体外研究
(In Vitro) | DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has an inhibitory activity of DNMT3A with an IC50value of 0.39 μM, which increases linearly with DNA concentration (IDT-01)[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has inhibitory activity against DNMT1, DNMT3B and G9a with IC50values of 13.0 μM, 105 μM and ＞500 μM, respectively[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) has cell viability in cancer cells with IC50values of 0.7 μM, 0.3 μM, 0.7 μM, 0.5 μM, 2.1 μM, 1.7 μM and 91 μM for THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell, respectively[1].
DY-46-2 (0.1-100 μM, 24, 48 and 72 h) markedly inhibits the proliferation of cancer cells and shows low cytotoxicity in peripheral blood mononuclear cells (PBMCs)[1].
DY-46-2 (1 μM, 72 h) obviously decreases DNMT3A protein levels, as well as reactive expression of a silenced TSG (p53) in HCT116 cells[1].
Cell Viability Assay[1] | Cell Line: | THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell | | Concentration: | 0.1-100 μM | | Incubation Time: | 24, 48 and 72 h | | Result: | Had remarkable inhibitory potency in the dose- and time-dependent manners and no cytotoxicity in non-tumoral PBMCs (IC50>100 μM). |
Cell Proliferation Assay[1] | Cell Line: | THP-1, HCT116, U937, K562, A549, DU145 and PBMC cell | | Concentration: | 0.1-100 μM | | Incubation Time: | 24, 48 and 72 h | | Result: | Exhibited high anti-proliferative activity with a micromolar range cytotoxicity in all cancer cells. |
Western Blot Analysis[1] | Cell Line: | HCT116 cells | | Concentration: | 1 μM | | Incubation Time: | 72 h | | Result: | Decreased DNMT3A and p53 protein levels in the HCT116 cells, apparently sufficient to reactive expression of a silenced TSG (p53). |
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