Herein, based on previous study, we studied the anticancer activities of Fe(PIP)3SO4 (Chen et al., 2015) against glioma U87 cells, including regulating the expression levels of p53 and 4E-BP1, triggering cell apoptosis and cycle arrest to inhibit cell proliferation, downregulating cellular reactive oxygen species (ROS) levels and TrxR activity, and penetrating across BBB, which was accompanied with negligible toxicity on normal tissues in vivo. The gene discussed is TP53; the disease is glioma.