2598242-66-9

NG-497 is a selective human adipose triglyceride lipase (ATGL) inhibitor that targets the enzymatically active patatin-like domain of human ATGL. NG-497 has potential value for tumor research[1].

NG-497 is a non-cytotoxicsubstrate-competitivereversible and highly selective human/primate adipose triglyceride lipase (ATGL; IPLA2-zeta; PNPLA2) inhibitor (IC50 = 1 μMKi = 0.5 μM) with little activity toward related human lipid hydrolases or ATGL orthologues from other species (<20% inhibition of mouseratgoatpigdogmarmoset ATGL at 50 μM). NG-497 abolishes hormone-induced lipolysis in human adipocytes (IC50 = 1.5 and 0.5 μM against 1 μM isoproterenol-induced total or hormonesensitive lipase (HSL)-independent FA release in Simpson-Golabi-Behmel syndrome adipocytes)but not in HepG2 th at lacks ATGL hydrolase activity.

[1] Gernot F Grabner, et al. Small-Molecule Inhibitors Targeting Lipolysis in Human Adipocytes. J Am Chem Soc. 2022 Apr 13;144(14):6237-6250. DOI:10.1021/jacs.1c10836