CAY10499 is a non-selective lipase inhibitor (IC50s = 144, 90, and 14 nM for human recombinant MAGL, HSL, and FAAH, respectively). It also inhibits ATGL, DAGLa, ABHD6, and CES1 by 95, 60, 90, and 95%, respectively, when used at a concentration of 5 mM. CAY10499 inhibits the growth of MCF-7, MDA-MB-231, COV318, and OVCAR-3 cancer cells (IC50s = 4.2, 46, 106.7, and 79.8 μM, respectively). In vivo, CAY10499 reduces FRUC diet- and AIN-93M diet-induced increases in cytosolic lipase activity in rats.
