GSK2578215A

GSK2578215A is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC₅₀ = 8.9 nM) that also inhibits the G2019S mutant of LRRK2 (IC₅₀ = 10.1 nM).¹ It displays selectivity for LRRK2 over a panel of 460 other kinases. GSK2578215A prevents phosphorylation of both wild-type and G2019S LRRK2 in mouse spleen and kidney, but not in brain, following intraperitoneal injection of 100 mg/kg.¹ GSK2578215A induces protective autophagy in SH-SY5Y cells and blocks LRRK2-dependent Na⁺/Ca²⁺ exchanger activity in dendritic cells.^2,3

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1. Reith, A.D., Bamborough, P., Jandu, K., et al. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg. Med. Chem. Lett. 22(17), 5625-5629 (2012).

2. Saez-Atienzar, S., Bonet-Ponce, L., Blesa, J.R., et al. The LRRK2 inhibitor GSK2578215A induces protective autophagy in SH-SY5Y cells: Involvement of Drp-1-mediated mitochondrial fission and mitochondrial-derived ROS signaling. Cell Death Dis. 14(5), e1368 (2014).

3. Yan, J., Almilaji, A., Schmid, E., et al. Leucine-rich repeat kinase 2-sensitive Na⁺/Ca²⁺ exchanger activity in dendritic cells. FASEB J. 29(5), 1701-1710 (2015).