GNE-886 CAS No.: 2101957-05-3

Chemical Structure : GNE-886

CAS No.: 2101957-05-3

 

GNE-886

Catalog No.: URK-V2526 Only Used For Lab.

GNE-886 is a promising new inhibitor of LRRK2 kinase that has demonstrated potent activity in biochemical and cell-based assays, as well as in rodent models of PD. Its ability to cross the blood-brain barrier and inhibit LRRK2 kinase activity in vivo make it an attractive candidate for further development as a potential therapeutic agent for PD.

Biological Activity

GNE-886 is a potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2), a highly promising target for the treatment of Parkinson's disease (PD).
LRRK2 is a large, multi-domain protein kinase that has been implicated in the pathogenesis of both familial and sporadic PD. GNE-886 has been shown to potently inhibit LRRK2 kinase activity at low nanomolar concentrations in biochemical and cell-based assays, and to significantly reduce LRRK2-mediated neurotoxicity in primary neurons.
GNE-886 has also been found to inhibit other kinases, including RPS6KA1 and RPS6KA3, at higher concentrations. However, its selectivity for LRRK2 over these other kinases is still considerable, indicating a potential therapeutic window for the treatment of PD.
GNE-886 is able to effectively cross the blood-brain barrier in rodents, leading to its significant accumulation in the brain and subsequent inhibition of LRRK2 kinase activity in vivo.

Physicochemical Properties

References

1. Deng X, Dzamko N, Prescott A, et al. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol. 2011 Sep 18;7(4):203-5.

2. Li X, Wang Q, Pan N, et al. Design, synthesis and biological evaluation of novel pyridazines as potent LRRK2 inhibitors. Eur J Med Chem. 2018 Jun 25;154:187-201.

3. Fuji RN, Flagella M, Baca M, et al. Effect of selective LRRK2 kinase inhibition on nonhuman primate lung. Sci Transl Med. 2015 Aug 26;7(273):273ra15.

URK-V2526_COA

URk-V2526_SDS

URK-V2526_TDS

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