Netropsin (dihydrochloride) 是一种小分子(MGB) 小沟结合剂，抑制分离的拓扑异构酶的催化活性，并干扰拓扑异构酶 II 和 I 在细胞核中的可切割复合物的稳定性。Netropsin (dihydrochloride) 通过以非插入方式与 dsDNA 结合而具有潜在的抗生素和抗病毒特性，它通过干扰 HMGA1 DNA 与核心NOS2 启动子的结合来减弱 NOS2 的诱导作用，从而提高小鼠内毒素血症的存活率。DNA 溶液中 的 Netropsin (dihydrochloride) 由于其高结合亲和力和高结构稳定性而具有辐射诱导损伤的辐射保护能力，电离辐射产生的羟基自由基 (OH*) 不能对 netropsin-DNA 复合物进行放射性降解。
CAS：18133-22-7
分子式：C18H28Cl2N10O3
分子量：503.39
纯度：98%
存储：Store at -20°C

Background:

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.