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DMU-212 Sale

(Synonyms: 3,4,5,4'-四甲氧基二苯乙烯) 目录号 : GC61466

DMU-212 is a methylated derivative of Resveratrol, with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities, which can induce mitotic arrest via induction of apoptosis and activation of extracellular-signal-regulated kinase1/2 (ERK1/2) protein.

DMU-212 Chemical Structure

Cas No.:134029-62-2

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10mM (in 1mL DMSO)
¥990.00
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10 mg
¥900.00
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25 mg
¥1,800.00
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50 mg
¥3,150.00
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产品描述

DMU-212 is a methylated derivative of Resveratrol, with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities, which can induce mitotic arrest via induction of apoptosis and activation of extracellular-signal-regulated kinase1/2 (ERK1/2) protein.

[1] Androutsopoulos VP, et al. Exp Dermatol. 2015 Aug;24(8):632-4.

Chemical Properties

Cas No. 134029-62-2 SDF
别名 3,4,5,4'-四甲氧基二苯乙烯
Canonical SMILES COC1=CC=C(/C=C/C2=CC(OC)=C(OC)C(OC)=C2)C=C1
分子式 C18H20O4 分子量 300.35
溶解度 DMSO: 20 mg/mL (66.59 mM) 储存条件 Store at -20°C
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1 mM 3.3294 mL 16.6472 mL 33.2945 mL
5 mM 0.6659 mL 3.3294 mL 6.6589 mL
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Research Update

DMU-212 inhibits tumor growth in xenograft model of human ovarian cancer

Biomed Pharmacother 2014 May;68(4):397-400.PMID:24768110DOI:10.1016/j.biopha.2014.02.001.

DMU-212 has been shown to evoke a mitochondrial apoptotic pathway in transformed fibroblasts and breast cancer. However, recently published data indicated the ability of DMU-212 to evoke apoptosis in both mitochondria- and receptor-mediated manner in two ovarian cancer cell lines, namely A-2780 and SKOV-3, which showed varied sensitivity to the compound tested. The pronounced cytotoxic effects of DMU-212 observed in A-2780 cells were related to the execution of extracellular apoptosis pathway and cell cycle arrest in G2/M phase. In view of the great anticancer potential of DMU-212 against A-2780 cell line, the aim of the current study was to assess antiproliferative activity of DMU-212 in xenograft model of ovarian cancer. To evaluate in vitro metabolic properties of cells that were to be injected into SCID mice, uptake and decline of DMU-212 in A-2780 ovarian cancer cell line was investigated. It was found that the concentration of the test compound in A-2780 cells was growing within first eight hours, and then the gradual decline was observed. A-2780 cells stably transfected with pcDNA3.1/Zeo(-)-Luc vector were subcutaneously inoculated into the right flanks of SCID mice. After seven days of the treatment with DMU-212 (50mg/kg b.w), tumor growth appeared to be suppressed in the animals treated with the compound tested. At day 14 of the experiment, tumor burden in mice treated with DMU-212 was significantly lower, as compared to untreated controls. Our findings suggest that DMU-212 might be considered as a potential anticancer agent used in ovarian cancer therapy.

Gene expression profiling of DMU-212-induced apoptosis and anti-angiogenesis in vascular endothelial cells

Pharm Biol 2016;54(4):660-6.PMID:26428916DOI:10.3109/13880209.2015.1071414.

Context: trans-3,4,5,4'-Tetramethoxystilbene (DMU-212), an derivative of resveratrol, shows strong antiproliferative activities against many cancer cells. In our previous study, we demonstrated that DMU-212 possesses potent proapoptosis and antiangiogenesis effects on vascular endothelial cells (VECs), which made it a promising agent for the treatment of angiogenesis-related diseases. Objective: We studied the gene expression profile of DMU-212-treated VECs to gain further insight into the mechanisms by which DMU-212 exerts its potent pro-apoptosis and antiangiogenesis effects. Materials and methods: The potential changes in the gene expression of VECs incubated with DMU-212 were identified and analyzed using the Affymetrix HG-U133 Plus 1.0 array. In addition, the gene expression profile was validated by quantitative real-time PCR (qRT-PCR) analysis for seven of those altered genes. Results and conclusion: DMU-212 was found to regulate a diverse range of genes, including cytokines (IL8, selectin E, MPZL2, EGR1, CCL20, ITGB8, CXCL1, VCAM1, KITLG, and AREG), transport proteins (TRPC4, SLC41A2, SLC17A5, and CREB5), metabolism (CYP1B1, CYP1A1, PDK4, CSNK1G1, MVK, TCEB3C, and CDKN3), enzymes (RAB23, SPHK1, CHSY3, PLAU, PLA2G4C, and MMP10), and genes involved in signal transduction (TMEM217, DUSP8, and SPRY4), chromosome organization (HIST1H2BH and GEM), cell migration and angiogenesis (ERRFI1, HBEGF, and NEDD9), and apoptosis (TNFSF15, TNFRSF9, CD274, BCL2L11, BIRC3, TNFAIP3, and TIFA), as well as other genes with unknown function (PGM5P2, SNORD1142, LOC151760, KRTAP5-2, C1orf110, SNORA14A, MIR31, C2CD4B, SCARNA4, C2orf66, SC4MOL, LOC644714, and LOC283392). This is the first application of microarray technique to investigate and analyze the profile of genes regulated by DMU-212 in VECs. Our results lead to an increased understanding of the signaling pathways involved in DMU-212-induced apoptosis and antiangiogenesis.

