5.04462

IWR-1

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

• Sinonimo/i: InSolution Wnt Antagonist I, IWR-1-endo, Inhibitor of Wnt Response-1, TNKS1/2 Inhibitor II, Tankyrase1/2 Inhibitor II, Wnt Pathway Inhibitor I
• Formula empirica (notazione di Hill): C₂₅H₁₉N₃O₃
• Numero CAS: 1127442-82-3
• Peso molecolare: 409.44
• Codice UNSPSC: 12352200

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: liquid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• Temperatura di conservazione: −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+; ZGSXEXBYLJIOGF-ALFLXDJESA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
Axin

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Irritant (B)

Stato fisico

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

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 10 - Combustible liquids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): 188.6 °F - (refers to pure substance)
• Punto d’infiammabilità (°C): 87 °C - (refers to pure substance)