NP19 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50 = 12.5 nM in a homogenous time-resolved fluorescence (HTRF) assay).1 It increases IFN-γ production by isolated human peripheral blood mononuclear cells (PBMCs) in co-culture with anti-CD3 single-chain variable fragment- and PD-L1-expressing Hep3B hepatoma cells (EC50 = ~3 ?M). NP19 (25, 50, and 100 mg/kg) reduces tumor growth in a B16/F10 murine melanoma model and an H22 murine hepatocellular carcinoma model.
1.Cheng, B., Ren, Y., Niu, X., et al.Discovery of novel resorcinol dibenzyl ethers targeting the programmed cell death-1/programmed cell death-ligand 1 interaction as potential anticancer agentsJ. Med. Chem.63(15)8338-8358(2020)