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. 
  • 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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  • Pacritinib EY0538

    Pacritinib (SB1518)对JAK2WT,JAK2V617F,FLT3,JAK1和JAK3的IC50分别为23nM,19nM,22nM,1280nM和520nM。

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  • SNS-032 EY0491

    SNS-032是CDK 9,2和7的抑制剂,IC50分别为4,38和62 nM。

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  • XL019 EY0457

    XL019是JAK2选择性抑制剂,IC50为2.2 nM,比对JAK1的抑制性高100倍,有很好的分子生物学和细胞活性。

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