CAY10499

CAY10499 is a non-selective lipase inhibitor (IC₅₀s = 144, 90, and 14 nM for human recombinant MAGL, HSL, and FAAH, respectively).^1,2 It also inhibits ATGL, DAGLa, ABHD6, and CES1 by 95, 60, 90, and 95%, respectively, when used at a concentration of 5 mM.³ 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).² In vivo, CAY10499 reduces FRUC diet- and AIN-93M diet-induced increases in cytosolic lipase activity in rats.⁴

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1. Ali, Y.B., Müller, G., Petry, S., et al. Kinetic characterization and specific inhibition of hormone sensitive lipase. Chem. Phys. Lipids 136(2), 155 (2005).

2. Granchi, C., Rizzolio, F., Bordoni, V., et al. 4-Aryliden-2-methyloxazol-5(4H)-one as a new scaffold for selective reversible MAGL inhibitors. J. Enzyme Inhib. Med. Chem. 31(1), 137-146 (2016).

3. Iglesias, J., Lamontagne, J., Erb, J., et al. Simplified assays of lipolysis enzymes for drug discovery and specificity assessment of known inhibitors. J. Lipid Res. 57(1), 131-141 (2016).

4. Rodrigues, H.A., Moreira, C.C.L., Mario, É.G., et al. Differential modulation of cytosolic lipases activities in liver and adipose tissue by high-carbohydrate diets. Endocrine 53(2), 423-432 (2016).

Inazumi, T., Yamada, K., Shirata, N., et al. Prostaglandin E₂-EP₄ axis promotes lipolysis and fibrosis in adipose tissue leading to ectopic fat deposition and insulin resistance. Cell Rep. 33(2), 108265 (2020).

Tan, D., Ertunc, M.E., Konduri, S., et al. Discovery of FAHFA-containing triacyglycerols and their metabolic regulation. J. Am. Chem. Soc. 141(22), 8798-8806 (2019).

Kelkar, D., Ravikumar, G., Mehendale, N., et al. A chemical-genetic screen identifies ABHD12 as an oxidized-phosphatidylserine lipase. Nat. Chem. Biol. 15(2), 169-178 (2019).