5.34358

Wnt-β-Catenin Signaling Inhibitor, FzM1

• Synonim(y): Wnt-β-Catenin Signaling Inhibitor, FzM1, Frizzled4 Modulator, FzM1
• Wzór empiryczny (zapis Hilla): C₂₁H₁₆N₂O₂S
• Numer CAS: 1680196-54-6
• Masa cząsteczkowa: 360.43
• Kod UNSPSC: 12352200
• Identyfikator substancji w PubChem: 90478321

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: DMSO: 100 mg/mL
• temp. przechowywania: −20°C
• ciąg SMILES: C1=CC=C2C=C(C=CC2=C1)NC(=O)NC3=CC(=CC(=C3)C4=CC=CS4)O

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
Frizzled 4

Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3