Dehydroaltenusin (Synonyms: 脱氢阿霉素)

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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 (Synonyms: 脱氢阿霉素)

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]
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.

Dehydroaltenusin 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Human cancer cell line: A549, BALL-1, HeLa and NUGC-3 cells
Concentration: 38.0-44.4 μM
Incubation Time: 24 hours
Result: Inhibited cell growth of human cancer cell lines.

Cell Cycle Analysis[1]

Cell Line: HeLa cells
Concentration: 38.0 μM
Incubation Time: 6 hours
Result: Decreased to 45% of the control value after 6 h of incubation [3H]-thymidine.

Apoptosis Analysis[1]

Cell Line: HeLa cells
Concentration: 75.0 μM
Incubation Time: 12-24 hours
Result: Detected DNA ladders after 12 hours of incubation.

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.

Animal Model: Nude mice bearing HeLa solid tumors[1]
Dosage: 20 mg/kg
Administration: Injection; 20 mg/kg; 2-day intervals; 12-39 days
Result: Suppressed tumor growth.

分子量

288.25

Formula

C15H12O6
CAS 号

31186-13-7
中文名称

脱氢阿霉素
结构分类
  • Antibiotics
  • Disease Research
  • Anticancer
  • Phenols
  • Monophenols
  • Antibiotics
  • Other Antibiotics
初始来源
  • 微生物

Talaromyces flavus B 5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (538 KB) 产品使用指南 (1538 KB)

参考文献

  • [1]. Mizushina Y, et al. Dehydroaltenusin is a specific inhibitor of mammalian DNA polymerase α. Expert Opin Investig Drugs. 2011 Nov;20(11):1523-34.  [Content Brief]

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