Benzenepentanamide, α-oxo-N-[2-[4-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]ethyl]-

Biological Activity

LEI-110 is an inhibitor of adipose phospholipase A2 (AdPLA2; IC50 = 100 nM).1 It also inhibits HRas-like suppressor 2 (HRASL2), retinoid acid receptor responder protein 3 (RARRES3), and calcium-independent N-acyltransferase (iNAT; IC50s = 158, 158, and 25 nM, respectively). LEI-110 (10 μM) decreases arachidonic acid levels in U2OS cells expressing human AdPLA2 and prevents oleic acid-induced increases in lipid droplet formation in HepG2 cells.

References

1.Zhou, J., Mock, E.D., Martella, A., et al.Activity-based protein profiling identifies α-ketoamides as inhibitors for phospholipase A2 group XVIACS Chem. Biol.14(2)164-169(2019)