ML-209 is an antagonist of retinoic acid receptor-related orphan receptor γt (RORγt; IC50 = 1.1 µM in a reporter assay).1 It inhibits RORγt-induced transcription in HEK293T cells expressing the human receptor (IC50 = 300 nM). ML-209 inhibits RORγt-dependent differentiation of isolated naÏve cord blood human CD4+ T cells into Th17 T helper cells.
1.Huh, J.R., Englund, E.E., Wang, H., et al.Identification of potent and selective diphenylpropanamide RORγ inhibitorsACS Med. Chem. Lett.4(1)79-84(2013)