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The TSA caused inhibition of glioma cell growth by both cell cycle arrest and apoptosis. Cell cycle arrest was associated with an increase in p21WAF1 expression and a decrease in phosphorylated Rb. Apoptosis was mediated at least partly through the activation of caspase-3. Because of the differential effects in glioma cells compared with nonneoplastic cells, TSA may provide a novel strategy for achieving tumor growth inhibition and cytotoxicity. Further investigation is warranted.