CZC-25146-d3

CZC-25146 Hcl is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.IC50 value: 4.76 nM/6.87 nM(wild type/G2019S LRRK2) [1]Target: LRRK2 CZC-25146displayed a very clean profile, it inhibited only five kinases(PLK4, GAK, TNK1, CAMKK2 and PIP4K2C) with high potency, none of which have been classified as predictors of genotoxicity or hematopoietic toxicity. CZC-25146 neither caused cytotoxicity in human cortical neurons at concentrations below 5μM over a seven-day treatment in culture nor did it block neuronal development in vitro. CZC-25146 possesses favorable pharmacokinetic properties, such as a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/hr/kg that render it suitable for in-vivo studies.

Signaling Pathways >> Autophagy >> LRRK2

Research Areas >> Neurological Disease

[1]. Ramsden N, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8.

LRRK2-IN-1 | IKK-16 | MLi-2 | PF-06447475 | GNE7915 | GSK2578215A | GNE-9605 | CZC-54252 | GNE-0877 | HG-10-102-01 | JH-II-127 | CZC 25146