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- Oligomycin Complex
Oligomycin Complex
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.
- 1. Nanami Senoo, Dinesh K Chinthapalli, et al. "Functional diversity among cardiolipin binding sites on the mitochondrial ADP/ATP carrier." EMBO J. 2024 Jul;43(14):2979-3008. PMID: 38839991
- 2. Ren He, Xiaohan Li, et al. "Dexamethasone inhibits IL-8 via glycolysis and mitochondria-related pathway to regulate inflammatory pain." BMC Anesthesiol. 2023 Sep 18;23(1):317. PMID: 37723417
- 3. Fangfang Wang, Zhang Dan, et al. "ALCAM regulates multiple myeloma chemoresistant side population." Cell Death Dis. 2022 Feb 10;13(2):136. PMID:35145058
- 4. Beatriz Lapa, Ana Cristina Gon?alves, et al. "Acute myeloid leukemia sensitivity to metabolic inhibitors: glycolysis showed to be a better therapeutic target." Med Oncol. 2020 Jul 28;37(8):72. PMID:32725458
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 791.1 (Oligomycin A) 805.1 (Oligomycin B) 775.1 (Oligomycin C) |
| Cas No. | 1404-19-9 |
| Formula | C45H74O11(Oligomycin A) C45H72O12(Oligomycin B) C45H74O10(Oligomycin C) |
| Solubility | ≤30 mg/mL in ethanol; 20 mg/mL in DMSO; 30 mg/mL in dimethyl formamide |
| SDF | Download SDF |
| Canonical SMILES | O=C([C@H]([C@@H]([C@H](C([C@](C)([C@@H]([C@H](C/C=C/C=C/[C@]([H])(CC[C@@]1([C@@H]([C@]([H])(O2)[C@H]([C@@]3(O1)C(C[C@H]([C@]([H])(O3)C[C@H](C)O)C)=O)C)C)[H])CC)C)O)O)=O)C)O)C)[C@@H]([C@H]([C@@H](/C=C/C2=O)C)O)C.O=C([C@H]([C@@H]([C@H](C([C@](C)([C@@H]([C@H |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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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 |
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Reaction Conditions |
100 ng/ml oligomycin |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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Quality Control & MSDS
- View current batch:
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Purity ≥95.00% (Mixture of A, B, C)
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
Related Biological Data
