucleoside analogues are used aschemotherapy agents to treat cancer eg gemcitabine and 5-FUAntimetabolite is a chemical that inhibits the use of a metabolitewhich is another chemical that is part of normal metabolism Suchsubstances are often similar in structure to the metabolite that they
interfere with such as the antifolates that interfere with the use of folic acid The presence of antimetabolites can havetoxic effects on cells such as halting cell growth and cell division so these compounds are used as chemotherapy forcancer
104 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
wwwMedChemExpresscom 105
Purity gt98Clinical Data No Development ReportedSize 500 mg 100 mg 250 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 10 mg
Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 50 mg
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
Nucleoside AntimetaboliteAnalog Inhibitors amp Modulators
Bioactivity 1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is abicyclic nucleoside
Bioactivity 1-Methylcytosine is a methylated form of the DNA base cytosineand used as a nucleobase of hachimoji DNA in which it pairswith Isoguanine [1] [2]
Bioactivity 1-Methylinosine is a modified nucleotide found at position 37in tRNA 3 to the anticodon of eukaryotic tRNA [1]
Bioactivity 2-Deoxypseudoisocytidine is a nucleoside analogue
Bioactivity 2rsquo-O4rsquo-C-Methyleneuridine (Compound 15a) is a bicyclicnucleoside
Bioactivity 3-Azido-3-deoxy-5-fluorocytidine (Compound 12) is a cytidinederivative
Bioactivity 3-Azido-3-deoxy-beta-L-uridine (Compound 25) is a nucleosidederivative
Bioactivity 3-Methylcytidine a urinary nucleoside can be used as abiomarker of four different types of cancer lung cancergastric cancer colon cancer and breast cancer [1]
Bioactivity 5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methyluridine is a derivative of LNA-type nucleoside
Bioactivity 5-Aza-7-deazaguanine is a substrate for wild-type (WT) E coli and its Ser90Ala mutant in thepurine nucleoside phosphorylase
synthesis of base-modified nucleosides [1]
1-(2-O-4-C-Methylene-beta-D-ribofuranosyl)thymine Cat No HY-111638
1-Methylcytosine Cat No HY-W006395
1-Methylinosine (N1-Methylinosine) Cat No HY-113139
2-Deoxypseudoisocytidine Cat No HY-101968
2rsquo-O4rsquo-C-Methyleneuridine Cat No HY-111639
3-Azido-3-deoxy-5-fluorocytidine Cat No HY-111641
3-Azido-3-deoxy-beta-L-uridine Cat No HY-111642
3-Methylcytidine Cat No HY-111645
5-O-(44-Dimethoxytrityl)-2-O4-C-methylene-5-methylurid
ine
Cat No HY-111807
5-Aza-7-deazaguanine Cat No HY-111627
Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
100 mg
Purity gt98Clinical Data No Development ReportedSize 50 mg
Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
50 mg
Purity 9874Clinical Data Phase 4Size 10mM x 1mL in DMSO
50 mg 100 mg 500 mg
Purity 960Clinical Data LaunchedSize 50 mg 100 mg 500 mg
Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in Water
50 mg
Purity 9986Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity 9999Clinical Data Phase 2Size 10mM x 1mL in DMSO
100 mg 500 mg 1 g 5 g
Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 200 mg 500 mg
Bioactivity 5-Azacytidine is a nucleoside analogue of cytidine thatspecifically inhibits DNA methylation by trapping DNA
methyltransferases
Bioactivity 5-BrdU is a nucleoside analog that competes with thymidine forincorporation into DNA 5-BrdU is commonly used in thedetection of proliferating cells
Bioactivity 5-Fluorouracil is a potent antitumor agent that affectspyrimidine synthesis by inhibiting thymidylate synthetasethus depleting intracellular dTTP pools
Bioactivity 6-Amino-5-nitropyridin-2-one is a pyridine base and used as anucleobase of hachimoji DNA in which it pairs with5-aza-7-deazaguanine [1]
Bioactivity 6-Mercaptopurine is a purine analogue which acts as anantagonist of the and has been widely usedendogenous purinesas antileukemic agent and immunosuppressive drug
Bioactivity 6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MPhydrate) is a purine analogue which acts as an antagonist ofthe and has been widely used asendogenous purinesantileukemic agent and immunosuppressive drug
Bioactivity 6-O-Methyl Guanosine is a modified nucleoside 6-O-Methyl[1]
Guanosine (6-methylguanosine) inhibit colony-forming abilityin a malignant xeroderma pigmentosum cell line [2]
Bioactivity 7-Methylguanosine is a novel cNIIIB nucleotidase inhibitorwith IC value of 878 plusmn 75 microM50
Bioactivity 8-Azaguanine is a purine analogue which shows antineoplasticactivity
Bioactivity Adenosine is a nucleoside composed of a molecule of adenineattached to a ribose sugar molecule (ribofuranose) moiety viaa β-N9-glycosidic bond Target Nucleosideantimetaboliteanalog Adenosine plays an important role inbiochemical processes such as energy transfer mdash as adenosinehellip
106 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
5-Azacytidine (Ladakamycin 5-AzaC Azacitidine) Cat No HY-10586
5-BrdU (BUdR BRDU) Cat No HY-15910
5-Fluorouracil (5-FU) Cat No HY-90006
6-Amino-5-nitropyridin-2-one Cat No HY-50071
6-Mercaptopurine (Mercaptopurine 6-MP) Cat No HY-13677
6-Mercaptopurine hydrate (Mercaptopurine hydrate 6-MP hydrate) Cat No HY-13677A
6-O-Methyl Guanosine Cat No HY-111648
7-Methylguanosine Cat No HY-122524
8-Azaguanine Cat No HY-B1468
Adenosine (Adenine riboside D-Adenosine) Cat No HY-B0228
wwwMedChemExpresscom 107
Purity 9818Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg
Purity 9815Clinical Data No Development ReportedSize 10mM x 1mL in Water
10 mg 50 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
200 mg 1 g
Purity 9897Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity gt98Clinical Data LaunchedSize 100 mg 500 mg
Purity 9999Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg 1 g
Purity gt98Clinical Data No Development ReportedSize 1 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9997Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Bioactivity Capecitabine is an oral prodrug that is converted to itsactive metabolite 5-FU by thymidine phosphorylase
Bioactivity Carmofur is a derivative of fluorouracil an antimetaboliteused as an antineoplastic agent
Bioactivity Clofarabine(Clolar Clofarex) inhibits the enzymaticactivities of ribonucleotide reductase (IC50 = 65 nM) and DNApolymerase IC50 Value 65 nM Target in vitro Clofarabine isa second generation purine nucleoside analog withantineoplastic activity It is phosphorylated intracellularlyhellip
Bioactivity CNDAC is a major metabolite of oral drug sapacitabine and anucleoside analog
Bioactivity Cytarabine a nucleoside analog causes S phase cell cyclearrest and inhibits Cytarabine inhibitsDNA polymerase
with an of 16 nMDNA synthesis IC50
Bioactivity Cytarabine hydrochloride a nucleoside analog causes S phasecell cycle arrest and inhibits CytarabineDNA polymeraseinhibits with an of 16 nMDNA synthesis IC50
Bioactivity Cytidine is a nucleoside molecule that is formed when cytosineis attached to a ribose ring cytidine is a component of RNATarget Nucleoside antimetaboliteanalog Cytidine is anucleoside molecule that is formed when cytosine is attachedto a ribose ring (also known as a ribofuranose) via ahellip
Bioactivity Dacarbazine(DTIC-Dome DTIC) is an antineoplastic agent Ithas significant activity against melanomas Target Nucleosideantimetaboliteanalog Approved May 1975 Dacarbazine (DTIC) isthe only single-agent approved by the Food and DrugAdministration for treating metastatic melanoma With DTIC ashellip
Bioactivity Deoxycytidine triphosphate (dCTP) a nucleoside triphosphateis a raw material in DNA synthesis Deoxycytidine triphosphatehas many applications such as real-time PCR cDNA synthesisand DNA sequencing
Bioactivity Deoxypseudouridine is a nucleotide analog
Capecitabine Cat No HY-B0016
Carmofur (HCFU) Cat No HY-B0182
Clofarabine Cat No HY-A0005
CNDAC Cat No HY-16445A
Cytarabine (Cytosine β-D-arabinofuranoside Cytosine
Arabinoside Ara-C) Cat No HY-13605
Cytarabine hydrochloride (Cytosine β-D-arabinofuranoside
hydrochloride Cytosine Arabinoside hydrochloride hellip) Cat No HY-13605A
Cytidine (Cytosine β-D-riboside Cytosine-1-β-D-ribofuranoside) Cat No HY-B0158
Dacarbazine (Imidazole Carboxamide) Cat No HY-B0078
Deoxycytidine triphosphate (dCTP) Cat No HY-101400
Deoxypseudouridine Cat No HY-101970
Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 200 mg 500 mg 1 g
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9986Clinical Data LaunchedSize 10mM x 1mL in Water
1000u g 2500u g 5 mg 10 mg
Purity gt98Clinical Data LaunchedSize 2500u g 5 mg 10 mg
Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9928Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 200 mg 500 mg
Purity 9952Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity 9991Clinical Data LaunchedSize 10mM x 1mL in Water
1 g 5 g
Purity gt98Clinical Data No Development ReportedSize 50 mg
Bioactivity DMTr-LNA-5MeU-3-CED-phosphoramidite is a nucleoside derivative[1]
Bioactivity Doxifluridine is a thymidine phosphorylase activator forPC9-DPE2 cells with IC50 of 062 μM
Bioactivity Ethynylcytidine is a new nucleoside antimetabolite Bioactivity Floxuridine (5-fluorodeoxyuridine) is an oncology drug thatbelongs to the class known as antimetabolites with an GI50 of51 μM for the inhibition of PEPT1 IC50 value TargetNucleoside antimetaboliteanalog Floxuridine (Fludara) is aprodrug of floxuridine and an oncology agent with an GI50 ofhellip
Bioactivity Fludarabine (NSC 118218) is a inhibitor whichDNA synthesisalso inhibits phosphorylation of STAT1
Bioactivity Fludarabine (phosphate) is an analogue of adenosine anddeoxyadenosine which is able to compete with dATP forincorporation into DNA and inhibit DNA synthesis
Bioactivity Forodesine(BCX-1777 freebase Immucillin-H) is an orallybioavailable PNP inhibitor with picomolar potency inducesapoptosis mainly in T cells
Bioactivity Forodesine hydrochloride is a potent and oral purine nucleoside inhibitor with s ranging from 048 tophosphorylase (PNP) IC50
157 nM
Bioactivity Fosteabine is an oral and prodrug analogue of cytarabine whichis resistant to deoxycytidine deaminase
Bioactivity Gemcitabine (NSC 613327LY188011) is a inhibitorDNA synthesiswhich inhibits the growth of BxPC-3 Mia Paca-2 PANC-1 PL-45and AsPC-1 cells with s of 376 429 927 893 andIC501314 nM respectively
108 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
DMTr-LNA-5MeU-3-CED-phosphoramidite Cat No HY-111531
Doxifluridine (Ro 21-9738 5-Fluoro-5-deoxyuridine 5-DFUR) Cat No HY-B0021
Ethynylcytidine (ECyD TAS-106 3-C-Ethynylcytidine) Cat No HY-16200
Floxuridine (5-Fluorouracil 2-deoxyriboside) Cat No HY-B0097
Fludarabine (F-ara-A NSC 118218) Cat No HY-B0069
Fludarabine phosphate (NSC 118218 (phosphate)) Cat No HY-B0028
Forodesine (BCX-1777 freebase Immucillin-H) Cat No HY-16210
Forodesine hydrochloride (BCX-1777 Immucillin-H hydrochloride) Cat No HY-16209
Fosteabine (Cytarabine ocfosfate YNK 01) Cat No HY-106349
Gemcitabine (NSC 613327 LY188011) Cat No HY-17026
wwwMedChemExpresscom 109
Purity 9575Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg
Purity 9971Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
50 mg
Purity gt98Clinical Data No Development ReportedSize 10 mg
Purity 9829Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg 500 mg
Purity 9962Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
100 mg
Purity 9993Clinical Data LaunchedSize 10mM x 1mL in Water
100 mg 200 mg 500 mg 1 g
Purity 9924Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Bioactivity Gemcitabine elaidate(CP-4126 CO-101) is a lipophilicunsaturated fatty acid ester derivative of gemcitabine (dFdC)an antimetabolite deoxynucleoside analogue with potentialantineoplastic activity IC50 value Target Gemcitabineanalog Upon hydrolysis intracellularly by esterases thehellip
Bioactivity Gemcitabine hydrochloride is a inhibitor withDNA synthesiss of 376 429 927 893 and 1314 nM in BxPC-3 MiaIC50
Paca-2 PANC-1 PL-45 and AsPC-1 cells respectively
Bioactivity Isocytosine is a non-natural nucleobase and an isomer ofcytosine It is used in combination with Isoguanine in studiesof unnatural nucleic acid analogues of the normal base pairsin DNA and used as a nucleobase of hachimoji RNA [1] [2]
Bioactivity Isoguanine is a purine base that is an isomer of guanine Abuilding block in organic synthesis
Bioactivity LY2334737 is an orally available prodrug of gemcitabine whichis a nucleoside analog used as chemotherapy
Bioactivity N2-methylguanosine is a modified nucleoside that occurs atseveral specific locations in many tRNAs
Bioactivity N6N6-Dimethyladenosine is a modified ribonucleosidepreviously found in rRNA and also exhibits in mycobacteriumbovis Bacille Calmette-Gueacuterin tRNA [1]
Bioactivity N6-Etheno 2-deoxyadenosine is a reactive oxygen species(ROS)reactive nitrogen species (RNS)-induced DNA oxidationproduct used as a biomarker to evaluate chronic inflammationand lipid peroxidation in animal or human tissues [1]
