CDK


CDK (Cyclin-dependent kinases) is a group of serine/threonine kinases. It is activated by binding to cyclin and participates in the regulation of cell cycle.
Most of the known cyclin-CDK complexes regulate the progression through the cell cycle. Animal cells contain at least nine CDKs, four of which, CDK1, 2, 3, and 4, are directly involved in cell cycle regulation. In mammalian cells, CDK1, with its partners cyclin A2 and B1, alone can drive the cell cycle. Another one, CDK7, is involved indirectly as the CDK-activating kinase. A cyclin-dependent kinase inhibitor (CKI) is a protein that interacts with a cyclin-CDK complex to block kinase activity, usually during G1 or in response to signals from the environment or from damaged DNA. 
  • WHI-P154 EY0718

    WHI-P154是JAK3抑制剂,IC50为1.8 μM,还能抑制EGFR,Src,Abl,VEGFR和MAPK,对JAK1和JAK2无活性。

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  • SU9516 EY0704

    SU-9516是CDK2选择性抑制剂,IC50值为22nM,对CDK1/CDK4抑制力弱(IC50=40/200nM),对PKC、EGFR、p38MAPK等无抑制作用。

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  • NU6027 EY0613

    NU6027是一种有效的ATR/CDK抑制剂,抑制CDK1/2, ATR和DNA-PK时,Ki分别为2.5 μM/1.3 μM, 0.4 μM和 2.2 μM ,进入细胞时比6-氨基嘌呤类抑制剂更容易。

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  • P276-00 EY0596

    P276-00是一种新型的CDK1,CDK4和CDK9抑制剂,IC50分别为79 nM, 63 nM和20 nM。

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  • JNJ-7706621 EY0559

    JNJ-7706621是CDK抑制剂,对CDK1/2的抑制性最强,对应的IC50分别为9 nM/4 nM,比对CDK3/4/6的抑制性强超过6倍,对Aurora A/B有抑制性,而对Plk1和Wee1无活性。

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