5.34358

Wnt-β-Catenin Signaling Inhibitor, FzM1

• Sinónimos: Wnt-β-Catenin Signaling Inhibitor, FzM1, Frizzled4 Modulator, FzM1
• Fórmula empírica (notación de Hill): C₂₁H₁₆N₂O₂S
• Número de CAS: 1680196-54-6
• Peso molecular: 360.43
• Código UNSPSC: 12352200
• ID de la sustancia en PubChem: 90478321
• NACRES: NA.77

Propiedades

• Análisis: ≥98% (HPLC)
• Nivel de calidad: 100
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: white
• solubilidad: DMSO: 100 mg/mL
• temp. de almacenamiento: −20°C
• cadena SMILES: C1=CC=C2C=C(C=CC2=C1)NC(=O)NC3=CC(=CC(=C3)C4=CC=CS4)O

Descripción

Descripción general

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.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
Frizzled 4

Reversible: yes

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

Generoso, S., et al. 2015. Nat. Chem. Bio.11, 280.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3