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681669

Sigma-Aldrich

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).

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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

Quality Level

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

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681669

Wnt Antagonist I, IWR-1-endo

vibrant-m

575545

Tankyrase1/2 Inhibitor, XAV939

vibrant-m

368050

Granzyme B Inhibitor I

vibrant-m

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Wnt Antagonist II, IWP-2

form

solid

form

solid

form

solid

form

solid

assay

≥95% (HPLC)

assay

≥97% (HPLC)

assay

≥95% (HPLC)

assay

≥97% (HPLC)

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

solubility

DMSO: 10 mg/mL

solubility

DMSO: 25 mg/mL

solubility

DMSO: 5 mg/mL

solubility

DMSO: 2.5 mg/mL

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

2-8°C

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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