Bioactivity Nelarabine (Arranon 506U78) is a purine nucleoside analog andDNA synthesis inhibitor with IC50 from 0067-215 μM in tumorcells Nelarabine is a chemotherapy drug used in T-cell acutelymphoblastic leukemia
Bioactivity Orotic acid (OA) is an intermediate in pyrimidine metabolismIC50 Value Target Nucleoside antimetaboliteanalog in vitroOA increases cell proliferation and decreases apoptosis inserum-starved SK-Hep1 hepatocellular carcinoma cells whichmay ascribe to the inhibition of AMP-activated protein kinasehellip
Gemcitabine elaidate (CP-4126 CO-101 Gemcitabine 5-elaidate) Cat No HY-13538
Gemcitabine Hydrochloride (LY 188011 hydrochloride) Cat No HY-B0003
Isocytosine Cat No HY-W002272
Isoguanine Cat No HY-124143
LY2334737 Cat No HY-13672
N2-Methylguanosine Cat No HY-111647
N6N6-Dimethyladenosine Cat No HY-101984
N6-Etheno 2-deoxyadenosine Cat No HY-111646
Nelarabine (506U78 GW 506U78 Nelzarabine) Cat No HY-13701
Orotic acid (6-Carboxyuracil Vitamin B13) Cat No HY-N0157
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 200 mg 500 mg
Purity 9972Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg
Purity 9969Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 100 mg 200 mg
Purity 9999Clinical Data LaunchedSize 10mM x 1mL in Water
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9783Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg
Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9887Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9745Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Bioactivity Pseudothymidine is a C-nucleoside analog of thymidine Bioactivity Raltitrexed is an antimetabolite drug used in chemotherapyacting by inhibiting thymidylate synthase
Bioactivity RX-3117(TV-1360 Fluorocyclopentenylcytosine) is novel acytidine analog shows anticancer activity in several cancercell lines including gemcitabine-resistant variants
Bioactivity Sapacitabine is an orally available prodrugnucleoside analogthat is structurally related to cytarabine
Bioactivity Tegafur (FT 207 NSC 148958) is a chemotherapeutic 5-FUprodrug used in the treatment of cancers is a component oftegafur-uracil
Bioactivity Tipiracil is a thymidine phosphorylase ( ) inhibitorTPase
Bioactivity Tipiracil (hydrochloride) is a thymidine phosphorylaseinhibitor (TPI) used for cancer research
Bioactivity Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT)is an irreversible inhibitor andthymidylate synthasethereby suppresses Trifluridine is an antiviralDNA synthesisdrug for infectionherpes simplex virus (HSV)
Bioactivity Trifluridine-tipiracil hydrochloride mixture (TAS-102) is anovel oral combination drug that consists of an antineoplasticthymidine-based nucleoside analog trifluorothymidine and apotent inhibitor tipiracil in athymidine phosphorylase105 molar ratio
Bioactivity Vidarabine (Ara-A) an antiviral drug which is active againstherpes simplex and varicella zoster viruses
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Pseudothymidine (5-Methyl-2-Deoxypseudouridin) Cat No HY-101969
Raltitrexed (ZD1694 D1694 ICI-D1694) Cat No HY-10821
RX-3117 (TV-1360 fluorocyclopentenylcytosine) Cat No HY-15228
Sapacitabine (CS682 CYC682) Cat No HY-16445
Tegafur (FT 207NSC 148958) Cat No HY-17400
Tipiracil Cat No HY-A0063A
Tipiracil hydrochloride Cat No HY-A0063
Trifluridine (Trifluorothymidine 5-Trifluorothymidine TFT) Cat No HY-A0061
Trifluridinetipiracil hydrochloride mixture (TAS-102) Cat No HY-16478
Vidarabine (Ara-A Adenine Arabinoside
9-β-D-Arabinofuranosyladenine) Cat No HY-B0277
wwwMedChemExpresscom 111
p97VCPCdc48
p97 an abundant hexameric ATPase of the AAA family is involved inhomotypic membrane fusion It is thought to disassemble SNAREcomplexes formed during the process of membrane fusion Twostructures have been reported a crystal structure of the N-terminaland D1 ATPase domains of murine p97 at 29 A resolution and acryoelectron microscopy structure of full-length rat p97 at 18 Aresolution Together these structures show that the D1 and D2hexamers pack in a tail-to-tail arrangement and that the N domain isflexible A comparison with NSF D2 (ATP complex) reveals possibleconformational changes induced by ATP hydrolysis
Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9765Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9986Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9995Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
p97 Inhibitors amp Modulators
Bioactivity CB-5083 is a potent selective and orally bioavailable p97inhibitor with an value of 11 nMIC50
Bioactivity DBeQ is a selective potent reversible and ATP-competitive inhibitor with an value of 15 μM and 16 μM forp97 IC50
p97(wt) and p97(C522A) respectively DBeQ also inhibits Vps4with an of 115 μMIC50
Bioactivity ML240 is a potent inhibitor inhibiting p97 ATPase withp97 value of 100 nMIC50
Bioactivity ML241 hydrochloride is a potent inhibitor inhibiting p97p97ATPase with value of 100 nMIC50
Bioactivity NMS-859 is a potent covalent inhibitor withVCP (p97)s of 037 and 036 μM for wild-type VCP in the presence ofIC50
60 μM and 1 mM ATP in cells respectively
Bioactivity NMS-873 is a potent selective allosteric inhibitorVCPp97with value of 30 nMIC50
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CB-5083 Cat No HY-12861
DBeQ (JRF 12) Cat No HY-15945
ML240 Cat No HY-19795
ML241 hydrochloride Cat No HY-19797A
NMS-859 Cat No HY-15714
NMS-873 Cat No HY-15713
wwwMedChemExpresscom 113
PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cellproliferation and cell survival PAKs are SerThr kinases that areclassified into two groups on the basis of their structural andfunctional features group I (PAK1ndash3) and group II (PAK4ndash6) Group IPAKs have an auto-inhibitory domain (also called an inhibitory switchdomain) and a kinase domain (catalytic domain CD) and are activatedby the binding of the active (that is GTP-bound) forms of RhoGTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPasesBecause the deregulation of PAKs is closely associated with varioushuman diseasessmall-molecule inhibitors of these kinases have great
potential as therapeutic agents In addition these compounds can also be used as powerful tools in studies aimed atunderstanding the PAK signaling pathwayPAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actinremodelling and their ability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role intumor cell invasion and metastasis The current evidence suggests the involvement of PAKs in motility cell survivalanchorage-independent growth angiogenesis invasion migration and regulation of cell cycle and mitosisConsequently PAKs have also been implicated in a number of pathological conditions including cancer
Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9819Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg
Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9902Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9976Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 200 mg 1 g 5 g
Purity 9995Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 g
PAK Inhibitors amp Modulators
Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB
Bioactivity Fingolimod is a ( ) antagonistsphingosine 1-phosphate S1Pwith of 0033 nM in K562 and NK cells Fingolimod also isIC50a activatorpak1
Bioactivity Fingolimod hydrochloride is a ( )sphingosine 1-phosphate S1Pantagonist with an of 0033 nM in K562 and NK cellsIC50Fingolimod hydrochloride also is a activatorpak1
Bioactivity FRAX1036 is a inhibitor with s of 233 nM 724 nM andPAK Ki24 μM for PAK1 PAK2 and PAK4 respectively
Bioactivity FRAX486 is a p21-activated kinase ( ) inhibitor with sPAK IC50of 14 33 and 39 nM for PAK1 PAK2 and PAK3 respectively
Bioactivity FRAX597 is a potent group I p21-activated Kinases ( s)PAKinhibitor with of 8 13 and 19 nM for and IC50 PAK1 2 3
Bioactivity G-5555 is a potent p21-activated kinase 1 ( ) inhibitorPAK1with s of 37 nM and 11 nM for PAK1 and PAK2 respectivelyKi
Bioactivity G-5555 hydrochloride is a potent and selective p21-activatedkinase 1 ( ) inhibitor with a of 37 nMPAK1 Ki
Bioactivity IPA-3 is a selective non-ATP competitive inhibitor withPAK1 of 25 μM and shows no inhibition to group II PAKs (PAKsIC50
4-6)
Bioactivity NVS-PAK1-1 is a potent and selective allosteric PAK1inhibitor with an of 5 nMIC50
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5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod hydrochloride (FTY720) Cat No HY-12005
FRAX1036 Cat No HY-19538
FRAX486 Cat No HY-15542B
FRAX597 Cat No HY-15542A
G-5555 Cat No HY-19635
G-5555 hydrochloride Cat No HY-19635A
IPA-3 Cat No HY-15663
NVS-PAK1-1 Cat No HY-100519
wwwMedChemExpresscom 115
Purity 9995Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Bioactivity PAK-IN-1 is a inhibitor that displays group IIPAKselectivity PAK-IN-1 inhibits PAK4 PAK5 and PAK6 with sIC50of 75 36 126 nM respectively
Bioactivity PF-3758309 is an inhbitor of with of 13 nM forPAK IC50PAK4
PAK-IN-1 Cat No HY-12632
PF-3758309 Cat No HY-13007
PARPpoly ADP ribose polymerase
PARP is a family of proteins involved in a number of cellular processesinvolving mainly DNA repair and programmed cell death The PARPfamily comprises 17 members They have all very different structuresand functions in the cell PARP1 PARP2 VPARP (PARP4) Tankyrase-1and -2 (PARP-5a or TNKS and PARP-5b or TNKS2) have a confirmedPARP activity Others include PARP3 PARP6 TIPARP (or PARP7)PARP8 PARP9 PARP10 PARP11 PARP12 PARP14 PARP15 andPARP16 PARP is found in the cellrsquos nucleus The main role is to detectand signal single-strand DNA breaks (SSB) to the enzymaticmachinery involved in the SSB repair
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wwwMedChemExpresscom 117
Purity 9924Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 990Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 980Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg
Purity 9839Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9941Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9859Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9992Clinical Data Phase 2Size 10mM x 1mL in Water
200 mg 500 mg
PARP Inhibitors amp Modulators
Bioactivity 3-Aminobenzamide is a potent inhibitor of with of appr 50 nM in CHO cellsPARP IC50
and acts as a mediator of oxidant-induced myocyte dysfunctionduring reperfusion
Bioactivity A-966492 is a novel and potent inhibitor of and with of 1 nM andPARP1 PARP2 Ki
15 nM respectively
Bioactivity AG14361 is a potent inhibitor with a of lt 5 nMPARP-1 Kiand in permeabilized SW620 and intact SW620 cells the sIC50are 29 nM and 14 nM respectively
Bioactivity AZ6102 is a potent dual and inhibitor withTNKS1 TNKS2s of 3 nM and 1 nM respectively and alao has 100-foldIC50
selectivity against other PARP family enzymes with s ofIC5020 μM 05 μM and gt3 μM for PARP1 PARP2 and PARhellip
Bioactivity AZD-2461 is a potent inhibitor with s of 5 nM 2 nMPARP IC50and 200 nM for PARP1 PARP2 and PARP3 respectively
Bioactivity BGP-15 is a inhibitor with an and a of 120 andPARP IC50 Ki57 μM respectively
Bioactivity BRCA1-IN-1 is a novel small-molecule-like inhibitorBRCA1with and of 053 μM and 071 μM respecrivelyIC50 Ki
Bioactivity Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolatedfrom traditional Chinese herb WT WangCorydalis yanhusuoDehydrocorydaline regulates protein expression of Bax Bcl-2activates and inactivates caspase-7 caspase-8 PARP
Bioactivity E7449 is a potent and inhibitor and alsoPARP1 PARP2inhibits and with s of 20 10 50 andTNKS1 TNKS2 IC5050 nM for PARP1 PARP2 TNKS1 and TNKS2 respectively using
P-NAD as substrate32 +
Bioactivity G007-LK is a potent and selective inhibitor of andTNKS1 with s of 46 nM and 25 nM respectivelyTNKS2 IC50
3-Aminobenzamide (PARP-IN-1) Cat No HY-12022
A-966492 Cat No HY-10614
AG14361 Cat No HY-12032
AZ6102 Cat No HY-12975
AZD-2461 Cat No HY-13536
BGP-15 Cat No HY-100828
BRCA1-IN-1 Cat No HY-100863
Dehydrocorydaline (13-Methylpalmatine) Cat No HY-N0674
E7449 Cat No HY-12418
G007-LK Cat No HY-12438
Purity 9952Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9858Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg
Purity 9993Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity 9910Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9965Clinical Data Phase 3Size 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 200 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
Bioactivity GeA-69 is a selective highly cell permeable allostericinhibitor of poly-adenosine-diphosphate-ribose polymerase 14
targeting macrodomain 2 with a of 21 microM (PARP14) Kd[1]
Bioactivity Iniparib (BSI-201) is an irreversible inhibitor of PARP1used in the research of triple negative breast cancer
Bioactivity JW 55 is a potent and selective signaling pathwayβ-catenininhibitor which functions via inhibition of the PARP domainof tankyrase 1 and tankyrase 2 (TNKS12) JW 55 decreasesauto-PARsylation of TNKS12 in vitro with s of 19 μM andIC50830 nM respectively
