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Beschreibung

A cell-permeable dihydropyrazinyl-thioacetamide that acts as an ATP-competitive MARK inhibitor (IC50 = 3.6 microM, [ATP] = 100 microM) with much reduced or little activity against GSK-3&beta,, SAD-kinase B/BRSK-1, MARKK/TAO-1, Cdc2/cycB, and p38/SAPK (30%, 20%, 11%, 4%, and 0% inhibition, respectively, [inhibitor] = 50 microM). Shown to effectively block primary rat cortical neuron axon growth (5.7 microm/hr vs 32.5 microm/hr with or without 20 microM inhibitor) and prevent MARK2 overexpression-induced Tau Ser262 phosphorylation and cytotoxicity due to microtubule network breakdown in CHO cells (10 microM)., A cell-permeable dihydropyrazinyl-thioacetamide that acts as an ATP-competitive MARK-selective inhibitor (IC50 = 3.6 microM, [ATP] = 100 microM). Shown to effectively block primary rat cortical neuron axon growth (5.7 microm/hr vs 32.5 microm/hr with or without 20 microM inhibitor) and prevent MARK2 overexpression-induced Tau Ser262 phosphorylation and cytotoxicity in CHO cells (10 microM).