Cat. No. 2156
Chemical Name: 2,5-Dihydroxy-3-undecyl-2,5-cyclohe
Biological ActivityCell-permeable, non-peptide inhibitor of X-linked inhibitor of apoptosis (XIAP) (IC50 = 4.1 μM 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 μM), but has a weaker effect on normal prostate cells (IC50 = 19 - 20 μM). 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.
Certificate of Analysis / Safety Data Sheet
Modak et al (2013) Probing p300/CBP associated factor (PCAF)-dependent pathways with a small molecule inhibitor. ACS Chem.Biol. 8 1311. PMID: 23570531.
Nikolovska-Coleska et al (2004) 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. J.Med.Chem. 47 2430. PMID: 15115387.
Chitra et al (1994) Antitumor, anti-inflammatory and analgesic property of embelin, a plant product. Chemotherapy 40 109. PMID: 7510605.
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Keywords: Embelin, supplier, inhibitors, inhibits, X-linked, apoptosis, XIAP, cell-permeable, antitumor, c-IAP, Tocris Bioscience, Inhibitor of Apoptosis Inhibitor products