5.00556

Tankyrase1/2 Inhibitor V, WIKI4

• Sinónimos: Tankyrase1/2 Inhibitor V, WIKI4, 2-(3-((4-(4-methoxyphenyl)-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)sulfanyl)propyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione, Wnt Pathway Inhibitor XVIII, TNKS1/2 Inhibitor V
• Fórmula empírica (notación de Hill): C₂₉H₂₃N₅O₃S
• Número de CAS: 838818-26-1
• Peso molecular: 521.59
• Código UNSPSC: 12352200
• ID de la sustancia en PubChem: 2984337
• NACRES: NA.77

Propiedades

• Análisis: ≥98% (HPLC)
• Nivel de calidad: 100
• formulario: powder
• potencia: 15 nM IC₅₀
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: pale yellow
• solubilidad: DMSO: 5 mg/mL
• temp. de almacenamiento: 2-8°C
• cadena SMILES: COC1=CC=C(C=C1)N2C(=NN=C2SCCCN3C(=O)C4=CC=CC5=C4C(=CC=C5)C3=O)C6=CC=NC=C6

Descripción

Descripción general

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).

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.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
TNKS2

Reversible: yes

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable