219332

β-Catenin/Tcf Inhibitor III, iCRT3

The β-Catenin/Tcf Inhibitor III, iCRT3 controls the biological activity of β-Catenin/Tcf. This small molecule/inhibitor is primarily used for Biochemicals applications.

• Synonyme(s) : β-Catenin/Tcf Inhibitor III, iCRT3, 2-(((2-(4-Ethylphenyl)-5-methyl-1,3-oxazol-4-yl)methyl)sulfanyl)-N-(2-phenylethyl)acetamide, Inhibitor of β-Catenin Responsive Transcription, C3, Wnt Pathway Inhibitor VIII, C3, 2-(((2-(4-Ethylphenyl)-5-methyl-1,3-oxazol-4-yl)methyl)sulfanyl)-N-(2-phenylethyl)acetamide, Inhibitor of β-Catenin Responsive Transcription, Wnt Pathway Inhibitor VIII
• Formule empirique (notation de Hill) : C₂₃H₂₆N₂O₂S
• Poids moléculaire : 394.53
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥95% (HPLC)
• Form: powder
• Storage condition: OK to freeze, protect from light

Propriétés

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: tan
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: −20°C

Description

General description

A cell-permeable oxazole compound that acts as a selective CRT (β-catenin responsive transcription) inhibitor (IC₅₀ = 8.2 nM against Wnt3a-dependent SuperTopFlash STF16-luc reporter activity in HEK293 cultures) by interfering with β-cat-TCF4 interaction via direct β-catenin (β-cat) binding, while exhibiting much reduced activity against Hedgehog, Jak/Stat, or Notch signaling pathway-dependent transcription activation. Effectively inhibits cellular expression of CRT target genes, including WISP1, AXN2, and CYCD1, in a dose-dependent manner (25 to 75 µM), and selectively inhibits the proliferation of HCT116 (75 µM), HT29 (75 µM), and several primary human colon cancer cultures (6.25 to 100 µg/ml; average IC₅₀ ~36 µg/ml) that require sustained Wnt/CRT activity for survival.

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

Lee, E., et al. 2013. Proc. Natl. Acad. Sci. USA110, 15710.

Gonsalves, F.C., et al. 2011. Proc. Natl. Acad. Sci. USA108, 5954.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Informations sur la sécurité

• Classe de stockage: 11 - Combustible Solids
• Que se passe-t-il ?: WGK 3