Description
CAY10499 is a non-selective lipase inhibitor (IC
50s = 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 (IC
50s = 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.
References
[1] muccioli g g, labar g, lambert d m. cay10499, a novel monoglyceride lipase inhibitor evidenced by an expeditious mgl assay[j]. chembiochem, 2008, 9(16): 2704-2710.
[2] ben ali y, muller g, petry s, et al. kinetic characterization and specific inhibition of hormone sensitive lipase[c]//chemistry and physics of lipids. elsevier house, brookvale plaza, east park shannon, co, clare, 00000, ireland: elsevier ireland ltd, 2005, 136(2): 155-155.
[3] kraemer f b, shen w j. hormone-sensitive lipase control of intracellular tri-(di-) acylglycerol and cholesteryl ester hydrolysis[j]. journal of lipid research, 2002, 43(10): 1585-1594.
