Netropsin dihydrochloride (Synonyms: Congocidine, Sinanomycin)

Netropsin (dihydrochloride) is a small-molecule MGB (minor-groove binder), inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei[1]. Netropsin (dihydrochloride) has potential antibiotic and antiviral properties by binding to dsDNA in a non-intercalative manner, it improves survival from murine endotoxaemia by attenuating NOS2 induction through interference with HMGA1 DNA binding to the core NOS2 promoter[2]. Netropsin (dihydrochloride) in solutions of DNA has radioprotective ability against radiation-induced damage due to its high binding affinity and high structural stabilization, hydroxyl radical (OH*) generated by ionizing radiation cannot radiolyse the netropsin-DNA complex[3].

[1]. Beerman TA et al. Netropsin and bis-netropsin analogs as inhibitors of the catalytic activity of mammalian DNA topoisomerase II and topoisomerase cleavable complexes. Biochim Biophys Acta. 1991 Aug 27;1090(1):52-60. [2]. Grant MA, et al. Netropsin improves survival from endotoxaemia by disrupting HMGA1 binding to the NOS2 promoter. Biochem J. 2009 Feb 15;418(1):103-12. [3]. Mishra K et al. Netropsin, a minor groove binding ligand: a potential radioprotective agent. Radiat Res. 2009 Dec;172(6):698-705.