Methanesulfonamide, N-[2-[[5-chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-, hydrochloride (1:1)

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.1CZC-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.2Cell 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] NIGEL RAMSDEN*. Chemoproteomics-Based Design of Potent LRRK2-Selective Lead Compounds That Attenuate Parkinson’s Disease-Related Toxicity in Human Neurons[J]. ACS Chemical Biology, 2011, 6 10: 1021-1028. DOI:10.1021/cb2002413
[2] THOMAS KRAMER. Small Molecule Kinase Inhibitors for LRRK2 and Their Application to Parkinson’s Disease Models[J]. ACS Chemical Neuroscience, 2012, 3 3: 151-160. DOI:10.1021/cn200117j