体外研究 (In Vitro) | Bcl-2-IN-8 (compound 4m) (48 h) shows selective cytotoxicity against MDA-MB-231, MCF-7/ADR, MCF-10A cells with IC50s of 0.51, 0.38, 3.56 μM, respectively[1]. Bcl-2-IN-8 (0-8 μM; 24, 48, 72 h) inhibits cell proliferation in a dose-time dependently[1]. Bcl-2-IN-8 (0-2 μM; 24 h) induces cell cycle arrest at G1 phase in MDA-MB-231 cells[1]. Bcl-2-IN-8 (0-2 μM; 24 h) induces apoptosis in MDA-MB-231 cells[1]. Bcl-2-IN-8 (0-3 μM; 24 h) up-regulates the expression of Bax, cytochrome c and down-regulates Bcl-2, P53 protein in a concentration dependently in MDA-MB-231 cells[1]. Bcl-2-IN-8 (0-3 μM; 24 h) decreases the ΔΨm and induces ROS (reactive oxygen species) generation by activating the p38MAPK-Akt signaling pathway in MDA-MB-231 cells[1]. Bcl-2-IN-8 (0-2 μM; 24 h) increases intracellular Ca2+concentration from 9.9 treated with DMSO to 37.4 treated at 2 μM in MDA-MB-231 cells[1]. Bcl-2-IN-8 (0-3 μM; 24 h) significantly inhibits migration in a dose-dependent manner in MDA-MB-231 cells[1]. Bcl-2-IN-8 (0-3 μM; 24 h) increases the expression levels of Smad 7 but decreases the expression levels of p-Smad 3 in MDA-MB-231 cells[1].
Cell Cytotoxicity Assay[1]. Cell Line: | MB-231, MCF-7, MCF-7/adriamycin (adriamycin-resistant MCF-7 cell line) cells | Concentration: | | Incubation Time: | 48 h | Result: | Showed potent inhibitory activities on MDA-MB-231, MCF-7, MCF-7/ADR (adriamycin) cells with IC50s of 0.51, 2.01, 0.38 μM, respectively. |
Cell Proliferation Assay[1]. Cell Line: | MDA-MB-231 cells | Concentration: | 0-8 μM | Incubation Time: | 24, 48, 72 h | Result: | Inhibited cell proliferation in a dose-time dependently. |
Cell Cycle Analysis[1]. Cell Line: | MDA-MB-231 cells | Concentration: | 0.5, 1, 2 μM | Incubation Time: | 24 h | Result: | Arrested the cell-cycle at the G1 phase and the percentage of cells in the G1 phase from 54.8 to 74.6%. |
Western Blot Analysis[1]. Cell Line: | MDA-MB-231 cells | Concentration: | 0.5, 1, 2, 3 μM | Incubation Time: | 24 h | Result: | Decreased the expression of cyclin D1, CDK4 and CDK6 protein, but did not influence the expression of c-myc proteins. |
Apoptosis Analysis[1]. Cell Line: | MDA-MB-231 cells | Concentration: | 0, 0.5, 1, 2 μM | Incubation Time: | 24 h | Result: | The total percentage of early and late apoptosis increased to 10.2%, 17.6%, 56.4% with the concentration of 0.5 μM, 1 μM, 2 μM. |
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