Overall, our data demonstrated that in GBM cells 1) EB148 acts as a dual and irreversible-like ligand targeting both MDM2 and TSPO proteins, 2) the long-lasting activation of the two targets induced irreversible apoptosis, and 3) the ERK pathway is likely one of the molecular mechanism involved in the p53-mediated effects. The gene discussed is TSPO; the disease is glioblastoma.