681669

Wnt Antagonist I, IWR-1-endo

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).

• Synonym(s): Wnt Antagonist I, IWR-1-endo, Inhibitor of Wnt Response-1, Wnt Pathway Inhibitor I, TNKS1/2 Inhibitor II, Tankyrase1/2 Inhibitor II, Wnt Pathway Inhibitor I, Inhibitor of Wnt Response-1, Tankyrase1/2 Inhibitor II, TNKS1/2 Inhibitor II
• Empirical Formula (Hill Notation): C₂₅H₁₉N₃O₃
• Molecular Weight: 409.44
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

A 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.

A 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).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Chen, B., et al. 2009. Nature Chem. Biol.5, 100.
Huang, S.M., et al. 2009. Nature461, 614.

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable