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Key Documents

361549

Sigma-Aldrich

GSK-3β Inhibitor VIII

The GSK-3β Inhibitor VIII, also referenced under CAS 487021-52-3, controls the biological activity of GSK-3β. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Sinônimo(s):

GSK-3β Inhibitor VIII, AR-A014418, N-(4-Methoxybenzyl)-Nʹ-(5-nitro-1,3-thiazol-2-yl)urea

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About This Item

Fórmula empírica (Notação de Hill):
C12H12N4O4S
Número CAS:
Peso molecular:
308.31
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

Ensaio

≥95% (HPLC)

forma

solid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

cor

yellow

solubilidade

DMSO: 5 mg/mL

Condições de expedição

ambient

temperatura de armazenamento

2-8°C

InChI

1S/C12H12N4O4S/c1-20-9-4-2-8(3-5-9)6-13-11(17)15-12-14-7-10(21-12)16(18)19/h2-5,7H,6H2,1H3,(H2,13,14,15,17)

chave InChI

YAEMHJKFIIIULI-UHFFFAOYSA-N

Descrição geral

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.
A cell-permeable, potent inhibitor of glycogen synthase kinase-3 (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.

Ações bioquímicas/fisiológicas

Cell permeable: yes
Primary Target
Gsk-3β
Product competes with ATP.
Reversible: no
Target IC50: 104 nM against GSK-3β

Embalagem

Packaged under inert gas

Advertência

Toxicity: Carcinogenic / Teratogenic (D)

Reconstituição

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Noble, W., et al. 2005. Proc. Natl. Acad. Sci. USA102, 6990.
Bhat, R., et al. 2003. J. Biol. Chem.278, 45937.

Informações legais

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

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3


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