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500556 Tankyrase1/2 Inhibitor V, WIKI4 - CAS 838818-26-1 - Calbiochem

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Synonymes: 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

Primary Target: TNKS2
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500556
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Tableau de caractéristiques principal

CAS #Empirical Formula
838818-26-1C₂₉H₂₃N₅O₃S

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      Description
      OverviewA 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.
      Catalogue Number500556
      Brand Family Calbiochem®
      Synonyms2-(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
      References
      ReferencesJames, R.G., et al. 2012. PLoS. One.7, e50457.
      Product Information
      CAS number838818-26-1
      FormPale yellow powder
      Hill FormulaC₂₉H₂₃N₅O₃S
      Chemical formulaC₂₉H₂₃N₅O₃S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetTNKS2
      Primary Target IC<sub>50</sub>15 nM
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowig reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5.00556.0001 04055977244939

      Documentation

      Tankyrase1/2 Inhibitor V, WIKI4 - CAS 838818-26-1 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      James, R.G., et al. 2012. PLoS. One.7, e50457.
      Fiche technique

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision10-May-2013 JSW
      Synonyms2-(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
      DescriptionA 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).
      FormPale yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number838818-26-1
      Chemical formulaC₂₉H₂₃N₅O₃S
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowig reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesJames, R.G., et al. 2012. PLoS. One.7, e50457.