361549
GSK-3β Inhibitor VIII
AR-A014418, N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea
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23 May 2013
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A cell-permeable thiazole-containing urea compound that acts as a potent inhibitor of GSK-3. Shown to inhibit GSK-3β 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 Aβ-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. A 25 mM (5 mg/649 µl) solution of GSK-3β Inhibitor VIII (Cat. No. 361557) in DMSO is also available.
| Product information | |||
|---|---|---|---|
| Form | Yellow solid | ||
| Primary Target | Gsk-3β | ||
| Primary Target IC50 | 104 nM | ||
| Secondary target | ATP (Ki = 38 nM) | ||
| Molar mass | 308.3 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Cell permeable | Yes | ||
| ATP Competitive | Yes | ||
| Purity | ≥95% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C12H12N4O4S | ||
| CAS number | 487021-52-3 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Carcinogenic / Teratogenic |
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