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Nifuroxazide

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Chemical Structure| 965-52-6 同义名 : 硝呋酚酰肼
CAS号 : 965-52-6
货号 : A887401
分子式 : C12H9N3O5
纯度 : 98%
分子量 : 275.22
MDL号 : MFCD00079482
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 150 mg/mL(545.02 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • STAT1
描述 Signal transducers and activators of transcription (STATs) are a family of transcription factors essential for the pathogenesis of many cancers. STAT3 in particular has been found to be a critical mediator in the pathogenesis of many tumors. Nifuroxazide is a potent inhibitor of STAT3 through the inhibition of STAT3 tyrosine phosphorylation. Treatment of myeloma cell lines U266 or INA6 cells with nifuroxazide for 48h resulted in a dose-dependent loss of cell viability with an EC50 of approximately 4.5 μM in both cell lines[3]. In animal experiments, intraperitoneal administration of 50 mg/kg/day nifuroxazide inhibited 4T1 (the human breast cancer cell line) tumor growth, blocked formation of pulmonary metastases without detectable toxicity and decreased Ki-67, MMP-9 and increased cleaved caspase-3 expression[4]. Oral administration of nifuroxazide at 25 mg/kg/day to diabetic rats for eight weeks attenuated diabetes induced damage in renal structure, ameliorated oxidative stress, triggered antioxidant defense, educed NF-κB nuclear translocation and cleaved caspase-3 expression and down regulated the activity of apoptotic enzymes (caspase-3/caspase-8/caspase-9) in diabetic kidney[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
human U3A cells Function assay 1 h Inhibition of STAT3 expressed in human U3A cells after 1 hr by luciferase reporter gene assay, EC50=3 μM 22650325
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.63mL

0.73mL

0.36mL

18.17mL

3.63mL

1.82mL

36.33mL

7.27mL

3.63mL
参考文献

[1]Yang F, Hu M, et al. Nifuroxazide induces apoptosis and impairs pulmonary metastasis in breast cancer model. Cell Death Dis. 2015 Mar 26;6:e1701.

[2]Nelson EA, Walker SR, et al. Nifuroxazide inhibits survival of multiple myeloma cells by directly inhibiting STAT3. Blood. 2008 Dec 15;112(13):5095-102.

[3]Nelson EA, Walker SR, Kepich A, Gashin LB, Hideshima T, Ikeda H, Chauhan D, Anderson KC, Frank DA. Nifuroxazide inhibits survival of multiple myeloma cells by directly inhibiting STAT3. Blood. 2008 Dec 15;112(13):5095-102. doi: 10.1182/blood-2007-12-129718. Epub 2008 Sep 29. PMID: 18824601; PMCID: PMC2597607.

[4]Yang F, Hu M, Lei Q, Xia Y, Zhu Y, Song X, Li Y, Jie H, Liu C, Xiong Y, Zuo Z, Zeng A, Li Y, Yu L, Shen G, Wang D, Xie Y, Ye T, Wei Y. Nifuroxazide induces apoptosis and impairs pulmonary metastasis in breast cancer model. Cell Death Dis. 2015 Mar 26;6(3):e1701. doi: 10.1038/cddis.2015.63. PMID: 25811798; PMCID: PMC4385941.

[5]Elsherbiny NM, Zaitone SA, Mohammad HMF, El-Sherbiny M. Renoprotective effect of nifuroxazide in diabetes-induced nephropathy: impact on NFκB, oxidative stress, and apoptosis. Toxicol Mech Methods. 2018 Jul;28(6):467-473. doi: 10.1080/15376516.2018.1459995. Epub 2018 Apr 16. PMID: 29606028.