General description

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

A cell-permeable dihydropyrazinyl-thioacetamide that acts as an ATP-competitive MARK-selective inhibitor (IC₅₀ = 3.6 µM; [ATP] = 100 µM). Shown to effectively block primary rat cortical neuron axon growth (5.7 µm/hr vs 32.5 µm/hr with or without 20 µM inhibitor) and prevent MARK2 overexpression-induced Tau Ser262 phosphorylation and cytotoxicity in CHO cells (10 µM).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Timm, T., et al. 2011. J. Biol. Chem.286, 41711.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)