GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC50 = 10.1 nM). It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type and G2019S LRRK2 in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg. GSK2578215A induces protective autophagy in SH-SY5Y cells and blocks LRRK2-dependent Na+/Ca2+ exchanger activity in dendritic cells.