LP-935509 is a potent, selective and brain-penetrant adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50 of 3.3 nM.
LP-935509 inhibited μ2 protein phosphorylation in HEK293 cells overexpressing human AAK1 with IC50 of 2.8 nM.
LP-935509 also potent inhibits closely related BIKE and GAK with IC50 of 14 nM and 320 nM, respectively in a panel of 389 kinases.
LP-935509 reduces pain response in phase II formalin and reverses fully established pain behavior in vivo.
