5.04462

IWR-1

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

• 別名: InSolution Wnt Antagonist I, IWR-1-endo, Inhibitor of Wnt Response-1, TNKS1/2 Inhibitor II, Tankyrase1/2 Inhibitor II, Wnt Pathway Inhibitor I
• 実験式（ヒル表記法）: C₂₅H₁₉N₃O₃
• CAS番号: 1127442-82-3
• 分子量: 409.44
• MDL番号: MFCD18086875
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: liquid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• 保管温度: −70°C
• SMILES記法: N4(C(=O)[C@@H]5[C@@H]([C@H]6C[C@@H]5C=C6)C4=O)c1ccc(cc1)C(=O)Nc2c3ncccc3ccc2
• 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+
• InChI Key: ZGSXEXBYLJIOGF-ALFLXDJESA-N

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Axin

Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

物理的形状

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

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 10 - Combustible liquids
• WGK: WGK 2
• 引火点(°F): 188.6 °F - (refers to pure substance)
• 引火点(℃): 87 °C - (refers to pure substance)