Nigericin sodium salt
(Synonyms: 尼日利亚菌素钠盐) 目录号 : GC15811
尼杆菌素钠盐是一种来自湿地链霉菌的电中性K+/H+离子载体，它是一种亲脂性抗生素，可以选择性地导致钾从线粒体膜中流失。
Cas No.:28643-80-3
Sample solution is provided at 25 µL, 10mM.
Nigericin sodium salt is an electrically neutral K +/H + ionophore from Streptomyctus hygroscopicus an antibiotic that is lipophilic and selectively causes potassium to drain from the mitochondrial membrane[8,9]. Nigericin sodium salt is a NLRP3 activator[1].
Nigericin sodium salt inhibited the migration and invasion of H460 lung cancer cells[1]. Nigericin sodium salt (0.1-10 nM) has apparently a dual effect on cell volume, that is a shrinking effect at lower Nigericin sodium salt concentrations and a swelling effect at higher concentrations[2].Nigericin sodium salt exhibits higher toxicity on S18 cells than S26 cells, with IC50 of 2.03±0.55 μM and 4.77±2.35 μM, respectively. Nigericin sodium salt dramatically reduces the migration ability of S18 and HONE-1 cells[3]. Nigericin sodium salt exhibits toxicity for the HT29 and SW116 cell line with IC50 of 12.92±0.25 μmol and 15.86±0.18 μmol. Nigericin sodium salt also shows a decreased ability to form colonies under anchorage-independent conditions in a standard soft agar assay[4].Using a combination of live-cell imaging and biochemical approaches, prototypical NLRP3 stimuli, the potassium ionophore nigericin, or millimolar concentrations of ATP exert both NLRP3-independent and -dependent effects on macrophages that result in cytokine release and cell death[5].Treatment of MN9D cells with Nigericin sodium salt led to an increase of LC3-II and p62 levels with concomitant activation of caspase. Ultrastructural examination revealed accumulation of autophagic vacuoles and swollen vacuoles in nigericin-treated cells[7].
In mice, Ngericin significantly reduces tumor growth. Nigericin sodium salt markedly decreases Bmi-1 in vivo. Overexpression of Bmi-1 partially restores CSC content and metastatic ability of NPC cells under Nigericin sodium salt treatment. The downregulation of Bmi-1 may be involved in the inhibitory effect of Nigericin sodium salt on CSCs in NPC[3].Nigericin sodium salt exerts anticancer effects on human osteosarcoma cancer cells by directly targeting STAT3. Nigericin sodium salt can significantly inhibit tumor migration and invasion. Nigericin sodium salt inhibits tumor growth in a mouse osteosarcoma model[6].
References:
[1]: Yakisich JS, Azad N, et,al. Nigericin decreases the viability of multidrug-resistant cancer cells and lung tumorspheres and potentiates the effects of cardiac glycosides. Tumour Biol. 2017 Mar;39(3):1010428317694310. doi: 10.1177/1010428317694310. PMID: 28351327.
[2]: Bissinger R, Malik A, et,al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9. doi: 10.1111/bcpt.12503. Epub 2015 Nov 13. PMID: 26458067.
[3]: Deng CC, Liang Y, et,al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006. doi: 10.1016/j.biocel.2013.06.023. Epub 2013 Jul 4. PMID: 23831840.
[4]: Zhou HM, Dong TT, et,al. Suppression of colorectal cancer metastasis by nigericin through inhibition of epithelial-mesenchymal transition. World J Gastroenterol. 2012 Jun 7;18(21):2640-8. doi: 10.3748/wjg.v18.i21.2640. PMID: 22690072; PMCID: PMC3370000.
[5]: Heid ME, Keyel PA, et,al. Mitochondrial reactive oxygen species induces NLRP3-dependent lysosomal damage and inflammasome activation. J Immunol. 2013 Nov 15;191(10):5230-8. doi: 10.4049/jimmunol.1301490. Epub 2013 Oct 2. PMID: 24089192; PMCID: PMC3833073.
[6]: Yang Z, Xie J, et,al. Nigericin exerts anticancer effects through inhibition of the SRC/STAT3/BCL-2 in osteosarcoma. Biochem Pharmacol. 2022 Apr;198:114938. doi: 10.1016/j.bcp.2022.114938. Epub 2022 Jan 31. PMID: 35114189.
[7]: Lim J, Lee Y, et,al. Nigericin-induced impairment of autophagic flux in neuronal cells is inhibited by overexpression of Bak. J Biol Chem. 2012 Jul 6;287(28):23271-82. doi: 10.1074/jbc.M112.364281. Epub 2012 Apr 5. PMID: 22493436; PMCID: PMC3390606.
[8]: Fruth IA, Arrizabalaga G. Toxoplasma gondii: induction of egress by the potassium ionophore nigericin. Int J Parasitol. 2007 Dec;37(14):1559-67. doi: 10.1016/j.ijpara.2007.05.010. Epub 2007 Jun 9. PMID: 17618633; PMCID: PMC2221775.
[9]:Kucejova B, Kucej M, et,al. A screen for nigericin-resistant yeast mutants revealed genes controlling mitochondrial volume and mitochondrial cation homeostasis. Genetics. 2005 Oct;171(2):517-26. doi: 10.1534/genetics.105.046540. Epub 2005 Jul 14. PMID: 16020778; PMCID: PMC1456768.
尼杆菌素钠盐是一种来自湿地链霉菌的电中性K+/H+离子载体,它是一种亲脂性抗生素,可以选择性地导致钾从线粒体膜中流失[8,9]。尼杆菌素钠盐是NLRP3激活剂[1]。
Nigericin钠盐抑制了H460肺癌细胞的迁移和侵袭[1]。在较低浓度下（0.1-10 nM）,Nigericin钠盐似乎对细胞体积有收缩作用,而在较高浓度下则具有膨胀作用[2]。 Nigericin钠盐对S18细胞的毒性比对S26细胞更高,IC50分别为2.03±0.55μM和4.77±2.35μM。 Nigericin钠盐显著降低了S18和HONE-1细胞的迁移能力[3]。 Nigericin钠盐对HT29和SW116细胞系表现出毒性,IC50分别为12.92±0.25 μmol 和15.86±0.18 μmol。 Nigericin钠盐还显示出在标准软琼脂糖酸试验中,在无锚定条件下形成集落的能力降低[4]。使用活体显微镜成像和生化方法相结合,原型NLRP3刺激物—— 钾离子载体nigericin或ATP 的毫摩尔浓度都会产生 NLRP3非依赖性和依赖性效应,并导致巨噬细胞释放细胞因子和死亡[5]。将MN9D细胞处理Nigericin钠盐后,LC3-II和p62水平增加,并伴随着caspase的激活。超微结构检查显示nigericin处理的细胞中有自噬泡和肿大的空泡积累[7]。
在小鼠中,Nigericin显著减少肿瘤生长。Nigericin钠盐明显降低体内的Bmi-1水平。在Nigericin钠盐治疗下,Bmi-1的过度表达部分恢复了NPC细胞的CSC含量和转移能力。Bmi-1的下调可能参与了Nigericin钠盐对NPC CSCs的抑制作用。[3] Nigericin钠盐通过直接靶向STAT3,在人类骨肉瘤癌细胞上发挥抗癌作用。 Nigericin钠盐可以显著抑制肿瘤迁移和侵袭,并且在小鼠骨肉瘤模型中抑制肿瘤生长。[6]
| Cell experiment [1]: | |
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Cell lines |
H460 cells |
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Preparation Method |
Migration and invasion assays were performed using cells serum-starved overnight. For migration assays, H-460 cells were seeded in Transwell inserts in RPMI 1640 with or without drugs or Nigericin sodium salt(1 uM). Inserts were placed in plates with RPMI 1640 containing 10% FBS in the presence of DMSO, or Nigericin sodium salt (1 uM). After 24 h, cell migration was quantified. |
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Reaction Conditions |
1 µM Nigericin sodium salt for 24h |
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Applications |
Nigericin sodium salt inhibited the migration and invasion of H460 lung cancer cells. |
| Animal experiment [2]: | |
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Animal models |
Nude mice(S18 cells were injected near the scapula of the nude mice) |
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Preparation Method |
The mice were randomly divided into four groups with six animals each. DDP (2.5 mg/kg) was injected intraperitoneally for five continuous days and Nigericin sodium salt (4 mg/kg) was administrated intraperitoneally every two days. |
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Dosage form |
4 mg/kg Nigericin sodium salt every two days. |
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Applications |
Nigericin sodium salt significantly reduced tumor growth. |
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References: [1]. Yakisich JS, Azad N, et,al. Nigericin decreases the viability of multidrug-resistant cancer cells and lung tumorspheres and potentiates the effects of cardiac glycosides. Tumour Biol. 2017 Mar;39(3):1010428317694310. doi: 10.1177/1010428317694310. PMID: 28351327. [2]. Deng CC, Liang Y, et,al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006. doi: 10.1016/j.biocel.2013.06.023. Epub 2013 Jul 4. PMID: 23831840. |
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| Cas No. | 28643-80-3 | SDF | |
| 别名 | 尼日利亚菌素钠盐 | ||
| 分子式 | C40H67NaO11 | 分子量 | 746.94 |
| 溶解度 | 25mg/mL in EtOH | 储存条件 | Store 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 | 1.3388 mL | 6.694 mL | 13.388 mL |
| 5 mM | 0.2678 mL | 1.3388 mL | 2.6776 mL |
| 10 mM | 0.1339 mL | 0.6694 mL | 1.3388 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Treatment of A549 and MCF-7 cells with high K+ buffer of 10.0 μM nigericin(GlpBio) for 30 min resulted in pHi calibration, and a red signal was detected that continually enhanced with the decreasing pHi.
Acta Biomaterialia (2022). PMID: 36087865 IF: 10.6335 -
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Confocal fluorescence microscopic images of Hela cells stained with Hcy-Rh (10 μM in PBS, 60 min, 37 °C) and BODIPY (10 nM in PBS,10 min, 37 °C) upon further incubation with buffers containing high concentrations of K+ at different pH values.
Then, cells were further incubated with high-K+ buffers (30 mM NaCl, 120 mM KCl, 1 mM CaCl2, 0.5 mM MgSO4, 1 mM NaH2PO4, 5 mM glucose, 20 mM HEPES, and 20 mM NaOAc) of pH 6.0, 7.5,and 8.5 in the presence of 10.0 μM nigericin(GlpBio) for 20 min at 37 °C.
Analytical Chemistry (2022). PMID: 34989555 IF: 6.983 -
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NLRP3 activation reversed the anti-pyroptosis effect of MRS2211 after gp120 treatment in PC12 cells. (B)After the combination of MRS2211 and nigericin, the NLRP3 expression was significantly higher than that in MRS2211- treated gp120 group, but significantly lower than that in nigericin treated group.
MRS2211(10 μmol/L) or/and nigericin (20 μmol/L, GLPBIO) were added to the medium for 30–45 min, respectively.
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Related Biological Data
LNP/miR-22 suppresses hippocampal pyroptosis through NLRP3 in mice with I/R injury. The hippocampus pyroptosis was analyzed using double immunofluorescent stained with caspase-1 and TUNEL.
In the I/R+LNP/miR-22+Nigericin group, mice were administered both LNP/miR-22 through intraventricular stereotactic injection and NLRP3 activator Nigericin sodium salt(4 mg/kg, GLPBIO) intraperitoneally.
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Related Biological Data
Effect of Vitamin K on Pyroptosis in THP-1 Cells.(E–G) The LDH activity was measured in the supernatant. LPS plus nigericin (Nig) treatment was used to induce pyroptosis in THP-1 cells after 1 h pretreatment with Vitamin K1, K2 and K3.
Briefly, 1 × 10^6/mL cells were cultured with RPMI 1640 medium containing 2% FBS overnight and then treated with 1 µg/mL LPS for 3 h, followed by 8 µg/mL Nigericin(GlpBio) treatment for 1 h.
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