GNE0877 (CAS 1374828-69-9) is a potent and selective small-molecule inhibitor of leucine-rich repeat kinase 2 (LRRK2), an enzyme associated with Parkinson's disease pathology. In vitro assays demonstrate GNE0877 effectively inhibits intracellular LRRK2 activity (IC50 approximately 3 nM), displays minimal metabolic turnover in human hepatic models, and lacks glucuronidation. Kinase selectivity profiling indicated minimal off-target effects across 188 kinases tested. In vivo, GNE0877 dose-dependently suppresses Ser1292 autophosphorylation of mutant G2019S LRRK2 in transgenic mice, underscoring its suitability for investigating LRRK2-related signaling in preclinical neuroscience research.
Chemical Properties
Physical Appearance
A crystalline solid
Storage
Store at -20°C
M.Wt
339.32
Cas No.
1374828-69-9
Formula
C14H16F3N7
Solubility
≥21 mg/mL in DMSO; ≥20 mg/mL in EtOH; insoluble in H2O