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317701 Sigma-Aldrich

Dkk Inhibitor II, IIIC3a - Calbiochem

Synonym: 9-Carboxy-3-(dimethyliminio)-6,7-dihydroxy-10-methyl-3H-phenoxazin-10-ium iodide, Dkk Inhibitor II, IIIC3a - Calbiochem

  • Empirical Formula (Hill Notation) C16H16I2N2O5

  • Molecular Weight 570.12

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Properties

Quality Level   100
assay   ≥90% (HPLC)
form   powder
mfr. no.   Calbiochem®
storage condition   OK to freeze
  desiccated
  protect from light
storage conditions   +2C to +8C
color   black
solubility   DMSO: 10 mg/mL
  hydrogen: 2.5 mg/mL
shipped in   ambient

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 & Documentation

Safety Information

WGK Germany 
WGK 3
Flash Point(F) 
Not applicable
Flash Point(C) 
Not applicable
Protocols & Articles
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