Nonactin
(Synonyms: 无活菌素; Ammonium ionophore I) 目录号 : GC12090A mixture of macrotetralide antibiotics that act as ionophores
Cas No.:6833-84-7
Sample solution is provided at 25 µL, 10mM.
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Nonactin, monactin, and dinactin mixture is a macrotetralide antibiotic.[1] This product is a mixture of the macrotetralide antibiotic homologs nonactin, monactin, and dinactin that all act as ionophores for monovalent cations.[2],[3],[4],[5],[6],[7] Nonactin is a mitochondrial membrane uncoupler and an inhibitor of adenine nucleotide translocase (ANT; IC50s = 4.4, 3.3, 4.7, and 3.3 µM for recombinant human ANT1-4, respectively).[8],[9] It selectively induces apoptosis in cancer cells and induces tumor regression in mouse xenograft models expressing mutant β-catenin over cancer cells and xenografts expressing wild-type β-catenin.8 Monactin induces swelling of rat liver mitochondria in medium containing either potassium or sodium, stimulates respiration, and uncouples oxidative phosphorylation.[10] It also inhibits Wnt signaling via inhibition of TCF-β-catenin transcriptional activity.[11] Dinactin inhibits T cell proliferation and cytokine production in vitro and reduces pulmonary eosinophilia in antigen-challenged mice.[12]
Reference:
[1]. Pampaloni, F., Mayer, B., Kabat Vel-Job, K., et al. A novel cellular spheroid-based autophagy screen applying live fluorescence microscopy identifies nonactin as a strong inducer of autophagosomal turnover. SLAS Discov. 22(5), 558-570 (2017).
[2]. Hall, J.E., and Latorre, R. Nonactin-K+ complex as a probe for membrane asymmetry. Biophys.J. 16(1), 99-103 (1976).
[3]. Browne, A., and O'Donnell, M.J. Ammonium secretion by Malpighian tubules of Drosophila melanogaster: Application of a novel ammonium-selective microelectrode. J.Exp.Biol. 216(Pt 20), 3818-3827 (2013).
[4]. Skulskii, I.A., Saris, N.-E.L., Savina, M.V., et al. Uptake of thallous ions by mitochondria is stimulated by nonactin but not by respiration alone. Eur.J.Biochem. 120(2), 263-266 (1981).
[5]. Beck, J., Gerlach, H., Prelog, V., et al. Metabolic products of actinomycetes. XXXV. Constitution of the macrotetrolides, monactin, dinactin, and trinactin. Helvetica Chimica Acta 45, 620-630 (1962).
[6]. Harold, F.M., and Baarda, J.R. Effects of nigericin and monactin on cation permeability of Streptococcus faecalis and metabolic capacities of potassium-depleted cells. J. Bacteriol. 95(3), 816-823 (1968).
[7]. Laprade, R., Grenier, F., Pagé-Dansereau, M., et al. Carrier-mediated ion transport in lipid bilayer membranes. Can. J. Biochem. Cell Biol. 62(8), 738-751 (1984).
[8]. Shikata, Y., Kiga, M., Futamura, Y., et al. Mitochondrial uncoupler exerts a synthetic lethal effect against β-catenin mutant tumor cells. Cancer Sci. 108(4), 772-784 (2017).
[9]. Zhang, Y., Tian, D., Matsuyama, H., et al. Human adenine nucleotide translocase (ANT) modulators identified by high-throughput screening of transgenic yeast. J. Biomol. Screen. 21(4), 381-390 (2016).
[10]. Graven, S.N., Lardy, H.A., and Estrada-O, S. Antibiotics as tools for metabolic studies. 8. Effect of nonactin homologs on alkali metal cation transport and rate of respiration in mitochondria. Biochem. 6(2), 365-371 (1967).
[11]. Tamai, Y., Toume, K., Arai, M.A., et al. Nonactin and related compounds found in a screening program for Wnt signal inhibitory activity. Heterocycles 84(2), 1245-1250 (2012).
[12]. Umland, S.P., Shah, H., Jakway, J.P., et al. Effects of cyclosporin A and dinactin on T-cell proliferation, interleukin-5 production, and murine pulmonary inflammation. Am. J. Respir. Cell Mol. Biol. 20(3), 481-492 (1999).
