PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2 / PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway.