AR-A014418
N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea Yellow solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable thiazole-containing urea compound that acts as a potent inhibitor of GSK-3. Shown to inhibit GSK-3b 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 µM). Shown to prevent tau phosphorylation at a GSK-3-specific site. Also shown to protect neuronal cells against Ab-mediated neurodegeneration in vitro and reduce tauopathy in mice in vivo (30 µmol/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. Purity: ≥95% by HPLC. CAS 487021-52-3. Ref.: Noble, W., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 6990. Bhat, R., et al. 2003. J. Biol. Chem. 278, 45937. |
