体外研究
(In Vitro) | HDAC-IN-9 (compound 4s) shows anti-proliferative activity (IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, 0.371 μM for MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells, respectively)[1].
HDAC-IN-9 displays 6.1, 3.2 and 4.6-fold selectivity ratios for 293 T, macrophages, and L02 cells respectively (IC50s of 10.89, 5.63, 8.14 μM for 293 T, macrophages, and L02 cells, respectively)[1].
HDAC-IN-9 shows inhibition activities against HDAC isoforms (IC50s of 6.8, 0.06, 0.12, 8.5 μM for HDAC 1, HDAC 2, HDAC 6, HDAC 10, respectively)[1].
HDAC-IN-9 (1, 2, 4 μM; 72 h; A459 cells) induces cell cycle arrest at the G2/M phase in a concentration-dependent manner[1].
HDAC-IN-9 (1, 2, 4 μM; 72 h) induces apoptosis via a Caspase-dependent intrinsic mitochondrial-mediated pathway in A549 cells[1].
HDAC-IN-9 (0, 0.5, 1, 2 μM; 48 h) shows anti-proliferative activity by the inhibition of angiogenesis and the reduction of endothelial cell metastasis in A549 cells[1].
HDAC-IN-9 (0, 1, 2, 4 μM, 48 h) inhibits the invasion and migration of A549 cells[1].
Cell Proliferation Assay[1] | Cell Line: | MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells | | Concentration: | | | Incubation Time: | 72 h | | Result: | Showed anti-proliferative activity (IC50s of 1.821, 2.538, 4.84, 1.782, 2.525, 0.371 μM for MCF-7, MGC-803, HeLa, A549, HepG2, U937 cells, respectively). |
Cell Cycle Analysis[1] | Cell Line: | A459 cells | | Concentration: | 0, 1, 2, 4 μM | | Incubation Time: | 72 h | | Result: | Cells were arrested at the G2/M phase with a dose-dependent manner. |
Apoptosis Analysis[1] | Cell Line: | A459 cells | | Concentration: | 0, 1, 2, 4 μM | | Incubation Time: | 72 h | | Result: | Induced apoptosis via a Caspase-dependent intrinsic mitochondrial-mediated pathway in A549 cells. |
Western Blot Analysis[1] | Cell Line: | A459 cells | | Concentration: | 0, 1, 2, 4 μM | | Incubation Time: | 72 h | | Result: | Showed down regulation of Cyclin B1 and Pcdc2 levels. |
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体内研究
(In Vivo) | HDAC-IN-9 (0, 10, 20, 40 μM) suppresses the formation of intersegmental blood vessels (ISVs) in zebrafish embryos[1].
HDAC-IN-9 (0, 2.5, 5, 10 μM; 3 days) inhibits the proliferation and metastasis of A549 cells in zebrafish xenograft models[1].
| Animal Model: | embryos of Tg(flk:EGFP) transgenic zebrafish (transgenic zebrafish model Tg(flk1:EGFP))[1] | | Dosage: | 0, 10, 20, 40 μM | | Administration: | | | Result: | Suppressed the formation of ISVs in zebrafish embryos. |
| Animal Model: | zebrafish xenograft models[1] | | Dosage: | 0, 2.5, 5, 10 μM | | Administration: | 3 days | | Result: | Inhibited the proliferation and metastasis of A549 cells in zebrafish xenograft models. |
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