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 oral bioavailability[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> MAPK/ERK Pathway >> ERK

Signaling Pathways >> Stem Cell/Wnt >> ERK

DMU-212 (0.3125-40 μM) inhibits growth of A375, MeWo, Bro and M5 cells human melanoma cells[1]. DMU-212 (30-50 μM; 24 hours) induces upregulation of cell cycle inhibitors, apoptosis and ERK activation in A375 cells[1]. DMU-212 induces upregulation of cell cycle inhibitors, apoptosis and ERK activation in A375 cells[1]. DMU-212 induces G2/M arrest and apoptosis in cancer cells[1]. DMU-212 induces mitotic arrest, apoptosis and activation of ERK1/2 protein[1]. Cell Proliferation Assay[1] Cell 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 (IC50=0.5 μM for A375 and Bro and IC50= 1.25 μM for MeWo and M5 cells). Cell Cycle Analysis[1] Cell 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 Analysis[1] Cell Line: A375 cells Concentration: 20 μM, 30 μM, 50 μM Incubation Time: 24 hours Result: Significant upregulation of Bax, caspase 3 and caspase 9 protein levels, while the levels of the anti-apoptotic protein Bcl-2 were decreased.

DMU-212 (50 mg/kg; i.g.; three times a week; for 14 days) inhibits tumor growth in xenograft model of human ovarian cancer[2]. Animal Model: 6-weeks-old SCID female mice (20-24 g), with ovarian cancer xenografts[2] Dosage: 50 mg/kg Administration: Oral gavage, three times a week, for 14 days Result: Lower tumor burden.

[1]. Vasilis Pericles Androutsopoulos, et al. Activation of ERK1/2 is required for the antimitotic activity of the resveratrol analogue 3,4,5,4'-tetramethoxystilbene (DMU-212) in human melanoma cells. Exp Dermatol. 2015 Aug;24(8):632-4.

[2]. Hanna Piotrowska, et al. DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer. Biomed Pharmacother. 2014 May;68(4):397-400.