Embelin (550-24-3) inhibits the lysine acetyl transferase PCAF in vitro and in vivo (in vitro IC50=7.2 mM). Inhibits H3K9 acetylation in mouse liver tissue while leaving levels of H3K14, H4K8, H4K12 unchanged1. Also inhibits X-linked inhibitor of apoptosis (XIAP) (IC50 = 4.1 μM, competing with Smac peptide). Binds to the BIR3 domain, preventing XIAP interaction with caspase-9 and Smac. Induces apoptosis and alters gene expression profiles in breast cancer cells3. Possesses anti-inflammatory and analgesic activity in vivo4. Cell-permeable.
1) Modak et al. (2013), Probing p300/CBP associated factor (PCAF)-dependent pathways with a small molecule inhibitor; ACS Chem. Biol., 8 1311
2) 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
3) Shah et al. (2016), Embelin inhibits proliferation, induces apoptosis and alters gene expression profiles in breast cancer cells; Pharmacol. Rep., 68 638
4) Chitra et al. (1994), Antitumor, anti-inflammatory and analgesic property of embelin, a plant product.; Chemotherapy, 40 109