Active Motif's Embelin inhibits the lysine acetyltransferase PCAF in vitro and in vivo (in vitro IC50 = 7.2 uM). It inhibits H3K9 acetylation in mouse liver tissue while leaving levels of H3K14, H4K8, and H4K12 unchanged. It also inhibits X-linked inhibitor of apoptosis (XIAP) (IC50 = 4.1 uM, competing with Smac peptide). Embelin to the BIR3 domain, preventing XIAP interaction with caspase-9 and Smac. It induces apoptosis and alters gene expression profiles in breast cancer cells. Embelin possesses anti-inflammatory and analgesic activity in vivo, and it is cell permeable.
