Nitroxoline (5-nitroquinolin-8-ol) is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections.

使用分光荧光测定法，Nitroxoline可明显减少所有受测癌症细胞株细胞外 DQ 胶原 IV 的降解。Nitroxoline 还能明显减少实时监测到的肿瘤细胞侵袭，并减少多细胞肿瘤球体的侵袭生长，这种肿瘤球体可用作肿瘤侵袭的三维玻璃体模型。在体外血管生成试验中，Nitroxoline可显著减少内皮管的形成[1]。

Nitroxoline 在LPB纤维肉瘤和MMTV-PyMT乳腺癌小鼠模型中显著抑制了肿瘤生长、血管生成和转移[1]。

In Vitro Kinase Assays : The potency of SP600125 towards kinases, including MPS1, JNK, and Aurora kinase A, is determined based on the specific measurement of radioactive phosphotransfer to the substrate. For each enzyme, the absolute Km values for ATP and the specific substrate are initially determined and each assay is then run at optimized [ATP] (2·αKm) and [substrate] (5·Km) concentrations. MPS1 activity is measured using 5 nM of MPS1 recombinant protein in 50 mM HEPES pH 7.5, 2.5 mM MgCl2, 1 mM MnCl2, 1 mM DTT, 3 μM NaVO3, 2 mM β-glycerophosphate, 0.2 mg/mL BSA, 200 μM P38-βtide substrate-peptide (KRQADEEMTGYVATRWYRAE), and 8 μM ATP with 1.5 nM 33P-γ-ATP. Ten serial 1:3 dilutions (from 30 μM to 1.5 nM) of SP600125 are tested and IC50 determined.

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. (Only for Reference)