HG-10-012-01

• CAT Number: I001354
• CAS Number: 1351758-81-0
• Molecular Formula: C₁₇H₂₀ClN₅O₃
• Molecular Weight: 377.83
• Purity: ≥95%
• Synonyms: (E)-(4-((5-chloro-6-(methylimino)-1,6-dihydropyrimidin-2-yl)amino)-2-methoxyphenyl)(morpholino)methanone
• Target: LRRK2; MNK
• Solubility: DMSO: ≥ 50 mg/mL
• Storage: Store at -20°C
• IC50: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1]
• IUPAC Name: [4-[[5-chloro-4-(methylamino)pyrimidin-2-yl]amino]-3-methoxyphenyl]-morpholin-4-ylmethanone
• InChI: InChI=1S/C17H20ClN5O3/c1-19-15-12(18)10-20-17(22-15)21-13-4-3-11(9-14(13)25-2)16(24)23-5-7-26-8-6-23/h3-4,9-10H,5-8H2,1-2H3,(H2,19,20,21,22)
• InChIKey: YEVOZZZLKJKCCD-UHFFFAOYSA-N
• SMILES: CNC1=NC(=NC=C1Cl)NC2=C(C=C(C=C2)C(=O)N3CCOCC3)OC

HG-10-102-01（Cat No.:I001354） is a chemical compound that acts as a potent and selective inhibitor of both wild-type LRRK2 (leucine-rich repeat kinase 2) and the G2019S mutant, which is a common genetic mutation associated with Parkinson’s disease. It exhibits an IC50 of 23.3 nM for inhibiting wild-type LRRK2 and an IC50 of 3.2 nM for inhibiting the G2019S mutant. This compound shows promise as a potential therapeutic agent for targeting LRRK2-related diseases, particularly Parkinson’s disease.

Reference

[1]. Choi HG, et al. Brain Penetrant LRRK2 Inhibitor. ACS Med Chem Lett. 2012 Aug 9;3(8):658-662.
Abstract
Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson/’s disease (PD) patients and may represent an attractive therapeutic target. Here we report a 2-anilino-4-methylamino-5-chloropyrimidine, HG-10-102-01(4) is a potent and selective inhibitor of wild-type LRRK2 and the G2019S mutant. Compound 4 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 ?M in cells and is the first compound reported to be capable of inhibiting Ser910 and Ser935 phosphorylation in mouse brain following intraperitoneal delivery of doses as low as 50 mg/kg.