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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

AZD-7762 是一种有效的ATP竞争性的细胞周期检测点激酶 (checkpoint kinase,Chk) 抑制剂,抑制Chk1,IC50 为 5 nM。

BML-277 HY-13946

BML-277 是一种选择性的检测点激酶 2 (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 hydrochloride 是一种有效的选择性 ATP 竞争性的 CHK2 抑制剂,IC50 为 3 nM,Ki 为 1.16 nM。

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 是一种有效的,选择性的 Chk1 抑制剂,IC50 值为 0.3 nM;同时可有效抑制 PDGFRFLT3IC50 值分别为 6.6 nM 和 5.8 nM。

LY2603618 HY-14720

LY2603618 是一种有效的选择性的 Chk1 抑制剂,IC50 为 7 nM。

LY2606368 HY-18174

LY2606368 是一种有效的,选择性的,ATP 竞争性的 Chk1 抑制剂,Ki 值为 0.9 nM。

LY2606368 dihydrochloride HY-18174A

LY2606368 dihydrochloride 是一种有效的,选择性的,ATP 竞争性的 Chk1 抑制剂,Ki 值为 0.9 nM。

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 是一种有效的,选择性的,可口服的 Chk1 抑制剂,IC50 值为 3 nM;对 CDK2 和 Chk2 的抑制作用稍弱,IC50值分别为 160 nM 和 1500 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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