317701

Dkk Inhibitor II, IIIC3a

• Sinônimo(s): Dkk Inhibitor II, IIIC3a, 9-Carboxy-3-(dimethyliminio)-6,7-dihydroxy-10-methyl-3H-phenoxazin-10-ium iodide
• Fórmula empírica (Notação de Hill): C₁₆H₁₆I₂N₂O₅
• Peso molecular: 570.12
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥90% (HPLC)
• Nível de qualidade: 100
• Formulário: powder
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic); protect from light
• cor: black
• solubilidade: DMSO: 10 mg/mL; hydrogen: 2.5 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

An enhanced in solution stable gallocyanine analog that directly and reversibly targets human LRP5/6 (low density lipoprotein-related protein 5/6), and disrupts its interaction with Dkk (Dickkopf) in a competitive manner. Shown to potently reverse DKK1/2/4-mediated inhibition of WNT3A-stimulated reporter gene activity (IC₅₀ ~ 10 - 30 µM in in NIH 3T3 cells) with no effects on sFRP4-mediated inhibition of Wnt signaling. Blocks Dkk-2 - alkaline phosphatase binding to cells expressing LRP5 (IC₅₀ = 1 µM in LRP5 transfected NIH 3T3 cells). Reduces blood glucose levels, improves glucose tolerance, and increases insulin sensitivity in type 2 diabetic mice (1.5 mg/kg, i.p. daily), mainly via its antagonistic action on DKK2. These effects are not observed in DKK2 ^-/- mice.

Ações bioquímicas/fisiológicas

Primary Target
LRP5/6

Reversible: yes

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.

Use only fresh DMSO for reconstitution.

Outras notas

Li, X., et al. 2012. Proc. Natl. Acad. Sci. USA109, 11402.

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