In this work we presented the 8-MOP, a well-known drug that has been used for decades in the treatment of skin disease (Tzaneva et al., 2009), as a novel promising molecule to develop new GST-π inhibitors, detailing its mechanism of action, and showing the potential for cancer therapy by using an in vitro model of glioblastoma. This evidence concerns the gene GSTP1 and glioblastoma.