Effect of resveratrol analogue, DMU-212, on antioxidant status and apoptosis-related genes in rat model of hepatocarcinogenesis

Hum Exp Toxicol 2017 Feb;36(2):160-175.PMID:27048571DOI:10.1177/0960327116641734.

The aim of the study was to examine whether antioxidant properties of 3,4,4',5-tetramethoxystilbene (DMU-212) contribute to its anticarcinogenic activity and whether DMU-212 affects the expression of apoptosis-related genes. Two-stage model of hepatocarcinogenesis was used; male Wistar rats were challenged with N-nitrosodiethylamine (NDEA), 200 mg/kg body weight (b.w.), intraperitoneal, then phenobarbital (PB) in drinking water (0.05%) was administered. Simultaneously, DMU-212 was given per os at a dose 20 or 50 mg/kg b.w. two times a week for 16 weeks. DMU-212 caused a moderate decrease in hepatic thiobarbituric acid reactive substances and protein carbonyls concentration elevated in rats treated with NDEA/PB. The activity of antioxidant enzymes examined reduced by NDEA/PB treatment was not restored in rats coadministered with DMU-212. Effects of DMU-212 on messenger RNA (mRNA) expression of antioxidant enzymes in rats challenged with NDEA/PB were diversified; no changes in their protein expression were noted in any of the groups. The expression of 17,000 genes was analyzed by Affymetrix® Rat Gene 1.1 ST Array; 15 apoptosis-related genes were selected and validated by RT-q PCR. The combined treatment with NDEA/PB and DMU-212 increased the mRNA level of some genes driving mitochondria-mediated apoptosis, whereas the mRNA expression of some anti-apoptotic genes triggering receptor-mediated apoptosis was reduced. The expression of genes encoding caspases-4, -8, -9, and -12 was also increased in rats treated with DMU-212. Although antioxidant effect of DMU-212 in rats challenged with NDEA/PB was moderate, its potential anticarcinogenic properties were demonstrated as evidenced by modulation of apoptosis-related genes.

The Effect of 3'-Hydroxy-3,4,5,4'-Tetramethoxy -stilbene, the Metabolite of the Resveratrol Analogue DMU-212, on the Motility and Proliferation of Ovarian Cancer Cells

Int J Mol Sci 2020 Feb 7;21(3):1100.PMID:32046103DOI:10.3390/ijms21031100.

Targeting tumor cell motility and proliferation is an extremely important challenge in the prevention of metastasis and improving the effectiveness of cancer treatment. We recently published data revealing that DMU-214, the metabolite of firmly cytotoxic resveratrol analogue DMU-212, exerted significantly higher biological activity than the parent compound in ovarian cancer cells. The aim of the present study was to assess the molecular mechanism of the potential anti-migration and anti-proliferative effect of DMU-214 in ovarian cancer cell line SKOV-3. We showed that DMU-214 reduced the migratory capacity of SKOV-3 cells. The microarray analysis indicated ontology groups of genes involved in processes of negative regulation of cell motility and proliferation. Furthermore, we found DMU-214 triggered changes in expression of several migration- and proliferation-related genes (SMAD7, THBS1, IGFBP3, KLF4, Il6, ILA, SOX4, IL15, SRF, RGCC, GPR56) and proteins (GPR56, RGCC, SRF, SMAD7, THBS1), which have been shown to interact to each other to reduce cell proliferation and motility. Our study showed for the first time that DMU-214 displayed anti-migratory and anti-proliferative activity in SKOV-3 ovarian cancer cells. On the basis of whole transcriptome analysis of these cells, we provide new insight into the role of DMU-214 in inhibition of processes related to metastasis.

Heteroaromatic analogs of the resveratrol analog DMU-212 as potent anti-cancer agents

Bioorg Med Chem Lett 2015 Jul 15;25(14):2763-7.PMID:26022840DOI:10.1016/j.bmcl.2015.05.019.

Heteroaromatic analogs of DMU-212 (8-15) have been synthesized and evaluated for their anti-cancer activity against a panel of 60 human cancer cell lines. These novel analogs contain a trans-3,4,5-trimethoxystyryl moiety attached to the C2 position of indole, benzofuran, benzothiazole or benzothiophene ring (8, 11, 13 and 14, respectively) and showed potent growth inhibition in 85% of the cancer cell lines examined, with GI50 values <1 μM. Interestingly, trans-3,4- and trans-3,5-dimethoxystyryl DMU-212 analogs 9, 10, 12 and 15 exhibited significantly less growth inhibition than their 3,4,5-trimethoxystyryl counterparts, suggesting that the trans-3,4,5-trimethoxystyryl moiety is an essential structural element for the potent anti-cancer activity of these heterocyclic DMU-212 analogs. Molecular modeling studies showed that the four most active compounds (8, 11, 13 and 14) all bind to the colchicine binding site on tubulin, and that their binding modes are similar to that of DMU-212.