ZE 132 binds to programmed cell death-ligand 1 (PD-L1) with high affinity (KD = 19.36 nM); it potently and selectively inhibits the interaction between programmed cell death-1 (PD-1) and PD-L1 (IC50 = 23.49 nM). ZE 132 promotes CD8+ T cell activation and improves the in vitro cytotoxic killing activity of T-cells. ZE 132 treatment can increase Cxcl9 mRNA expression and lower Tgfb1 mRNA expression in CT26 mouse colorectal cancer model. ZE 132 shows antitumor effects, inhibiting growth of CT26 tumors in mice by 64%.