GNE0877
Catalog No.
B4633
Potent and selective LRRK2 inhibitor
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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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 339.32 |
Cas No. | 1374828-69-9 |
Formula | C14H16F3N7 |
Solubility | ≥21 mg/mL in DMSO; ≥20 mg/mL in EtOH; insoluble in H2O |
Chemical Name | 2-methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)propanenitrile |
SDF | Download SDF |
Canonical SMILES | FC(F)(C1=CN=C(N=C1NC)NC2=CN(C(C)(C#N)C)N=C2C)F |
Shipping Condition | Small 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. |
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 |
Quality Control & MSDS
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Chemical structure
