1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. 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) Isoform Specific Products:

  • Chk1

  • Chk2

Checkpoint Kinase (Chk) Related Products (19):

Cat. No. Product Name Effect Purity
  • HY-18174
    Prexasertib Inhibitor
    Prexasertib (LY2606368) is a potent, selective and ATP-competitive checkpoint kinase 1 (Chk1) inhibitor, with an IC50 and a Ki of <1 nM and 0.9 nM, respectively.
  • HY-10992
    AZD-7762 Inhibitor 99.90%
    AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
  • HY-14720
    Rabusertib Inhibitor 99.69%
    Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.
  • HY-18958
    CCT245737 Inhibitor 99.24%
    CCT245737 is a orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM.
  • HY-18174A
    Prexasertib dihydrochloride Inhibitor 99.41%
    Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with IC50s of <1 nM and 8 nM for CHK1 and CHK2, respectively, and a Ki of 0.9 nM against purified CHK1.
  • HY-128601
    CHK1-IN-3 Inhibitor
    CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM.
  • HY-14715B
    CCT241533 hydrochloride Inhibitor 99.98%
    CCT241533 hydrochloride is a potent and selective CHK2 inhibitor with an IC50 of 3 nM and a Ki of 1.16 nM.
  • HY-15532
    SCH900776 Inhibitor 99.65%
    SCH900776 is a potent, selective and oral inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. It shows 50- and 500-fold selectivity over CDK2 andChk2, respectively.
  • HY-13263
    CHIR-124 Inhibitor 98.77%
    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-13946
    BML-277 Inhibitor 98.02%
    BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
  • HY-10032
    PF 477736 Inhibitor 98.07%
    PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, 100-fold selectivity versus Chk2 (Ki, 47 nM).
  • HY-18175
    CCT244747 Inhibitor >99.0%
    CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
  • HY-112167
    GDC-0575 Inhibitor >98.0%
    GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.
  • HY-112167A
    GDC-0575 dihydrochloride Inhibitor 99.83%
    GDC-0575 dihydrochloride is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
  • HY-14715
    CCT241533 Inhibitor
    CCT241533 is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
  • HY-104022
    CHK1 inhibitor
    CHK1 inhibitor is an inhibitor of CHK1.
  • HY-18174B
    Prexasertib Mesylate Hydrate Inhibitor
    Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM.
  • HY-111369
    CHK1-IN-2 Inhibitor
    CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.
  • HY-U00345
    CHK-IN-1 Inhibitor
    CHK-IN-1 is an inhibitor of CHK1 and CHK2, with anti-proliferative activities.
Isoform Specific Products

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