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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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
500556
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
838818-26-1C₂₉H₂₃N₅O₃S

Products

Catalogue NumberPackaging Qty/Pack
5.00556.0001 Glass bottle
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
Catalogue Number GTIN
5.00556.0001 04055977244939

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Reference overview
James, R.G., et al. 2012. PLoS. One.7, e50457.
Data Sheet

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.