5.05767

GSK-3beta Inhibitor XXVII, CESI

• Sinônimo(s): GSK-3beta Inhibitor XXVII, CESI, 2-(3-chloro-4-hydroxyphenyl)-8-(1,1-dioxidoisothiazolidin-2-yl)-3-hydroxy-6-methyl-4H-chromen-4-one
• Fórmula empírica (Notação de Hill): C₁₉H₁₆ClNO₆S
• Número CAS: 372102-47-1
• Peso molecular: 421.85
• Código UNSPSC: 51111800
• ID de substância PubChem: 9910100
• NACRES: NA.77

Propriedades

• Ensaio: ≥96% (HPLC)
• Nível de qualidade: 100
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: CC1=CC2=C(C(=C1)N3CCCS3(=O)=O)OC(=C(C2=O)O)C4=CC(=C(C=C4)O)Cl

Descrição

Descrição geral

A cell-permeable, 3-hydroxychromone derived compound that acts as a selective and reversible inhibitor of GSK-3β (IC₅₀<100 nM). Shown to increase phosphorylation at Ser9. Does not show any inhibitory effect on a panel of 15 other protein kinases, including AMPK and Akt. By blocking GSK-3β activity, it acts as a positive regulator of b-catenin signaling. Does not affect the viability or the growth rate of 3T3-L1 preadipocytes, however, it significantly reduces their differentiation into adipocytes (˜ 50 to 100 nM). Exerts anti-adipogenic activity by down-regulating C/EBPa and PPARg. Shown to reduce adipocyte size and diminish weight gain in diet-induced obese mice without affecting their daily food intake.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
GSK3b

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

S. Lee et al. 2013, Biochemical Pharmacology85, 965.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable