5.34358
Wnt-β-Catenin Signaling Inhibitor, FzM1
Synonym(s):
Wnt-β-Catenin Signaling Inhibitor, FzM1, Frizzled4 Modulator, FzM1
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About This Item
Empirical Formula (Hill Notation):
C21H16N2O2S
CAS Number:
Molecular Weight:
360.43
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
PubChem Substance ID:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
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
InChI
1S/C21H16N2O2S/c24-19-12-16(20-6-3-9-26-20)11-18(13-19)23-21(25)22-17-8-7-14-4-1-2-5-15(14)10-17/h1-13,24H,(H2,22,23,25)
InChI key
OBTSACXGWYGCPK-UHFFFAOYSA-N
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
Frizzled 4
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 3
Certificates of Analysis (COA)
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