计算溶液所需的质量、体积或浓度。
| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | PubMed Id | doi | Assay Aladdin ID |
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提供 ≥98% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways
In Vitro
VII-31 (100 nM, 200 nM; 48 hours) inhibits the cell viability of gastric cell line MGC803 with an IC 50 of 0.09±0.01 μM. VII-31 also inhibits the cell viability of MCF-7 and PC-3 with IC 50 s of 0.10±0.006 and 1.15±0.28μM , respectively. VII-31 (50-150 nM; 24 hours) arrests MGC803 cells cycle in G2/M phase. VII-31 (50-150 nM; 48 hours) induces apoptosis via intrinsic and extrinsic pathways. VII-31 (50-150 nM; 24 hours) activates NEDDylation in MGC803 cells. VII-31 (50-150 nM; 48 hours) up-regulates pro-apoptotic proteins FADD, Fasl, PIDD, Bax, Bad; while down-regulates anti-apoptotic proteins Bcl-xL, Bcl-2, XIAP, c-IAP1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Gastric cancer MGC803 cells Concentration: 100, 200 nM Incubation Time: 48 hours Result: Inhibited the cell viability in dose-depend manner. Cell Cycle AnalysisCell Line: MGC803 cells Concentration: 50, 100, 150 nM Incubation Time: 24 hours Result: Arrested cells in G2/M phase, and a clear sub-G1 peak was observed in the high dose group. Apoptosis AnalysisCell Line: MGC803 cells Concentration: 50, 75, 100, and 150 nM Incubation Time: 48 hours Result: High dose (150 nM) treatment significantly elevated the early and late apoptosis rate to 92.8% from 4.8%. Western Blot AnalysisCell Line: MGC803 cells Concentration: 50, 100, 150 nM Incubation Time: 24 hours Result: Resulted in NEDDylation activation of MGC803 cells, the NEDDylation of 3 important proteins NAE1, Ubc12 and CUL1 has been activated.
In Vivo
VII-31 inhibits the tumor progression in vivo, while showing no obvious toxicity to mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice bearing MGC803 xenograft tumors Dosage: 50, 100, 150 mg/kg Administration: Subcutaneous injection; daily for 28 days Result: The mice had a much smaller tumor compared with vehicle control. The tumor volumes of middle/high dose treated mice at certain time points were evidently decreased comparing with untreated group.
Form:Solid
IC50& Target:NEDDylation
分类树(Taxonomy Tree)
| 界(kingdom) | 有机化合物 |
|---|---|
| 超类(Superclass) | 苯类化合物 |
| 类(Class) | 苯及其取代衍生物 |
| 亚类(Subclass) | 苯胺类 |
| 中间层级节点(Intermediate Tree Nodes) | 暂无 |
| 直接上位类(Direct Parent) | 苯胺类 |
| 其他上位类(Alternative Parents) | 苯氧基化合物 甲氧基苯 茴香醚 烷基芳基醚 噻吩类 叔羧酸酰胺 杂芳族化合物 有机硫化合物 有机光子化合物 有机氮化合物 有机氧化物 碳氢化合物衍生物 |
| 分子骨架(Molecular Framework) | 芳香族杂单环化合物 |
| 取代基(Substituents) | 芳基醚 - 苯胺类化合物 - 茴香醚 - 芳香族杂单环化合物 - 羧酰胺基 - 羧酸衍生物 - 乙醚 - 杂芳香族化合物 - 烃衍生物 - 甲氧基苯 - 有机硝基化合物 - 有机氧化物 - 有机氧化合物 - 有机杂环化合物 - 有机氮化合物 - 有机氧化合物 - 有机氮化合物 - 有机硫化合物 - 苯酚醚 - 苯氧基化合物 - 叔羧酸酰胺 - 噻吩 |
| 描述(Description) | 该化合物属于有机化合物中的苯胺类。这类有机杂环化合物由氧酸RkE(=O)l(OH)m(l≠0)通过将羟基OH替换为N-羧基NHPh基团或经环取代形成的衍生物而衍生。 |
| 外部描述符(External Descriptors) | 暂无 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
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