5.34358

Wnt-β-Catenin Signaling Inhibitor, FzM1

• Synonym(s): Wnt-β-Catenin Signaling Inhibitor, FzM1, Frizzled4 Modulator, FzM1
• Empirical Formula (Hill Notation): C₂₁H₁₆N₂O₂S
• CAS Number: 1680196-54-6
• Molecular Weight: 360.43
• UNSPSC Code: 12352200
• PubChem Substance ID: 90478321
• NACRES: NA.77

Properties

• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3