An LRRK2 inhibitor
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MLi-2

Item No. 19305

Technical Information
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
Purity
≥98%
A crystalline solid
DMSO: 15 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    MLi-2 is an inhibitor of leucine-rich repeat kinase 2 (LRRK2; IC50 = 0.76 nM).1 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.2 Dietary administration of MLi-2 (30 mg/kg per day) inhibits cortical LRRK2 phosphorylation in the MitoPark mouse model of Parkinson's disease.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fell, M.J., Mirescu, C., Basu, K., et alMLi-2, a potent, selective, and centrally active compound for exploring the therapeutic potential and safety of LRRK2 kinase inhibition. J. Pharmacol. Exp. Ther. 355(3), 397-409 (2015).

    2. Ysselstein, D., Nguyen, M., Young, T.J., et alLRRK2 kinase activity regulates lysosomal glucocerebrosidase in neurons derived from Parkinson’s disease patients. Nat. Commun. 10(1), 5570 (2019).