Wnt Antagonist I, IWR-1-endo

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).

Packaged under inert gas

Toxicity: Standard Handling (A)

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

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

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