CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50 = 15 nM in a homologous time-resolved fret (HTRF) assay).1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50 = 6.6 µM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+ and CD8+ T cells co-cultured with aAPCs.
1.Konieczny, M., Musielak, B., Kocik, J., et al.Di-bromo-based small-molecule inhibitors of the PD-1/PD-L1 immune checkpointJ. Med. Chem.63(19)11271-11285(2020)