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CAS No.: 1127442-82-3
Synonyms: endo-IWR 1;IWR-1-endo
IWR-1-endo is a small-molecule inhibitor of Wnt signaling (IC50 of 180 nM in L-cells expressing Wnt3A) by stabilizing the Axin destruction complex with an EC50 of 0.2 μM.
生物活性
靶点 | Wnt EC50:0.2μM |
实验方案
技术信息
CAS号 | 1127442-82-3 | 储存条件 |
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分子式 | C25H19N3O3 | 运输 | 蓝冰 | |||||||||||||
分子量 | 409.44 | 别名 | endo-IWR 1;IWR-1-endo | |||||||||||||
溶解度 |
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动物实验配方 |
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Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
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Escherichia coli BL21 (DE3) cells | - | 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 |
HEK293 cells | - | Function assay | - | Displacement of IWR-PB from Axin2 in HEK293 cells by Western blot method | 19125156 |
human DLD1 cells | - | Function assay | 2 h | Induction of Axin2 stabilization in human DLD1 cells assessed as decreased transcription of Axin2 after 2 hrs by RT-PCR method. | 19125156 |
human HEK293T cells | - | Function assay | - | Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay, IC50=0.026 μM | 22191557 |
human HT29 cells | - | Function assay | 24 h | 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 |
human HT29 cells | 25 μM | Function assay | 24 h | 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 |
human SW480 cells | - | Function assay | 40 to 48 h | Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs, IC50=0.25 μM | 23701517 |
human SW480 cells | - | Function assay | 24 h | Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method | 23701517 |
mouse L-Wnt-STF cells | - | Function assay | - | 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 |
mouse L-Wnt-STF cells | - | Function assay | - | 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 |
靶点 | Description | IC50 |
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Wnt | EC50:0.2μM |
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