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GNE0877

Catalog No.
B4633
Potent and selective LRRK2 inhibitor
Grouped product items
SizePriceStock Qty
2mg
$95.00
In stock
5mg
$196.00
In stock
10mg
$313.00
In stock
25mg
$620.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

GNE0877 (CAS 1374828-69-9) is a potent and selective small-molecule inhibitor of leucine-rich repeat kinase 2 (LRRK2), an enzyme associated with Parkinson's disease pathology. In vitro assays demonstrate GNE0877 effectively inhibits intracellular LRRK2 activity (IC50 approximately 3 nM), displays minimal metabolic turnover in human hepatic models, and lacks glucuronidation. Kinase selectivity profiling indicated minimal off-target effects across 188 kinases tested. In vivo, GNE0877 dose-dependently suppresses Ser1292 autophosphorylation of mutant G2019S LRRK2 in transgenic mice, underscoring its suitability for investigating LRRK2-related signaling in preclinical neuroscience research.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt339.32
Cas No.1374828-69-9
FormulaC14H16F3N7
Solubility≥21 mg/mL in DMSO; ≥20 mg/mL in EtOH; insoluble in H2O
Chemical Name2-methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)propanenitrile
SDFDownload SDF
Canonical SMILESFC(F)(C1=CN=C(N=C1NC)NC2=CN(C(C)(C#N)C)N=C2C)F
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description GNE-0877 is a highly potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with Ki value of 0.7 nM.
Targets LRRK2          
IC50 Ki=0.7 nM          

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