1. Cell Cycle/DNA Damage
  2. Checkpoint Kinase (Chk)

Checkpoint Kinase (Chk)

Checkpoint Kinases (Chk) 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) Related Products (13):

Cat. No. Product Name Effect Purity
  • HY-18174
    LY2606368 Inhibitor
    LY2606368 is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with a Ki of 0.9 nM against purified CHK1.
  • HY-14715B
    CCT241533 hydrochloride Inhibitor
    CCT241533 hydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
  • HY-10992
    AZD-7762 Inhibitor
    AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with IC50 of 5 nM for Chk1.
  • HY-15532
    SCH900776 Inhibitor
    SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC50 of 3 nM, and has much greater selectivity against Chk2 (IC50=1500 nM) and cyclin-dependent kinase CDK2 (IC50=160 nM).
  • HY-13263
    CHIR-124 Inhibitor
    CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
  • HY-14720
    LY2603618 Inhibitor
    LY2603618 is a potent and selective inhibitor of Chk1 protein kinase activity in vitro with IC50 of 7 nM.
  • HY-13946
    BML-277 Inhibitor
    BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
  • HY-18174A
    LY2606368 dihydrochloride Inhibitor
    LY2606368 dihydrochloride is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with a Ki of 0.9 nM against purified CHK1.
  • HY-18958
    CCT245737 Inhibitor
    CCT245737 is a potent, ATP-competitive CHK1 inhibitor with an IC50 of 30-220 nM.
  • HY-10032
    PF 477736 Inhibitor
    PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes; shows ~100-fold selectivity for Chk1 than Chk2.
  • HY-18175
    CCT244747 Inhibitor
    CCT244747 is potent, highly selective, orally active, ATP competitive CHK1 inhibitor with IC50 of 29-170nM.
  • HY-14715
    CCT241533 Inhibitor
    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.
  • HY-15532B
    SCH900776 S-isomer
    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).