Dimethyl bisphenolate (Compound DMB) is a novel natural lignan derivative with oral antitumor activity. It inhibits cancer cell proliferation, invasion, and migration. Dimethyl bisphenolate activates the p53 signaling pathway, upregulates the expression of p21 protein, and suppresses the activity of the CDK1-cyclin B1 complex, causing cell cycle arrest in the G2/M phase. Additionally, it induces the production of reactive oxygen species (ROS), upregulates pro-apoptotic proteins Noxa and Bim, downregulates anti-apoptotic protein Bcl-2, activates caspase-9 and caspase-3, ultimately leading to apoptosis. Dimethyl bisphenolate is applicable in glioblastoma research.