Catalog No.: PC-43416Not For Human Use, Lab Use Only.
GSK2578215A is a highly potent, selective, BBB-permeable LRRK2 inhibitor with IC50 of 10.9 and 9.9 nM for wild-type LRRK2 and the G2019S mutant, respectively.
GSK2578215A is a highly potent, selective, BBB-permeable LRRK2 inhibitor with IC50 of 10.9 and 9.9 nM for wild-type LRRK2 and the G2019S mutant, respectively.
GSK2578215A shows 8-fold reduced potentcy against A2016T mutant LRRK2 (IC50=81 nM).
GSK2578215A inhibits Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2 G2019S stably transfected into HEK293 cells at 0.1-0.3 uM, also induces dephosphorylation of Ser910 and 935 at 1-3 μM in the inhibitor-resistant LRRK2[A2016T+ G2019S] and LRRK2 [A2016T] mutants.
GSK2578215A induces protective autophagy in SH-SY5Y cells.
