切换导航

Oligomycin A

现货
Catalog No.
A5588
线粒体ATP合成酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,500.00
Ship with 10-15 days
5mg
¥ 1,350.00
Ship with 10-15 days
25mg
¥ 4,000.00
Ship with 10-15 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

Oligomycin A is an inhibitor of ATP synthase, which inhibits the process taking place on mitochondria coupling membrane that depended on ATP and oxidative phosphorylation [1].

Oligomycin A blocks proton channel of ATP synthase, which is necessary for transforming ADP to ATP by oxidative phosphorylation, accomplishing the inhibition of ATP synthase. The process which oligomycin A inhibits ATP synthesis can significantly reduce electron flow through the electron transport chain.

Experiments which performed in testing against 60 human cancer cell lines that from the National Cancer Institute showed that oligomycin is among the top 0.1% of the most cell line selective cytotoxic agents of 37,000 molecules. In the HeLa carcinoma cell line, the inhibitors of H+ -ATP-synthase oligomycin (5 mg/ml) was shown to strongly suppress, and the cell respiration, showing that it is tightly coupled to ATP synthesis. It was reported that Oligomycin at 100 ng/ml completely inhibits the activity of oxidative phosphorylation in 1h and induces different levels of glycolysis gains by 6 h in a group of cancer cell. As an inhibitor of the F0 part of H+-ATP-synthase, Oligomycin also suppresses the apoptosis which was induced by TNF. Treatment with different concentrations of oligomycin and rotenone severely reduced the oxygen consumption by up to 94%, indicating a major role for mitochondria in this process. And treatment with oligomycin could abolish the H2O2 increase completely [2-4].

References:
[1].  Jastroch M, Divakaruni AS, Mookerjee S, et al. Mitochondrial proton and electron leaks. Essays Biochemistry, 2010, 47:53-67.
[2].  Shchepina LA, Pletjushkina OY, Avetisyan AV, et al. Oligomycin, inhibitor of the F-0 part of H+-ATP-synthase, suppresses the TNF-induced apoptosis. Oncogene, 2002, 53: 8149-8157.
[3].  Salomon AR, Voehringer DW, Herzenberg LA, et al. Understanding and exploiting the mechanistic basis for selectivity of polyketide inhibitors of F0F1-ATPase. Proceedings of The National Academy of Sciences of The United States of America, 2000, 97(26): 14766-14771.
[4].  Alexander R, Adina V, Ivan B, et al. Overcoming intrinsic multi-drug resistance in melanoma by blocking the mitochondrial respiratory chain of slow-cycling JARID1Bhigh cells. Cancer Cell, 2013, 23(6): 811-825.

文献引用

1. Tian C, Yuan Z, et al. "Inhibition of glycolysis by a novel EGFR/HER2 inhibitor KU004 suppresses the growth of HER2+ cancer." Exp Cell Res. 2017 May 19. pii: S0014-4827(17)30297-5. PMID:28532652

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt791.06
Cas No.579-13-5
FormulaC45H74O11
Solubility≥9.9mg/mL in DMSO, ≥17.43 mg/mL in EtOH, <2.33 mg/mL in H2O
Chemical Name4-ethyl-11,12,15,19-tetrahydroxy-6'-(2-hydroxypropyl)-5',10,12,14,16,18,20,26,29-nonamethylspiro[24,28-dioxabicyclo[23.3.1]nonacosa-5,7,21-triene-27,2'-oxane]-13,17,23-trione
SDFDownload SDF
Canonical SMILESCCC1CCC2C(C(C(C3(O2)CCC(C(O3)CC(C)O)C)C)OC(=O)C=CC(C(C(C(=O)C(C(C(C(=O)C(C(C(CC=CC=C1)C)O)(C)O)C)O)C)C)O)C)C
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

人喉癌耐多烯紫杉醇DRHEp2细胞

溶解方法

在DMSO中的溶解度大于9.9mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

72 h,2 μg/ml

应用

Oligomycin A是F0-ATP酶的抑制剂。Oligomycin A以剂量依赖的方式增加DRHEp2细胞对多烯紫杉醇的敏感性。联合使用Oligomycin A和多烯紫杉醇可增加线粒体ROS的产生。

References:

[1]. Mizumachi T, Suzuki S, Naito A, et al. Increased mitochondrial DNA induces acquired docetaxel resistance in head and neck cancer cells[J]. Oncogene, 2008, 27(6): 831-838.

质量控制

质量控制和MSDS

批次:

化学结构

Oligomycin A