LRRK2-IN-1

LRRK2-IN-1 is a potent inhibitor of Leucine-rich repeat kinase 2 (LRRK2). Mutations in LRRK2 are associated with Parkinson's disease. LRRK2-IN-1 inhibits wild-type and G2019S mutant LRRK2 with IC₅₀ values of 13 nM and 6 nM, respectively. It suppresses LRRK2 kinase activity in vivo leading to dephosphorylation of Ser910/Ser935, loss of 14-3-3 binding and accumulation of LRRK2 within aggregate structures. It stimulates autophagy in H4 neuroglioma cells.