Chk
Chk (Checkpoint kinases) are protein kinases that are involved in cell cycle control. Two checkpoint kinase subtypes have been identified, Chk1 and Chk2. Chk1 is an Serine/threonine-specific protein kinase that in humans, is encoded by the CHEK1 gene. Chk1 coordinates the DNA damage response (DDR) and cell cycle checkpoint response. Activation of Chk1 results in the initiation of cell cycle checkpoints, cell cycle arrest, DNA repair and cell death to prevent damaged cells from progressing through the cell cycle. Chk1 impacts various stages of the cell cycle including the S phase, G2/M transition and M phase.CHEK2 is the official symbol for the human gene Checkpoint kinase 2. CHEK2 is located on the long (q) arm of chromosome 22. CHEK2 is tumor suppressor gene that encodes the protein CHK2, a serine threonine kinase. CHK2 operates in an intricate network of proteins to elicit DNA repair, cell cycle arrest or apoptosis in response to DNA damage. Mutations to the CHEK2 gene have been linked to a wide range of cancers including breast cancer.
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MK-8776 (SCH 900776)是一种选择性Chk1抑制剂，IC50为3 nM，比作用于Chk2选择性高50倍,是高效口服生物相容性的Chk1抑制剂,对Chk2和CDK2的IC50则分别为1500 nM和160 nM。
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AZD7762是Chk1的抑制剂，IC50为5 nM，对Chk2的抑制性与Chk1相近，但对CAM，Yes，Fyn，Lyn，Hck和Lck的抑制性较弱。
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CHIR-124是高活性的Chk1抑制剂，IC50为0.3 nM，比对Chk2，CDK2/4和Cdc2的抑制性高2000倍，500倍和5000倍。
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PF-477736是一种有效的，选择性，ATP竞争性Chk1抑制剂，Ki为0.49 nM，也抑制VEGFR2， Aurora-A， FGFR3， Flt3， Fms (CSF1R)， Ret和Yes。作用于Chk1比作用于Chk2选择性高100倍左右。
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LY2603618是Chk1蛋白激酶选择性抑制剂，IC50为7 nM，是第一个进入临床实验的Chk1选择性抑制剂。
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