IC50: 0.006-0.10 μM

PD-1/PD-L1 inhibitor 1 is a PD-1/PD-L1 interaction inhibitor.

Plenty of studies show that blocking the PD-1/PD-Ll interactions can lead to the restorage and augment of T cell activation in many systems. In preclinical animal models, it has been found that blocking the PD-1/PD-Ll pathway by monoclonal antibodies can enhance the immune response and result in tumor shrinkage or control of virus infection. Recent clinical studies have shown that the therapies with a monoclonal antibody to PD-Ll can give benefits to patients with advanced cancer.

In vitro: PD-1/PD-L1 inhibitor 1 has been identified to be a potent and selective small molecule inhibitor blocking the interaction of programmed cell death protein 1 (PD-1) with its ligand protein (PD-L1). PD-1/PD-L1 inhibitor 1 was also found to act as an immunomodulator. In preclinical studies, PD-1/PD-L1 inhibitor 1 was able to block PD-1/PD-Ll interactions with an IC50 value between 6 and 100 nM, which was measured by a homogenous time-resolved fluorescence (HTRF) binding assay. Thus, PD-1/PD-L1 inhibitor 1 might potentially be used for the treatment of cancer as well as infectious diseases, such as hepatitis C [1].

In vivo: So far, there is no animal in vivo data reported for PD-1/PD-L1 inhibitor 1.

Clinical trial: Up to now, PD-1/PD-L1 inhibitor 1 is still in the preclinical development stage.

Reference:
[1] https://www. google.com/patents/WO2015034820A1