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IWR-1-endo

现货
Catalog No.
B2306
Wnt抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
10mg
¥ 700.00
现货
25mg
¥ 1,500.00
现货

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Background

IWR-1-endo is a small molecule inhibitor of Wnt Response with IC50 value of 180nM [1].

IWR-1-endo is a small molecule antagonists of the Wnt/β-catenin pathway screened out from a diverse synthetic chemical library. It acts as an inhibitor of Wnt response. IWR-1-endo can inhibit the activity of Wnt1, 2 and 3. In cultured cells, IWR-1-endo inhibits Wnt-induced β-catenin accumulation which is a downstream event of Lrp6 and Dvl2. It is proved that IWR-1-endo promote β-catenin destruction through promoting stability of Axin-scaffolded destruction complexes in the DLD-1 colorectal cancer (CRC) cell line. IWR-1-endo is also shown to inhibit tailfin regeneration and epithelial stem cell self-renewal in zebrafish. These two processes are both dependent on Wnt/β-catenin signaling. Furthermore, IWR-1-endo can block aberrant cell growth supported by hyperactivation of Wnt/β-catenin resulting from Apc loss [1].

References:
[1] Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.

文献引用

1.Suknuntha K, Tao L, et al. "Optimization of Synthetic mRNA for Highly Efficient Translation and its Application in the Generation of Endothelial and Hematopoietic Cells from Human and Primate Pluripotent Stem Cells." Stem Cell Rev. 2018 Mar 8. PMID:29520567

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt409.44
Cas No.1127442-82-3
FormulaC25H19N3O3
Solubility≥20.45mg/mL in DMSO
Chemical Name4-((3aR,4S,7R,7aS)-1,3-dioxo-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindol-2(3H)-yl)-N-(quinolin-8-yl)benzamide
SDFDownload SDF
Canonical SMILESO=C([C@@]1([H])[C@]2([H])[C@]3([H])C([H])([H])[C@@]1([H])C([H])=C3[H])N(C4=C([H])C([H])=C(C(N([H])C5=C([H])C([H])=C([H])C6=C5N=C([H])C([H])=C6[H])=O)C([H])=C4[H])C2=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

DLD-1结肠直肠癌(CRC)细胞系

溶解方法

该化合物在DMSO中的溶解度大于20.5 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

1 μM,2.5 μM,10 μM

应用

在DLD-1结肠直肠癌(CRC)细胞系中,IWR-1-endo通过促进Axin-脚手架破坏复合体的稳定性来破坏β-连环蛋白。IWR-1-endo阻断由Apc损失引起的Wnt/β-连环蛋白过度活化造成的异常细胞生长。

动物实验 [1]:

动物模型

斑马鱼

给药剂量

10 mM,24 h

应用

IWR-1-endo抑制斑马鱼尾巴再生和上皮干细胞自我更新。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.

生物活性

描述 IWR-1-endo是Wnt信号应答的小分子抑制剂,IC50值为180 nM[1]。
靶点 Wnt signaling          
IC50 180 nM          

质量控制

化学结构

IWR-1-endo

相关生物数据

IWR-1-endo