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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Pacritinib (SB1518)对JAK2WT,JAK2V617F,FLT3,JAK1和JAK3的IC50分别为23nM,19nM,22nM,1280nM和520nM。
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SNS-032是CDK 9,2和7的抑制剂,IC50分别为4,38和62 nM。
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XL019是JAK2选择性抑制剂,IC50为2.2 nM,比对JAK1的抑制性高100倍,有很好的分子生物学和细胞活性。
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NVP-BSK805是ATP竞争性JAK2抑制剂,IC50为0.5 nM,比对JAK1,JAK3和TYK2的抑制性高超出20倍。
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