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PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8?nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model[1].

[1] Qin M, et al. Discovery of the programmed cell death-1/programmed cell death-ligand 1 interaction inhibitors bearing an indoline scaffold. Eur J Med Chem. 2020 Jan 15;186:111856. DOI:10.1016/j.ejmech.2019.111856