317701

Dkk Inhibitor II, IIIC3a

• Sinonimo/i: Dkk Inhibitor II, IIIC3a, 9-Carboxy-3-(dimethyliminio)-6,7-dihydroxy-10-methyl-3H-phenoxazin-10-ium iodide
• Formula empirica (notazione di Hill): C₁₆H₁₆I₂N₂O₅
• Peso molecolare: 570.12
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥90% (HPLC)
• Livello qualitativo: 100
• Stato: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Colore: black
• Solubilità: DMSO: 10 mg/mL; hydrogen: 2.5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Primary Target
LRP5/6

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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.

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable