JH-II-127 is a potent and selective inhibitor of both wild-type and G2019S mutant LRRK2 with IC50 of 6.6 and 2.2 nM, respectively.
JH-II-127 also inhibits LRRK2 A2016T with IC50 of 47.7 nM.
JH-II-127 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at 0.1-0.3 uM in a variety of cell types.
JH-II-127 inhibits Ser935 phosphorylation in mouse brain; orally active.
