Oligomycin Complex |
Catalog No.GC16533
One-Click Copy Product Info
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Oligomycin complex consiste en una mezcla de oligomicinas A, B, y C.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1404-19-9
Sample solution is provided at 25 µL, 10mM.
Oligomycin complex consiste en una mezcla de oligomicinas A, B, y C. Oligomycin es una clase de antibióticos macrólidos similares de 26 miembros aislados de Streptomyces amylase chromogenes. Oligomycin tiene actividad antifúngica, inhibición de la fosforilación oxidativa y actividad insecticida[1]. Oligomycin A ejerce principalmente su efecto inhibidor sobre la fosforilación oxidativa mitocondrial al bloquear el canal de protones (subunidad F0) de la ATP sintasa, inhibiendo así la síntesis de ATP. Además, reduce el aumento compensatorio de la fosforilación oxidativa en las células tumorales, lo que lleva a una disminución en los niveles de glucólisis celular[2-4].Oligomycin B actúa como un inhibidor no selectivo de las ATP sintasas, ralentizando efectivamente el agotamiento de ATP en casos de isquemia miocárdica. Oligomycin C es un inhibidor de la mitocondrial F1F0-ATP sintasa, que induce una muerte celular más sensible y cambia el patrón de muerte celular de apoptosis a necrosis.
Oligomycin(0-50µg/ml; 24h) indujo la despolarización de la membrana mitocondrial y la liberación del citocromo c en las células HepG2 y R-HepG2[5]. Oligomycin A(0-16 µM;12-48 h) proueve la supervivencia y proliferación de las células HT29[6]. En las células A549, 100 ng/ml de Oligomycin podría inhibir completamente la actividad de fosforilación de OXPHOS en 1 hora y estimular varios niveles de ganancias de glucólisis[7]. 5 µg/ml Oligomycin podría inhibir la parte F0 de H+-ATP-synthase, y suprimir fuertemente la liberación del citocromo c y la apoptosis en las células Hela inducidas por TNF[8]. Oligomycin B(1 µM) indujo vasodilataciones que fueron un 39-61% más pequeñas en el receptor de sulfonilurea 2 nulo (SUR2(nl)) que en las arterias de tipo salvaje SUR2 (SUR2(wt)) [9].
References:
[1]. SMITH RM, PETERSON WH, et,al.Oligomycin, a new antifungal antibiotic. Antibiot Chemother (Northfield). 1954 Sep;4(9):962-70. PMID: 24543225.
[2]. Vestergaard M, NØhr-Meldgaard K, et al. Inhibition of the ATP synthase eliminates the intrinsic resistance of Staphylococcus aureustowards polymyxins[J].mBio, 2017, 8(5): e01114-17.
[3]. Untereiner AA, Pavlidou A, et al. Drug resistance induces the upregulation of H2S-producing enzymes in HCT116 colon cancer cells[J].Biochem Pharmacol, 2018, 149: 174-185.
[4]. Ruas JS, Siqueira-Santos ES, et al. High glycolytic activity of tumor cells leads to underestimation of electron transport system capacity when mitochondrial ATP synthase is inhibited[J].Sci Rep, 2018, 8(1): 17383.
[5]. Li YC, Fung KP, et,al. Mitochondria-targeting drug oligomycin blocked P-glycoprotein activity and triggered apoptosis in doxorubicin-resistant HepG2 cells. Chemotherapy. 2004 Jun;50(2):55-62. doi: 10.1159/000077803. PMID: 15211078.
[6]. Li X, Tian R, et,al. Oligomycin A promotes radioresistance in HT29 colorectal cancer cells and its mechanisms. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2021 Feb 28;46(2):113-120. English, Chinese. doi: 10.11817/j.issn.1672-7347.2021.200063. PMID: 33678646.
[7]. Hao W, Chang CP, et al. Oligomycin-induced bioenergetic adaptation in cancer cells with heterogeneous bioenergetic organization. J Biol Chem. 2010 Apr 23;285(17):12647-54. doi: 10.1074/jbc.M109.084194. Epub 2010 Jan 28. PMID: 20110356; PMCID: PMC2857128.
[8]. Shchepina LA, Pletjushkina OY, et al. Oligomycin, inhibitor of the F0 part of H+-ATP-synthase, suppresses the TNF-induced apoptosis. Oncogene. 2002 Nov 21;21(53):8149-57. doi: 10.1038/sj.onc.1206053. PMID: 12444550.
[9]. Adebiyi A, McNally EM, et al. Vasodilation induced by oxygen/glucose deprivation is attenuated in cerebral arteries of SUR2 null mice. Am J Physiol Heart Circ Physiol. 2011 Oct;301(4):H1360-8. doi: 10.1152/ajpheart.00406.2011. Epub 2011 Jul 22. PMID: 21784985; PMCID: PMC3197357.
| Experimentos celulares [1]: | |
Líneas celulares | Células R-HepG2 y HepG2 |
Método de preparación | Las células se trataron con oligomycin a la concentración indicada o solo en el medio a 37°C, 5% de CO2 durante 24 h. |
Condiciones de reacción | 0-50μg/ml; 24h |
Áreas de aplicación | Oligomycin indujo la despolarización mitocondrial en las células R-HepG2 y HepG2. |
| Experimentos con animales [2]: | |
Modelos animales | Células HT29 |
Método de preparación | Las células se cultivaron con diferentes concentraciones de oligomycin A durante 12,24,36 y 48 h. |
Forma de dosificación | 0-16 μM;12-48 h |
Áreas de aplicación | Oligomycin promueve la supervivencia y proliferación de las células HT29. |
References: [1]. Li YC, Fung KP, et,al. Mitochondria-targeting drug oligomycin blocked P-glycoprotein activity and triggered apoptosis in doxorubicin-resistant HepG2 cells. Chemotherapy. 2004 Jun;50(2):55-62. doi: 10.1159/000077803. PMID: 15211078. [2]. Li X, Tian R, et,al. Oligomycin A promotes radioresistance in HT29 colorectal cancer cells and its mechanisms. Zhong Nan Da Xue Xue Bao Yi Xue Ban. 2021 Feb 28;46(2):113-120. English, Chinese. doi: 10.11817/j.issn.1672-7347.2021.200063. PMID: 33678646. | |
| Cas No. | 1404-19-9 | 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 | ||
| Formula | C45H74O11 for Oligomycin A; C45H72O12 for Oligomycin B; C45H74O10 for Oligomycin C. | M.Wt | 791.06 for Oligomycin A; 805.1 for Oligomycin B; 775.1 for Oligomycin C. |
| Solubility | ≤30mg/ml in ethanol;20mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.2641 mL | 6.3206 mL | 12.6413 mL |
| 5 mM | 252.8 μL | 1.2641 mL | 2.5283 mL |
| 10 mM | 126.4 μL | 632.1 μL | 1.2641 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)