GNE-6468 (GNE6468) is a potent and selective RORc (RORγ) inverse agonist (EC50=2 nM) with >1,000-fold selectivity for RORc over PPARγ.
GNE-6468 displays excellent selectivity profiles against a panel of other nuclear receptors in Gal4 human transcription assays.
GNE-6468 displays potent inhibition of IL-17 production with EC50 of 30 nM in human PBMC cytokine production assays, without effect on IFNγ production.
GNE-6468 is a chemical biology tool to further explore the role of RORc in human biology.
