GSK 366

GSK 366 is a type II kynurenine-3-monooxygenase (KMO) inhibitor with IC₅₀ values of 2.3 nM and 0.7 nM for human KMO and P. fluorescens-KMO (Pf-KMO). GSK 366 binds to KMO’s substrate site, prevents productive NADPH association, substrate binding, and FAD hydroperoxy species formation. GSK 366 does not stimulate hydrogen peroxide (H₂O₂) production and reduces H₂O₂ levels. GSK 366 can be used for the researches of inflammation and neurological disease, such as acute pancreatitis multiple organ dysfunction syndrome and Alzheimer’s disease^[1]. IC50 & Target:IC50: 2.3 nM (human KMO), 0.7 nM (Pf-KMO)^[1] In Vitro:GSK366 potently inhibits purified Pf-KMO with an IC₅₀ of 0.7 nM^[1].
GSK366 potently inhibits human KMO from Sf9 cell membranes with an IC₅₀ of 2.3 nM and an estimated K_i of ~12 pM^[1].
GSK366 (5 nM; 0-400 min) exhibits slow association kinetics with human KMO from Sf9 cell membranes and exhibits very slow dissociation kinetics^[1].
GSK366 (0.0001-100 μM; 15 min) does not stimulate hydrogen peroxide production in Pf-KMO or human KMO from Sf9 cell membranes, and reduces basal hydrogen peroxide levels in human KMO^[1].