CZC-54252

Description	CZC-54252 inhibited the activity of recombinant human wild-type LRRK2 with an IC50 ranging from ～1 to ～5 nM. The G2019S mutant was inhibited with an IC50 ranging from ～2 to ～7 nM in a TF-FRET assay. In addition, they were screened against a kinase panel of 185 kinases and exhibited good selectivity. CZC-25146 (19) inhibited five other kinases, PLK4, GAK, TNK1, CAMKK2, and PIP4K2C, with high potency only, but none of them have been classified as predictors of genotoxicity or hematopoietic toxicity [1]. G2019S LRRK2-induced human neuronal injury was attenuated by CZC-25146 with an EC50 of ~4 nM (EC50 CZC-54252 ~1 nM) and fully reversed to wild-type levels by both compounds at concentrations as low as 8 nM (1.6 nM for CZC-54252) . in vivo: In vivo pharmacology established a volume of distribution of 5.4 L/kg and a clearance of 2.3 L/h/kg for CZC-25146.
Related Products	1784253-05-9（CZC 54252 hydrochloride）
Pathways	Others Pathway
Targets	LRRK2

Part data of this page collected from the open network resources, so Biochempartner can not guarantee its accuracy.

For product details of different batches, please contact our Customer

Products are for research use only and not for human use. We do not sell to patients.