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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BMS-265246是CDK1/2抑制剂，对CDK1/cyclin B和CDK2/cyclin E的IC50分别为6 nM和9 nM。
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AT7519是CDK抑制剂，对CDK1，2，4，6和9的IC50为10-210 nM，对CDK3的抑制性较低，而对CDK7则几乎无抑制性。
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Purvalanol A(NG-60)是CDKs高效细胞渗透性抑制剂，对cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1和Cdk5-p35的IC50值分别为4, 70, 35, 850和75 nM。
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Flavopiridol (Alvocidib)与ATP竞争性抑制CDKs，包括CDK1， CDK2， CDK4和CDK6，IC50约为40 nM。作用于CDK1， 2， 4， 6比作用于CDK7选择性强7.5倍。Flavopiridol最初被发现能抑制EGFR和PKA。
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R547是一种有效的，ATP竞争性CDK1/2/4抑制剂，Ki为2 nM/3 nM/1 nM，对CDK7和GSK3α/β作用效果稍弱，而抑制其他激酶活性。
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