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A cell-permeable triazole derivative that acts as a reversible TNKS inhibitor (IC₅₀ = 15 nM in cell-free TNKS2 auto-ribosylation assays) and selectively inhibits Wnt/β-catenin, but not NF-κB, TGFβ, or retinoic acid, signaling pathway-dependent reporter activity. Although structurally distinct from XAV939, both compounds are shown to induce basal axin1/2 protein accumulation in DLD1 colon cancer cells with mutant APC (2.5 µM; 2 to 4 h) and prevent Wnt3a-induced axin1 protein degradation and β-catenin accumulation in A375 melanoma cells (1 µM; and up to 24 h) with similar potency. Likewise, WIKI4 also effectively inhibits the Wnt/β-catenin pathway-dependent growth of DLD1 (37% and 67% inhibition of colony formation in 10 days, respectively, in the presence of 0.1 and 1 µM WIKI4).,官网链接:https://www.sigmaaldrich.cn/product/mm/500556
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