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编 号:F755802
分子式:C23H24ClN7O
分子量:449.94
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生物活性:
HDAC-IN-37 is a potent HDAC inhibitor with IC50s of 0.0551 μM, 1.24 μM, 0.948 μM and 34.2 μM for HDAC1, HDAC3, HDAC8 and HDAC6, respectively. HDAC-IN-37 induces histone acetylation in a slow-off manner. HDAC-IN-37 prevents cell transition from G1 phase to S phase and induces early cell apoptosis.

体外研究:
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.HDAC-IN-37 (0 - 10 μM; 24 hours) significantly induces the accumulation of acetylated histones at H3K9 and H4K5 in HCT-116 cells.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.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.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.
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