DMU-212

DMU-212 is a methylated derivative of Resveratrol ( HY-16561 ), with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2 protein. DMU-212 has orally active.

In Vitro

DMU-212 (0.3125-40 μM) inhibits growth of A375, MeWo, Bro and M5 human melanoma cells. DMU-212 (30-50 μM; 24 hours) induces upregulation of cell cycle inhibitors, apoptosis and ERK activation in A375 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: A375 cells, MeWo cells, M5 cells, Bro cells Concentration: 0.3125 μM, 0,625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM Incubation Time: 96 hours Result: Inhibited the cellular proliferation of human melanoma cells at submicromolar or micromolar concentrations (IC 50 =0.5 μM for A375 and Bro and IC 50 = 1.25 μM for MeWo and M5 cells). Cell Cycle AnalysisCell Line: A375 cells Concentration: 20 μM, 30 μM, 50 μM Incubation Time: 24 hours Result: Caused a marked increase in the levels of p21, p53 and cyclin B1 proteins with a concomitant decrease in the levels of cyclin A2. Western Blot AnalysisCell Line: A375 cells Concentration: 20 μM, 30 μM, 50 μM Incubation Time: 24 hours Result: Significant upregulated Bax, caspase 3 and caspase 9 protein levels, while decreased the levels of the anti-apoptotic protein Bcl-2. Apoptosis AnalysisCell Line: A375 cells Concentration: 10 μM, 20 μM Incubation Time: 24 hours, 36 hours Result: Induced apoptosis.

In Vivo

DMU-212 (50 mg/kg; i.g.; three times a week; for 14 days) inhibits tumor growth in xenograft model of human ovarian cancer. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-weeks-old SCID female mice (20-24 g), with ovarian cancer xenograftsDosage: 50 mg/kg Administration: Oral gavage, three times a week, for 14 days Result: Lowered tumor burden.