O6-Benzylguanine (O6-BG) is a synthetic derivative of guanine often used to examine DNA repair mechanisms. O6-BG acts as an inhibitor of O6-methylguanine DNA methyltransferase (MGMT), an enzyme that repairs damage to guanine residues in DNA. As many alkylating and cross-linking chemotherapeutics…

A guanine analog with antineoplastic activity; irreversibly inactivates AGT, with 40% reduction in alkyltransferase activity achieved at 0.06 µM with recombinant human AGT; effective in vivo as well as in vitro.