Catalog No.: PC-25235Not For Human Use, Lab Use Only.
Ofirnoflast (HT-6184) is first-in-class, allosteric and orally bioavailable NEK7 inhibitor that disrupts NEK7-NLRP3 protein interaction, thereby preventing the formation of the NLRP3 inflammasome.
Ofirnoflast (HT-6184) is first-in-class, allosteric and orally bioavailable NEK7 inhibitor that disrupts NEK7-NLRP3 protein interaction, thereby preventing the formation of the NLRP3 inflammasome. Ofirnoflast (HT-6184) dose-dependently suppresses ASC specks, IL-1β release, and pyroptotic cell death in THP-1 macrophages and human iPSC-derived microglia. Ofirnoflast (HT-6184) stabilizes NEK7 in a unique conformation. Ofirnoflast (HT-6184) engages a conserved allosteric site adjacent to NEK7's ATP-binding pocket, inducing conformational shifts that impair its scaffolding function. Ofirnoflast (HT-6184) significantly reduces cytokine levels and improves clinical and histopathological outcomes in DSS-induced colitis model.
