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|438195-10MG||Glass bottle||10 mg||
|Overview||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 95.9 nM, respectively,against human wt LRRK2 and G2019S, A2016T, G2019S/A2016T LRRK2 mutant; [ATP] = 100 µM), displaying much reduced potency against MNK2 and MLK1 (IC50 = 0.6 and 2.1 µM, respectively; [ATP] = 100 µM) and little activity toward a panel of 136 other kinases. Although both HG-10-102-01 and LRRK2-In-1 (Cat. No. 438193) inhibit cellular wt and G20195 LRRK2 phosphorylation (Optimal conc. 1 to 3 µM), only HG-10-102-01 is effective against cellular A2016T and G2019S/A2016T LRRK2 phosphorylations (IC50 <3 µM). And only HG-10-102-01, but not LRRK2-In-1 or CZC-25146 (Cat. No. 438194), can cross blood-brain-barrier for LRRK2 phosphorylation inhibition in mice (30 mg/kg to 50 mg/kg i.p.) in vivo.|
|Synonyms||(4-(5-Chloro-4-(methylamino)pyrimidin-2-ylamino)-3-methoxyphenyl)(morpholino)methanone, Mixed-Lineage Kinase 1 Inhibitor I, MLK1 Inhibitor I, MNK Inhibitor III, Leucine-Rich Repeat Kinase 2 Inhibitor III|
|References||Choi, H.G., et al. 2012. ACS Med. Chem. Lett. 3, 658.|
|Structure formula Image|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Choi, H.G., et al. 2012. ACS Med. Chem. Lett. 3, 658.|
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