322338

Dvl-PDZ Domain Inhibitor II

The Dvl-PDZ Domain Inhibitor II, also referenced under CAS 294891-81-9, controls the biological activity of Dvl-PDZ. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(s): Dvl-PDZ Domain Inhibitor II, Wnt Pathway Inhibitor IV, 2-((3-(2-Phenylacetyl)amino)benzoyl)amino)benzoic acid, 3289-8625
• Empirical Formula (Hill Notation): C₂₂H₁₈N₂O₄
• CAS Number: 294891-81-9
• Molecular Weight: 374.39
• MDL number: MFCD01186172
• UNSPSC Code: 12352200
• NACRES: NA.28
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: N(c2cc(ccc2)C(=O)Nc3c(cccc3)C(=O)O)C(=O)Cc1ccccc1
• InChI: 1S/C22H18N2O4/c25-20(13-15-7-2-1-3-8-15)23-17-10-6-9-16(14-17)21(26)24-19-12-5-4-11-18(19)22(27)28/h1-12,14H,13H2,(H,23,25)(H,24,26)(H,27,28)
• InChI key: OBGIRQUECFHUEY-UHFFFAOYSA-N

Description

General description

A cell-permeable amidobenzanilide compound that disrupts Fz-Dvl (frizzled-dishevelled) interaction by targeting the PDZ domain (K_d = 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)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable