Highly invasive and angiogenic nature of glioma contributes to the dismal outcome. However, instead of fighting against those aggressive characteristics, TMZ efficacy could be compromised by glioma invasion and angiogenesis. To determine whether KU0060648 inhibited invasive properties of glioma, U87 cells were treated with KU0060648 alone or in combination with TMZ for 16 hours and then assessed by Matrigel-coated Transwell assay. As shown in Figure 4A, 100 μM TMZ could not inhibit the invasiveness of U87, but rather slightly increased cells invasion. In contrast, 1 or 10 μM KU0060648 alone significantly decreased the invasive ability of U87 cells and profoundly prompted the anti-invasive ability of TMZ.