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Chk

Inhibitory Selectivity

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.

38 个项目

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  1. AZD7762
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    AZD7762

    Catalog No. A10113
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    Chk1 & Chk2 抑制剂
    AZD7762是一种有效的ATP竞争性检查点激酶抑制剂，可促进检查点废止并增强DNA靶向疗法。 了解更多
  2. CHIR-124
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    CHIR-124

    Catalog No. A11046
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    CHK 抑制剂
    CHIR-124是一种新型有效的Chk1抑制剂（Chk1和Chk2的IC50：分别为0.32 nM和697 nM）。 了解更多
  3. LY2606368
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    LY2606368

    Catalog No. A13684
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    Chk1 抑制剂
    LY2606368是具有潜在抗肿瘤活性的检查点激酶1（chk1）抑制剂。 了解更多
  4. PD0166285
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    PD0166285

    Catalog No. A15863
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    Wee1 抑制剂
    PD0166285是一种有效的Wee1和Chk1抑制剂，在纳摩尔浓度下具有活性。PD0166285是一种新型的G2检查点消除剂。 了解更多
  5. CCT241533
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    CCT241533

    Catalog No. A11108
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    Chk2 抑制剂
    CCT241533是CHK2的有效和选择性抑制剂，可增强PARP抑制剂的细胞毒性。 了解更多
  6. GNE-900
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    GNE-900

    Catalog No. A14178
    Chk1 抑制剂
    GNE-900是一种ATP竞争性、选择性和生物可利用的chk1抑制剂。 了解更多
  7. BML-277
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    BML-277

    Catalog No. A13575
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    Chk2 抑制剂
    BML-277（Chk2抑制剂II）是Chk2（检查点激酶2）抑制剂。 了解更多
  8. GDC-0575 (ARRY-575, RG7741)
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    GDC-0575 (ARRY-575, RG7741)

    Catalog No. A16811
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    Chk1 抑制剂
    GDC-0575 (ARRY-575,RG7741)是一种有效的选择性CHK1抑制剂，IC50为1.2 nM。 了解更多
  9. CCT245737
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    • 最新产品

    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%. 了解更多
  10. PF 477736
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    PF 477736

    Catalog No. A11520
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    Chk 抑制剂
    PF 477736是选择性检查点激酶1 (Chk1)抑制剂(Chk1和Chk2的ki值分别为0.49和47 nM)。 了解更多
  11. CHK1-IN-3
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    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. 了解更多
  12. SCH900776 (S-isomer)
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    SCH900776 (S-isomer)

    Catalog No. A12703
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    CHK1 抑制剂
    SCH900776 (S-isomer)是靶向细胞周期检查点激酶1（Chk1）抑制剂，无细胞试验中IC50为3 nM，比作用于Chk2选择性高500倍。具有潜在的放射增敏和化学增敏活性。 了解更多
  13. CCT244747
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    CCT244747

    Catalog No. A15550
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    CHK1 抑制剂
    CCT244747是一种新型的有效，高选择性活性，ATP竞争性CHK1抑制剂，具有潜在的抗癌活性， 了解更多
  14. SB 218078
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    SB 218078

    Catalog No. A15480
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    Chk1 抑制剂
    SB 218078是检查点激酶1（Chk1）的抑制剂，对其他蛋白激酶具有选择性（Chk1，cdc2和PKC的IC50值分别为15、250和1000 nM）。 了解更多
  15. AAPK-25
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    AAPK-25

    Catalog No. A19085
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    Aurora/PLK dual 抑制剂
    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. 了解更多
  16. Poloxime
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    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. 了解更多
  17. CHK1-IN-2
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    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. 了解更多
  18. Poloxin
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    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. 了解更多
  19. Centrinone-B
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    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. 了解更多
  20. Centrinone
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    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. 了解更多
  21. GDC-0575 dihydrochloride
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    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. 了解更多
  22. SBE13
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    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). 了解更多
  23. TAK-960 hydrochloride
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    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. 了解更多
  24. CCT241533 hydrochloride
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    CCT241533 hydrochloride

    Catalog No. A15038
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    Chk2 抑制剂
    CCT241533 hydrochloride是一种有效的丝氨酸/苏氨酸检查点激酶（Chk2）抑制剂，IC50为3 nM；显示在1 uM下与一组激酶的交叉反应最小。 了解更多
  25. SBE 13 HCl
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    SBE 13 HCl

