GNE-9605 is a highly potent, selective, brain penetrant LRRK2 inhibitor with Ki of 2 nM, pLRRK2 IC50 of 19 nM.
GNE-9605 dispalys excellent selectivity against 178-membered Invitrogen kinase panel, as well as a representative panel of receptors and ion channels.
GNE-9605 demonstrates robust concentration-dependent inhibition of LRRK2 Ser1292 autophosphorylation (IC50=20 nM) in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation.
