5.04462

IWR-1

InSolution, ≥95%, 25 mM in DMSO, Wnt Antagonist I, endo

• Synonim(y): InSolution Wnt Antagonist I, IWR-1-endo, Inhibitor of Wnt Response-1, TNKS1/2 Inhibitor II, Tankyrase1/2 Inhibitor II, Wnt Pathway Inhibitor I
• Wzór empiryczny (zapis Hilla): C₂₅H₁₉N₃O₃
• Numer CAS: 1127442-82-3
• Masa cząsteczkowa: 409.44
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Formularz: liquid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• temp. przechowywania: −70°C
• InChI: 1S/C25H19N3O3/c29-23(27-19-5-1-3-14-4-2-12-26-22(14)19)15-8-10-18(11-9-15)28-24(30)20-16-6-7-17(13-16)21(20)25(28)31/h1-12,16-17,20-21H,13H2,(H,27,29)/t16-,17+,20-,21+
• Klucz InChI: ZGSXEXBYLJIOGF-ALFLXDJESA-N

Opis

Opis ogólny

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 (Tankyrase1/2 Inhibitor; >Cat. No. 575545) 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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
Axin

Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Irritant (B)

Postać fizyczna

A 25 mM (5 mg/489 µL) solution of Wnt Antagonist I, IWR-1-endo (Cat. No. 681669) in DMSO.

Rekonstytucja

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.

Inne uwagi

Wang, H., et al. 2011. ACS Chem. Biol.6, 192.
Chen, B., et al. 2009. Nature Chem. Biol.5, 100.
Huang, S.M., et al. 2009. Nature461, 614.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 10 - Combustible liquids
• Klasa zagrożenia wodnego (WGK): WGK 2
• Temperatura zapłonu (°F): 188.6 °F - (refers to pure substance)
• Temperatura zapłonu (°C): 87 °C - (refers to pure substance)