Bioactivity K-756 is a direct and selective ( ) inhibitortankyrase TNKSwhich inhibits the ADP-ribosylation activity of andTNKS1
with s of 31 and 36 nM respectivelyTNKS2 IC50
Bioactivity ME0328 is a potent and selective inhibitor withARTD3 PARP3an of 089plusmn028 μMIC50
Bioactivity MN-64 is a potent inhibitor with s of 6 nMtankyrase 1 IC5072 nM 191 μM and 394 μM for TNKS2 ARTD1 andTNKS1ARTD2 respectively
Bioactivity Niraparib (MK-4827) is a highly potent and PARP1 PARP2inhibitor with s of 38 and 21 nM respectivelyIC50
Bioactivity Niraparib hydrochloride (MK-4827 hydrochloride) is anexcellent and inhibitor with of 38 and 21PARP1 PARP2 IC50nM respectively
Bioactivity Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent inhibitor with of 24 nMPARP1 IC50
Bioactivity Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1and inhibitor with an of 38 and 21 nMPARP2 IC50respectively
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GeA-69 Cat No HY-108708
Iniparib (BSI-201 NSC-746045 IND-71677) Cat No HY-12015
JW 55 Cat No HY-13968
K-756 Cat No HY-U00422
ME0328 Cat No HY-100225
MN-64 Cat No HY-19351
Niraparib (MK-4827) Cat No HY-10619
Niraparib hydrochloride (MK-4827 (hydrochloride)) Cat No HY-10619A
Niraparib R-enantiomer (MK 4827 (R-enantiomer)) Cat No HY-10619D
Niraparib tosylate (MK-4827 (tosylate)) Cat No HY-10619B
wwwMedChemExpresscom 119
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity gt98Clinical Data No Development ReportedSize 100 mg 250 mg
Purity 9768Clinical Data No Development ReportedSize 10mM x 1mL in Water
10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9997Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2 g
Purity 9931Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg
Purity 9908Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Bioactivity NMS-P118 is a potent orally available and highly selective Inhibitor for cancer therapyPARP-1
Bioactivity NMS-P515 is a potent and stereospecific inhibitorPARP-1with an of 27 nM in hela cells Anti-tumor activity IC50
[1]
Bioactivity NVP-TNKS656 is a highly potent selective and orally active inhibitor with of 6 nM and is gt 300 foldTNKS2 IC50
selectivity against and PARP1 PARP2
Bioactivity Olaparib (AZD2281KU0059436) is a potent and oral PARPinhibitor with s of 5 and 1 nM for and IC50 PARP1 PARP2
respectively
Bioactivity Pamiparib is a inhibitor which can be used for thePARPtreatment of various cancers including the solid tumorextracted from patent WO 2013097225 A1
Bioactivity PARP-2-IN-1 is a potent and selective inhibitor withPARP-2an of 115 nMIC50
Bioactivity PJ34 is a potent specific inhibitor of with ofPARPl 2 IC50110 nM and 86 nM respectively
Bioactivity PJ34 hydrochloride is an inhibitor of with of 110PARPl12 IC50nM and 86 nM respectively
Bioactivity PROTAC PARP1 degrader is a degrader based on thePARP1 technology It induces significant PARP1 cleavage andPROTAC
programmed cell death PROTAC PARP1 degrader at 10 μM at 24 hinhibits MDA-MB-231 cell line with an of 612 μMIC50
Bioactivity RK-287107 is a potent and specific inhibitor withtankyrases of 143 and 106 nM for and IC50 tankyrase-1 tankyrase-2
respectively RK-287107 blocks colorectal cancer cell growth[1]
NMS-P118 Cat No HY-18954
NMS-P515 Cat No HY-128599
NVP-TNKS656 (TNKS656) Cat No HY-13990
Olaparib (AZD2281 KU0059436) Cat No HY-10162
Pamiparib (BGB-290) Cat No HY-104044
PARP-2-IN-1 Cat No HY-102035
PJ34 Cat No HY-13688A
PJ34 hydrochloride Cat No HY-13688
PROTAC PARP1 degrader Cat No HY-114324
RK-287107 Cat No HY-123892
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9962Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9888Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9974Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9508Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9983Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9989Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9981Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 50 mg 100 mg
Bioactivity Rucaparib (AG014699) is an inhibitor of with of 14 nM for PARP1 in aPARP Ki
cell-free assay and also shows binding affinity to eightother PARP domains
Bioactivity Rucaparib Camsylate is an inhibitor of with a of 14PARP KinM for PARP1 and also shows binding affinity to eight otherPARP domains
Bioactivity Rucaparib phosphate (AG-014699 phosphate) is a potent and oral inhibitor with a of 14 nM for PARP1 in cell-freePARP Ki
assay also showing binding affinity to eight other PARPdomains
Bioactivity Talazoparib (BMN-673) is a highly potent inhibitorPARP12with s of 12 nM and 087 nM respectivelyKi
Bioactivity Talazoparib 8R9S (BMN-673 8R9S) is an enantiomer ofTalazoparib less active than Talazoparib on the inhibition of
with an of 144 nMPARP1 IC50
Bioactivity Talazoparib tosylate (BMN 673ts) is a novel potent and orallyavailable inhibitor with an of 057 nM forPARP12 IC50PARP1
Bioactivity UPF 1069 is a inhibitor with s of 8 and 03 μM forPARP IC50PARP-1 and PARP-2 respectively
Bioactivity Veliparib is a potent inhibitor inhibiting andPARP PARP1 with s of 52 and 29 nM respectivelyPARP2 Ki
Bioactivity Veliparib (dihydrochloride) is a potent inhibitor of and with s of 52PARP1 PARP2 Ki
nM and 29 nM in cell-free assays respectively
Bioactivity WD2000-012547 is a selective poly(ADP-ribose)-polymerase(PARP-1) inhibitor with a pK of 8221i
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Rucaparib (AG014699 PF-01367338) Cat No HY-10617A
Rucaparib Camsylate Cat No HY-102003
Rucaparib phosphate (AG-014699 phosphate PF-01367338 phosphate) Cat No HY-10617
Talazoparib (BMN-673 LT-673) Cat No HY-16106
Talazoparib 8R9S (BMN-673 (8R9S) (8R9S)-LT-673) Cat No HY-16106A
Talazoparib tosylate (BMN 673ts) Cat No HY-108413
UPF 1069 Cat No HY-14478
Veliparib (ABT-888) Cat No HY-10129
Veliparib dihydrochloride (ABT-888 dihydrochloride) Cat No HY-10130
WD2000-012547 Cat No HY-U00223
wwwMedChemExpresscom 121
Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Bioactivity XAV-939 is a inhibitor and an indirecttankyrase (TNKS)inhibitor of with s of 5 and 2Wntβ-catenin signaling IC50nM for TNKS1 and TNKS2 respectively
XAV-939 Cat No HY-15147
PERKProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinase
Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) isactivated in response to a variety of endoplasmic reticulum stressesimplicated in numerous disease states PERK is implicated intumorigenesis and cancer cell survival GSK2606414 is an orallyavailable potent and selective PERK inhibitor GSK2606414 inhibitsPERK activation in cells and inhibits the growth of a human tumorxenograft in mice PERK activation is independent of the largeincrease in unfolded nascent proteins within the ER followingtransient global brain ischemia
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Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9966Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9938Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
PERK Inhibitors amp Modulators
Bioactivity CCT020312 is capable of delivering potent and eukaryoticinitiation factor 2-alpha kinase 3 selective(EIF2AK3)proliferation control and also is an activator of RNA-likeendoplasmic reticulum kinase (PERK)
Bioactivity GSK2606414 is a cell-permeable and orally available proteinkinase R-like endoplasmic reticulum (ER) kinase (PERK)inhibitor with an of 04 nMIC50
Bioactivity GSK2656157 is a selective and ATP-competitive inhibitor ofprotein kinase R (PKR)-like endoplasmic reticulum kinase (
) with an of 09 nMPERK IC50
Bioactivity ISRIB (trans-isomer) is a potent inhibitor of with anPERK of 5 nMIC50
CCT020312 Cat No HY-119240
GSK2606414 Cat No HY-18072
GSK2656157 Cat No HY-13820
ISRIB trans-isomer Cat No HY-12495
Polo-like Kinase (PLK)
Polo-like Kinases (PLKs) are important regulators of the cell cycle Plksare involved in the formation of and the changes in the mitoticspindle and in the activation of CDKcyclin complexes duringM-phase of the cell cyclePolo-like kinases (Plks) are a family ofconserved serinethreonine kinases involved in the regulation of cellcycle progression through G2 and mitosis Mammalian polo-likekinases include Plk1 (Xenopus Plx1) Plk2Snk (Xenopus Plx2)Plk3PrkFnK (Xenopus Plx3) Plk4Sak and Plk5 Plk1 is involved in theregulation of key steps during cell division DNA damage repairpathways apoptosis and the progression of the cell cycle Plk3 is amultifunctional stress response protein that responses to signals
induced by DNA damage andor mitotic spindle disruption
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Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9925Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9975Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9982Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg
Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9845Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9897Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9857Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9995Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Polo-like Kinase (PLK) Inhibitors amp Modulators
Bioactivity BI 2536 is a dual and inhibitor with s of 083PLK1 BRD4 IC50
and 25 nM respectively BI-2536 suppresses IFNB[1]
(encoding IFN-β) gene transcription [4]
Bioactivity Centrinone (LCR-263) is a selective and reversible inhibitorof polo-like kinase 4 ( ) with a of 016 nMPlK4 Ki
Bioactivity Centrinone-B (LCR-323) is a potent and highly selective PLK4inhibitor with a of 059 nMKi
Bioactivity CFI-400945 free base is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively
Bioactivity CFI-400945 fumarate is a potent selective and orallybioavailable inhibitor with a and an of 026 nMPLK4 Ki IC50and 28 nM respectively
Bioactivity GSK461364 is a selective reversible and ATP-competitive inhibitor with a value of 22 nMPolo-like kinase 1 (PLK1) Ki
Bioactivity GW843682X is a selective ATP-competitive inhibitor of PLK1and with s of 22 nM and 91 nM respectively andPLK3 IC50is also gt100-fold selective against 30 other kinases
Bioactivity HMN-214 an orally bioavailable prodrug of HMN-176 is aninhibitor of polo-like kinase-1 ( ) with antitumorplk1activity
Bioactivity LFM-A13 is a potent inhibitor inhibitsBTK JAK2 PLKrecombinant BTK Plx1 and PLK3 with s of 25 μM 10 μM andIC5061 μM LFM-A13 shows no effects on JAK1 and JAK3 Src familykinase HCK EGFR and IRK
Bioactivity MLN0905 is a potent inhibitor with an of 2 nMPLK1 IC50
BI 2536 Cat No HY-50698
Centrinone (LCR-263) Cat No HY-18682
Centrinone-B (LCR-323) Cat No HY-18683
CFI-400945 free base Cat No HY-12300
CFI-400945 fumarate Cat No HY-12300B
GSK461364 (GSK461364A) Cat No HY-50877
GW843682X (GW843682) Cat No HY-11003
HMN-214 (IVX-214) Cat No HY-12045
LFM-A13 Cat No HY-18009
MLN0905 (PLK1 Inhibitor) Cat No HY-15155
Purity 9759Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9861Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg
Purity 9949Clinical Data Phase 3Size 10mM x 1mL in Water
5 mg 10 mg 50 mg 100 mg
Purity 9809Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9626Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 950Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 500 mg 1 g
Purity 9970Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9806Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity Mps1-IN-2 is a potent selective and ATP-competitive dual inhibitor with an and a of 145 nM andMps1Plk1 IC50 Kd
12 nM for Mps1 and a of 61 nM for Plk1Kd
Bioactivity NMS-1286937 is a potent selective and orally available PLK1inhibitor with an of 2 nMIC50
Bioactivity Poloxime a hydrolysis product of poloxin is anon-ATP-competitive inhibitor with moderate Plk1Plk1inhibitory activity
Bioactivity Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1)inhibitor that targets the polo-box domain with an ofIC50appr 48 μM
Bioactivity Rigosertib (ON-01910) is a multi-kinase inhibitor and aselective anti-cancer agent which induces apoptosis byinhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib is a selective andhellip[1] [2]
Bioactivity Rigosertib sodium (ON-01910 sodium) is a multi-kinaseinhibitor and a selective anti-cancer agent which inducesapoptosis by inhibition the pathway promots thePI3 kinaseAktphosphorylation of histone H2AX and induces G2M arrest incell cycle Rigosertib sodium is a selective andhellip[1] [2]
Bioactivity Ro3280 is a potent highly selective inhibitor of withPLK1an and a of 3 nM and 009 nM respectively andIC50 Kdnearly has no effect on PLK2 and PLK3
Bioactivity SBE13 is a potent and selective inhibitor with an ofPlk1 IC50200 pM SBE13 poorly inhibits Plk2 (IC gt66 μM) or Plk350(IC =875 nM)50
Bioactivity SBE13 Hydrochloride is a potent and selective inhibitorPlk1with an of 200 pM SBE13 Hydrochloride poorly inhibitsIC50Plk2 (IC gt66 μM) or Plk3 (IC =875 nM)50 50
Bioactivity TAK-960 is an orally available selective inhibitor of with an of 08 nM at 10 μMpolo-like kinase 1 (PLK1) IC50
