Active Motif's Arecoline hydrobromide is an inhibitor of acetyl-CoA acetyltransferase 1 (ACAT1). Tyrosine 407 phosphorylation activates mitochondrial acetyl-CoA ACAT1 by stabilizing its tetramer. This is believed to be the mechanisms by which ACAT1 is "hijacked" and contributes to the Warburg effect in cancer. Arecoline is a covalent inhibitor of ACAT1 which binds to and disrupts only ACAT1 tetramers (IC50 = 11.1 uM). ACAT2 and DLAT are not inhibited. Treatment of xenograft nude mice with Arecoline resulted in a dose-dependent reduction in tumor mass. It is an agonist at muscarinic acetylcholine receptors M1-M5 (EC50 in the range of 7-410 nM), and may be involved in dementia.
