O6BTG-C8-αGlu is an O6-methylguanine-DNA methyltransferase (MGMT) inhibitor with an IC50 of 0.45 μM. At a concentration of 0.1 μM, O6BTG-C8-αGlu can completely inhibit MGMT in HeLaS3 cells. Even when applied chronically at high doses (up to 20 μM), it does not exhibit cytotoxicity. O6BTG-C8-αGlu is suitable for research on MGMT-related cancer diseases[1].