CZC-54252 (1191911-27-9) is a novel, potent and selective inhibitor of the leucine-rich repeat kinase-2 (LRRK2), IC50 = 1.28 nM. Also inhibits G2019S mutant LRRK2, IC50 = 1.85 nM1. CZC-54252 attenuates the neuronal damage elicited by the action of LRRK2 G2019S mutant in primary human neurons (EC50 = 1 nM)1. The G2019S mutant is a common mutation found in familial Parkinson’s disease patients2. Cell permeable.
1) Ramsden et al. (2011), Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson’s disease-related toxicity in human neurons; ACS Chem. Biol., 6 102
2) Kramer et al. (2012), Small molecule kinase inhibitors for LRRK2 and their application to Parkinson’s disease models; ACS Chem. Neurosci., 3 151