Merck, 322338-10MG, Dvl-PDZ Domain Inhibitor II

General description
A cell-permeable amidobenzanilide compound that disrupts Fz-Dvl (frizzled-dishevelled) interaction by targeting the PDZ domain (Kd = 10.6 µM) of Dvl, blocking Wnt3a-induced (10 ng/ml) transcription activity (~50% inhibition at 3 µM in 293 cell SuperTopflash reporter assays) and suppressing the Wnt pathway-dependent growth of prostate cancer PC-3 cells (by 16% in 72 h at ≥50 µM; IC₅₀ = 12.5 µM). Shown to effectively prevent Wnt3A mRNA injection-induced xenopus embryo deformation (effective conc. = 25 µM) and suppress Wnt pathway-mediated apoptosis of the hyaloid vescular endothelial cells in the mouse eyes via vitreous injection (144 fmol/120 nl/eye) in vivo.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Grandy, D., et al. 2009. J. Biol. Chem.284, 16256.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)