NSC 95397

NSC 95397 is a quinone-based small molecule that acts as a potent inhibitor of dual-specificity phosphatases (DUSPs), most notably the Cdc25 family (Cdc25A, B, and C) and mitogen-activated protein kinase phosphatase-1 (MKP-1/DUSP1). By inhibiting these phosphatases, it prevents the dephosphorylation of their substrates, such as cyclin-dependent kinases (Cdks) and mitogen-activated protein kinases (MAPKs) like ERK1/2, thereby inducing cell cycle arrest (typically at G2/M) and apoptosis. It has been extensively studied in various cancer models, including neuroendocrine tumors, colon cancer, and breast cancer. Additionally, NSC 95397 has been identified as an inhibitor of protein arginine deiminases (PADs) and can covalently modify S100A4, disrupting its interaction with myosin-IIA. However, its utility as a drug candidate is complicated by its activity as a redox cycling compound that generates reactive oxygen species (ROS).

Other names

2,3-bis(2-hydroxyethylsulfanyl)-1,4-naphthoquinone2,3-bis(2-hydroxyethylthio)-1,4-naphthoquinone