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.