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
Molecular Weight: 570.12. Empirical Formula: C16H16I2N2O5. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 317701-25MG
