BKM120 is an inhibitor of PI3K that is currently in clinical trials as a potential treatment for brain metastases of HER2+ breast cancer and other solid tumors. BKM120 exhibits anticancer chemotherapeutic and anti-metastatic activities, inducing G2/M phase cell cycle arrest, polyploidy, and apoptosis in glioblastoma cells. Additionally, BKM120 decreases levels of Mcl-1 and enhances TRAIL-dependent apoptosis in lung cancer cells. BKM120 also binds tubulin, inhibiting microtubule polymerization. This compound prevents invasion and epithelial-to-mesenchymal transition (EMT) in cellular and animal models of squamous cell lung cancer.