体外研究
(In Vitro) | HDAC-IN-37 (compound 9d) exhibits the potent antiproliferative activities on the HCT116, MDA-MB-231, K562 cell lines at IC50s of 0.50, 0.38, 0.12 μM, respectively[1].
HDAC-IN-37 (0 - 10 μM; 24 hours) significantly induces the accumulation of acetylated histones at H3K9 and H4K5 in HCT-116 cells[1].
HDAC-IN-37 (0 - 10 μM; 24 hours) induces cell apoptosis in HCT-116 cells by 35.22%, 58.34, 80.7% at 0.5, 1, 5 μM, mainly occurring in early apoptosis[1].
HDAC-IN-37 (0 - 10 μM; 6, 12, 24 hours) causes G0/G1 phase arrest of HCT-116 cells in a time-dependent manner, effectively preventing cell cycle progression[1].
HDAC-IN-37 (0, 0.1, 0.5, 1, 5 and 10 μM; 0, 6, 12, 24, 36, 48 hours) down-regulates the levels of CDK2, Cyclin D1 and the up-regulates P21 with dose- and time-dependent manners in HCT-116 cells, and decreases Bcl-2 of Bcl-2 family in dose- and time-dependent manners[1].
Cell Proliferation Assay | Cell Line: | HCT-116, MDA-MB-231, HepG2, A549, SGC7901 and K562[1] | | Concentration: | 0-10 μM | | Incubation Time: | 48 hours | | Result: | Exhibited the potent antiproliferative activities on the HCT116, MDA-MB-231, K562 cell lines at IC50of 0.50, 0.38, 0.12 μM, respectively. |
Western Blot Analysis | Cell Line: | HCT-116[1] | | Concentration: | 0, 0.1, 0.5, 1, 5 and 10 μM | | Incubation Time: | 24 hours | | Result: | Significantly induced the accumulation of acetylated histones at H3K9 and H4K5 in HCT-116 cells. |
Apoptosis Analysis | Cell Line: | HCT-116[1] | | Concentration: | 0.1, 0.5, 1, 5 and 10 μM | | Incubation Time: | 24 hours | | Result: | Induced cell apoptosis in HCT-116 cells by 35.22%, 58.34, 80.7% at 0.5, 1, 5 μM, mainly occurring in early apoptosis. |
Cell Cycle Analysis | Cell Line: | HCT-116[1] | | Concentration: | 0.1, 0.5, 1, 5 and 10 μM | | Incubation Time: | 0, 6, 12 and 24 hours | | Result: | Caused G0/G1 phase arrest of HCT-116 cells in a time-dependent manner, effectively preventing cell cycle progression. |
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