Glioblastoma is the most common type of primary brain tumor in adults, with high mortality and morbidity rates. More effective therapeutic strategies are imperative. Previous studies have shown that the known p110-β-selective inhibitor TGX-221 blocks the activation of PKB/Akt in PTEN-deficient cells. We treated U87 and U251 glioblastoma cells with TGX-221 to determine the effect of TGX-221. We performed a Cell Counting Kit-8 (CCK-8) test, EDU staining and cell cycle distribution analysis and found that TGX-221 inhibited glioblastoma cell proliferation. Next, the effect of TGX-221 on cell apoptosis was investigated using flow cytometry. These results demonstrated that TGX-221 induced apoptosis in glioblastoma cells. Moreover, migration and invasion assays revealed that TGX-221 inhibited human glioblastoma cell migration and invasion. Collectively, our study revealed that TGX-221 could inhibit proliferation and induce apoptosis in glioblastoma cells.