317701

Dkk Inhibitor II, IIIC3a

• Synonym(s): Dkk Inhibitor II, IIIC3a, 9-Carboxy-3-(dimethyliminio)-6,7-dihydroxy-10-methyl-3H-phenoxazin-10-ium iodide
• Empirical Formula (Hill Notation): C₁₆H₁₆I₂N₂O₅
• Molecular Weight: 570.12
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥90% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: black
• solubility: DMSO: 10 mg/mL; hydrogen: 2.5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

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.

Biochem/physiol Actions

Primary Target
LRP5/6

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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.

Other Notes

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

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable