Size : 10mg
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Target: ATP synthase
GI50: 270 nM
Oligomycin complex is a mixture of oligomycins A, B, and C. Oligomycin A is a selective inhibitor of ATP synthase, which can inhibit oxidative phosphorylation and all the ATP-dependent processes occurring on the coupling membrane of mitochondria, and induces apoptosis in a variety of cell types. Oligomycin B is a nonselective inhibitor of ATP synthases, which can reduce the rate of ATP depletion in myocardial ischemia.
In Vitro: In A549, H1299, H1975, H520, 786-0, H838, and U87mG cancer cell lines, 100 ng/mL Oligomycin could completely inhibit OXPHOS phosphorylation activity and stimulate various levels of glycolysis gains [1]. Besides, 5 μg/mL Oligomycin could inhibit the F0 part of H+-ATP-synthase, and strongly suppress cytochrome c release and apoptosis in Hela cells induced by TNF [2]. Furthermore, Oligomycin could inhibit mitochondrial respiration, and sensitize melanoma cells to cisplatin treatment to inhibit cell invasion [3].
In Vivo: no data available.
Clinical trial: no data available.
References:[1] Hao W, Chang C B, Tsao C, et al. Oligomycin-induced Bioenergetic Adaptation in Cancer Cells with Heterogeneous Bioenergetic Organization [J]. Journal of Biological Chemistry, 2010, 285 (17): 12647-12654.[2] Shchepina L A, Pletjushkina O Y, Avetisyan A V, et al. Oligomycin, inhibitor of the F0 part of H+-ATP-synthase, suppresses the TNF-induced apoptosis [J]. Oncogene, 2002, 21 (53): 8149.[3] Roesch A, Vultur A, Bogeski I, et al. Overcoming Intrinsic Multidrug Resistance in Melanoma by Blocking the Mitochondrial Respiratory Chain of Slow-Cycling JARID1Bhigh Cells [J]. Cancer Cell, 2013, 23 (6): 811-825.
Cell lines
Human cancer cell lines NCIH1299 (H1299), A549, NCI-H1975 (H1975), NCI-H1650 (H1650), NCI-H520 (H520), 786-0, NCI-H838 (H838), and U87MG
Reaction Conditions
100 ng/ml oligomycin
Applications
Oligomycin at 100 ng/ml completely inhibited oxidative phosphorylation (OXPHOS) activity in 1 h and induced various levels of glycolysis gains by 6 h. In general, cell lines with higher respiration levels showed larger gains in glycolysis flux upon oligomycin treatment. Oligomycin, as a mitochondrial ATPase inhibitor, could be used to study OXPHOS suppression-related pharmacological effects in a variety of cancer cells, including glycolysis acceleration, ATP imbalance, AMPK activation, phosphorylation of AMPK substrate acetyl-CoA carboxylase at Ser79, and cell growth inhibition.
Note
The technical data provided above is for reference only.
References:
1. Hao W, Chang CP, Tsao CC, et al. Oligomycin-induced bioenergetic adaptation in cancer cells with heterogeneous bioenergetic organization. Journal of Biological Chemistry, 2010, 285(17): 12647-12654.