Description
A non-peptidomimetic inhibitor of IAP protein-peptide interactions; inhibits the protein-peptide interaction between the IAP1 and XIAP BIR3 domains with a Smac-derived peptide in cell-free assays (IC50s = 50 = 2.8 nM); induces displacement of Smac from XIAP in A375 melanoma cells; induces apoptosis in MDA-MB-231, A375, and SK-MEL-28 cells in a TNF-α-dependent manner; reduces tumor growth in MDA-MB-231 and A375 mouse xenograft models at 20 mg/kg