EOS200271 is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO-1; IC50 = 0.15 ?M for the human enzyme).1 It is selective for IDO-1 over IDO-2 up to a concentration of 200 ?M for the human recombinant enzymes. EOS200271 inhibits IDO-1-mediated production of kynurenine induced by IFN-γ in HeLa cells (IC50 = 1.8 ?M) and by LPS and IFN-γ in THP-1 cells and human-derived whole blood ex vivo (IC50s = 1.7 and 4.7 ?M, respectively).
1.Crosignani, S., Bingham, P.M., Bottemanne, P., et al.Discovery of a novel and selective indoleamine 2,3-dioxygenase (IDO-1) inhibitor 3-(5-fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and its characterization as a potential clinical candidateJ. Med. Chem.60(23)9617-9629(2017)