CZC-54252

CZC-54252 is a potent and selective LRRK2 inhibitor with IC₅₀s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC₅₀ of ~1 nM. CZC-54252 has a neuroprotective activity^[1]. IC50 & Target: IC50: 1.28 nM (Wild-type LRRK2) and 1.85 nM (G2019S LRRK2)^[1] In Vitro: CZC-54252 inhibits the activity of recombinant human wild-type LRRK2 with an IC₅₀ ranging from ～1 to ～5 nM. The G2019S mutant is inhibited with an IC₅₀ ranging from ～2 to ～7 nM in a TF-FRET assay. In addition, they are screened against a kinase panel of 185 kinases and exhibited good selectivity^[1].
G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 with an EC₅₀ of ~1 nM and fully reversed to wild-type levels by CZC-54252 at concentration of 1.6 nM^[1].