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

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

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Description

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

M.Wt	498.58
Formula	C₂₈H₃₀N₆O₃
CAS No.	2101957-05-3
Appearance	Solid
Storage	Solide Powder -20 °C 3years; 4°C 2years	In Solvent -80°C 6 Months -20°C 1 Months
Solubility
Chemical Name

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.