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Description

A cell-permeable, potent inhibitor of glycogen synthase kinase-3 (GSK-3). Shown to inhibit GSK-3beta with high potency (IC50 = 104 nM). Inhibition is competitive with respect to ATP (Ki = 38 nM). Specificity has been reported using a panel of 28 different kinases, including Cdk2 and Cdk5 (IC50 >100 µ,M). Shown to prevent tau phosphorylation at a GSK-3-specific site. Also shown to protect neuronal cells against Abeta-mediated neurodegeneration in vitro and reduce tauopathy in mice in vivo (30 µ,mol/kg delivered with 40% PEG400 and 40% dimethylacetamide in water). Caution: Do not use delivering vehicles containing dimethylamine for in vivo studies, as it is highly toxic to animals., A cell-permeable thiazole-containing urea compound that acts as a potent inhibitor of GSK-3. Shown to inhibit GSK-3beta with high potency (IC50 = 104 nM). Inhibition is competitive with respect to ATP (Ki = 38 nM). Specificity has been reported using a panel of 28 different kinases, including Cdk2 and Cdk5 (IC50 >100 µ,M). Shown to prevent tau phosphorylation at a GSK-3-specific site. Also shown to protect neuronal cells against Abeta-mediated neurodegeneration in vitro and reduce tauopathy in mice in vivo (30 µ,mol/kg delivered with 40% PEG400 and 40% dimethylacetamide in water). Caution: Do not use delivering vehicles containing dimethylamine for in vivo studies, as it is highly toxic to animals. A 25 mM (5 mg/649 µ,l) solution of GSK-3beta Inhibitor VIII (Cat. No. 361557) in DMSO is also available.