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.

Legal Information

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

Other Notes

Lee, E., et al. 2013. Proc. Natl. Acad. Sci. USA110, 15710.r>Gonsalves, F.C., et al. 2011. Proc. Natl. Acad. Sci. USA108, 5954.

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)