Description: MLi-2 is a structurally novel, highly potent, and selective LRRK2 kinase inhibitor with central nervous system activity. MLi-2 exhibits exceptional potency in a purified LRRK2 kinase assay in vitro (IC50 = 0.76 nM), a cellular assay monitoring dephosphorylation of LRRK2 pSer935 LRRK2 (IC50 = 1.4 nM),...

MLi-2 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2, IC50 = 0.76 nM). It is greater than 100-fold selective for LRRK2 over a panel of 308 protein kinases, as well as a panel of receptors and ion channels, at 10 µM. It increases glucocerebrosidase (GCase) activity in dopaminergic neurons differentiated from...