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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Purity & Documentation Purity:
>98% (HPLC)
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
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M.Wt
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411.46
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Formula
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C25H21N3O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-(7,8-dimethoxy-1-methyl-3-phenyl-3H-pyrazolo[3,4-c]isoquinolin-5-yl)phenol
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References
1. Shih-Hsun Chen, et al. Cell Death Dis. 2025 Jun 18;16(1):459.
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