Nigericin sodium salt is an antibiotic from Streptomyces hygroscopicus that works by acting as an H⁺, K⁺, and Pb²⁺ ionophore, a NLRP3 activator^[1].

Nigericin (0.1 µM) decreases inhibits proliferation and clonogenicity of H460 lung cancer cells in a dose dependent manner. Nigericin inhibits migration and invasion of H460 lung cancer cells^[1]. Nigericin (0.1-10 nM) has apparently a dual effect on cell volume, that is a shrinking effect at lower Nigericin concentrations and a swelling effect at higher concentrations. Nigericin (0.1-1 nM) significantly decreases cytosolic pH (pHi), and slightly increases the pHi at 5 and 10 nM^[2]. Nigericin 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 can selectively kill cancer stem cells in NPC in vitro. Nigericin dramatically reduces the migration ability of S18 and HONE-1 cells^[3]. Nigericin exhibits gteat toxicity for the HT29 and SW116 cell line with IC₅₀ of 12.92±0.25 μmol and 15.86±0.18 μmol. Nigericin also shows a decreased ability to form colonies under anchorage-independent conditions in a standard soft agar assay^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Ngericin (4 mg/kg, i.p.) significantly reduces tumor growth and acts synergistically with the chemotherapeutic agent DDP, as shown by the tumor volumes. Nigericin markedly decreases Bmi-1 in vivo. Overexpression of Bmi-1 partially restores CSC content and metastatic ability of NPC cells under Nigericin treatment. The downregulation of Bmi-1 may be involved in the inhibitory effect of Nigericin on CSCs in NPC^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

746.94

C₄₀H₆₇NaO₁₁

28643-80-3

尼日利亚菌素钠盐；尼日利亚菌素钠

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

In Vitro: 

Ethanol : ≥ 50 mg/mL (66.94 mM)

* “≥” means soluble, but saturation unknown.

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% EtOH    90% corn oil

  Solubility: ≥ 6.25 mg/mL (8.37 mM); Clear solution

  此方案可获得 ≥ 6.25 mg/mL (8.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。

• 2.

  请依序添加每种溶剂： 10% EtOH    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (3.35 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (3.35 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 3.

  请依序添加每种溶剂： 10% EtOH    90% (20% SBE-β-CD in saline)

  Solubility: 2.5 mg/mL (3.35 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (3.35 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

• [1]. Yakisich JS, 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

  [2]. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9

  [3]. Deng CC, et al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006

  [4]. Zhou HM, 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

For RCCs, cells (appr 2000 cells/well) are plated in 96-well cell-culture microplates and incubated over nigericinht in complete media (CM)-RPMI 1640 supplemented with 5% FBS and 2 mM l-glutamine. Cells are then exposed to the appropriate concentration of drug or vehicle for 72 h. For PPSS, cells (appr 500 cells/well) are plated in 96-well cell-culture microplates incubated over Nigericinht in CM to allow them to adhere and then maintained in serum-free media for 7-8 days and then treated with the appropriate concentration of drug or vehicle for 72 h in SFM. Cell viability for cells growing under RCCs and PPSS are evaluated by the MTT assay. The absorbance of solubilized formazan is read at 570 nm using ELISA (enzyme-linked immunosorbent assay) reader. In all cases, the highest concentration of DMSO is used in the control and this concentration is maintained below 0.001% (v/v). This DMSO concentration does not show any significant antiproliferative effect on the cell line in a short-term assay.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Mice^[3]
The S18 cells are injected near the scapula of the nude mice. Nine days after injection, the mice are randomly divided into four groups with six animals each (control, DDP, Nigericin and DDP combined with Nigericin). DDP (2.5 mg/kg) is injected intraperitoneally for five continuous days and nigericin (4 mg/kg) is administrated intraperitoneally every two days. Tumor length and width are measured with a vernier caliper every other day. Tumor volume is calculated using the formula V=0.5×(length×width²). The body weights of the mice are recorded every two days. Mice are humanely euthanized when the tumor volume reach 2000 mm³.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Yakisich JS, 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

  [2]. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9

  [3]. Deng CC, et al. Nigericin selectively targets cancer stem cells in nasopharyngeal carcinoma. Int J Biochem Cell Biol. 2013 Sep;45(9):1997-2006

  [4]. Zhou HM, 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