Mitoxantrone (mitozantrone) is an inhibitor of topoisomerase II (Topo II), an inhibitor of protein kinase C (PKC) (IC50=8.5 μM). Mitoxantrone has antitumor activity for the treatment of acute myeloid leukemia, hepatocellular carcinoma, and breast cancer.

Daudi cells:0.005 μM, HaCaT cells:3.9 μM, CH1 cells:0.00265 μM, C6 cells:10.9 μg/mL, HCT116 cells:0.022 μM, A2780 cells:0.00055 μM, Cancer cells:0.75 nM, Caco-2 cells:1.4 μM, PKC:8.5 μM, Bel-7402 cells:116.6 nM, CCRF-CEM cells:0.036 μM, A549 cells:0.036 nM, MCF-7 cells:1.17 µM, A375 cells:111.5 nM, 2008 cells:7.8 nM

activity-based protein profiling (ABPP): Mouse brains are Dounce-homogenized in PBS, pH7.5, followed by a low-speed spin (1,400×, 5 min) to remove debris. The supernatant is then subjected to centrifugation (64,000×, 45 min) to provide the cytosolic fraction in the supernatant and the membrane fraction as a pellet. The pellet is washed and resuspended in PBS buffer by sonication. Total protein concentration in each fraction is determined using a protein assay kit. Samples are stored at -80 °C until use. Mouse brain membrane proteomes, are diluted to 1 mg/mL in PBS and pre-incubated with varying concentrations of inhibitors (1 nM to 10 mM) for 30 min at 37 °C before the addition of FP-rhodamine at a final concentration of 2 mM in a 50 mL total reaction volume. After 30 min at 25 °C, the reactions are quenched with 4×SDS-PAGE loading buffer, boiled for 5 min at 90 °C, subjected to SDS-PAGE and visualized in-gel using a flatbed fluorescence s

The human breast carcinoma cell lines MDA-MB-231 and MCF-7 are seeded in standard 96-well plates. One day after seeding, the culture medium is changed and replaced by medium containing different concentration of Mitoxantrone (10-5 to 5 μM) with or without DHA (30 μM) during 7 days. Viability of cells are measured as a whole by the tetrazolium salt assay[3].