ATP TAK-960 also shows inhibitory activities against PLK2and with s of 169 and 502 nM respectivelyPLK3 IC50
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Mps1-IN-2 Cat No HY-13994
NMS-1286937 (NMS-P937) Cat No HY-15828
Poloxime Cat No HY-77195
Poloxin Cat No HY-12134
Rigosertib (ON-01910) Cat No HY-12037A
Rigosertib sodium (ON-01910 sodium) Cat No HY-12037
Ro3280 Cat No HY-15161
SBE13 Cat No HY-15158A
SBE13 Hydrochloride Cat No HY-15158
TAK-960 Cat No HY-15160
wwwMedChemExpresscom 127
Purity 9985Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity 9955Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg
Purity gt98Clinical Data Phase 1Size 5 mg 10 mg 50 mg 100 mg
Purity 9980Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity TAK-960 dihydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 dihydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50
Bioactivity TAK-960 hydrochloride is an orally available selectiveinhibitor of with an of 08 nMpolo-like kinase 1 (PLK1) IC50at 10 μM ATP TAK-960 hydrochloride also shows inhibitoryactivities against and with s of 169 hellipPLK2 PLK3 IC50
Bioactivity TC-S 7005 is a inhibitor with s ofPolo-like kinases (Plks) IC504 nM 24 nM and 214 nM for Plk2 Plk3 and Plk1 respectively
[1]
Bioactivity Volasertib is a highly potent Polo-like kinase 1 (PLK1)inhibitor with an of 087 nM as well as the two closelyIC50related kinases and with s of 5 and 56 nMPLK2 PLK3 IC50respectively
Bioactivity Wortmannin is a multi-target inhibitor Wortmannin inhibits PI3K [1] MLCK [1] DNA-PK [2] ATM [2] ATR [2]
and ( ) with s of 3 nM 200 nMPolo-like kinase 3 Plk3 [3] IC5016 nM 150 nM 18 μM and 48 nM respectively
TAK-960 dihydrochloride Cat No HY-15160B
TAK-960 hydrochloride Cat No HY-15160A
TC-S 7005 Cat No HY-108597
Volasertib (BI 6727) Cat No HY-12137
Wortmannin (SL-2052 KY-12420) Cat No HY-10197
PPARPeroxisome proliferator-activated receptors
PPARs (Peroxisome proliferator-activated receptors) areligand-activated transcription factors of nuclear hormone receptorsuperfamily comprising of the following three subtypes PPARαPPARγ and PPARβδ PPARs play essential roles in the regulation ofcellular differentiation development and metabolism (carbohydratelipid protein) and tumorigenesis of higher organisms All PPARsheterodimerize with the retinoid X receptor (RXR) and bind to specificregions on the DNA of target genes Activation of PPAR-α reducestriglyceride level and is involved in regulation of energy homeostasisActivation of PPAR-γ enhances glucose metabolism whereasactivation of PPAR-βδ enhances fatty acids metabolism
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Purity 9905Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg
Purity 9921Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 980Clinical Data Phase 4Size 50 mg
Purity 980Clinical Data LaunchedSize 5 mg 10 mg
Purity gt98Clinical Data Phase 2Size 1 mg
Purity 9900Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data Phase 3Size 10mM x 1mL in DMSO
100 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 g
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PPAR Inhibitors amp Modulators
Bioactivity 4-O-Methyl honokiol is a natural neolignan isolated from acts as a agonist and inhibtisMagnolia officinalis PPARγ
activity used for cancer and inflammation researchNF-κB
Bioactivity 5-Aminosalicylic acid acts as a specific agonist andPPARγalso inhibits p21-activated kinase 1 ( ) and PAK1 NF-κB
Bioactivity Adelmidrol exerts important anti-inflammatory effects that arepartly dependent on Adelmidrol reduces PPARγ NF-κBtranslocation and expressionCOX-2
Bioactivity Aleglitazar(R1439 RO-0728804) is a new dual PPAR-αγ agonistwith IC50 of 28 nM46 nM
Bioactivity Arhalofenate (MBX 102) is a selective partial agonist ofperoxisome proliferator-activated receptor used for(PPAR)-γthe treatment of type 2 diabetes
Bioactivity Astaxanthin a red dietary carotenoid isolated from is an inhibitor of and aHaematococcus pluvialis PPARγ
potent antioxidant with antiproliferative neuroprotective andanti-inflammatory activity Astaxanthin has potential in[1]
the treatment of various diseases such as cancers andhellip
Bioactivity Astragalus polysaccharide are active components of thepolysaccharides extract of Astragulus attenuatesTNF-α-induced insulin resistance by suppressing miR-721 andactivating and in 3T3-L1 adipocytesPPAR-γ PI3KAkt
Bioactivity AVE-8134 is a potent agonist with values of 100PPARα EC50and 3000 nM for human and rodent PPARα receptor respectively
Bioactivity Balaglitazone is a selective partial agonist with anPPARγ of 1351 μM for human EC50 PPARγ
Bioactivity Bezafibrate is an agonist of with s of 50 μM 60PPAR EC50μM 20 μM for and and 90 μMhuman PPARα PPARγ PPARδ55 μM 110 μM for and murine PPARα PPARγ PPARδrespectively Bezafibrate is used as an hypolipidemic agent
4-O-Methyl honokiol Cat No HY-U00450
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
Adelmidrol Cat No HY-B1026
Aleglitazar (R1439 RO0728804) Cat No HY-14728
Arhalofenate (MBX 102 JNJ 39659100) Cat No HY-14831
Astaxanthin Cat No HY-B2163
Astragalus polysaccharide (Astragalus Polysacharin) Cat No HY-N0937
AVE-8134 Cat No HY-U00014
Balaglitazone (DRF 2593 NN 2344) Cat No HY-16086
Bezafibrate (BM15075) Cat No HY-B0637
Purity 9877Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water
5 mg 10 mg 50 mg 100 mg
Purity 9966Clinical Data Phase 4Size 10mM x 1mL in DMSO
500 mg 1 g 5 g 10 g
Purity 9959Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9981Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity 9904Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Bioactivity BMS-687453 is a potent and selective agonist with anPPARα and of 10 nM and 260 nM for human and 4100EC50 IC50 PPARα
nM and gt15000 nM for PPARγ in PPAR-GAL4 transactivationassays
Bioactivity CDDO-Im (CDDO-imidazolide) is an activator of and Nrf2 PPARwith s of 232 and 344 nM for PPARα and PPARγKi
Bioactivity Chiglitazar is a dual agonist with of 12PPARαγ EC s50008 17 μM for PPARα PPARγ and PPARδ respectively
Bioactivity Choline Fenofibrate (ABT-335) is the choline salt offenofibric acid under clinical development as a combinationtherapy with rosuvastatin for the management of dyslipidemia
Bioactivity Ciprofibrate is a peroxisome proliferator-activated receptoragonist
Bioactivity Ciprofibrate D6 is deuterium labeled Ciprofibrate which is aperoxisome proliferator-activated receptor agonist
Bioactivity Clofibrate is an agonist of with s of 50 μM 500PPAR EC50μM for murine PPARα and PPARγ and 55 μM 500 μM for humanPPARα and PPARγ respectively
Bioactivity Daidzein is a soy isoflavone which acts as a activatorPPAR
Bioactivity DG172 dihydrochloride is a selective antagonist withPPARβδan of 27 nMIC50
Bioactivity Elafibranor is a agonist with s of 45 and 175PPARαδ EC50nM respectively
130 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
BMS-687453 Cat No HY-10678
CDDO-Im (RTA-403 TP-235 CDDO-Imidazolide) Cat No HY-15725
Chiglitazar Cat No HY-106266
Choline Fenofibrate (ABT-335) Cat No HY-14739
Ciprofibrate (Win35833) Cat No HY-B0664
Ciprofibrate D6 Cat No HY-B0664S
Clofibrate Cat No HY-B0287
Daidzein Cat No HY-N0019
DG172 dihydrochloride Cat No HY-19737A
Elafibranor (GFT505) Cat No HY-16737
wwwMedChemExpresscom 131
Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg
Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO
100 mg 500 mg 1 g
Purity 9993Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9938Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity 9992Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 g 10 g
Purity 9901Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Bioactivity Ertiprotafib is an inhibitor of PTP1B IkB kinase β (IKK-β)and a dual agonist with an of 16 μMPPARα and PPARβ IC50for PTP1B 400 nM for IKK-β an of ~1 μM forEC50PPARαPPARβ
Bioactivity Eupatilin a lipophilic flavonoid isolated from Artemisiaspecies is a agonist and possesses anti-apoptoticPPARαanti-oxidative and anti-inflammatory activities
Bioactivity Fenofibrate is a agonist with an of 30 μMPPARα EC50 Bioactivity Fenofibric acid an active metabolite of fenofibrate is a activitor with s of 224 microM 147 microM and 106 microMPPAR EC50
for PPARα PPARγ and PPARδ respectively Fenofibric acid alsoinhibits enzyme activity with an of 48 nMCOX-2 IC50
Bioactivity FH535 is an inhibitor of and withWntβ-catenin PPARanti-tumor activities
Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects
Bioactivity Fonadelpar is a agonist used in the research ofPPARδneuroparalytic keratopathy
Bioactivity Gemfibrozil is an activator of used as aPPAR-αlipid-lowering drug Gemfibrozil is also a nonselectiveinhibitor of several isoforms with values forP450 KiCYP2C9 2C19 2C8 and 1A2 of 58 24 69 and 82 μMrespectively
Bioactivity Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2Sanchinoside Rh1) is isolated from the root of Panax GinsengGinsenoside Rh1 inhibits the expression of PPAR-γ TNF-α
and IL-6 IL-1β
Bioactivity Glabridin is a natural isoflavan from bindsGlycyrrhiza glabrato and activates with an of 6115 nM GlabridinPPARγ EC50exhibits antioxidant anti-bacterial anti-nephriticanti-diabetic anti-fungal antitumor anti-inflammatoryantiosteoporotic cardiovascular protective neuroprotectivehellip
Ertiprotafib (PTP 112) Cat No HY-19383
Eupatilin Cat No HY-N0783
Fenofibrate Cat No HY-17356
Fenofibric acid (FNF acid) Cat No HY-B0760
FH535 Cat No HY-15721
Fisetin Cat No HY-N0182
Fonadelpar (NPS-005 SJP-0035) Cat No HY-17633
Gemfibrozil (CI-719) Cat No HY-B0258
Ginsenoside Rh1 (Prosapogenin A2 Sanchinoside B2 Sanchinoside Rh1) Cat No HY-N0604
Glabridin Cat No HY-N0393
Purity 9875Clinical Data Phase 3Size 10mM x 1mL in DMSO
100 mg 200 mg 500 mg
Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9804Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9913Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg
Purity 9727Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9927Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9667Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Bioactivity GSK0660 is a potent antagonist of and withPPARβ PPARδs of 155 nM for both isoformsIC50
Bioactivity GSK376501A is a selective peroxisome proliferator-activatedreceptor gamma ( ) modulator for the treatment of type 2PPARγdiabetes mellitus
Bioactivity GSK3787 is a selective and irreversible peroxisomeproliferator-activated receptor δ ( ) antagonist withPPARδ
of 66pIC50
Bioactivity GW 501516 is a agonist with an of 11 nMPPARδ EC50
Bioactivity GW 6471 is a potent antagonistPPARα Bioactivity GW0742 is a potent and agonist with an ofPPARβ PPARδ IC501 nM for human in binding assay and s of 1 nMPPARδ EC5011 μM and 2 μM for human PPARα and PPARγPPARδrespectively
Bioactivity GW1929 is a potent agonist with a of 884 forPPAR-γ pKihuman and s of 856 and 827 for human PPAR-γ pEC50 PPAR-γ
and murine respectivelyPPAR-γ
Bioactivity GW7647 is a potent agonist with s of 6 nM 11PPARα EC50μM and 62 μM for human PPARα PPARγ and PPARδ respectively
Bioactivity GW9662 is a potent and selective antagonist with anPPARγ of 33 nM showing 10 and 1000-fold selectivity overIC50
PPARα and PPARδ respectively
Bioactivity Icariin is a flavonol glycoside Icariin inhibits andPDE5 activities with s of 432 nM and 7350 μMPDE4 IC50
respectively Icariin also is a activatorPPARα
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GSK0660 Cat No HY-12377
GSK376501A Cat No HY-101746
GSK3787 Cat No HY-15577
GW 501516 (GW 1516 GSK-516) Cat No HY-10838
GW 6471 Cat No HY-15372
GW0742 (GW610742) Cat No HY-13928
GW1929 Cat No HY-15655
GW7647 Cat No HY-13861
GW9662 Cat No HY-16578
Icariin (Ieariline) Cat No HY-N0014
wwwMedChemExpresscom 133
Purity 9972Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9889Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9914Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9921Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg
Purity gt98Clinical Data Phase 2Size 5 mg
Purity 9942Clinical Data Phase 2Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 20 mg
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg 20 mg
Bioactivity Imiglitazar (TAK559) is a potent and dual human andPPARα agonist with values of 67 and 31 nMPPARγ1 EC50
Bioactivity Indeglitazar is an orally available peroxisomeproliferator-activated receptor ( ) pan-agonist for allPPARthree PPAR subtypes alpha (α) delta (δ) and gamma (γ)
Bioactivity Inolitazone a novel high-affinity agonist that isPPARγdependent upon PPARγ for its biological activity with ofIC5008 nM for growth inhibition
Bioactivity Inolitazone dihydrochloride is a novel high-affinity PPARγagonist that is dependent upon PPARγ for its biologicalactivity with of 08 nM for growth inhibitionIC50
Bioactivity KD3010 is a potent orally active and selective PPARδagonist
Bioactivity L-165041 is a cell permeable agonist with s of 6 nMPPARδ Kiand appr 730 nM for PPARδ and PPARγ respectively and inducesadipocyte differentiation in NIH-PPARδ cells
