Chk

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Chk Inhibitors (5)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1532 AZD7762 AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM in a cell-free assay. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1.
  • Nat Biotechnol, 2011, 29(6):542-6
  • Cancer Discov, 2012, 2(6):524-39
  • Cell rep, 2014, 10.1016/j.celrep.2014.10.024
S2626 LY2603618 LY2603618 is a selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. Phase 2.
  • J Pathol, 2015, 10.1002/path.4528
  • Cancer Lett, 2014, 356(2 Pt B):656-68
  • J Hematol Oncol, 2014, 7(1):53
S2735 MK-8776 (SCH 900776) MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2.
S2683 CHIR-124 CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM in a cell-free assay. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2.
  • Cancer Res, 2015, 75(17):3583-95
  • J Pathol, 2015, 10.1002/path.4528
  • Oncotarget, 2014, 5(3):667-78
S2904 PF-477736 PF-477736 is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM in a cell-free assay and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes. It shows ~100-fold selectivity for Chk1 than Chk2. Phase 1.
  • BMC Cancer, 2015, 15:196
  • BMC Cancer, 2014, 14(1):570

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1532 AZD7762 <1 mg/mL 50 mg/mL <1 mg/mL
S2626 LY2603618 <1 mg/mL 13 mg/mL <1 mg/mL
S2735 MK-8776 (SCH 900776) <1 mg/mL 3 mg/mL <1 mg/mL
S2683 CHIR-124 <1 mg/mL 7 mg/mL <1 mg/mL
S2904 PF-477736 <1 mg/mL 6 mg/mL <1 mg/mL
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