Chk
Catalog No. | Inhibitor Name | Chk1 | Chk2 | Other |
---|---|---|---|---|
A10113 | AZD7762 | *** | ||
A11036 | LY2603618 | *** | ||
A11167 | MK-8776 | *** | * | CDK2 |
A11046 | CHIR-124 | **** | * | FLT3,PDGFR,GSK-3 |
A11520 | PF-477736 | **** | ** | VEGFR2,Fms,YES |
A11108 | CCT241533 | **** | ||
A13575 | BML-277 | *** | ||
A15480 | SB 218078 | *** | cdc2, PKC | |
A15550 | CCT244747 | ** |
Notes:
1.Hover mouse over " " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
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NMS-1286937
Catalog No. A13045 PLK inhibitorNMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Learn More -
TAK-960 hydrochloride
Catalog No. A21703 PLK1 inhibitorTAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. Learn More -
SBE13
Catalog No. A21696 Plk1 inhibitorSBE13 is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 poorly inhibits Plk2 (IC50>66?μM) or Plk3 (IC50=875?nM). Learn More -
GDC-0575 dihydrochloride
Catalog No. A21567 CHK1 inhibitorGDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity. Learn More -
Centrinone
Catalog No. A20858 PLK4 inhibitorCentrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM. Learn More -
Centrinone-B
Catalog No. A20855 PLK4 inhibitorCentrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. Learn More -
Poloxin
Catalog No. A11524 PLK1 inhibitorPoloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM. Learn More -
CHK1-IN-2
Catalog No. A13142 CHK1 inhibitorCHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM. Learn More -
Poloxime
Catalog No. A12145 PLK1 inhibitorPoloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity. Learn More -
AAPK-25
Catalog No. A19085 Aurora/PLK dual inhibitorAAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. Learn More -
SB 218078
Catalog No. A15480 Chk1 InhibitorSB 218078 is an inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively) Learn More -
CCT244747
Catalog No. A15550 CHK1 inhibitorCCT244747 is a novel potent, highly selective, orally active ATP-competitive CHK1 inhibitor with potential anticancer activity, Learn More -
CCT241533 hydrochloride
Catalog No. A15038 Chk2 inhibitorCCT241533 Hcl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM. Learn More -
SBE 13 HCl
Catalog No. A14426 PLK inhibitorSBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). Learn More -
BI 2536
Catalog No. A10134 PLK inhibitorBI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations. Learn More -
RO3280
Catalog No. A13245 PLK1 inhibitorRO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. Learn More -
LY2603618 (IC-83)
Catalog No. A11036 Chk inhibitorLY2603618 is a chk2 inhibitor that binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNA-damaging agents. Learn More -
MLN 0905
Catalog No. A12429 PLK1 inhibitorMLN0905 is a potent, selective small-molecule PLK1 inhibitor. MLN0905 inhibits cell proliferation in a broad range of human tumor cells including DLBCL cell lines. Learn More -
GSK461364
Catalog No. A10442 PLK InhibitorGSK461364 is an ATP-competitive inhibitor of polo-like kinase 1 (Plk1). Learn More -
GW843682X
Catalog No. A11438 PLK1/PLK3 inhibitorGW843682X is a selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively). Learn More -
HMN-214
Catalog No. A10452 PLK InhibitorHMN-214 inhibits polo-like and cyclin-dependent kinase activity, has potent antimicrotubular effects and results in profound apoptosis and antitumor activity in a broad spectrum of human xenografts. Learn More -
ON-01910 (rigosertib)
Catalog No. A10673 PLK InhibitorON-01910 is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. Learn More -
TAK-960
Catalog No. A11146 PLK1 inhibitorTAK-960 is a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity. Learn More -
R1530
Catalog No. A13111 Chk2, KDR, FGFR, Aurora A & Cdk2 inhibitorR1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2. Learn More -
BI6727 (Volasertib)
Catalog No. A10135 PLK InhibitorBI6727 is a highly potent and selective polo-like kinase (PLK) 1 inhibitor (enzyme IC50 = 0.87 nM, EC50 = 11-37 nM on a panel of cancer cell lines). Learn More -
SCH 900776 (MK-8776)
Catalog No. A11167 Chk1 inhibitorSCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. It specifically binds to and inhibits Chk1, which may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases to undergo DNA repair prior to entry into mitosis; tumor cells may thus be sensitized to the DNA-damaging effects of ionizing radiation and alkylating chemotherapeutic agents.
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New
CCT245737
Catalog No. A17239 CHK1 inhibitorCCT245737 is a potent, selective and orally active checkpoint kinase 1 (CHK1) inhibitor. CCT245737 showed CHK1 IC50 = 1.3 nM, CHK2 IC50 = 2440 nM, G2 check point abrogation IC50 = 30 nM. Mouse F (oral)=100%. Learn More -
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AZD7762
Catalog No. A10113 Chk1 & Chk2 inhibitorAZD7762 is a potent ATP-competitive checkpoint kinase inhibitor that drives checkpoint abrogation and potentiates DNA-targeted therapies. Learn More -
CHIR-124
Catalog No. A11046 CHK InhibitorCHIR-124 is a novel and potent Chk1 inhibitor (IC50: 0.32 nM and 697 nM for Chk1 and Chk2 respectively). Learn More -
CCT241533
Catalog No. A11108 Chk2 inhibitorCCT241533 is a potent and selective Inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors. Learn More -
CHK1-IN-3
Catalog No. A18443 CHK1 inhibitorCHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM. Learn More -
GDC-0575 (ARRY-575, RG7741)
Catalog No. A16811 Chk1 inhibitorGDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2?nM. Learn More -
PD0166285
Catalog No. A15863 Wee1/Chk inhibitorPD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator. Learn More -
PF 477736
Catalog No. A11520 Chk InhibitorPF 477736 is a selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively). Learn More -
SCH900776 (S-isomer)
Catalog No. A12703 CHK1 InhibitorSCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. Learn More -
LY2606368
Catalog No. A13684 Chk1 inhibitorLY2606368 is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity. Learn More -
GNE-900
Catalog No. A14178 Chk1 inhibitorGNE-900 is an ATP-competitive, selective, and orally bioavailable ChK1 inhibitor. Learn More -
BML-277
Catalog No. A13575 Chk2 InhibitorBML-277 (Chk2 Inhibitor II) is a Chk2 (checkpoint kinase 2) inhibitor. Learn More