[1]. Pampaloni, F., Mayer, B., Kabat Vel-Job, K., et al. A novel cellular spheroid-based autophagy screen applying live fluorescence microscopy identifies nonactin as a strong inducer of autophagosomal turnover. SLAS Discov. 22(5), 558-570 (2017).
[2]. Hall, J.E., and Latorre, R. Nonactin-K+ complex as a probe for membrane asymmetry. Biophys.J. 16(1), 99-103 (1976).
[3]. Browne, A., and O'Donnell, M.J. Ammonium secretion by Malpighian tubules of Drosophila melanogaster: Application of a novel ammonium-selective microelectrode. J.Exp.Biol. 216(Pt 20), 3818-3827 (2013).
[4]. Skulskii, I.A., Saris, N.-E.L., Savina, M.V., et al. Uptake of thallous ions by mitochondria is stimulated by nonactin but not by respiration alone. Eur.J.Biochem. 120(2), 263-266 (1981).
[5]. Beck, J., Gerlach, H., Prelog, V., et al. Metabolic products of actinomycetes. XXXV. Constitution of the macrotetrolides, monactin, dinactin, and trinactin. Helvetica Chimica Acta 45, 620-630 (1962).
[6]. Harold, F.M., and Baarda, J.R. Effects of nigericin and monactin on cation permeability of Streptococcus faecalis and metabolic capacities of potassium-depleted cells. J. Bacteriol. 95(3), 816-823 (1968).
[7]. Laprade, R., Grenier, F., Pagé-Dansereau, M., et al. Carrier-mediated ion transport in lipid bilayer membranes. Can. J. Biochem. Cell Biol. 62(8), 738-751 (1984).
[8]. Shikata, Y., Kiga, M., Futamura, Y., et al. Mitochondrial uncoupler exerts a synthetic lethal effect against β-catenin mutant tumor cells. Cancer Sci. 108(4), 772-784 (2017).
[9]. Zhang, Y., Tian, D., Matsuyama, H., et al. Human adenine nucleotide translocase (ANT) modulators identified by high-throughput screening of transgenic yeast. J. Biomol. Screen. 21(4), 381-390 (2016).
[10]. Graven, S.N., Lardy, H.A., and Estrada-O, S. Antibiotics as tools for metabolic studies. 8. Effect of nonactin homologs on alkali metal cation transport and rate of respiration in mitochondria. Biochem. 6(2), 365-371 (1967).
[11]. Tamai, Y., Toume, K., Arai, M.A., et al. Nonactin and related compounds found in a screening program for Wnt signal inhibitory activity. Heterocycles 84(2), 1245-1250 (2012).
[12]. Umland, S.P., Shah, H., Jakway, J.P., et al. Effects of cyclosporin A and dinactin on T-cell proliferation, interleukin-5 production, and murine pulmonary inflammation. Am. J. Respir. Cell Mol. Biol. 20(3), 481-492 (1999).
| Cas No. | 6833-84-7 | SDF | |
| 别名 | 无活菌素; Ammonium ionophore I | ||
| 化学名 | (1R,2R,5R,7R,10S,11S,14S,16S,19R,20R,23R,25R,28S,29S,32S,34S)-2,5,11,14,20,23,29,32-octamethyl-4,13,22,31,37,38,39,40-octaoxapentacyclo[32.2.1.17,10.116,19.125,28]tetracontane-3,12,21,30-tetrone | ||
| Canonical SMILES | O=C([C@H](C)[C@@H]1O[C@H]2CC1)O[C@H](C)C[C@@H]3O[C@H]([C@H](C)C(O[C@@H](C)C[C@H]4O[C@@H]([C@@H](C)C(O[C@H](C)C[C@@H]5O[C@H]([C@H](C)C(O[C@@H](C)C2)=O)CC5)=O)CC4)=O)CC3 | ||
| 分子式 | C40H64O12 | 分子量 | 736.94 |
| 溶解度 | 1mg/mL in ethanol, 0.25mg/mL in DMSO, 10mg/mL in DMF | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.357 mL | 6.7848 mL | 13.5696 mL |
| 5 mM | 0.2714 mL | 1.357 mL | 2.7139 mL |
| 10 mM | 0.1357 mL | 0.6785 mL | 1.357 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet