Cell-permeable, non-peptide inhibitor of X-linked inhibitor of apoptosis (XIAP) (IC50
= 4.1 μ
M in competition binding assay with Smac peptide); binds to the BIR3 domain, preventing XIAP interaction with caspase-9 and Smac. Inhibits cell growth, induces apoptosis and activates caspase-9 in prostate cancer cells (IC50
4 - 6 μ
M), but has a weaker effect on normal prostate cells (IC50
= 19 - 20 μ
M). Overcomes the protective effect of XIAP on apoptosis in XIAP-transfected Jurkat cells. Anti-tumor, analgesic and anti-inflammatory in vivo
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All Tocris products are intended for laboratory research use only.
Probing p300/CBP associated factor (PCAF)-dependent pathways with a small molecule inhibitor.
Modak et al.
ACS Chem.Biol., 2013;8:1311
Antitumor, anti-inflammatory and analgesic property of embelin, a plant product.
Chitra et al.
Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional herbal medicine three-dimensional structure database.
Nikolovska-Coleska et al.