货号 | 16332-10mg |
描述 | 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.1O6-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.2,3O6-Benzylguanine is effective in vivo as well as in vitro.4 Inactivation of AGT increases the chemotherapeutic effectiveness of chloroethylating and methylating agents.5 |
别名 | NSC 637037; |
供应商 | Cayman |
应用文献 | |
1.Pegg, A.E. Multifaceted roles of alkyltransferase and related proteins in DNA repair, DNA damage, resistance to chemotherapy, and research tools. Chemical Research in Toxicology 24(5), 618-639 (2011). 2.Goodtzova, K.,Crone, T.M. and Pegg, A.E. Activation of human O6-alkylguanine-DNA alkyltransferase by DNA. Biochemistry 33(28), 8385-8390 (1994). 3.Elder, R.H.,Margison, G.P. and Rafferty, J.A. Differential inactivation of mammalian and Escherichia coli O6-alkylguanine-DNA alkyltransferases by O6-benzylguanine. Biochemistry Journal 298, 231-235 (1994). 4.Kreklau, E.L.,Kurpad, C.,Williams, D.A., et al. Prolonged inhibition of O6-methylguanine DNA methyltransferase in human tumor cells by O6-benzylguanine in vitro and in vivo. Journal of Pharmacology and Experimental Therapeutics 291(3), 1269-1275 (1999). 5.Dolan, M.E. and Pegg, A.E. O6-Benzylguanine and its role in chemotherapy. Clinical Cancer Research 3, 837-847 (1997). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 241.2 |
分子式 | C12H11N5O |
CAS号 | 19916-73-5 |
稳定性 | ≥ 2 years |
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