产品说明
一般描述
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.
生化/生理作用
Cell permeable: yes
Primary Target
Axin
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Irritant (B)
外形
A 25 mM (5 mg/489 µL) solution of Wnt Antagonist I, IWR-1-endo (Cat. No. 681669) in DMSO.
重悬
Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C25H19N3O3 |
分子量 | 409.44 |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | liquid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze avoid repeated freeze/thaw cycles desiccated (hygroscopic) protect from light |
储存温度 | −70℃ |
安全信息
储存分类代码 | 10 - Combustible liquids |
WGK | WGK 2 |
闪点(F) | 188.6 °F - (refers to pure substance) |
闪点(C) | 87 ℃ - (refers to pure substance) |