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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BS-181盐酸盐是CDK7高效选择性抑制剂，IC50值21nM，对CDK1/92/4/5/6/9作用弱。
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LY2835219对CDK4和CDK6的IC50分别为2 nM和10 nM。
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Dinaciclib (SCH727965)是一种新型有效的CDK抑制剂，作用于CDK2， CDK5， CDK1和CDK9，IC50分别为1 nM， 1 nM， 3 nM和4 nM，也抑制胸甘(dThd) DNA摄入。
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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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