GNE0877

• CAT Number: I001447
• CAS Number: 1374828-69-9
• Molecular Formula: C14H16F3N7
• Molecular Weight: 339.3
• Purity: ≥95%
• Synonyms: 2-methyl-2-(3-methyl-4-((4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)-1H-pyrazol-1-yl)propanenitrile
• Target: LRRK2
• Solubility: DMSO: ≥ 34 mg/mL
• Storage: Store at -20°C
• IC50: 3 nM
• IUPAC Name: 2-methyl-2-[3-methyl-4-[[4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-yl]amino]pyrazol-1-yl]propanenitrile
• InChI: InChI=1S/C14H16F3N7/c1-8-10(6-24(23-8)13(2,3)7-18)21-12-20-5-9(14(15,16)17)11(19-4)22-12/h5-6H,1-4H3,(H2,19,20,21,22)
• InChIKey: ZPPUMAMZIMPJGP-UHFFFAOYSA-N
• SMILES: CC1=NN(C=C1NC2=NC=C(C(=N2)NC)C(F)(F)F)C(C)(C)C#N

GNE0877（Cat No.:I001447） is a potent and selective small molecule inhibitor of leucine-rich repeat kinase 2 (LRRK2), a protein kinase implicated in the pathogenesis of Parkinson’s disease. With an IC50 of 3 nM, GNE0877 effectively inhibits the activity of LRRK2. It is also notable for its high brain penetration ability, allowing it to effectively target LRRK2 in the central nervous system. GNE0877 holds promise as a potential therapeutic agent for the treatment of Parkinson’s disease by modulating the activity of LRRK2.

Reference

[1]. Estrada AA, et al. Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem. 2014 Feb 13;57(3):921-36.