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Description

A cell-permeable triazole derivative that acts as a reversible TNKS inhibitor (IC50 = 15 nM) and selectively inhibits Wnt/beta-catenin, but not NF-kappaB, TGFbeta, or retinoic acid, signaling pathway-dependent transcription activity. Both WIKI4 and XAV939 (Cat. No. 575545) are shown to induce basal axin1/2 protein accumulation in DLD1 colon cancer cells (2.5 µ,M, 2 to 4 h) and prevent Wnt3a-induced axin1 protein degradation and beta-catenin accumulation in A375 melanoma cells (1 µ,M, up to 24 h) with similar potency. Likewise, WIKI4 also effectively inhibits the Wnt/beta-catenin pathway-dependent growth of DLD1 (by 67% in 10 days,1 µ,M).Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., 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/beta-catenin, but not NF-kappaB, TGFbeta, or retinoic acid, signaling pathway-dependent reporter activity. Although structurally distinct from XAV939 (Cat. No. 575545), both compounds are shown to induce basal axin1/2 protein accumulation in DLD1 colon cancer cells with mutant APC (2.5 µ,M, 2 to 4 h) and prevent Wnt3a-induced axin1 protein degradation and beta-catenin accumulation in A375 melanoma cells (1 µ,M, and up to 24 h) with similar potency. Likewise, WIKI4 also effectively inhibits the Wnt/beta-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 µ,M WIKI4).