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XIAP-CASP7 inhibitor 643943

Chemical Structure : XIAP-CASP7 inhibitor 643943

CAS No.: 305337-75-1

XIAP-CASP7 inhibitor 643943

Catalog No.: PC-24910Not For Human Use, Lab Use Only.

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.

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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 411.46
    Formula C25H21N3O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    4-(7,8-dimethoxy-1-methyl-3-phenyl-3H-pyrazolo[3,4-c]isoquinolin-5-yl)phenol

    References

    1. Shih-Hsun Chen, et al. Cell Death Dis. 2025 Jun 18;16(1):459.

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