MLi-2

MLi-2 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2, IC50 = 0.76 nM). It is greater than 100-fold selective for LRRK2 over a panel of 308 protein kinases, as well as a panel of receptors and ion channels, at 10 µM. It increases glucocerebrosidase (GCase) activity in dopaminergic neurons differentiated from induced pluripotent stem cells generated from skin fibroblasts isolated from patients with Parkinson's disease expressing LRRK2 mutations when used at a concentration of 600 nM. Dietary administration of MLi-2 (30 mg/kg per day) inhibits cortical LRRK2 phosphorylation in the MitoPark mouse model of Parkinson's disease.Formal Name: rel-3-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-pyrimidinyl]-5-[(1-methylcyclopropyl)oxy]-1H-indazole. CAS Number: 1627091-47-7. Molecular Formula: C21H25N5O2. Formula Weight: 379.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 15 mg/ml. lambdamax: 221, 253, 332 nm. SMILES: C[C@H](C1)O[C@@H](C)CN1C2=NC=NC(C3=NNC4=C3C=C(OC5(CC5)C)C=C4)=C2. InChi Code: InChI=1S/C21H25N5O2/c1-13-10-26(11-14(2)27-13)19-9-18(22-12-23-19)20-16-8-15(28-21(3)6-7-21)4-5-17(16)24-25-20/h4-5,8-9,12-14H,6-7,10-11H2,1-3H3,(H,24,25)/t13-,14+. InChi Key: ATUUNJCZCOMUKD-OKILXGFUSA-N.