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534358 Wnt-β-Catenin Signaling Inhibitor, FzM1

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₁H₁₆N₂O₂S

Products

Catalog NumberPackaging Qty/Pack
5.34358.0001 Glass bottle 10 mg
Description
OverviewA 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.
Catalogue Number534358
Brand Family Calbiochem®
SynonymsFrizzled4 Modulator, FzM1
References
ReferencesGeneroso, S., et al. 2015. Nat. Chem. Bio. 11, 280.
Product Information
FormWhite solid
Hill FormulaC₂₁H₁₆N₂O₂S
Chemical formulaC₂₁H₁₆N₂O₂S
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetFrizzled 4
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
5.34358.0001 04054839318177

Documentation

Wnt-β-Catenin Signaling Inhibitor, FzM1 SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Generoso, S., et al. 2015. Nat. Chem. Bio. 11, 280.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision24-October-2017
SynonymsFrizzled4 Modulator, FzM1
DescriptionA 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.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₁H₁₆N₂O₂S
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesGeneroso, S., et al. 2015. Nat. Chem. Bio. 11, 280.