Abstract: Objective to investigate the effects of pirarubicin on proliferation and apoptosis of bladder cancer cells and its mechanism. Methods After treatment with THP, Flow cytometry was used to measure apoptosis of T24 and BIU-87 cells; The effects of pirarubicin on cell proliferation of T24 and BIU-87 cell lines were detected by MTT; QRT-PCR、RT-PCR were used to examine the mRNA expression of PLCε，BCL-2 in T24 and BIU-87 cell lines with or without pirarubicin treatment，the protein expression of PLCε in pirarubicin treatment cells was determined by western blot ; After combination treatment of THP with Ad-shPLCε in T24 and BIU-87 cells, MTT was used to evaluate cells proliferation and the protein expression of BCL-2 was detected by western blot in each group. Results Pirarubicin showed significantly dose- and time-dependent inhibitory effect on the proliferation of T24 and BIU-87 cell lines, and the inhibition ratios of 1.6 and 3.2 mg /L THP were higher than that of 0. 4 and 0.8 mg /L THP ( P ＜ 0. 05),in addition, the inhibition ratios of treatment with THP for 72h were higher than that of 24h and 48h THP( P ＜ 0. 05).Moreover , Cell apoptotic rate increased in cell with pirarubicin treatment（P<0.05）.The mRNA and protein expression of PLCε were suppressed in cell lines after treatment with THP. Meanwhile, the expression of BCL-2 at mRNA was repressed by Pirarubicin treatment. Combined treatment of THP with Ad-shPLCε exhibited synergistic inhibitory effects on cells proliferation and BCL-2 protein expression compared with THP treatment group (P<0.05). Conclusions Pirarubicin induced cell apoptosis and inhibited cell proliferation, which may be through suppress the expression of PLCε and BCL-2 in bladder cancer cell lines.