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681669

IWR-1-endo

≥95% (HPLC), solid, Wnt antagonist, Calbiochem®

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

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About This Item

Empirical Formula (Hill Notation):
C25H19N3O3
Molecular Weight:
409.44
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
100
Storage condition:
OK to freeze, protect from light
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Product Name

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).

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

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.

Packaging

Packaged under inert gas

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

flash_point_f

Not applicable

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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