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| Product Name | LRRK2 Inhibitor III, HG-10-102-01 |
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| Description | Purity ~99% (HPLC). 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. Solubility: DMSO Primary Target: LRRK2 Primary Target IC50: 20.3, 3.2, 153.7 and 95.9nM, respectively, against Nictide phosphorylation by recombinant human wt LRRK2 and |
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| Size | 10mg |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | 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) |
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| Gene, Accession, CAS # | n/a |
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| Catalog # | 217519 |
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| Order / More Info | LRRK2 Inhibitor III, HG-10-102-01 from UNITED STATES BIOLOGICAL |
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| Product Specific References | n/a |
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