Bioactivity Lanifibranor is a pan peroxisome proliferator-activated ( ) agonist with s of 15 087 and 021receptor PPAR EC50
μM for human and respectivelyPPARα PPARσ PPARγ
Bioactivity LJ570 is a dual agonist with s of 105PPARα PPARγ EC50
and 012 μM respectively [1]
Bioactivity MA-0204 is a potent highly selective and orally availableperoxisome proliferator activated receptor δ ( )PPARδmodulator with s of 04 nM 79 nM and 10 nM for humanEC50mouse and rat PPARδ respectively Potential treatment hellip
Bioactivity Magnolol a natural lignan isolated from the stem bark of is a dual agonist of both andMagnolia officinalis RXRα
with values of 104 microM and 177 microMPPARγ EC50respectively
Imiglitazar (TAK-559) Cat No HY-101649
Indeglitazar (PPM 204) Cat No HY-14817
Inolitazone (Efatutazone CS-7017 RS5444) Cat No HY-14792
Inolitazone dihydrochloride (Efatutazone (dihydrochloride)
CS-7017 (dihydrochloride) RS5444 (dihydrochloride)) Cat No HY-14792B
KD-3010 Cat No HY-111068
L-165041 Cat No HY-20019
Lanifibranor (IVA337) Cat No HY-104049
LJ570 Cat No HY-111775
MA-0204 Cat No HY-114739
Magnolol Cat No HY-N0163
Purity 9639Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9918Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
Purity 9978Clinical Data Phase 3Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in Ethanol
10 mg
Purity gt98Clinical DataSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9872Clinical Data Phase 1Size 10mM x 1mL in DMSO
100 mg 500 mg 1 g 5 g
Bioactivity Naringenin is the predominant flavanone in grapefruitdisplays strong anti-inflammatory and antioxidant activities
Bioactivity Naveglitazar racemate is the racemate of NaveglitazarNaveglitazar is a nonthiozolidinedione peroxisomeproliferator-activated receptor ( ) α-γ dual γ-dominantPPARagonist that has shown glucose-lowering potential in animalmodels and in the clinic
Bioactivity NXT629 is a potent selective and competitive PPAR-αantagonist with an of 77 nM for human PPARα shows highIC50selectivity over other nuclear hormone receptor such asPPARδ PPARγ ERβ GR and TRβ s are 60 15 152 3hellipIC50
Bioactivity Oleoylethanolamide is a high affinity endogenous PPAR-αagonist which plays an important role in the treatment ofobesity and arteriosclerosis
Bioactivity Palmitelaidic acid is the trans isomer of palmitoleic acidPalmitoleic acid is one of the most abundant fatty acids inserum and tissue
Bioactivity Peliglitazar racemate is the racemate of PeliglitazarPeliglitazar is a novel dual αγ PPAR activator
Bioactivity Pemafibrate is a highly selective agonist with anPPARα of 1 nMEC50
Bioactivity Pemafibrate racemate is the racemate of pemafibrate andactivates activity with s of 1 nM gt10 μM andPPARα EC5017 μM for h-PPARα h-PPARγ and h-PPARδ respectively
Bioactivity Pioglitazone is a potent and selective agonist withPPARγhigh affinity binding to the PPARγ ligand-binding domain with
of 093 and 099 μM for human and mouse PPARγEC50respectively
Bioactivity Pioglitazone hydrochloride is a potent and selective PPARγagonist with s of 093 and 099 μM for human and mouseEC50PPARγ respectively
134 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Naringenin Cat No HY-N0100
Naveglitazar racemate Cat No HY-U00036
NXT629 Cat No HY-114263
Oleoylethanolamide (N-(2-Hydroxyethyl)oleamide
N-Oleoyl-2-aminoethanol N-Oleoylethanolamide hellip) Cat No HY-107542
Palmitelaidic Acid (9-trans-Hexadecenoic acid trans-Palmitoleic acid) Cat No HY-N2341
Peliglitazar racemate (BMS 426707-01 racemate) Cat No HY-101738A
Pemafibrate ((R)-K-13675) Cat No HY-17618
Pemafibrate racemate (K13675 (racemate)) Cat No HY-17618A
Pioglitazone (U 72107) Cat No HY-13956
Pioglitazone hydrochloride (U 72107A AD 4833) Cat No HY-14601
wwwMedChemExpresscom 135
Purity 9921Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 200 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9836Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 500 mg 1 g 5 g
Purity 9991Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
100 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9948Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 250 mg
Bioactivity Pirinixic acid (Wy-14643) is a potent agonist of withPPARαs of 063 μM 32 μM for murine and PPARγ and 50EC50 PPARα
μM 60 μM 35 μM for human PPARγ and PPARδPPARαrespectively
Bioactivity PPAR agonist 1 is an agonist of and usedPPAR α PPAR γfor reducing blood glucose lipid levels lowering cholesteroland reducing body weight
Bioactivity PPARα-MO-1 is a potent modulator extracted from patentPPARαWO2004110982A1 formula I
Bioactivity PPARδ agonist is a agonist extracted from patentPPARδUS20180071304 compound example 10
Bioactivity Pparδ agonist 1 is a agonist with an of 506PPAR-δ EC50nM used in the research of PPAR-delta related diseases suchas mitochondrial diseases muscular diseases vasculardiseases demyelinating diseases and metabolic diseases
Bioactivity Pparδ agonist 2 is a agonist extracted from patent WOPPARδ2016057656 A1
Bioactivity Raspberry ketone is a major aromatic compound of redraspberry widely used as a fragrance in cosmetics and as aflavoring agent in foodstuff also shows agonisticPPAR-αactivity
Bioactivity Retinoic acid is a metabolite of vitamin A that playsimportant roles in cell growth differentiation andorganogenesis Retinoic acid is a natural agonist of RARnuclear receptors with s of 14 nM for RARαβγ RetinhellipIC50
Bioactivity RG-12525 is a a specific competitive and orally effectiveantagonist of the and peptidoleukotrienes LTC4 LTD4 LTE4inhibiting LTC4- LTD4- and LTE4-inducd guinea pig parenchymalstrips contractions with s of 26 nM 25 nM and 7 nMIC50respectively RG-12525 is also a peroxisomehellip
Bioactivity Rosiglitazone (BRL49653) is a selective agonist withPPARγs of 30 nM 100 nM and 60 nM for andEC50 PPARγ1 PPARγ2
respectivelyPPARγ
Pirinixic acid (Wy-14643) Cat No HY-16995
PPAR agonist 1 Cat No HY-U00340
PPARα-MO-1 Cat No HY-U00068
Pparδ agonist Cat No HY-112597
Pparδ agonist 1 Cat No HY-107901
Pparδ agonist 2 Cat No HY-100120
Raspberry ketone (Frambione 4-(4-Hydroxyphenyl)-2-butanone) Cat No HY-N1426
Retinoic acid (ATRA Tretinoin Vitamin A acid all-trans-Retinoic acid) Cat No HY-14649
RG-12525 (NID 525) Cat No HY-101676
Rosiglitazone (BRL49653) Cat No HY-17386
Purity 9953Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9852Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9885Clinical Data Phase 3Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg
Purity 9803Clinical Data Phase 3Size 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9925Clinical Data LaunchedSize 100 mg 500 mg
Bioactivity Rosiglitazone maleate is a potent and selective activator of with s of 30 nM 100 nM and 60 nM for PPARγ EC50 PPARγ1
and respectively and a of appr 40 nMPPARγ2 PPARγ Kdfor Rosiglitazone maleate is also an modulator of PPARγ hellip
Bioactivity Saroglitazar is a novel peroxisome proliferator-activatedreceptor ( ) agonist with predominant PPARα and moderatePPARPPARγ activity with values of 065 pM and 3 nM in HepG2EC50cells respectively
Bioactivity Saroglitazar magnesium is a novel peroxisomeproliferator-activated receptor ( ) agonist withPPARpredominant PPARα and moderate PPARγ activity with EC50values of 065 pM and 3 nM in HepG2 cells respectively
Bioactivity Seladelpar is an orally active potent (50 effectconcentration 2 nM) and specific agonistEC50 PPAR-δ
Bioactivity Seladelpar sodium salt (MBX-8025) is an orally active potentand specific agonist with an of 2 nM showingPPARδ EC50more than 750-fold and 2500-fold selectivity over the PPARαand PPARγ receptors respectively
Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki
Bioactivity Troglitazone is a agonist with s of 550 nM andPPARγ EC50780 nM for human and murinePPARγ receptor respectively
136 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Rosiglitazone maleate (BRL 49653C) Cat No HY-14600
Saroglitazar Cat No HY-19937
Saroglitazar Magnesium Cat No HY-19937A
Seladelpar (MBX-8025) Cat No HY-19522
Seladelpar sodium salt (MBX-8025 sodium salt RWJ-800025 sodium salt) Cat No HY-19522A
T0070907 Cat No HY-13202
Troglitazone (CS-045) Cat No HY-50935
wwwMedChemExpresscom 137
RAD51
RAD51 protein family assist in repair of DNA double strand breaksRAD51 family members are homologous to the bacterial RecA andyeast Rad51 In humans RAD51 is a 339-amino acid protein that playsa major role in homologous recombination of DNA during doublestrand break repair RAD51 is involved in the search for homologyand strand pairing stages of the process RAD51 can interact with thessDNA-binding protein RPA BRCA2 PALB2 and RAD52 Recentstudies using fluorescent labeled Rad5 has indicated that Rad51fragments elongate via multiple nucleation events followed bygrowth with the total fragment terminating when it reaches about 2μm in length
Purity 9934Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9930Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9918Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9814Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9978Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
500 mg
RAD51 Inhibitors amp Modulators
Bioactivity Harmine is a natural dual-specificity tyrosinephosphorylation-regulated kinase ( ) inhibitor with(DYRK)anticancer and anti-inflammatory activities
Bioactivity IBR2 is a specific inhibitorRAD51
Bioactivity RAD51 Inhibitor B02 (B02) is an inhibitor of human withRAD51an of 274 μMIC50
Bioactivity RAD51-IN-2 (compound example 67A) is a inhibitorRAD51extracted from patent WO2019051465A1 [1]
Bioactivity RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM Bioactivity RI-2 is a reversible inhibitor with an of 4417RAD51 IC50μM and specifically inhibits homologous recombination repairin human cells
Bioactivity RS-1 is a activator and also increasesRAD51-mediated knock-in efficienciesCRISPRCas9
Bioactivity T0070907 is a potent antagonist with a of 1 nMPPARγ Ki
138 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Harmine (Telepathine) Cat No HY-N0737A
IBR2 Cat No HY-103710
RAD51 Inhibitor B02 (B02) Cat No HY-101462
RAD51-IN-2 Cat No HY-111887
RI-1 Cat No HY-15317
RI-2 Cat No HY-16904
RS-1 Cat No HY-19793
T0070907 Cat No HY-13202
wwwMedChemExpresscom 139
ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROK
ROCK (Rho-associated protein kinase) is a kinase belonging to theAGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopusinvertebrates and chicken Human ROCK1 has a molecular mass of158 kDa and is a major downstream effector of the small GTPaseRhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces thekinase activity of ROCKs by an autoinhibitory intramolecular fold ifRhoA-GTP is not present ROCK plays a role in a wide range ofdifferent cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators
of the cytoskeleton
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9801Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9805Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg 100 mg
Purity 9991Clinical Data LaunchedSize 10mM x 1mL in DMSO
200 mg 500 mg
Purity gt98Clinical Data LaunchedSize 100 mg 200 mg 500 mg
Purity 9976Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg 100 mg
Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9954Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
ROCK Inhibitors amp Modulators
Bioactivity AT13148 is an orally active and ATP-competitive multi- AGC inhibitor with s of 38 nM402 nM50 nM 8 nM 3 nMkinase IC50
and 6 nM4 nM for Akt123 p70S6K PKA and ROCKIIIrespectively
Bioactivity Azaindole 1 is an orally active and ATP-competitive ROCKinhibitor with s of 06 and 11nM for human andIC50 ROCK-1
respectivelyROCK-2
Bioactivity BDP5290 is a potent inhibitor of both and withROCK MRCKs of 5 nM 50 nM 10 nM and 100 nM for IC50 ROCK1 ROCK2
and respectivelyMRCKα MRCKβ
Bioactivity Chroman 1 is a highly potent inhibitor with an ofROCK2 IC501 nM
Bioactivity Fasudil (HA-1077 AT877) a potent inhibitor of with aROCK of 033 μM for ROCK1 which is also a potent Ki Ca channel2+
antagonist and vasodilator
Bioactivity Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877Hydrochloride) a potent inhibitor of with a of 033ROCK Ki
μM for ROCK1 which is also a potent antagonistCa channel2+
and vasodilator
Bioactivity GSK180736A is a G protein-coupled receptor kinase 2 ( )GRK2inhibitor with an of 077 μMIC50
Bioactivity GSK269962A is a potent inhibitor with s of 16 and 4ROCK IC50nM for recombinant human and respectivelyROCK1 ROCK2
Bioactivity GSK429286A is a selective inhibitor of with an ROCK1 IC50value of 14 nM
Bioactivity H-1152 is a membrane-permeable and selective inhibitorROCKwith a value of 16 nM and an value of 12 nM forKi IC50
ROCK2
140 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
AT13148 Cat No HY-16071
Azaindole 1 (TC-S 7001) Cat No HY-10319
BDP5290 Cat No HY-12437
Chroman 1 Cat No HY-15392
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil Hydrochloride (HA-1077 (Hydrochloride) AT-877 (Hydrochloride)) Cat No HY-10341
