Tankyrase1/2 Inhibitor V, WIKI4-Calbiochem

C₂₉H₂₃N₅O₃S

521.59

A cell-permeable triazole derivative that acts as a reversible TNKS inhibitor (IC₅₀ = 15 nM) and selectively inhibits Wnt/β-catenin, but not NF-κB, TGFβ, 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 µM; 2 to 4 h) and prevent Wnt3a-induced axin1 protein degradation and β-catenin accumulation in A375 melanoma cells (1 µM; up to 24 h) with similar potency. Likewise, WIKI4 also effectively inhibits the Wnt/β-catenin pathway-dependent growth of DLD1 (by 67% in 10 days;1 µM).

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/β-catenin, but not NF-κB, TGFβ, 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 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).

Cell permeable: yes
Primary Target
TNKS2
Reversible: yes

Toxicity: Standard Handling (A)

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

James, R.G., et al. 2012. PLoS. One.7, e50457.

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

100

≥98% (HPLC)

powder

15 nM IC₅₀

Calbiochem^®

OK to freeze
protect from light

pale yellow

DMSO: 5 mg/mL

2-8℃

Packaged under inert gas

11 - Combustible Solids

WGK 3