XIAP-CASP7 inhibitor 643943 is a specific reversible XIAP-caspase 7 (CASP7) PPI inhibitor, binds to CASP7 Cys246 in an allosteric site, causes dissociation of XIAP to activate CASP7 and induces CASP7-mediated apoptosis.
XIAP-CASP7 inhibitor 643943 is a specific reversible XIAP-caspase 7 (CASP7) PPI inhibitor, binds to CASP7 Cys246 in an allosteric site, causes dissociation of XIAP to activate CASP7 and induces CASP7-mediated apoptosis.
643943 exhibits the great cytotoxic effect on MCF-7 cells with EC50 of 8.48 uM in MTT assays, but not normal breast MCF-10A cells.
643943 binds to CASP7 releases CASP7 from the inactive complex with XIAP.
643943 exhibits selective lethality in XIAP:CASP7 accumulated breast cancer cell lines with EC50 of 4.1, 5.2, and 6.7 μM against BT-483, MDA-MB-468 and ZR-75-1 to be 4.1, 5.2, and 6.7 μM.
643943 (20 mg/kg/day) exhibits anti-tumor activity in MCF-7- and MDA-MB-468-bearing mouse model.
