O<sup>6</sup>-Benzylguanine

O6-Benzylguanine

CAT N°: 16332
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From 48.00 40.80

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.{26735} In the process, AGT is alkylated and irreversibly inactivated.{26735} 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.{26730,26728} O6-Benzylguanine is effective in vivo as well as in vitro.{26733} Inactivation of AGT increases the chemotherapeutic effectiveness of chloroethylating and methylating agents.{26725}

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