Nitroxoline

Catalog No.S4591 Batch:S459102

Technical Data

Formula	C₉H₆N₂O₃
Molecular Weight	190.16	CAS No.	4008-48-4
Solubility (25°C)*	In vitro	DMSO	38 mg/mL (199.83 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Nitroxoline (8-Hydroxy-5-nitroquinoline, 5-nitroquinolin-8-ol, 5-Nitro-8-quinolinol, 5-Nitro-8-hydroxyquinoline) is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. Nitroxoline impairs tumor progression in vitro and in vivo by inhibiting cathepsin B activity.

Targets

cathepsin B ^[2]

In vitro

Nitroxoline significantly reduces extracellular DQ-collagen IV degradation by all evaluated cancer cell lines using spectrofluorimetry. Nitroxoline also markedly decreases tumor cell invasion monitored in real time and reduces the invasive growth of multicellular tumor spheroids, used as a 3D in vitromodel of tumor invasion. Endothelial tube formation is significantly reduced by nitroxoline in an in vitro angiogenesis assay^[1].

In vivo

Nitroxoline significantly abrogates tumor growth, angiogenesis and metastasis in vivo in LPB fibrosarcoma and MMTV-PyMT breast cancer mouse models^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines MCF-10A neoT, Primary MMTV-PyMT mammary carcinoma cells, Human glioma cell line U-87 MG, LPB fibrosarcoma cell line Concentrations 2.5, 5 μM Incubation Time 72 h Method cell suspension are seeded in the wells of an E-plate 16 according to the manufacturer's instructions. After seeding, the CI is monitored every 15 min. After ∼10 h (MCF-10A neoT and MMTV-PyMT), 14 h (U-87 MG) or 24 h (LPB), when the cells are in their log phase of growth, 50 μl of the compound or 0.1% DMSO is added, and the experiment allowed to run for 72 h. Once every 24 h the medium is replaced with fresh medium containing the inhibitor or suitable control to prevent cell death due to medium depletion. Compounds and their concentrations are: nitroxoline (5 μM) and CA-074 (5 μM) for all cell lines other than MCF-10A neoT cell line, where nitroxoline was used at 2.5 μM. All measurements were performed in quadruplicate.
Animal Study:^{^[1]}	Animal Models C57Bl/6 female mice Dosages 0±7 mg/kg Administration oral administration

Cell Assay:^{^[1]}

Cell lines
MCF-10A neoT, Primary MMTV-PyMT mammary carcinoma cells, Human glioma cell line U-87 MG, LPB fibrosarcoma cell line
Concentrations
2.5, 5 μM
Incubation Time
72 h
Method
cell suspension are seeded in the wells of an E-plate 16 according to the manufacturer's instructions. After seeding, the CI is monitored every 15 min. After ∼10 h (MCF-10A neoT and MMTV-PyMT), 14 h (U-87 MG) or 24 h (LPB), when the cells are in their log phase of growth, 50 μl of the compound or 0.1% DMSO is added, and the experiment allowed to run for 72 h. Once every 24 h the medium is replaced with fresh medium containing the inhibitor or suitable control to prevent cell death due to medium depletion. Compounds and their concentrations are: nitroxoline (5 μM) and CA-074 (5 μM) for all cell lines other than MCF-10A neoT cell line, where nitroxoline was used at 2.5 μM. All measurements were performed in quadruplicate.

Animal Study:^{^[1]}

Animal Models
C57Bl/6 female mice
Dosages
0±7 mg/kg
Administration
oral administration

References

Selleck's Nitroxoline has been cited by 5 publications

Melatonin alleviates chronic stress-induced hippocampal microglia pyroptosis and subsequent depression-like behaviors by inhibiting Cathepsin B/NLRP3 signaling pathway in rats [ Transl Psychiatry, 2024, 14(1):166]	PubMed: 38538614
Nitroxoline suppresses metastasis in bladder cancer via EGR1/circNDRG1/miR-520h/smad7/EMT signaling pathway [ Int J Biol Sci, 2022, 18(13):5207-5220]	PubMed: 35982887
Activity of Drug Combinations against Mycobacterium abscessus Grown in Aerobic and Hypoxic Conditions [ Microorganisms, 2022, 10(7)1421]	PubMed: 35889140
Functional Assessment of 2,177 U.S. and International Drugs Identifies the Quinoline Nitroxoline as a Potent Amoebicidal Agent against the Pathogen Balamuthia mandrillaris. [ mBio, 2018, 9(5)]	PubMed: 30377287
Repurposing the quinoline antibiotic nitroxoline to treat infections caused by the brain-eating amoeba Balamuthia mandrillaris [ bioRxiv, 2018, 10.1101/331785]	PubMed: N/A

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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