GSK180736A Cat No HY-18990
GSK269962A (GSK 269962) Cat No HY-15556
GSK429286A Cat No HY-11000
H-1152 Cat No HY-15720
wwwMedChemExpresscom 141
Purity gt98Clinical Data No Development ReportedSize 100 mg 500 mg 250 mg
Purity 9726Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data LaunchedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9975Clinical Data LaunchedSize 10mM x 1mL in Water
5 mg 10 mg 25 mg 50 mg 100 mg
Purity gt98Clinical DataSize 10 mg
Purity 9994Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 9929Clinical Data Phase 2Size 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg 100 mg
Purity 9940Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9813Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Bioactivity H-1152 dihydrochloride is a membrane-permeable and selective inhibitor with a value of 16 nM and an valueROCK Ki IC50
of 12 nM for ROCK2
Bioactivity Hydroxyfasudil is a inhibitor with s of 073 andROCK IC50072 μM for and respectivelyROCK1 ROCK2
Bioactivity Hydroxyfasudil hydrochloride is a inhibitor with sROCK IC50of 073 and 072 μM for and respectivelyROCK1 ROCK2
Bioactivity LX7101 is a potent inhibitor of and with LIMK ROCK2 IC50values of 24 16 and 10 nM for LIMK1 LIMK2 and ROCK2respectively also inhibits with an less than 1 nMPKA IC50
Bioactivity Narciclasine is a plant growth modulator Narciclasinemodulates the RhoRho kinaseLIM kinasecofilin signalingpathway greatly increasing GTPase RhoA activity as well asinducing actin stress fiber formation in a RhoA-dependentmanner
Bioactivity Pentanoic acid a short-chain fatty acid is a product ofbacterial metabolism and are associated with allergic skindisorders Pentanoic acid activates signaling pathwayROCK
Bioactivity Ripasudil (K-115) is a specific inhibitor of with sROCK IC50of 19 and 51 nM for and respectivelyROCK2 ROCK1
Bioactivity Ripasudil free base (K-115 free base) is a specific inhibitorof with s of 19 and 51 nM for and ROCK IC50 ROCK2 ROCK1
respectively
Bioactivity RKI-1447 is a potent small molecule inhibitor of andROCK1 with values of 145 nM and 62 nM respectivelyROCK2 IC50
Bioactivity ROCK inhibitor-2 is a selective dual and ROCK1 ROCK2inhibitor with s of 17 nM and 2 nM respectively IC50
[1]
H-1152 dihydrochloride Cat No HY-15720A
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
LX7101 Cat No HY-12659
Narciclasine (Lycoricidinol) Cat No HY-16563
Pentanoic acid Cat No HY-N6056
Ripasudil (K-115) Cat No HY-15685
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
RKI-1447 Cat No HY-15755
ROCK inhibitor-2 Cat No HY-119937
Purity 9983Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g 2g
Purity 9965Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9932Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 990Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg
Purity 9981Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9843Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Bioactivity ROCK-IN-1 is a potent inhibitor of with an of 12ROCK IC50nM for ROCK2
Bioactivity ROCK2-IN-2 is a selective inhibitor extracted fromROCK2patent US20180093978A1 Compound A-30 has an of lt1IC50μM
Bioactivity SAR407899 is a selective potent and ATP-competitive ROCKinhibitor with an of 135 nM for and s of 36IC50 ROCK-2 KinM and 41 nM for human and rat respectivelyROCK-2
Bioactivity SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an of 135 nM forROCK IC50
and s of 36 nM and 41 nM for human and rat ROCK-2 Ki ROCK-2
respectively
Bioactivity SB-772077B dihydrochloride is an aminofurazan-based Rho inhibitor with s of 56 nM and 6 nM towardkinase( ROCK) IC50
ROCK1 and ROCK2 respevtively [1]
Bioactivity SLx-2119 (KD-025) is a selective inhibitor of with anROCK2 of 105 nMIC50
Bioactivity SR-3677 is a potent and selective inhibitor with anROCK-II of ~3 nMIC50
Bioactivity Thiazovivin is a potent inhibitor which can protectROCKhuman embryonic stem cells
Bioactivity Y-27632 is an ATP-competitive inhibitor of and ROCK-I ROCK-IIwith of 220 nM and 300 nM for and Ki ROCK-I ROCK-II
respectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip
Bioactivity Y-27632 dihydrochloride is a cell-permeable ATP-competitiveinhibitor of and with s of 220 and 300 nMROCK-I ROCK-II Kirespectively which primes human induced pluripotent stemcells (hIPSCs) to selectively differentiate towardsmesendodermal lineage via epithelial-mesenchymalhellip
142 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
ROCK-IN-1 Cat No HY-U00351
ROCK2-IN-2 Cat No HY-103620
SAR407899 Cat No HY-15687A
SAR407899 hydrochloride Cat No HY-15687
SB-772077B dihydrochloride Cat No HY-108518
SLx-2119 (KD-025) Cat No HY-15307
SR-3677 Cat No HY-13300
Thiazovivin Cat No HY-13257
Y-27632 Cat No HY-10071
Y-27632 dihydrochloride Cat No HY-10583
wwwMedChemExpresscom 143
Purity 9923Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9792Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9898Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Bioactivity Y-33075 is a selective inhibitor derived from Y-27632ROCKand is more potent than Y-27632 with an of 36 nMIC50
Bioactivity Y-33075 dihydrochloride is a selective inhibitor with anROCK of 36 nMIC50
Bioactivity ZINC00881524 is a inhibitorROCK
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 dihydrochloride Cat No HY-10069
ZINC00881524 Cat No HY-101244
Sirtuin
Sirtuin (Sir2 proteins) are a class of proteins that possess eithermono-ADP-ribosyltransferase or deacylase activity includingdeacetylase desuccinylase demalonylase demyristoylase anddepalmitoylase activity Sirtuins regulate important biologicalpathways in bacteria archaeaand eukaryotes Sirtuins have beenimplicated in influencing a wide range of cellular processes like agingtranscription apoptosis inflammation and stress resistance as well asenergy efficiency and alertness during low-calorie situations Sirtuinscan also control circadian clocks and mitochondrial biogenesis
144 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
wwwMedChemExpresscom 145
Purity 9891Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9802Clinical Data Phase 2Size 10mM x 1mL in DMSO
100 mg 500 mg 1 g
Purity 9909Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
100 mg
Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9959Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg
Purity 9866Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity 9987Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Sirtuin Inhibitors amp Modulators
Bioactivity 3-TYP is a selective inhibitor with an of 16 nMSIRT3 IC50more potent over SIRT1 ( =88 nM) SIRT2 ( =92 nM)IC50 IC50
Bioactivity AGK2 is a selective inhibitor with of 35 μM AGK2SIRT2 IC50can also inhibit and with of 30 and 91 μMSIRT1 SIRT3 IC50respectively
Bioactivity AK-1 is a potent specific and cell-permeable inhibitorSIRT2with an of 125 μMIC50
Bioactivity AK-7 is a selective cell- and brain-permeable inhibitorSIRT2with an of 155 μMIC50
Bioactivity Cambinol is a and inhibitor with values of 56SIRT1 SIRT2 IC50and 59 μM respectively
Bioactivity CAY10602 is a activatorSIRT1
Bioactivity Dihydrocoumarin is a compound found in Melilotus Dihydrocoumarin is a inhibitorofficinalis yeast Sir2p
Dihydrocoumarin also inhibits and withhuman SIRT1 SIRT2s of 208 μM and 295 μM respectively IC50
[1]
Bioactivity Fisetin is a natural flavonol found in many fruits andvegetables with various benefits such as antioxidantanticancer neuroprotection effects
Bioactivity Ginkgolide C is a flavone isolated from leavesGinkgo bilobapossessing multiple biological functions such as decreasingplatelet aggregation and ameliorating Alzheimer disease
Bioactivity Inauhzin is a dual inhibitor and acts as anSirT1IMPDH2activator used in the research of cancerp53
3-TYP Cat No HY-108331
AGK2 Cat No HY-100578
AK-1 Cat No HY-101465
AK-7 Cat No HY-16691
Cambinol Cat No HY-100732
CAY10602 Cat No HY-104073
Dihydrocoumarin (Hydrocoumarin Chroman-2-one) Cat No HY-N1926
Fisetin Cat No HY-N0182
Ginkgolide C (BN-52022 Ginkgolide-C) Cat No HY-N0785
Inauhzin (INZ) Cat No HY-15869
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg
Purity 9850Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity 9982Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9876Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Purity 9822Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
1 g 5 g
Purity 9922Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg
Bioactivity MC3482 is a specific sirtuin5 ( ) inhibitorSIRT5 Bioactivity Nicotinamide is a form of vitamin B3 that plays essentialroles in cell physiology through facilitating NAD+ redoxhomeostasis and providing NAD+ as a substrate to a class ofenzymes that catalyze non-redox reactions Nicotinamide is aninhibitor of SIRT1
Bioactivity OSS_128167 is a selective inhibitor with s of 89SIRT6 IC501578 and 751 μM for and respectivelySIRT6 SIRT1 SIRT2
Bioactivity PROTAC Sirt2 Degrader-1 is a SirReal-based acts as aPROTAC degrader composed of a highly potent andSirt2
isotype-selective inhibitor a linker and a bona fideSirt2cereblon ligand for E3 ubiquitin ligase PROTAC Sirt2Degrader-1 shows an of 025 μM for Sirt2 with no effecthellipIC50
Bioactivity Salermide is an inhibitor of and can cause strongSirt1 Sirt2cancer-specific apoptotic cell death
Bioactivity Selisistat (EX-527) is a potent and selective inhibitorSIRT1with of 98 nMIC50
Bioactivity Selisistat S-enantiomer (EX-527 S-enantiomer) is theS-enantiomer of Selisistat with an of 123 nM for SIRT1IC50Selisistat S-enantiomer is much more potent than SelisistatR-enantiomer
Bioactivity SIRT-IN-1 is a potent inhibitor of with of 15SIRT123 IC s5010 33 μM respectively
Bioactivity SIRT-IN-2 is a potent inhibitor of with of 4SIRT123 IC s504 7 μM respectively
Bioactivity Sirt2-IN-1 (Compound 9) is a ( ) inhibitor withsirtuin 2 Sirt2an of 163 nM IC50
[1]
146 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
MC3482 Cat No HY-112587
Nicotinamide (Niacinamide Nicotinic acid amide Vitamin B3) Cat No HY-B0150
OSS_128167 Cat No HY-107454
PROTAC Sirt2 Degrader-1 Cat No HY-103636
Salermide Cat No HY-101073
Selisistat (EX-527) Cat No HY-15452
Selisistat S-enantiomer (EX-527 (S-enantiomer)) Cat No HY-15452A
SIRT-IN-1 Cat No HY-16615
SIRT-IN-2 Cat No HY-16616
Sirt2-IN-1 Cat No HY-112427
wwwMedChemExpresscom 147
Purity 9824Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg 100 mg
Purity 9939Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize
Purity 9887Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg 200 mg 500 mg 1 g
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 500 mg 100 mg
Purity 9944Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Bioactivity SIRT5 inhibitor 1 is a potent Human deacylaseSirtuin 5inhibitor with an of 011 μMIC50
Bioactivity Sirtinol is a inhibitor with s of 48 μM 577 μMsirtuin IC50and 131 μM for ySir2 hSIRT2 and hSIRT2 respectively
Bioactivity Sirtuin modulator 1 is a modulator of a homolog of SIRTl SIRT3with EC of lt 1 μM extracted from patent WO 201007185315A1 Compound No4
Bioactivity SRT 1460 a potent activator with an Sirtuin-1 (SIRT1) EC15value of 29 μM shows good selectivity for activation ofSIRT1 versus SIRT2 and SIRT3 (EC15 gt 300 μM) and is morepotent than Resveratrol and the closest sirtuin homologhellip
Bioactivity SRT 1720 is a selective activator of human with anSIRT1 of 016 μM and shows less potent activities agaiinstEC15
SIRT2 and SIRT3 with EC s of 37 μM and gt 300 μM15respectively
Bioactivity SRT 1720 Hydrochloride is a selective activator of withSIRT1an of 016 μM and shows less potent activities onEC15SIRT2 and SIRT3 with EC s of 37 μM and 300 μM15respectively
Bioactivity SRT 2104 is a first-in-class highly selective andbrain-permeable activator of the NAD dependent deacetylase+
increases Sirt1 protein but shows no effect on Sirt1Sirt1mRNA Used in the research of diabetes mellitus hellip
Bioactivity SRT 2183 is a selective activator with anSirtuin-1 (SIRT1) value of 036 μM SRT 2183 induces growth arrestEC15
[1]
and apoptosis concomitant with deacetylation of STAT3 andNF-κB and reduction of c-Myc protein levels [2]
Bioactivity Tenovin-1 is an inhibitor of and ansirtuin 1 sirtuin 2activator of and may have potential in the management ofp53cancer
Bioactivity Tenovin-6 is an inhibitor of and slightly inhibitsSIRT1 SIRT2 and is also a potent activator of with s ofHDAC8 p53 IC50
21 μM 10 μM and 67 μM for SirT1 SirT2 and SirT3respectively
SIRT5 inhibitor 1 Cat No HY-112634
Sirtinol Cat No HY-13515
Sirtuin modulator 1 Cat No HY-19758A
SRT 1460 Cat No HY-124037
SRT 1720 Cat No HY-10532
SRT 1720 Hydrochloride Cat No HY-15145
SRT 2104 Cat No HY-15262
SRT 2183 Cat No HY-19759
Tenovin-1 Cat No HY-13423
Tenovin-6 Cat No HY-15510
Purity 9855Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9884Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 50 mg 100 mg
Bioactivity Tenovin-6 Hydrochloride is an inhibitor of and SIRT1 SIRT2slightly inhibits and is also a potent activator ofHDAC8
