Cayman O6-Benzylguanine

O⁶-Alkylguanine-DNA alkyltransferase (AGT, also known as methylguanine DNA methyltransferase, or MGMT) is a DNA repair protein that directly removes alkyl groups located on the O⁶-position of guanine from DNA, restoring DNA integrity in a single step.¹ In the process, AGT is alkylated and irreversibly inactivated.¹ O⁶-Benzylguanine is a guanine analog with antineoplastic activity. It serves as a pseudosubstrate for AGT, transferring a benzyl moiety to the active site cysteine of the enzyme. This leads to irreversible inactivation, with 40% reduction in alkyltransferase activity of recombinant human AGT achieved at 0.06 µM.^2,3 O⁶-Benzylguanine is effective in vivo as well as in vitro.⁴ Inactivation of AGT increases the chemotherapeutic effectiveness of chloroethylating and methylating agents.⁵

WARNING This product is not for human or veterinary use.