GNE-0877

Description: GNE-0877 (GNE 0877; GNE0877) is a novel, highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with important biological activity. It inhibits LRRK2 with a Ki of 0.7 nM. GNE-0877 showed significantly enhanced LRRK2 cellular potency (3 nM) and low turnover in human liver microsomes and hepatocytes with no evidence of glucuronidation. Invitrogen kinase-selectivity profiling (188 kinases) of GNE-0877 at 0.1 uM resulted in only four kinases showing greater than 50% inhibition and suggested that GNE-0877 is a highly selective LRRK2 inhibitor. Furthermore, GNE-0877 possessed a 212-fold biochemical-selectivity index over TTK (Ki = 150 nM).

References: J Med Chem. 2014 Feb 13; 57(3):921-36.