with s of 21 μM 10 μM and 67 μM for SirT1 SirT2p53 IC50and SirT3 respectively
Bioactivity Thiomyristoyl is a potent and specific inhibitor with anSIRT2 of 28 nMIC50
Bioactivity UBCS039 is the first synthetic specific Sirtuin 6 (SIRT6)activator inducing autophagy in human tumor cells with an
of 38 μM EC50[1]
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Tenovin-6 Hydrochloride Cat No HY-15510B
Thiomyristoyl Cat No HY-101278
UBCS039 Cat No HY-115453
wwwMedChemExpresscom 149
SRPKSerine-arginine protein kinases
SRPKs is a critical enzyme family that regulates splicing activity in thecell The first serine-arginine (SR) protein kinase identified is SRPK1which is isolated from mitotic cells and it is described tophosphorylate SR proteins and to promote their release from nuclearspeckles during the G2M phase of the cell cycle SRPK1 is theprototype of the SRPK family which also includes the twohomologous SRPK2 and SRPK3 proteins SRPKs are characterized by abipartite catalytic domain separated by a unique spacer sequence andare mainly localized in the cytoplasm of mammalian cellsSRPKs can translocate into the nucleus of cells under severalconditions such as during the G2M phase of the cell cycle or after
osmotic stress or as a consequence of activation of the epidermal growth factor (EGF) signal transduction pathway
Purity gt98Clinical Data No Development ReportedSize 500 mg 250 mg
Purity 9996Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9917Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
SRPK Inhibitors amp Modulators
Bioactivity SPHINX31 is a potent and selective inhibitor of with an ofserinearginine-rich protein kinase 1 (SRPK1) IC50
59 nM SPHINX31 inhibits phosphorylation ofserinearginine-rich splicing factor 1 (SRSF1) SPHINX31 is apotential topical therapeutic for neovascular eye diseasehellip
Bioactivity SRPIN340 is an ATP-competitive serine-arginine-rich proteinkinase ( ) inhibitor with a of 089 μM for SRPK1SRPK Ki
Bioactivity SRPKIN-1 is a covalent and irreversible inhibitorSRPK12with s of 356 and 98 nM respectively Anti-angiogenesisIC50
effect [1]
150 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
SPHINX31 Cat No HY-117661
SRPIN340 (SRPK inhibitor) Cat No HY-13949
SRPKIN-1 Cat No HY-116856
wwwMedChemExpresscom 151
Telomerase
Telomerase is a ribonucleoprotein that is an enzyme that adds DNAsequence repeats (TTAGGG in all vertebrates) to the 3 end of DNAstrands in the telomere regions which are found at the ends ofeukaryotic chromosomes This region of repeated nucleotide calledtelomeres contains noncoding DNA and hinders the loss of importantDNA from chromosome ends As a result every time the chromosomeis copied only 100ndash200 nucleotides are lost which causes no damageto the organisms DNA Telomerase is a reverse transcriptase thatcarries its own RNA molecule which is used as a template when itelongates telomeres which are shortened after each replication cycleTelomerase a eukaryotic ribonucleoprotein (RNP) complex contains
both an essential RNA and a protein reverse transcriptase subunit By reverse transcription the telomerase RNPmaintains telomere length stability in almost all cancer cells
Purity 980Clinical Data No Development ReportedSize 100 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9955Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 980Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Telomerase Inhibitors amp Modulators
Bioactivity 360A is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay
Bioactivity 360A iodide is a selective stabilizer of and alsoG-quadruplexinhibits activity with an of 300 nM fortelomerase IC50telomerase in TRAP-G4 assay
Bioactivity BIBR 1532 is a potent selective and non-competitive inhibitor with of 100 nM intelomerase IC50
a cell-free assay
Bioactivity Telomerase-IN-1 is a inhibitor with an ofTelomerase IC50019 μM
Bioactivity TMPyP4 tosylate (TMP 1363) is a -specific ligandquadruplexwhich inhibits the interaction between G-quadruplexes andIGF-1 TMPyP4 tosylate (TMP 1363) is a [1] telomeraseinhibitor with antitumor effects in osteosarcoma cell lihellip
152 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
360A Cat No HY-15595
360A iodide (360 A iodide) Cat No HY-15595A
BIBR 1532 Cat No HY-17353
Telomerase-IN-1 Cat No HY-U00268
TMPyP4 tosylate (TMP 1363) Cat No HY-108477
wwwMedChemExpresscom 153
TOPKT-LAK cell-originated protein kinase
TOPK (T-lymphokine-activated killer cellndashoriginated protein kinasealso known as PBK or PDZ-binding kinase) is a SerThr protein kinasethat is highly expressed in many types of human cancer includingbreast and lung cancers TOPK is included in the ldquoconsensus stemnessranking signaturerdquo gene list that is up-regulated in cancer stemcell-enriched tumors and is associated with poor prognosis inmultiple types of cancerTOPKPBK is an oncogenic kinase upregulated in most humancancers TOPK is important for mitotic cell division and thatphosphorylation by Cdk1 is needed for its activationTOPK a member of the MEK36-related MAPKK family is expressed in
a wide range of proliferating cells and tissues including cancer cells and testis TOPK negatively regulates the activityof p38α by phosphorylating the p38α-specific phosphatase MKP1 and enhancing the stability of MKP1 The MAPKphosphatase MKP1 an archetypal member of the MKP family plays a pivotal role in the deactivation of p38 through adephosphorylation reaction
Purity 9563Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9905Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9936Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
TOPK Inhibitors amp Modulators
Bioactivity HI-TOPK-032 is a potent and specific inhibitorTOPK Bioactivity OTS-964 is a potent T-lymphokine-activated killer inhibitor ( =28cell-originated protein kinase (TOPK) IC50
nM) which inhibits TOPK kinase activity with high affinityand selectivity
Bioactivity OTS514 is a highly potent inhibitor which inhibits TOPKTOPKkinase activity with a median inhibitory concentration ( )IC50value of 26 nM
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HI-TOPK-032 Cat No HY-101550
OTS-964 Cat No HY-12467
OTS514 Cat No HY-18621
wwwMedChemExpresscom 155
Topoisomerase
Topoisomerases are enzymes that regulate the overwinding orunderwinding of DNA The winding problem of DNA arises due to theintertwined nature of its double-helical structure Topoisomerases areisomerase enzymes that act on the topology of DNA Type Itopoisomerase cuts one strand of a DNA double helix relaxationoccurs and then the cut strand is reannealed Type I topoisomerasesare subdivided into two subclasses type IA topoisomerases whichshare many structural and mechanistic features with the type IItopoisomerases and type IB topoisomerases which utilize acontrolled rotary mechanism Type II topoisomerase cuts both strandsof one DNA double helix pass another unbroken DNA helix through
it and then reanneal the cut strands This class is also split into two subclasses type IIA and type IIB topoisomeraseswhich possess similar structure and mechanisms
Purity 9802Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg
Purity 9998Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg 500 mg
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Purity 980Clinical Data LaunchedSize 1 mg 5 mg
Purity 9975Clinical Data Phase 3Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9243Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg
Purity 9808Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg
Purity 9889Clinical Data Phase 2Size 10mM x 1mL in DMSO
2 mg 5 mg 10 mg 25 mg
Topoisomerase Inhibitors amp Modulators
Bioactivity 9-Aminocamptothecin is a inhibitor withtopoisomerase Ipotent anticancer activity
Bioactivity Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) afluorescent molecule and the first described non-peptidicinhibitor showing discrete specificity for the CTRL(chymotrypsin-like) activity of the 20S proteasome [1]
Aclacinomycin A hydrochloride is also a dual inhibitor ofhellip
Bioactivity Aldoxorubicin (INNO-206) is an albumin-binding prodrug ofdoxorubicin which is released from albumin under acidicconditions Aldoxorubicin (INNO-206) has potent antitumoractivities in various cancer cell lines and in murine tumormodels
Bioactivity Amonafide is a inhibitor and DNAtopoisomerase IIintercalator that induces apoptotic signaling by blocking thebinding of Topo II to DNA
Bioactivity Amrubicin (SM-5887) is a DNA inhibitortopoisomerase IIused for the research of cancer
Bioactivity Amrubicin (hydrochloride) (SM-5887 (hydrochloride)) is a DNA inhibitor used for the research of cancertopoisomerase II
Bioactivity Amsacrine (m-AMSA) is an inhibitor of andtopoisomerase IIacts as an antineoplastic agent which can intercalates intothe DNA of tumor cells
Bioactivity Amsacrine hydrochloride (mAMSA hydrochloride) is an inhibitorof and acts as an antineoplastic agenttopoisomerase IIwhich can intercalates into the DNA of tumor cells
Bioactivity Banoxantrone D12 (AQ4N D12) is the deuterium labeledbanoxantrone Banoxantrone is a novel bioreductive agent thatcan be reduced to a stable DNA-affinic compound AQ4 which isa potent inhibitortopoisomerase II
Bioactivity Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) isthe deuterium labeled banoxantrone dihydrochlorideBanoxantrone is a novel bioreductive agent that can be reducedto a stable DNA-affinic compound AQ4 which is a potent
inhibitortopoisomerase II
156 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
9-amino-CPT (9-amino-20(S)-camptothecin) Cat No HY-100309
Aclacinomycin A hydrochloride (Aclarubicin hydrochloride) Cat No HY-N2306A
Aldoxorubicin (INNO-206 DOXO-EMCH) Cat No HY-16261
Amonafide (AS1413) Cat No HY-10982
Amrubicin (SM-5887 AMR) Cat No HY-B0067
Amrubicin hydrochloride (SM-5887 (hydrochloride) AMR (hydrochloride)) Cat No HY-B0067A
Amsacrine (m-AMSA acridinyl anisidide) Cat No HY-13551
Amsacrine hydrochloride (m-AMSA hydrochloride acridinyl anisidide hydrochloride) Cat No HY-13551A
Banoxantrone D12 (AQ4N D12) Cat No HY-13562S
Banoxantrone D12 dihydrochloride (AQ4N D12 dihydrochloride) Cat No HY-13562AS
wwwMedChemExpresscom 157
Purity 9927Clinical Data LaunchedSize 10mM x 1mL in Water
10 mg 50 mg 100 mg 200 mg 500 mg
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Purity 9856Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
2 mg 5 mg 10 mg
Purity 9826Clinical Data Phase 4Size 10mM x 1mL in DMSO
100 mg 500 mg
Purity 9635Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Purity 9818Clinical Data Phase 2Size 10mM x 1mL in DMSO
100 mg 200 mg 500 mg
Purity 9956Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 g
Purity gt98Clinical Data LaunchedSize 100 mg 500 mg
Purity 9880Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9817Clinical Data No Development ReportedSize 10mM x 1mL in Water
5 mg 10 mg 25 mg
Bioactivity Banoxantrone dihydrochloride is a novel bioreductive agentthat can be reduced to a stable DNA-affinic compound AQ4which is a potent inhibitortopoisomerase II
Bioactivity Belotecan hydrochloride (CKD-602 hydrochloride) a inhibitor is a synthetic and water-solubleTopoisomerase I
camptothecin derivative
Bioactivity Berberine chloride is an alkaloid isolated from the Chineseherbal medicine Huanglian as an Berberine chlorideantibioticinduces reactive oxygen species ( ) generation andROSinhibits Antineoplastic propertiesDNA topoisomerase
[1]
Bioactivity Berberine chloride hydrate is an alkaloid isolated from theChinese herbal medicine Huanglian as an Berberineantibioticchloride hydrate induces reactive oxygen species ( )ROSgeneration and inhibits AntineoplasticDNA topoisomeraseproperties [1]
Bioactivity Betulinic acid is a natural pentacyclic triterpenoid acts asa eukaryotic inhibitor with an of 5topoisomerase I IC50μM and possesses anti-HIV anti-malarial anti-inflammatoryand anti-tumor properties
Bioactivity Bisantrene is a highly effective antitumor drug targetseukaryotic type II topoisomerases
Bioactivity Campathecin is a potent DNA enzyme topoisomerase Iinhibitor with an of 679 nMIC50
Bioactivity Daun02 is a prodrug of the inhibitortopoisomeraseDaunorubicin
Bioactivity Daunorubicin (RP 13057 Daunomycin Rubidomycin) is a inhibitor with potent antineoplastictopoisomerase II
activities Daunorubicin inhibites inDNA and RNA synthesissensitive and resistant Ehrlich ascites tumor cells
Bioactivity Daunorubicin Hydrochloride is a inhibitortopoisomerase IIwith potent antineoplastic activities DaunorubicinHydrochloride inhibites in sensitive andDNA and RNA synthesisresistant Ehrlich ascites tumor cells
Banoxantrone dihydrochloride (AQ4N dihydrochloride) Cat No HY-13562A
Belotecan hydrochloride (CKD-602) Cat No HY-13566A
Berberine chloride (Natural Yellow 18 (chloride)) Cat No HY-18258
Berberine chloride hydrate (Natural Yellow 18 (chloride hydrate)) Cat No HY-17577
Betulinic acid (Lupatic acid Betulic acid) Cat No HY-10529
Bisantrene (CL216942) Cat No HY-100875
Campathecin (Camptothecin (S)-(+)-Camptothecin CPT) Cat No HY-16560
