361549

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.

• Synonim(y): GSK-3β Inhibitor VIII, AR-A014418, N-(4-Methoxybenzyl)-Nʹ-(5-nitro-1,3-thiazol-2-yl)urea
• Wzór empiryczny (zapis Hilla): C₁₂H₁₂N₄O₄S
• Numer CAS: 487021-52-3
• Masa cząsteczkowa: 308.31
• Numer MDL: MFCD08277040
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: yellow
• rozpuszczalność: DMSO: 5 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 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)
• Klucz InChI: YAEMHJKFIIIULI-UHFFFAOYSA-N

Opis

Opis ogólny

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 (K_i = 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 (K_i = 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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
Gsk-3β

Product competes with ATP.

Reversible: no

Target IC₅₀: 104 nM against GSK-3β

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Carcinogenic / Teratogenic (D)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3