IWR-1-endo
别名: endo-IWR 1, IWR-1
IWR-1-endo (endo-IWR 1, IWR-1)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-endo Chemical Structure
CAS: 1127442-82-3
客户使用Selleck的IWR-1-endo发表文献119篇
产品质控
常与IWR-1-endo一起在实验中被使用的化合物
IWR-1-endo相关产品
| 相关靶点 | WNT β-catenin Wnt/β-catenin | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 FDA药物库 干细胞小分子化合物库 GPCR小分子化合物库 干细胞分化化合物库 | 点击展开 |
相关信号通路图
Wnt/beta-catenin抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| DLD1 | Function assay | 1 to 20 uM | 24 hrs | Inhibition of tankyrase in human DLD1 cells assessed as inhibition of TCF-dependent transcriptional activity at 1 to 20 uM after 24 hrs by dual luciferase reporter gene assay | 24527792 |
| DLD1 | Cytotoxicity assay | 1 to 20 uM | 10 days | Cytotoxicity against human DLD1 cells assessed as growth inhibition at 1 to 20 uM measured on day 10 by crystal violet staining | 24527792 |
| HT29 | Function assay | 25 uM | 24 hrs | Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity at 25 uM after 24 hrs by dual luciferase reporter gene assay relative to control | 24950489 |
| HT29 | Function assay | 25 uM | 24 hrs | Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity at 25 uM after 24 hrs by dual luciferase reporter gene assay relative to control in presence of GSK-3beta inhibitor LiCl | 24950489 |
| HT29 | Function assay | 25 uM | 24 hrs | Inhibition of Wnt/beta-catenin signaling in human HT29 cells assessed as increase in axin2 mRNA expression at 25 uM after 24 hrs by quantitative real-time PCR assay | 24950489 |
| DLD1 | Function assay | 10 uM | Induction of Axin2 in human DLD1 cells overexpressing IWR-IS assessed as decrease in Wnt pathway activity at 10 uM by STF reporter assay method | 19125156 | |
| HT29 | Function assay | 24 hrs | Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control, IC50 = 24.4 μM. | 24950489 | |
| L-Wnt-STF | Function assay | 24 hrs | Inhibition of TNKS-1 in mouse L-Wnt-STF cells assessed as disruption of Wnt signaling after 24 hrs by luciferase reporter gene assay, IC50 = 0.131 μM. | 24527792 | |
| L-Wnt-STF | Function assay | 24 hrs | Inhibition of TNKS-2 in mouse L-Wnt-STF cells assessed as disruption of Wnt signaling after 24 hrs by luciferase reporter gene assay, IC50 = 0.056 μM. | 24527792 | |
| SW480 | Function assay | 40 to 48 hrs | Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs, IC50 = 0.25 μM. | 23701517 | |
| SW480 | Function assay | 24 hrs | Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method, EC50 = 2.5 μM. | 23701517 | |
| BL21 (DE3) | Function assay | 90 mins | Activity of N-terminus hexaHis-tagged human TNSK2 expressed in Escherichia coli BL21 (DE3) cells using biotinylated NAD+ as substrate after 90 mins by Western blot analysis, EC50 = 0.2 μM. | 22233320 | |
| DLD1 | Function assay | 2 hrs | Induction of Axin2 stabilization in human DLD1 cells assessed as decreased transcription of Axin2 after 2 hrs by RT-PCR method | 19125156 | |
| HEK293T | Function assay | Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay, IC50 = 0.026 μM. | 22191557 | ||
| HEK293 | Function assay | Displacement of IWR-PB from Axin2 in HEK293 cells by Western blot method | 19125156 | ||
| DLD1 | Function assay | Inhibition of Axin2 protein degradation in human DLD1 cells by Western blot analysis | 19125156 | ||
| DLD1 | Function assay | Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Thr41 phosphorylated beta-casein levels by Western blot analysis | 19125156 | ||
| DLD1 | Function assay | Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Ser37 phosphorylated beta-casein levels by Western blot analysis | 19125156 | ||
| DLD1 | Function assay | Decrease in beta-casein accumulation in human DLD1 cells expressing in APC mutant | 19125156 | ||
| DLD1 | Function assay | Induction of Axin2 accumulation in human DLD1 cells assessed as decrease in free beta-casein levels by Western blot analysis | 19125156 | ||
| DLD1 | Function assay | Induction of Axin2 stabilization in human DLD1 cells assessed as inhibition of Wnt/beta-casein pathway | 19125156 | ||
| DLD1 | Function assay | Induction of Axin2 accumulation in human DLD1 cells assessed as increase in Ser33 phosphorylated beta-casein levels by Western blot analysis | 19125156 | ||
| DLD1 | Function assay | Induction of Axin2 accumulation in human DLD1 cells by Western blot analysis | 19125156 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | IWR-1-endo (endo-IWR 1, IWR-1)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 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 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] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Survivin p-Akt / Akt E-cadherin / N-cadherin / Snail / Vimentin |
|
26450645 | |
化学信息&溶解度
| 分子量 | 409.44 | 分子式 | C25H19N3O3 |
| CAS号 | 1127442-82-3 | SDF | -- |
| Smiles | C1C2C=CC1C3C2C(=O)N(C3=O)C4=CC=C(C=C4)C(=O)NC5=CC=CC6=C5N=CC=C6 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 82 mg/mL ( (200.27 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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