Biological Activity
NG-497 is a non-cytotoxic, substrate-competitive, reversible and highly selective human/primate adipose triglyceride lipase (ATGL; IPLA2-zeta; PNPLA2) inhibitor (IC50 = 1 μM, Ki = 0.5 μM) with little activity toward related human lipid hydrolases or ATGL orthologues from other species (<20% inhibition of mouse, rat, goat, pig, dog, marmoset 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.