341329

Fatostatin

A cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 precursors to the active nuclear forms by blocking SREBPs-SCAP ER to Golgi translocation.

• Sinônimo(s): Fatostatin, 125B11, 2-Propyl-4-(4-(p-tolyl)thiazol-2-yl)pyridine, HBr, SREBP Processing Inhibitor II
• Fórmula empírica (Notação de Hill): C₁₈H₁₈N₂S · xHBr
• Número CAS: 298197-04-3
• Peso molecular: 294.41 (free base basis)
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic); protect from light
• cor: pale yellow
• solubilidade: DMSO: 10 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• InChI: 1S/C18H18N2S.BrH/c1-3-4-16-11-15(9-10-19-16)18-20-17(12-21-18)14-7-5-13(2)6-8-14;/h5-12H,3-4H2,1-2H3;1H
• chave InChI: RJCFNQZVFUMORB-UHFFFAOYSA-N

Descrição

Descrição geral

A cell-permeable diarylthiazole compound that prevents the cellular activation of the SREBP-1/2 (Sterol Regulatory Element Binding Proteins 1/2) precursors to the active nuclear forms (>95% inhibition at 20 µM in CHO-K1 cells) by blocking SREBPs-SCAP (SREBP Cleavage-Activating Protein) ER to Golgi translocation with little effect against the transcription activity of the mature SREBPs. Binding studies employing recombinant SCAP truncation constructs reveal that Fatostatin targets SCAP between aa 448 to 767 in a reversible manner and is of no effect against SREBP-SCAP interaction. Fatostatin effectively suppresses SREBPs-dependent cellular functions in vitro, such as insulin-induced 3T3-L1 adipogenesis (complete inhibition at ≤20 µg/ml) and IGF1-dependent DU-145 proliferation (IC₅₀ = 100 nM), and exhibits in vivo efficacy in lowering blood glucose level (by 70%) and body weight (by 12%) of ob/ob mice over a 28-day treatment period (30 mg/kg daily i.p.) without affecting animal food intake or apparent adverse effects.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Outras notas

Kamisuki, S., et al. 2009. Chem. Biol.16, 882.
Choi, Y., et al. 2003. J. Biol. Chem.278, 7320.

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 1
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable