85-2074-20　［取扱停止］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) 10mg　217519

特徴

• 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.
• Molecular Formula:C₁₇H₂₀ClN₅O₃
• 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 G2019S, A2016T, G2019S/A2016T LRRK2 mutant constructs
• Molar Mass:377.8
• Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.