Sulfaphenazole

Description: Sulfaphenazole (Plisulfan) is an inhibitor of CYP2C9 (Ki: 0.3 µM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Ki: 63/29 µM for CYP2C8/CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19). At 10 µM, sulfaphenazole has been shown to inhibit endothelium-derived hyperpolarizing factor synthase, a CYP450 isozyme in the porcine coronary artery homologous to CYP2C8/9 that generates reactive oxygen species in coronary endothelial cells and modulates vascular tone and homeostasis. Target: Antibacterial, P450. Smiles: NC1=CC=C(C=C1)S(=O)(=O)NC1=CC=NN1C1=CC=CC=C1. References: Annah Mancy, et al. Interaction of Sulfaphenazole Derivatives with Human Liver Cytochromes P450 2C: Molecular Origin of the Specific Inhibitory Effects of Sulfaphenazole on CYP 2C9 and Consequences for the Substrate Binding Site Topology of CYP 2C9[J]. Biochemistry, 1996, 35(50):16205.