CZC-25146 (hydrochloride)

CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases[1][2][3].

Product Specifications

CAS Number

[1330003-04-7]

UNSPSC

12352005

Hazard Statement

H301-H319

Target

LRRK2; TNK1

Type

Reference compound

Related Pathways

Autophagy; Protein Tyrosine Kinase/RTK

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/czc-25146-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

CS(=O)(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCOCC4)C=C3OC)=NC=C2F)=O.Cl

Molecular Formula

C22H26ClFN6O4S

Molecular Weight

525.00

Precautions

P264-P270-P280-P305+P351+P338-P330-P405-P501

References & Citations

[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.|[2]Atashrazm F, et al. LRRK2 inhibitors and their potential in the treatment of Parkinson's disease: current perspectives. Clin Pharmacol. 2016 Oct 20;8:177-189.|[3]Deniz Kent, et al. Small molecule screen employing patient-derived iPS hepatocytes identifies LRRK2 as a novel therapeutic target for Alpha1 Antitrypsin Deficiency.