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Key Documents

681669

Sigma-Aldrich

IWR-1-endo

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

Sinónimos:

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

Fórmula empírica (notación de Hill):
C25H19N3O3
Peso molecular:
409.44
Código UNSPSC:
12352200
NACRES:
NA.77

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).

Nivel de calidad

Análisis

≥95% (HPLC)

formulario

solid

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze
protect from light

color

off-white

solubilidad

DMSO: 10 mg/mL

Condiciones de envío

ambient

temp. de almacenamiento

2-8°C

Descripción general

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).

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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

Información legal

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

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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