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Home >> Signaling Pathways >> DNA Damage/DNA Repair >> Checkpoint Kinase (Chk)

Checkpoint Kinase (Chk)

<div class="colum_1 clearer"><p>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.</p></div>

Targets for  Checkpoint Kinase (Chk)

Products for  Checkpoint Kinase (Chk)

  1. Cat.No. Product Name Information
  2. GC39284 ANI-7 ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines. ANI-7 Chemical Structure
  3. GC50119 AZD 7762 hydrochloride Potent and selective ATP-competitive inhibitor of Chk1 and Chk2; also enhances CRISPR-Cpf1-mediated genome editing AZD 7762 hydrochloride Chemical Structure
  4. GC10546 AZD7762 Checkpoint kinase inhibitor,ATP competitive AZD7762 Chemical Structure
  5. GC11648 BML-277

    BML-277, C 3742, Checkpoint Kinase 2 Inhibitor II

     Chk2 inhibitor,potent and highly selective BML-277 Chemical Structure
  6. GC50085 CCT 241533 dihydrochloride Potent Chk2 inhibitor CCT 241533 dihydrochloride Chemical Structure
  7. GC18053 CCT241533 A selective Chk2 inhibitor CCT241533 Chemical Structure
  8. GC17105 CCT241533 hydrochloride A selective Chk2 inhibitor CCT241533 hydrochloride Chemical Structure
  9. GC14772 CCT244747 Potent and selective CHK1 inhibitor CCT244747 Chemical Structure
  10. GC19093 CCT245737 CCT245737 is a orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM. CCT245737 Chemical Structure
  11. GC15739 CHIR-124 Chk1 inhibitor,novel and potent CHIR-124 Chemical Structure
  12. GC33392 CHK-IN-1 CHK-IN-1 is an inhibitor of CHK1 and CHK2, with anti-proliferative activities. CHK-IN-1 Chemical Structure
  13. GC30106 CHK1 inhibitor

    GDC-0575 analog

     CHK1 inhibitor (GDC-0575 analog) is an inhibitor of CHK1. CHK1 inhibitor Chemical Structure
  14. GC33289 CHK1-IN-2 CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM. CHK1-IN-2 Chemical Structure
  15. GC35679 CHK1-IN-3 CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM. CHK1-IN-3 Chemical Structure
  16. GC72986 CHK1-IN-4 hydrochloride CHK1-IN-4 drochloride (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride Chemical Structure
  17. GC60698 Chk1-IN-5 Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model. Chk1-IN-5 Chemical Structure
  18. GC62986 GDC-0425 GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies. GDC-0425 Chemical Structure
  19. GC32885 GDC-0575 (ARRY-575, RG7741) GDC-0575 (ARRY-575, RG7741) (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2nM. GDC-0575 (ARRY-575, RG7741) Chemical Structure
  20. GC34127 GDC-0575 dihydrochloride (ARRY-575 dihydrochloride)

    ARRY-575 dihydrochloride; RG7741 dihydrochloride

     GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity. GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) Chemical Structure
  21. GC73822 GNE-900 GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 Chemical Structure
  22. GC15741 LY2603618

    IC-83, Rabusertib

     LY2603618 (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM. LY2603618 Chemical Structure
  23. GC15663 LY2606368

    Prexasertib

     LY2606368, an ATP-competitive CHK1 inhibitor, is currently in the clinical stage with a Ki of 0.9 nM and an IC50 of <1 nM. LY2606368 inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). LY2606368 Chemical Structure
  24. GC16374 MK-8776(SCH-900776)

    MK-8776

     MK-8776(SCH-900776) (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. MK-8776(SCH-900776) shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively. MK-8776(SCH-900776) Chemical Structure
  25. GC65435 Monalizumab

    Monalizumab is a first-in-class immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A).

     Monalizumab Chemical Structure
  26. GC38216 PD 407824 PD 407824 Chemical Structure
  27. GC18396 PD 407824

    PD 407824 is an inhibitor of the checkpoint kinases Chk1 and WEE1 (IC50s = 47 and 97 nM, respectively).

     PD 407824 Chemical Structure
  28. GC14234 PF-477736

    PF 00477736

     Chk1 inhibitor PF-477736 Chemical Structure
  29. GC36966 Prexasertib dihydrochloride Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity. Prexasertib dihydrochloride Chemical Structure
  30. GC36967 Prexasertib Mesylate Hydrate

    LY2606368 Mesylate Hydrate; LY2940930

     Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity. Prexasertib Mesylate Hydrate Chemical Structure
  31. GC72958 PV-1019

    NSC 744039

     PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 Chemical Structure
  32. GC11022 SB 218078 checkpoint kinase 1 (Chk1) inhibitor SB 218078 Chemical Structure
  33. GC72784 VRX0466617 VRX0466617, a selective Chk2 inhibitor, inhibits the phosphorylation of Chk2 Ser 19 and Ser33-35. VRX0466617 Chemical Structure
  34. GC49430 Wee1 Inhibitor Wee1 Inhibitor is a potent checkpoint Wee1 kinase inhibitor with an IC50 of 0.011 μM. Wee1 Inhibitor Chemical Structure

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