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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CEP-33779是JAK2新型选择性高效抑制剂,IC50值为1.8nM。
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AZ 960是一种新型的,ATP竞争性的JAK2抑制剂,IC50和Ki分别低于3 nM和0.45 nM,作用于JAK2比作用于JAK3选择性高3倍。
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AZD5438是一种有效的CDK1/2/9抑制剂,IC50为16 nM/6 nM/20 nM。对CDK5/6作用效果稍弱,也抑制GSK3β。
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GLPG0634 analogue is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
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LY2784544是一种有效的JAK2抑制剂,IC50为3 nM,作用于JAK2V617F有效,比作用于JAK1和JAK3选择性高8和20倍。
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