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Beschreibung

A cell-permeable oxazole compound that acts as a selective CRT (beta-catenin responsive transcription) inhibitor (IC50 = 8.2 nM against Wnt3a-dependent SuperTopFlash STF16-luc reporter activity in HEK293 cultures) by interfering with beta-cat-TCF4 interaction via direct beta-catenin (beta-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 µ,M), and selectively inhibits the proliferation of HCT116 (75 µ,M), HT29 (75 µ,M), and several primary human colon cancer cultures (6.25 to 100 µ,g/ml, average IC50 ~36 µ,g/ml) that require sustained Wnt/CRT activity for survival.