Dehydroaltenusin |
| Catalog No.GC35829 |
Dehydroaltenusin은 IC50 값이 0.68μM인 곰팡이에 의해 생성되는 항생제 유형인 진핵생물 DNA 중합효소 α의 소분자 선택적 억제제입니다. 포유류 pol α 활성에 대한 dehydroaltenusin의 억제 작용 방식은 DNA 주형 프라이머(Ki=0.23μM)와 관련하여 경쟁적이며 2'-deoxyribonucleoside 5'-triphosphate 기질(Ki=0.18μM)과 관련하여 비경쟁적입니다. . Dehydroaltenusin은 S기에서 암세포 주기를 정지시키고 세포자멸사를 유발합니다. Dehydroaltenusin은 생체 내에서 인간 선암종 종양에 대한 항종양 활성을 가지고 있습니다.
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Cas No.: 31186-13-7
Sample solution is provided at 25 µL, 10mM.
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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: 0.68 μM (DNA polymerase α)[1]
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]. Cell Proliferation Assay[1] Cell Line: Human cancer cell line: A549, BALL-1, HeLa and NUGC-3 cells
Dehydroaltenusin (injection; 20 mg/kg; 2-day intervals; 12-39 days) shows suppressed tumor growth from 21 days[1]. Animal Model: Nude mice bearing HeLa solid tumors[1]
[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.
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