General description
A cell-permeable, biarylurea derivative that acts as a reversible inhibitor of Wnt-b-catenin signaling (EC50 = 5.74 µM). Acts by blocking the phosphorylation and nuclear translocation of beta-catenin thereby reduces the transcription of TCF/LEF-regulatory genes. Also shown to block TCF/LEF activation induced by lithium chloride. However, it does not affect GSK3-β or the APC destruction complex. Induces con-formational changes in Fz4-WT that ultimately allow it to inhibit β-catenin nuclear transport. Shown to promote HA-Fz4-FEVR plasma membrane localization in U87MG glioblastoma cells and Caco-2 cells (~ 10 µM). Also reported to abolish Norrin-dependent TCF/LEF activation and gene transcription in HEK293 cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Frizzled 4
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 3 months at -20°C.
Other Notes
Generoso, S., et al. 2015. Nat. Chem. Bio.11, 280.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 360.43. Empirical Formula: C21H16N2O2S. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: white. solubility: DMSO: 100 . mg/mL. storage temp.: −. 20°C. SMILES string: C1: CC: C2C: C(C: CC2: C1)NC(: O)NC3: CC(: CC(: C3)C4: CC: CS4)O. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3.- UPC:
- 51172112
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5343580001
