1784253-05-9

CZC-54252 HCl (1784253-05-9) 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 nM.1?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 patients.2?Cell permeable.

CZC-54252 hydrochloride is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 hydrochloride with an EC50 of ~1 nM.CZC-54252 hydrochloride has a neuroprotective activity[1].

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