Abstract: Objective To investigate the effect of histone acetylation enzyme inhibitor（BML-210） on the proliferation， apoptosis and cell cycle of glioma U251 cells. Methods U251 cells were treated with 0， 5， 10 and 20 μmol／L BML-210. The proliferation inhibition rates of different concentrations at 24， 48， 72， and 96 h were detected by using live cell counting Kit （CCK-8）. Annexin-FITC／PI double staining method was used to detect the cell apoptosis. Cell cycle distribution was detected by flow cytometry at different concentrations at 48 h. Expressions of protein Bax， Cleaved caspase-3 and Bcl-2 were detected by Western blotting assay at 48 h. Results BML-210 could increase the cell proliferation inhibition rates of U251 cells in a dose and time dependent manner （P＜0.05）. In addition to the late apoptotic rate of 50 μmol／L BML-210， the early and late apoptotic rates of U251 cells in BML-210 treated group were higher than those in control group （P＜0.05）. The 48 h apoptotic rate of U251 cells in BML-210 treated group was higher than that of 24 h， and the difference was statistically significant （P＜0.05）. Compared with the control group， the Bcl-2 level and the proportion of S and G2／M were decreased， but the levels of Bax, Cleaved caspase-3 and the proportion of G0／G1 were increased in BML-210 treated groups with significant difference （P＜0.05）. Conclusion BML-210 can inhibit the proliferation of U251 cells and induce apoptosis and cell cycle arrest， which is valuable for the treatment of glioma.