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CAS: 1127442-82-3
分子式: C25H19N3O3
分子量: 409.44
中文名称: 
rel-4-[(3ar,4S,7R,7as)-1,3,3a,4,7,7a-六氢-1,3-二氧代-4,7-甲桥-2h-异吲哚-2-基]-n-8-喹啉基苯甲酰胺
英文名称: 
iwr-1
用途: IWR-1-endo是一种Wnt通路抑制剂,在表达 Wnt3A 的 L-细胞中IC50为180 nM,诱导Axin2蛋白水平,并通过稳定Axin骨架破坏复合体来促进β-catenin磷酸化。IWR-1 和XAV939作为Wnt通路的可逆抑制剂,在体内外具有相似的药理作用,IWR-1通过与Axin相互作用而发挥效果,而XAV939直接与TNKS结合。[1]
推荐供应商
货号品牌产品名称规格包装、参考价格
I796098MACKLINIWR-1-endo10mM in DMSO326元/1ml;   咨询
储存:-20°C
I872800MACKLINIWR-1-endo99%358元/5mg;   946元/25mg;   3485元/100mg;   咨询
储存:-20℃
状态:白色到棕色粉末到晶体
1189408J&KIWR-198%, 是端锚聚合酶抑制剂, 抑制Wnt/β-catenin信号传导途径380元/5MG;   680元/10MG;   咨询

基本信息

分子式C25H19N3O3
分子量409.44
存储条件Freezer -20℃

产品描述

IWR-1-endo是一种Wnt通路抑制剂,在表达 Wnt3A 的 L-细胞中IC50为180 nM,诱导Axin2蛋白水平,并通过稳定Axin骨架破坏复合体来促进β-catenin磷酸化。

靶点(IC50 & Targe)

Wnt,180nM

体外研究

IWR-1 和XAV939作为Wnt通路的可逆抑制剂,在体内外具有相似的药理作用,IWR-1通过与Axin相互作用而发挥效果,而XAV939直接与TNKS结合。[1]

参考文献

[1] Lu J, et al. Bioorg Med Chem Lett, 2009, 19(14), 3825-3827.

5.04462Sigma-AldrichInSolution Wnt Antagonist I, IWR-1-endo-CAS 1127442-82-3-Calbiochem1129.94元/5 MG;   咨询

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/tradenameCalbiochem®
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
WGKWGK 2
闪点(F)188.6 °F - (refers to pure substance)
闪点(C)87 ℃ - (refers to pure substance)
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