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| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | PubMed Id | doi | Assay Aladdin ID |
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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。
IZCZ-3 is a potent c-MYC transcription inhibitor with antitumor activity
In Vitro
IZCZ-3 (2.1 μM-15.9 μM; 24 hours) significantly inhibits SiHa, HeLa, Huh7, and A375 cancer cell proliferation (IC 50 s of 3.3, 2.1,4.1, and 4.2 μM, respectively). IZCZ-3 induces only weak growth inhibition in the BJ fibroblasts (IC 50 =15.9 μM) and mouse mesangial cells (IC 50 =15.6 μM), suggesting that IZCZ-3 is more effective against cancer cells than against c-MYC-independent normal cells. IZCZ-3 (0-5 μM; 12 hours) induces an apparent accumulation of cells in the G0/G1 phase in SiHa cells in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: SiHa, HeLa, Huh7, and A375 cancer cells (with overexpression of c-MYC protein) and in normal BJ fibroblasts and primary cultured mouse mesangial cells (with relatively low expression of c-MYC protein). Concentration: 2.1 μM-15.9 μM Incubation Time: 24 hours Result: IC 50 s of 3.3, 2.1,4.1, and 4.2 μM for SiHa, HeLa, Huh7, and A375 cancer cells; IC 50 s of 15.9 μM and 15.6 μM for BJ fibroblasts and mouse mesangial cells. Cell Cycle AnalysisCell Line: SiHa cells Concentration: 0, 1.25, 2.5, and 5 μM Incubation Time: 12 hours Result: Induced an apparent accumulation of cells in the G0/G1 phase (increasing from 61% to 70%) in a dose-dependent manner.
In Vivo
IZCZ-3 (20, 10, and 5 mg/kg; intraperitoneally; every other day for 24 days) inhibits tumor growth in BALB/c nude mice with SiHa human cervical squamous cancer xenograft . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c nude mice (5 weeks old) bearing SiHa human cervical squamous cancer xenograft model Dosage: 20, 10, and 5 mg/kg Administration: Treated intraperitoneally; every other day for 24 days Result: Treatment with 20, 10, and 5 mg/kg resulted in a significant reduction in tumor weight with tumor growth inhibition (TGI) of 69%, 64%, and 57%, respectively. Displayed time-dependent inhibition of tumor growth.
Form:Solid
IC50& Target:c-MYC transcription
分类树(Taxonomy Tree)
| 界(kingdom) | 有机化合物 |
|---|---|
| 超类(Superclass) | 有机杂环化合物 |
| 类(Class) | 吲哚及其衍生物 |
| 亚类(Subclass) | 咔唑类 |
| 中间层级节点(Intermediate Tree Nodes) | 暂无 |
| 直接上位类(Direct Parent) | 咔唑类 |
| 其他上位类(Alternative Parents) | 苯基哌嗪类 N-芳基哌嗪 苯基咪唑类 N-烷基吲哚 甲氧基苯胺 吲哚 1,2,4,5-四取代咪唑 苯氧基化合物 甲氧基苯 二烷基芳胺 茴香醚 N-甲基哌嗪 烷基芳基醚 取代吡咯 N-取代咪唑 杂芳族化合物 三烷基胺 氮杂环化合物 有机光子化合物 碳氢化合物衍生物 |
| 分子骨架(Molecular Framework) | 芳香族杂多环化合物 |
| 取代基(Substituents) | 1-苯基咪唑 - 1,2,4,5-四取代咪唑 - 1,4-二氮杂环丁烷 - 4-苯基吡啶 - 5-苯基咪唑 - 芳基醚 - 氨基酸 - 苯胺或取代苯胺 - 茴香醚 - 芳香族杂多环化合物 - 氮杂环 - 吡唑 - 苯基化合物 - 蒽醌 - 二烷基芳基胺 - 乙醚 - 杂芳香族化合物 - 烃衍生物 - 咪唑 - 吲哚 - 甲氧基苯胺 - 甲氧基苯 - 单环苯基基团 - N-烷基吲哚 - N-烷基哌嗪 - N-芳基哌嗪 - N-甲基哌嗪 - N-取代咪唑 - 有机硝基化合物 - 有机氧化合物 - 有机氮化合物 - 有机氧化合物 - 有机氮化合物 - 苯酚醚 - 苯氧基化合物 - 苯基哌嗪 - 哌嗪 - 吡咯 - 取代吡咯 - 三元脂肪胺 - 三级脂肪族/芳香族胺 - 三芳基胺 |
| 描述(Description) | 该化合物属于有机化合物中的咔唑类。这类化合物具有三环系统,其中吡咯环分别与两个苯环相连。 |
| 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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