Signaling Pathway

Checkpoint Kinase (Chk)

Checkpoint Kinase (Chk)

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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) Inhibitors & Modulators (13)

Product Name Catalog No. Brief Description
AZD-7762

HY-10992

AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM; equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.

BML-277

HY-13946

BML-277 (C 3742) is a selective Chk2 (checkpoint kinase 2) inhibitor with an IC50 of 15 nM.

CCT241533

HY-14715

CCT241533 is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM.

CCT241533 hydrochloride

HY-14715B

CCT241533 Hcl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM.

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 is a novel and potent chk1 inhibitor with an IC50 of 0.3 nM.

LY2603618

HY-14720

LY2603618(IC-83) is a potent and selective small molecule inhibitor of Chk1 protein kinase activity in vitro (IC50=7 nM) and the first selective Chk1 inhibitor to enter clinical cancer trials.

LY2606368

HY-18174

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

LY2606368 dihydrochloride

HY-18174A

LY2606368 2Hcl is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

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 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highly selective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinase CDK2 (IC50 = 160 nM).

SCH900776 S-isomer

HY-15532B

SCH900776 (S-isomer) is the S-isomer form of SCH900776(HY-15532), which is a potent, selective and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50 = 3 nM), highly selective against Chk2 (IC50 = 1500 nM) and cyclin-dependent kinase CDK2 (IC50 = 160 nM).