5.04462

IWR-1

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

• Synonym(e): InSolution Wnt Antagonist I, IWR-1-endo, Inhibitor of Wnt Response-1, TNKS1/2 Inhibitor II, Tankyrase1/2 Inhibitor II, Wnt Pathway Inhibitor I
• Empirische Formel (Hill-System): C₂₅H₁₉N₃O₃
• CAS-Nummer: 1127442-82-3
• Molekulargewicht: 409.44
• UNSPSC-Code: 12352200

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥95% (HPLC)
• Form: liquid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• Lagertemp.: −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+
• InChIKey: ZGSXEXBYLJIOGF-ALFLXDJESA-N

Beschreibung

Allgemeine Beschreibung

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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
Axin

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Irritant (B)

Physikalische Form

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

Rekonstituierung

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

Sonstige Hinweise

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.

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 10 - Combustible liquids
• WGK: WGK 2
• Flammpunkt (°F): 188.6 °F - (refers to pure substance)
• Flammpunkt (°C): 87 °C - (refers to pure substance)