    Catalog No. A14426
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    PLK 抑制剂
    SBE 13 HCl是PLK1的选择性抑制剂，对于PLK1，PLK3和PLK2，IC 50值分别为200pM，875nM和66μM。 了解更多
  26. NMS-1286937
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    NMS-1286937

    Catalog No. A13045
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    PLK 抑制剂
    NMS-1286937是一种小分子Polo样激酶1（PLK1）抑制剂，具有潜在的抗肿瘤活性。 了解更多
  27. RO3280
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    RO3280

    Catalog No. A13245
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    PLK1 抑制剂
    RO3280是一种有效的，高选择性的Polo样激酶1（PLK1）抑制剂，IC50为3 nM。 了解更多
  28. R1530
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    R1530

    Catalog No. A13111
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    Chk2, KDR, FGFR, Aurora A & Cdk2 抑制剂
    R1530是吡唑并苯并二氮杂小分子，具有潜在的抗血管生成和抗肿瘤活性。R1530也是一种有丝分裂-血管生成抑制剂(MAI),可抑制多种参与血管生成的受体酪氨酸激酶，如血管内皮生长因子受体(VEGFR)-1，-2，-3，血小板衍生生长因子受体(PDGFR)βFMS样酪氨酸激酶(Flt)-3和成纤维细胞生长因子受体(FGFR) -1，-2。 了解更多
  29. MLN 0905
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    MLN 0905

    Catalog No. A12429
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    PLK1 抑制剂
    MLN0905是有效的选择性小分子PLK1抑制剂。MLN0905抑制包括DLBCL细胞系在内的多种人类肿瘤细胞的细胞增殖。 了解更多
  30. GW843682X
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    GW843682X

    Catalog No. A11438
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    PLK1/PLK3 抑制剂
    GW843682X是polo-like激酶1（PLK1）和polo-like激酶3（PLK3）的选择性抑制剂（IC50值分别为2.2和9.1 nM）。 了解更多
  31. ON-01910 (rigosertib)
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    ON-01910 (rigosertib)

    Catalog No. A10673
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    PLK 抑制剂
    ON-01910 (rigosertib)通过涉及PI3K/AKT抑制和氧化应激诱导的双重作用机制对慢性淋巴细胞白血病细胞具有选择性的细胞毒性。 了解更多
  32. SCH 900776 (MK-8776)
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    SCH 900776 (MK-8776)

    Catalog No. A11167
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    Chk1 抑制剂
    SCH 900776 (MK-8776)是靶向细胞周期检查点激酶1（Chk1）的药物，无细胞试验中IC50为3 nM，比作用于Chk2选择性高500倍。具有潜在的放射增敏和化学增敏活性。 了解更多
  33. BI6727 (Volasertib)
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    BI6727 (Volasertib)

    Catalog No. A10135
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    PLK 抑制剂
    BI6727 (Volasertib)是一种高效且选择性的polo样激酶（PLK）1抑制剂（在一组癌细胞系中，酶IC50 = 0.87 nM，EC50 = 11-37 nM）。 了解更多
  34. TAK-960
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    TAK-960

    Catalog No. A11146
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    PLK1 抑制剂?
    TAK-960是新型的，口服可用的polo样激酶1选择性抑制剂，具有广谱的临床前抗肿瘤活性。 了解更多
  35. HMN-214
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    HMN-214

    Catalog No. A10452
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    PLK 抑制剂
    HMN-214抑制polo样和细胞周期蛋白依赖性激酶活性，具有强有力的抗微管作用，并在广泛的人类异种移植物中导致深度凋亡和抗肿瘤活性。 了解更多
  36. GSK461364
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    GSK461364

    Catalog No. A10442
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    PLK 抑制剂
    GSK461364 是polo样激酶1 (Plk1)的ATP竞争性抑制剂。 了解更多
  37. LY2603618 (IC-83)
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    LY2603618 (IC-83)

    Catalog No. A11036
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    Chk 抑制剂
    LY2603618 (IC-83)是一种chk2抑制剂，可与chk2结合并抑制其活性，这可能会阻止DNA损伤剂引起的DNA修复。 了解更多
  38. BI 2536
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    BI 2536

    Catalog No. A10134
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    PLK 抑制剂
    BI 2536是Plk1的选择性抑制剂，可在低纳摩尔浓度下抑制Plk1酶的活性。 了解更多

38 个项目

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