GSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

LRRK2-kinase inhibitor

white to beige powder

DMSO : 50 mg/mL (125.18 mM)

LRRK2 (G2019S),LRRK2 (WT)

GSK2578215A induces a dose-dependent inhibition of Ser910 and Ser935 phosphorylation in both wild-type LRRK2 and LRRK2 stably transfected into HEK293 cells, and induces similar dose-dependent Ser910 and Ser935 dephosphorylation of endogenous LRRK2 in mouse Swiss 3T3 cells. In SH-SY5Y cells, GSK2578215A impairs the autophagy flux by altering autophagosome–lysosome fusion, and induces mitophagy though induction of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling.

In vivo, GSK2578215A (100 mg/kg i.p.) inhibits Ser910 and Ser935 phosphorylation in mouse spleen and kidney, but not in brain.