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681669 Wnt Antagonist I, IWR-1-endo - Calbiochem

Wnt Antagonist I, IWR-1-endo, is a cell-permeable inhibitor of TNKS1/PARP5a (IC₅₀ = 131 nM) & TNKS2/PARP5b (IC₅₀= 56 nM). Suppress Wnt-stimulated transcription activity (IC₅₀ = 180 nM).

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

Synonyms: TNKS1/2 Inhibitor II, Wnt Pathway Inhibitor I, Inhibitor of Wnt Response-1, Tankyrase1/2 Inhibitor II

681669
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₅H₁₉N₃O₃

Products

Catalogue NumberPackaging Qty/Pack
681669-10MGCN Plastic ampoule 10 mg
Description
OverviewA cell-permeable p-imidobenzamidoquinoline, endo-diastereomer that is shown to inhibit the activity of TNKS1/PARP5a and TNKS2/PARP5b in in vitro auto-PARsylation assays (IC50 = 131 and 56 nM, respectively) and effectively suppress Wnt-stimulated transcription activity in L-Wnt-STF-based reporter assays (IC50 = 180 nM), while exhibiting little activity against PARP1 or PARP2 (IC50 >18.75 µM). Although both IWR-1-endo and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects both in vitro and in vivo, IWR-1-endo exerts its effect via interaction with Axin, while XAV939 binds TNKS directly. Also available as a 25 mM solution in DMSO (Cat. No. 504462).
Catalogue Number681669
Brand Family Calbiochem®
SynonymsTNKS1/2 Inhibitor II, Wnt Pathway Inhibitor I, Inhibitor of Wnt Response-1, Tankyrase1/2 Inhibitor II
References
ReferencesChen, B., et al. 2009. Nature Chem. Biol. 5, 100.
Huang, S.M., et al. 2009. Nature 461, 614.
Product Information
FormOff-white solid
Hill FormulaC₂₅H₁₉N₃O₃
Chemical formulaC₂₅H₁₉N₃O₃
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing 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
681669-10MGCN 04055977260274

Documentation

Wnt Antagonist I, IWR-1-endo - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Wnt Antagonist I, IWR-1-endo - Calbiochem Certificates of Analysis

TitleLot Number
681669

References

Reference overview
Chen, B., et al. 2009. Nature Chem. Biol. 5, 100.
Huang, S.M., et al. 2009. Nature 461, 614.
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.

Revision18-November-2009 RFH
SynonymsTNKS1/2 Inhibitor II, Wnt Pathway Inhibitor I, Inhibitor of Wnt Response-1, Tankyrase1/2 Inhibitor II
DescriptionA cell-permeable p-imidobenzamidoquinoline, endo-diastereomer that is shown to inhibit the activity of TNKS1/PARP5a and TNKS2/PARP5b in in vitro auto-PARsylation assays (IC50 = 131 and 56 nM, respectively) and effectively suppress Wnt-stimulated transcription activity in L-Wnt-STF-based reporter assays (IC50 = 180 nM), while exhibiting little activity against PARP1 or PARP2 (IC50 >18.75 µM). Although both IWR-1-endo and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects both in vitro and in vivo, IWR-1-endo exerts its effect via interaction with Axin, while XAV939 binds TNKS directly.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₅H₁₉N₃O₃
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesChen, B., et al. 2009. Nature Chem. Biol. 5, 100.
Huang, S.M., et al. 2009. Nature 461, 614.