Chk

Catalog No.Inhibitor Name Chk1Chk2Other
A10113AZD7762
***
A11036LY2603618
***
A11167MK-8776
***
*
CDK2
A11046CHIR-124
****
*
FLT3,PDGFR,GSK-3
A11520PF-477736
****
**
VEGFR2,Fms,YES
A11108CCT241533
****
A13575BML-277
***
A15480SB 218078
***
cdc2, PKC
A15550CCT244747
**

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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  1. NMS-1286937

    Catalog No. A13045
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    PLK inhibitor
    NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Learn More
  2. TAK-960 hydrochloride

    Catalog No. A21703
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    PLK1 inhibitor
    TAK-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
  3. SBE13

    Catalog No. A21696
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    Plk1 inhibitor
    SBE13 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
  4. GDC-0575 dihydrochloride

    Catalog No. A21567
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    CHK1 inhibitor
    GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity. Learn More
  5. Centrinone

    Catalog No. A20858
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    PLK4 inhibitor
    Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM. Learn More
  6. Centrinone-B

    Catalog No. A20855
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    PLK4 inhibitor
    Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. Learn More
  7. Poloxin

    Catalog No. A11524
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    PLK1 inhibitor
    Poloxin 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
  8. CHK1-IN-2

    Catalog No. A13142
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    CHK1 inhibitor
    CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM. Learn More
  9. Poloxime

    Catalog No. A12145
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    PLK1 inhibitor
    Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity. Learn More
  10. AAPK-25

    Catalog No. A19085
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    Aurora/PLK dual inhibitor
    AAPK-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
  11. SB 218078

    Catalog No. A15480
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    Chk1 Inhibitor
    SB 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
  12. CCT244747

    Catalog No. A15550
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    CHK1 inhibitor
    CCT244747 is a novel potent, highly selective, orally active ATP-competitive CHK1 inhibitor with potential anticancer activity, Learn More
  13. CCT241533 hydrochloride

    Catalog No. A15038
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    Chk2 inhibitor
    CCT241533 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
  14. SBE 13 HCl

    Catalog No. A14426
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    PLK inhibitor
    SBE 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
  15. BI 2536

    Catalog No. A10134
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    PLK inhibitor
    BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations. Learn More
  16. RO3280

    Catalog No. A13245
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    PLK1 inhibitor
    RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM. Learn More
  17. LY2603618 (IC-83)

    Catalog No. A11036
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    Chk inhibitor
    LY2603618 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
  18. MLN 0905

    Catalog No. A12429
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    PLK1 inhibitor
    MLN0905 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
  19. GSK461364

    Catalog No. A10442
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    PLK Inhibitor
    GSK461364 is an ATP-competitive inhibitor of polo-like kinase 1 (Plk1). Learn More
  20. GW843682X

    Catalog No. A11438
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    PLK1/PLK3 inhibitor
    GW843682X 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
  21. HMN-214

    Catalog No. A10452
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    PLK Inhibitor
    HMN-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
  22. ON-01910 (rigosertib)

    Catalog No. A10673
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    PLK Inhibitor
    ON-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
  23. TAK-960

    Catalog No. A11146
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    PLK1 inhibitor‎
    TAK-960 is a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity. Learn More
  24. R1530

    Catalog No. A13111
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    Chk2, KDR, FGFR, Aurora A & Cdk2 inhibitor
    R1530 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
  25. BI6727 (Volasertib)

    Catalog No. A10135
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    PLK Inhibitor
    BI6727 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
  26. SCH 900776 (MK-8776)

    Catalog No. A11167
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    Chk1 inhibitor

    SCH900776 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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    CCT245737

    Catalog No. A17239
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    CHK1 inhibitor
    CCT245737 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
  27. AZD7762

    Catalog No. A10113
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    Chk1 & Chk2 inhibitor
    AZD7762 is a potent ATP-competitive checkpoint kinase inhibitor that drives checkpoint abrogation and potentiates DNA-targeted therapies. Learn More
  28. CHIR-124

    Catalog No. A11046
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    CHK Inhibitor
    CHIR-124 is a novel and potent Chk1 inhibitor (IC50: 0.32 nM and 697 nM for Chk1 and Chk2 respectively). Learn More
  29. CCT241533

    Catalog No. A11108
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    Chk2 inhibitor
    CCT241533 is a potent and selective Inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors. Learn More
  30. CHK1-IN-3

    Catalog No. A18443
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    CHK1 inhibitor
    CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM. Learn More
  31. GDC-0575 (ARRY-575, RG7741)

    Catalog No. A16811
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    Chk1 inhibitor
    GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2?nM. Learn More
  32. PD0166285

    Catalog No. A15863
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    Wee1/Chk inhibitor
    PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator. Learn More
  33. PF 477736

    Catalog No. A11520
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    Chk Inhibitor
    PF 477736 is a selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively). Learn More
  34. SCH900776 (S-isomer)

    Catalog No. A12703
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    CHK1 Inhibitor
    SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. Learn More
  35. LY2606368

    Catalog No. A13684
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    Chk1 inhibitor
    LY2606368 is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity. Learn More
  36. GNE-900

    Catalog No. A14178
    Chk1 inhibitor
    GNE-900 is an ATP-competitive, selective, and orally bioavailable ChK1 inhibitor. Learn More
  37. BML-277

    Catalog No. A13575
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    Chk2 Inhibitor
    BML-277 (Chk2 Inhibitor II) is a Chk2 (checkpoint kinase 2) inhibitor. Learn More

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