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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Ribociclib是一种可口服的，高度特异性CDK4/6抑制剂。
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LDC000067是新型高选择性CDK9抑制剂，IC50值为32.7nM，对CDK2,1,4,6,7的选择性分别为55,125,210,>227,>227倍。
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Roscovitine (Seliciclib,CYC202)是一种选择性的CDK抑制剂，作用于Cdc2， CDK2和CDK5时，IC50分别为0.65 μM， 0.7 μM和0.16 μM，对CDK4/6几乎没有抑制效果。
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Flavopiridol与ATP竞争抑制CDK1，CDK2，CDK4和CDK6，IC50为40 nM。Flavopiridol还具有EGFR和PKA抑制性。
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ML167 is the first highly selective inhibitor of of Cdc2-like kinase 4 (Clk4) with an IC50 of 136 nM for Clk4, >10-fold selectivity for closely related kinases Clk1-3 and Dyrk1A/1B, and minimal activity against a panel of other kinases tested.
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