Luzopeptin A is a cyclic depsipeptide antibiotic first isolated from an actinomycete strain. It displays antitumor activity, as it is highly active in mice against a variety of experimental tumors. Luzopeptin A acts as a bifunctional DNA intercalator that strongly binds DNA and forms crosslinks between DNA molecules. It also inhibits reverse transcriptases from HIV-1 and HIV-2 (IC50s = 7 and 68 nM, respectively), as well as cellular DNA polymerases.