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Checkpoint Kinase (Chk)

Chks (Checkpoint kinases) are protein kinases that are involved in cell cycle control. Two checkpoint kinase subtypes have been identified, Chk1 and Chk2. Chk1 is a central component of genome surveillance pathways and is a key regulator of the cell cycle and cell survival. Chk1 is required for the initiation of DNA damage checkpoints and has recently been shown to play a role in the normal (unperturbed) cell cycle. Chk1 impacts various stages of the cell cycle including the S phase, G2/M transition and M phase. In addition to mediating cell cycle checkpoints, Chk1 also contributes to DNA repair processes, gene transcription, embryo development, cellular responses to HIV infection and somatic cell viability. Chk2 is a protein kinase that is activated in response to DNA damage and is involved in cell cycle arrest. In response to DNA damage and replication blocks, cell cycle progression is halted through the control of cell cycle regulators. The protein encoded by this gene is a cell cycle checkpoint regulator and putative tumor suppressor.

Checkpoint Kinase(Chk) (13)
产品名称 目录号 简述
AZD-7762 HY-10992

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。

BML-277 HY-13946

BML-277 (C 3742)是高效Chk2抑制剂,IC50为15 nM。

CCT241533 HY-14715

CCT241533是高活性丝氨酸/苏氨酸Chk2抑制剂,IC50为3 nM,与其它激酶有极小的交叉反应(1 uM)。

CCT241533 hydrochloride HY-14715B

CCT241533盐酸盐是丝氨酸/苏氨酸Chk2抑制剂,IC50为3 nM,在1 uM浓度下对其它激酶的交叉反应极低。

CCT244747 HY-18175

CCT244747 is potent, highly selective, orally active, ATP competitive CHK1 inhibitor with IC50 of 29-170nM.

CCT245737 HY-18958

CCT245737 is a potent, ATP-competitive CHK1 inhibitor with an IC50 of 30-220 nM.

CHIR-124 HY-13263

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。

LY2603618 HY-14720

LY2603618(IC-83)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。

LY2606368 HY-18174

LY2606368是ATP竞争性Chk1蛋白激酶抑制剂,在SW1990细胞中IC50为1.5 nM。

LY2606368 dihydrochloride HY-18174A

LY2606368二盐酸盐是Chk1蛋白激酶选择竞争性抑制剂,在SW1990细胞中IC50值为1.5nM。

PF 477736 HY-10032

PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively.

SCH900776 HY-15532

SCH900776是高效口服生物相容性的Chk1抑制剂,IC50为3 nM,对Chk2和CDK2的IC50则分别为1500 nM和160 nM。

SCH900776 S-isomer HY-15532B

SCH900776 (S-isomer)是SCH900776(HY-15532)的S型同分异构体。

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