Abstract: Wogonin, a naturally occurring flavonoid extracted from Scutellaria baicalensi Georgi (Lamiaceae),was reported to have potential antitumor effects in several studies. Recent research has suggested that a variety of signal pathways are regulated by wogonin. Wogonin potentially exerts its antitumor effect by up-regulating intracellular ROS level, down-regulating PI3K-AKT signal pathway, modulating MAPKs, up-regulating p53, inhibiting the NF-B signal pathway and inhibiting GSK-3 activation, as well as the expression of Np63, among other mechanisms. In this review, the recent in vivo and in vitro studies concerning the molecular mechanisms of the antitumor effects of wogonin are summarsized, with a special focus on the underlying signal pathways.