Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1532 AZD7762 <1 mg/mL 50 mg/mL <1 mg/mL
S2626 Rabusertib (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
S8526 GDC-0575 (ARRY-575, RG7741) <1 mg/mL 75 mg/mL 5 mg/mL
S7740 SAR-020106 <1 mg/mL 20 mg/mL 2 mg/mL
S8253 CCT245737 <1 mg/mL 75 mg/mL 9 mg/mL
S8632 Chk2 Inhibitor II (BML-277) <1 mg/mL 72 mg/mL 21 mg/mL
S7178 Prexasertib HCl (LY2606368) <1 mg/mL 2 mg/mL <1 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations


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.


Rabusertib (LY2603618)

Rabusertib (LY2603618) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated.


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.



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.



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.


GDC-0575 (ARRY-575, RG7741)

GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.



SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM.



CCT245737 is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1.


Chk2 Inhibitor II (BML-277)

Chk2 Inhibitor II (BML-277) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases.


Prexasertib HCl (LY2606368)

Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay.

Tags: Checkpoint activation | Checkpoint kinase | Checkpoint function | Checkpoint activity | Chk1 phosphorylation | Checkpoint pathway | Chk1 pathway | Chk2 pathway | Chk2 phosphorylation | Chk1 inhibitor clinical trial | Chk1 inhibition | Chk1 activation | Chk2 activation | Chk1 assay | Chk inhibitors review