Daun02 Cat No HY-13061
Daunorubicin (RP 13057 Daunomycin Rubidomycin) Cat No HY-13062A
Daunorubicin Hydrochloride (RP 13057 (Hydrochloride)
Daunomycin (Hydrochloride) Rubidomycin (Hydrochloride)) Cat No HY-13062
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg 10 mg
Purity 9965Clinical Data LaunchedSize 10mM x 1mL in DMSO
100 mg 200 mg 500 mg
Purity 9888Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data LaunchedSize 5 mg 10 mg
Purity 9808Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9839Clinical Data Phase 3Size 1 mg 5 mg 10 mg
Purity 9820Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg
Purity 9947Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 100 mg 200 mg 500 mg 1 g
Purity gt98Clinical Data LaunchedSize 50 mg 100 mg 200 mg 500 mg
Bioactivity Doxorubicin is a cytotoxic anthracycline antibiotic for thetreatment of multiple cancers The possible mechanisms bywhich doxorubicin acts in the cancer cell are intercalationinto DNA and disruption of -mediated DNAtopoisomerase-IIrepair
Bioactivity Doxorubicin hydrochloride is a cytotoxic anthracyclineantibiotic for the treatment of multiple cancers The possiblemechanisms by which doxorubicin acts in the cancer cell areintercalation into DNA and disruption of
-mediated DNA repairtopoisomerase-II
Bioactivity Dxd is a potent inhibitor with an ofDNA topoisomerase I IC50031 μM used as a conjugated drug of HER2-targeting ADC(DS-8201a)
Bioactivity Edotecarin is a potent inhibitor of that cantopoisomerase Iinduces single-strand DNA cleavage with of 50 nMIC50
Bioactivity Ellipticine (NSC 71795) is a potent antineoplastic agentinhibits activitiesDNA topoisomerase II
Bioactivity Ellipticine (NSC 71795) hydrochloride is a potentantineoplastic agent inhibits DNA topoisomerase IIactivities
Bioactivity Epirubicin is a semisynthetic L-arabino derivative ofdoxorubicin and an antineoplastic agent by inhibiting
Topoisomerase
Bioactivity Epirubicin (hydrochloride) is a semisynthetic L-arabinoderivative of doxorubicin and an antineoplastic agent byinhibiting Topoisomerase
Bioactivity Etoposide (VP-16 VP-16-213) a chemotherapy medication usedfor the treatments of a number of types of cancer inhibits
by forming a complex with topoisomerase II andDNA synthesisDNA Etoposide arrests cell cycle in G2 and induces apoptoshellip
Bioactivity Exatecan is a water soluble inhibitor withtopoisomerase Ian of 22 μM (0975 μgmL) and can be used in cancerIC50research
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Doxorubicin (Hydroxydaunorubicin) Cat No HY-15142A
Doxorubicin hydrochloride (Hydroxydaunorubicin (hydrochloride)) Cat No HY-15142
Dxd (Exatecan derivative for ADC) Cat No HY-13631D
Edotecarin (J 107088 PF 804950) Cat No HY-13618
Ellipticine (NSC 71795) Cat No HY-15753
Ellipticine hydrochloride (NSC 71795 (hydrochloride)) Cat No HY-15753A
Epirubicin Cat No HY-13624
Epirubicin hydrochloride (4-Epidoxorubicin hydrochloride) Cat No HY-13624A
Etoposide (VP-16 VP-16-213) Cat No HY-13629
Exatecan (DX-8951) Cat No HY-13631
wwwMedChemExpresscom 159
Purity 9830Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9978Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 100 mg 200 mg 500 mg
Purity 9975Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 100 mg 200 mg 500 mg
Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 100 mg 200 mg 500 mg
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg
Purity 980Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9962Clinical Data LaunchedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg
Purity 9803Clinical Data Phase 1Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9953Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg
Purity 9912Clinical Data Phase 3Size 10mM x 1mL in DMSO
50 mg 100 mg 250 mg 500 mg
Bioactivity Exatecan Mesylate is a water soluble topoisomerase Iinhibitor with an of 22 μM (0975 μgmL) and can beIC50used in cancer research
Bioactivity Flumequine (R-802) is a quinolone antibiotic and acts as a inhibitor with an of 15 μM (392topoisomerase II IC50
μgmL)
Bioactivity Genz-644282 is a non-camptothecin inhibitortopoisomerase Iused for cancer research
Bioactivity Idarubicin hydrochloride is an anthracycline antileukemicdrug It inhibits the interfering with thetopoisomerase IIreplication of DNA and RNA transcription
Bioactivity Indotecan (LMP-400) is a potent topoisomerase 1(Top1)inhibitor with values of 300 1200 560 nM for P388IC50HCT116 MCF-7 cell lines respectively
Bioactivity Intoplicine is a and inhibitorDNA topoisomerase I II
Bioactivity Irinotecan is a water soluble inhibitortopoisomerase Ipreventing religation of the DNA strand by binding totopoisomerase I-DNA complex
Bioactivity Irinotecan hydrochloride is a water soluble topoisomerase Iinhibitor mainly used to treat colon cancer and rectal cancer
Bioactivity Irinotecan hydrochloride trihydrate is a water soluble inhibitor with antitumor activitytopoisomerase I
Bioactivity Karenitecin (Cositecan) is a inhibitor withtopoisomerase Ipotent anti-cancer activity
Exatecan Mesylate (DX8951f) Cat No HY-13631A
Flumequine (R-802) Cat No HY-B0526
Genz-644282 Cat No HY-16228
Idarubicin hydrochloride (4-Demethoxydaunorubicin hydrochloride) Cat No HY-17381
Indotecan (LMP-400 NSC-724998) Cat No HY-18351
Intoplicine Cat No HY-101647
Irinotecan ((+)-Irinotecan CPT-11) Cat No HY-16562
Irinotecan hydrochloride (CPT-11 hydrochloride Camptothecin 11 hydrochloride) Cat No HY-16562A
Irinotecan hydrochloride trihydrate Cat No HY-16568
Karenitecin (Cositecan BNP 1350) Cat No HY-14812
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg 100 mg
Purity 9690Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9902Clinical Data LaunchedSize 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 20 mg
Purity 9702Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 100 mg
Purity 980Clinical Data LaunchedSize 10mM x 1mL in DMSO
50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
1 mg 5 mg 10 mg 50 mg
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg 10 mg 50 mg
Bioactivity LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I inhibitor with antitumor activity (Top1) [1]
Bioactivity LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNAintercalator and inhibitor withTopoisomerase I (Top1)antitumor activity [1]
Bioactivity MC-DOXHZN is an albumin-binding prodrug of Doxorubicin withacid-sensitive properties [1]
Bioactivity MC-DOXHZN hydrochloride is an albumin-binding prodrug ofDoxorubicin with acid-sensitive properties [1]
Bioactivity Mitoxantrone is a inhibitor also inhibitstopoisomerase IIprotein kinase C ( ) activity with an of 85 μMPKC IC50
Bioactivity Mitoxantrone dihydrochloride is a topoisomerase IIinhibitor also inhibits protein kinase C ( ) activityPKCwith an of 85 μMIC50
Bioactivity Namitecan is a potent inhibitor withtopoisomerase Iantitumor property
Bioactivity Pirarubicin is an anthracycline antibiotics acts as a inhibitor and is a widely used fortopoisomerase II
treatment of various cancers in particular solid tumors
Bioactivity Pirarubicin Hydrochloride is an anthracycline antibioticsacts as a inhibitor and is a widely usedtopoisomerase IIfor treatment of various cancers in particular solid tumors
Bioactivity Pixantrone is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity
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LMP744 (MJ-III65 NSC706744) Cat No HY-U00248
LMP744 hydrochloride (MJ-III65 hydrochloride NSC706744 hydrochloride) Cat No HY-U00248A
MC-DOXHZN (Doxorubicin(6-maleimidocaproyl)hydrazone) Cat No HY-16261A
MC-DOXHZN hydrochloride (Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride) Cat No HY-16261B
Mitoxantrone (mitozantrone) Cat No HY-13502
Mitoxantrone dihydrochloride (mitozantrone dihydrochloride) Cat No HY-13502A
Namitecan (ST-1968) Cat No HY-14821
Pirarubicin (THP) Cat No HY-13725
Pirarubicin Hydrochloride (THP Hydrochloride) Cat No HY-13725A
Pixantrone (BBR 2778) Cat No HY-13727
wwwMedChemExpresscom 161
Purity 9920Clinical Data LaunchedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Purity gt98Clinical Data No Development ReportedSize 250 mg 100 mg 500 mg
Purity 9984Clinical Data LaunchedSize 10mM x 1mL in DMSO
25 mg 50 mg 100 mg 200 mg
Purity 9970Clinical Data No Development ReportedSize 10mM x 1mL in Water
5 mg 10 mg 50 mg 100 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
Purity 9960Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Purity 9946Clinical Data Phase 2Size 10mM x 1mL in DMSO
50 mg 100 mg 200 mg 500 mg
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Purity 950Clinical Data LaunchedSize 10mM x 1mL in Water
5 mg 10 mg 50 mg 100 mg
Bioactivity Pixantrone dimaleate is a inhibitor and DNAtopoisomerase IIintercalator with anti-tumor activity
Bioactivity Podocarpusflavone A is a DNA topoisomerase I inhibitor havemoderated anti-proliferative activity induce cell apoptosis inMCF-7 is developing anti-tumor drugs target DNAtopoisomerase I In vitro podocarpusflavone-A show significantinhibitions against DLD KB MCF-7 HEp-2 tumor cell lineshellip
Bioactivity SN-38 (NK012) is an active metabolite of the Topoisomerase Iinhibitor Irinotecan SN-38 (NK012) inhibits and DNA RNA
with s of 0077 and 13 μM respectivelysynthesis IC50
Bioactivity SW044248 is a non-canonical inhibitor andtopoisomerase Iselectively toxic for certain non-small cell lung cancer(NSCLC) cell lines
Bioactivity TAS-103 is a dual inhibitor of DNA usedtopoisomerase IIIfor cancer research
Bioactivity TAS-103 dihydrochloride is a dual inhibitor of DNA used for cancer researchtopoisomerase III
Bioactivity Teniposide is a podophyllotoxin derivative acts as a inhibitor and used as a chemotherapeutictopoisomerase II
agent
Bioactivity Top1 inhibitor 1 (compound 28) is a potent human inhibitor with an value of 29topoisomerase I (Top1) IC50
nM [1]
Bioactivity Topotecan (SKF 104864A NSC 609669) is a Topoisomerase Iinhibitor The values of Topotecan at 24 h are 273plusmn025IC50μM of U251 cells 295plusmn023 μM of U87 cells 546plusmn041 μM ofGSCs-U251 and 595plusmn024 μM of GSCs-U87
Bioactivity Topotecan Hydrochloride (SKF 104864A Hydrochloride NSC 609669Hydrochloride) is a inhibitor with potentTopoisomerase Iantineoplastic activities
Pixantrone dimaleate (BBR 2778 dimaleate) Cat No HY-13727A
Podocarpusflavone A Cat No HY-N2198
SN-38 (NK012) Cat No HY-13704
SW044248 Cat No HY-19637
TAS-103 (BMS-247615) Cat No HY-13758
TAS-103 dihydrochloride (BMS-247615 dihydrochloride) Cat No HY-13758A
Teniposide (VM26) Cat No HY-13761
Top1 inhibitor 1 Cat No HY-126142
Topotecan (SKF 104864A NSC 609669) Cat No HY-13768
Topotecan Hydrochloride (SKF 104864A (Hydrochloride) NSC 609669 (Hydrochloride)) Cat No HY-13768A
Purity 9998Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
10 mg 50 mg 100 mg
Purity 9970Clinical Data Phase 3Size 5 mg 10 mg 50 mg
Purity gt98Clinical Data Phase 3Size 5 mg 10 mg 50 mg
Bioactivity Voreloxin is a first-in-class inhibitortopoisomerase IIthat intercalates DNA and induces site-selective DNA DSB G2arrest and apoptosis
Bioactivity Voreloxin Hydrochloride is a first-in-class topoisomerase IIinhibitor that intercalates DNA and induces site-selective DNADSB G2 arrest and apoptosis
Bioactivity β-Lapachone is a naturally occurring O-naphthoquinone acts asa inhibitor and induces apoptosis bytopoisomerase Iinhibiting cell cycle progression
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Voreloxin (SNS-595 Vosaroxin AG 7352) Cat No HY-10534
Voreloxin Hydrochloride (SNS-595 Hydrochloride Vosaroxin
Hydrochloride AG 7352 Hydrochloride) Cat No HY-16518
β-Lapachone (ARQ-501 NSC-26326) Cat No HY-13555
wwwMedChemExpresscom 163
Wee1
Wee1 is a nuclear kinase belonging to the SerThr family of proteinkinases in the fission yeast ( )Schizosaccharomyces pombe S pombeWee1 has amolecular mass of 96 kDa and it is a key regulator of cellcycle progression Wee1 influences cell size by inhibiting the entryinto mitosis through inhibiting Cdk1 Wee1 has homologues in manyother organisms including mammals Wee1 inhibits Cdk1 byphosphorylating it on two different sites Tyr15 and Thr14 Cdk1 iscrucial for the cyclin-dependent passage of the various cell cyclecheckpoints At least three checkpoints exist for which the inhibitionof Cdk1 by Wee1 is important G M checkpoint Cell size checkpoint2DNA damage checkpoint Wee1 is shown to phosphorylate histone
H2B at tyrosine 37 residue which regulates global expression of histones
Purity 9946Clinical Data No Development ReportedSize 10mM x 1mL in DMSO
5 mg 10 mg 25 mg 50 mg 100 mg
Purity 9996Clinical Data Phase 2Size 10mM x 1mL in DMSO
5 mg 10 mg 50 mg 100 mg
Wee1 Inhibitors amp Modulators
Bioactivity Adavosertib (AZD-1775 MK-1775) is a potent inhibitorWee1with an of 52 nMIC50
Bioactivity PD0166285 is a inhibitor and a weak inhibitorWEE1 Myt1with s of 24 and 72 nM respectivelyIC50
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Adavosertib (AZD1775 MK-1775) Cat No HY-10993
PD0166285 Cat No HY-13925