Nitroxoline

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Chemical Structure| 4008-48-4 同义名 : 5-硝基-8-羟基喹啉 ;8-Hydroxy-5-nitroquinoline;5-Nitro-8-quinolinol;Nitroxoline, 5-nitrox, 5-NOK, Cysto-saar plus, Nibiol;5-Nitro-8-hydroxyquinoline;5-nitroquinolin-8-ol
CAS号 : 4008-48-4
货号 : A193247
分子式 : C9H6N2O3
纯度 : 98%
分子量 : 190.155
MDL号 : MFCD00006791
存储条件:

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(262.94 mM),配合低频超声助溶,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
描述 Nitroxoline is an antibiotic that has proven to be very effective at combating biofilm infections. Nitroxoline is currently repurposed for the treatment of urinary tract infection, which active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infection. Nitroxoline showed a broad antimicrobial spectrum, with inhibition zone diameters and MICs of nitroxoline well below the EUCAST breakpoint for E. coli for most organisms (≤16mg/ml). Nitroxoline is active against the bacteria E. coli, S. aureus, E. faecalis, K. pneumoniae, and P. mirabilis in vitro (MIC90s = 4, 4, 8, 8, and 8 mg/L, respectively)[3]. Nitroxoline inhibits the growth of human U87 and U251 glioma, A549 lung, and PC3 prostate cancer cells (IC50s = 50, 6, 38, and 23 μg/ml, respectively)[4]. In vivo, it reduces tumor growth in a PTEN- and KRAS-driven glioma mouse model when administered at a dose of 80 mg/kg per day. Nitroxoline also inhibits the interaction between the first bromodomain of bromodomain-containing protein 4 (BRD4) with acetylated histone H4 with an IC50 value of 0.98 μM[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.26mL

1.05mL

0.53mL

26.29mL

5.26mL

2.63mL

52.59mL

10.52mL

5.26mL

参考文献

[1]Mirković B, Markelc B, et al. Nitroxoline impairs tumor progression in vitro and in vivo by regulating cathepsin B activity. Oncotarget. 2015 Aug 7;6(22):19027-42.

[2]Mirković B, Renko M, et al. Novel mechanism of cathepsin B inhibition by antibiotic nitroxoline and related compounds. ChemMedChem. 2011 Aug 1;6(8):1351-6.

[3] Sobke A, Makarewicz O, Baier M, et al. Empirical treatment of lower urinary tract infections in the face of spreading multidrug resistance: in vitro study on the effectiveness of nitroxoline. Int J Antimicrob Agents. 2018;51(2):213-220.

[4]Lazovic J, Guo L, Nakashima J, Mirsadraei L, Yong W, Kim HJ, Ellingson B, Wu H, Pope WB. Nitroxoline induces apoptosis and slows glioma growth in vivo. Neuro Oncol. 2015 Jan;17(1):53-62.

[5]Jiang, H., Xing, J., Wang, C., et al. Discovery of novel BET inhibitors by drug repurposing of nitroxoline and its analogues. Org. Biomol. Chem. 2017; 15(44), 9352-9361.