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Dehydroaltenusin (Synonyms: 脱氢阿霉素)
Dehydroaltenusin 脱氢阿霉素是真核DNA 聚合酶 α (DNA polymerase α) 的小分子选择性抑制剂，一种由真菌产生的抗生素，其 IC50值为 0.68 μM。 Dehydroaltenusin 对哺乳动物 polα 活性的抑制作用模式对 DNA 模板引物 (Ki=0.23 μM) 是竞争性的，对 2′-脱氧核糖核苷 5′-三磷酸底物是非竞争性的 (Ki=0.18 μM)。 Dehydroaltenusin 在 S 期阻止癌细胞周期并触发凋亡 apoptosis。 Dehydroaltenusin 在体内具有抗人类腺癌肿瘤的抗肿瘤活性。
Dehydroaltenusin Chemical Structure
CAS No. : 31186-13-7
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| 生物活性 |
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2′-deoxyribonucleoside 5′-triphosphate substrate (Ki=0.18 µM)[1]. Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis[1]. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo[1]. |
IC50 & Target |
IC50: 0.68 μM (DNA polymerase α)[1] |
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| 体外研究 (In Vitro) |
Dehydroaltenusin (38.0-44.4 μM; 24 hours) inhibits cell growth in a dose-dependent manner and the LD50 values varies from 38.0 to 44.4 μM[1]. Dehydroaltenusin (38.0 μM; 6 hours) inhibits cell growth by blocking the S-phase of DNA replication[1]. Dehydroaltenusin (75.0 μM; 24 hours) has a strong apoptotic effect on human cancer cells, DNA ladders can be detected after 12 h of incubation with dehydroaltenusin[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay[1]
Cell Cycle Analysis[1]
Apoptosis Analysis[1]
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| 体内研究 (In Vivo) |
Dehydroaltenusin (injection; 20 mg/kg; 2-day intervals; 12-39 days) shows suppressed tumor growth from 21 days[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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| 分子量 |
288.25 |
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| Formula |
C15H12O6 |
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| CAS 号 |
31186-13-7 |
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| 中文名称 |
脱氢阿霉素 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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| 参考文献 |
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