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.
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ZM39923盐酸盐是一种JAK1/3抑制剂, pIC50 of 4.4/7.1, 对JAK2几乎没有抑制活性。
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XL413盐酸盐是高活性Cdc7抑制剂,IC50为3.7 nM,比对CK2,PIM和其余100种蛋白激酶的抑制性高60倍,10倍和300倍以上。
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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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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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