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| Product | Description | |
|---|---|---|
| HG-10-102-01 | HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM) IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1] Target: LRRK2 HG-. Synonyms: HG-10-102-01; HG 10-102-01; HG10-102-01; HG-1010201; HG 1010201; HG1010201; LRRK2 inhibitor 1. Grades: >98%. CAS No. 1351758-81-0. Molecular formula: C17H20ClN5O3. Mole weight: 377.83. |  |
| LRRK2 Inhibitor III, HG-10-102-01 (Leucine-Rich Repeat Kinase 2 Inhibitor III, Mixed-Lineage Kinase 1 Inhibitor I, MLK1 Inhibitor I, MNK Inhibitor III, (4- (5-Chloro-4- (methylamino)pyrimidin-2-ylamino)-3-methoxyphenyl) (morpholino)methanone) | A cell-permeable 2,4-diaminopyrimidinyl compound that acts as a potent, ATP-competitive LRRK2-selective inhibitor (IC5050 = 20.3, 3.2, 153.7 and 95.9nM, respectively,against human wt LRRK2 and G2019S, A2016T, G2019S/A2016T LRRK2 mutant; [ATP] = 100uM), displaying much reduced potency against MNK2 and MLK1 (IC50 = 0.6 and 2.1uM, respectively; [ATP] = 100uM) and little activity toward a panel of 136 other kinases. Although both HG-10-102-01 and LRRK2-In-1 inhibit cellular wt and G20195 LRRK2 phosphorylation (Optimal conc. 1 to 3uM), only HG-10-102-01 is effective against cellular A2016T and G2019S/A2016T LRRK2 phosphorylations (IC50 <3uM). And only HG-10-102-01, but not LRRK2-In-1 or CZC-25146, can cross blood-brain-barrier for LRRK2 phosphorylation inhibition in mice (30mg/kg to 50mg/kg i.p.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??ClN?O?. US Biological Life Sciences. |  Worldwide |
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