| Description | Oligomycin A (MCH 32) is a natural product, a mitochondrial F0F1-ATPase inhibitor (Ki=1 μM). Oligomycin A inhibits mitochondrial oxidative phosphorylation and induces apoptosis.Oligomycin A has antifungal activity. |
| In vitro | 方法：人黑色素瘤细胞 WM3734 用 Oligomycin A (0.01-1 µg/mL) 处理 24 h，取培养上清液中测量乳酸的产生。结果：Oligomycin A 引起 WM3734 细胞中乳酸分泌的增加。[1]方法：人肺癌细胞 H1299 用 Oligomycin A (0.1-1000 ng/mL) 处理 100 min，使用 Oxygen Biosensor System plates 检测细胞呼吸。结果：在 100 和 1000 ng/mL 时，Oligomycin A 在大约一小时内完全抑制细胞呼吸。[2] |
| In vivo | 方法：为检测抗炎活性，将 Oligomycin A (0.25 mg/kg) 腹腔注射给银屑病模型的 C57BL6 小鼠，每天一次，持续五天。结果：Oligomycin A 减少了耳朵厚度、角质形成细胞增殖和免疫细胞浸润。[3] |
| Cell experiments | ATP and Oligomycin Dose-Response Growth Measurement. Cellular ATP changes are measured by CellTiter-Glo reagent. To measure oligomycin dose-response curves, the cells are plated in 96-well plates at about 400–500 cells/well in 100 μl of culture, dosed the next day, and grown for 4 additional days followed by assaying with Cell-Titer-Glo reagent. The dose-response curves are plotted with nonlinear regression analysis of GraphPad Prism.(Only for Reference) |
| Target activity | F0F1-ATPase:1 μM(Ki) |
| Synonyms | MCH 32, 寡霉素A |
| molecular weight | 791.06 |
| Molecular formula | C45H74O11 |
| CAS | 579-13-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 10 mg/mL (12.64 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Roesch A, et al. Overcoming intrinsic multidrug resistance in melanoma by blocking the mitochondrial respiratory chain of slow-cycling JARID1B(high) cells. Cancer Cell. 2013 Jun 10;23(6):811-25. 2. Hao W, et al. Oligomycin-induced bioenergetic adaptation in cancer cells with heterogeneous bioenergetic organization. J Biol Chem. 2010 Apr 23;285(17):12647-54. 3. Franchi L, et al. Inhibiting Oxidative Phosphorylation In Vivo Restrains Th17 Effector Responses and Ameliorates Murine Colitis. J Immunol. 2017 Apr 1;198(7):2735-2746. 4. Roesch A, et al. Cancer Cell, 2013, 23(6), 811-825. |
| Citations | 1. Jiang X C, Tu F H, Wei L Y, et al. Discovery of a Novel G-Quadruplex and Histone Deacetylase (HDAC) Dual-Targeting Agent for the Treatment of Triple-Negative Breast Cancer. Journal of Medicinal Chemistry. 2022 |