pd-1/pd-l1

PD-1 PD-L1-IN-32 (compound A56) is a potent inhibitor of PD-1 PD-L1 with an IC50 value of 2.4 nM, demonstrating significant anticancer activity. It effectively suppresses tumor growth in the hPD-L1 MC38 humanized mouse model and exhibits negligible toxicity to the normal functions of the mice [1].

PD-1 PD-L1-IN-27 is a potent inhibitor of PD-1 PD-L1, with an IC50 of 134 nM, and demonstrates antitumor effects with minimal T cell cytotoxicity. It activates CD8+ T cells and mitigates T cell exhaustion [1].

PD-1 PD-L1-IN-53 (compound B3) serves as an inhibitor targeting both the PD-1 PD-L1 and VISTA signaling pathways. It is utilized in cancer research.

PD-1 PD-L1 inhibitory peptide C8 disrupts the PD-1 PD-L1 interaction, leading to the activation of CD8+ and CD4+ T cells and an increase in IFN-γ secretion. In mouse models, PD-1 PD-L1 inhibitory peptide C8 has demonstrated antitumor activity.

PD-1 PD-L1-IN-26 (Compound II-14) is a potent PD-1 PD-L1 inhibitor with an IC50 of 0.0380 μM. It enhances the immune microenvironment by promoting CD4+ T cell infiltration into tumor tissues, suggesting its potential application in cancer research [1].

PD-1 PD-L1-IN-31 is a potent inhibitor of PD-1 PD-L1 (IC50=2.2 nM) that enhances IFN-γ secretion and activates the immune response of peripheral blood mononuclear cells (PBMCs), leading to the inhibition of tumor cells [1].

PD-1 PD-L1-IN-33 (Compound N11), a PD-1 PD-L1 inhibitor with an IC50 of 6.3 nM, effectively impedes the interaction between PD-1 and PD-L1. It enhances T-cell proliferation, activation, and infiltration within tumor environments, thereby exhibiting immunomodulatory and anticancer properties [1].

PD-1 PD-L1-IN-34 (Compound (1S,2S)-A25) effectively inhibits the PD-1 PD-L1 interaction (IC50 = 0.029 μM) and demonstrates selective binding affinity to PD-L1 (KD = 0.1554 μM), resulting in the activation of the immune microenvironment and suppression of tumor growth [1].

PD-1 PD-L1-IN-9, with an IC50 of 3.8 nM, is a potent and orally active inhibitor of the PD-1 PD-L1 interaction. It enhances the immune cells' ability to kill tumor cells and demonstrates significant antitumor activity in vivo in a CT26 mouse model.

Compound LG-12, known chemically as PD-1 PD-L1-IN-50, is an inhibitor of PD-1 PD-L1. It enhances the secretion of IFN-γ, promotes the activation of CD8+ T cells, and activates T cell-mediated anti-tumor immunity.

PD-1 PD-L1-IN-51 (Compound III-4) is an inhibitor of PD-1 PD-L1 (IC50: hPD-L1 at 2.9 nM). It binds directly to PD-L1, blocking the interaction between PD-1 and PD-L1, and enhancing the release of IFN-γ. Additionally, PD-1 PD-L1-IN-51 exhibits antitumor activity.

PD-1 PD-L1-IN-10 is an orally available PD-1 PD-L1 inhibitor (IC50 value of 2.7 nM) that shows anti-tumor activity.

PD-1 PD-L1-IN-52 (Compound Ⅲ-5) is an orally active inhibitor of PD-1 PD-L1 interaction, exhibiting an IC50 of 109.9 nM. It demonstrates antitumor activity in a C57BL 6 mouse model of MC38 colon carcinoma cells expressing human PD-1, achieving a tumor growth inhibition (TGI) rate of 49.6%.

PROTAC PD-1 PD-L1 degrader-1, a Cereblon E3 ligand-based compound, is a PD-1 PD-L1 PROTAC that effectively inhibits the PD-1 PD-L1 interaction with an IC50 of 39.2 nM. It restores the suppressed immune response in a co-culture model of Hep3B OS-8 hPD-L1 cells and CD3 T cells and moderately decreases PD-L1 protein levels through a lysosome-dependent mechanism.

PD-1 PD-L1-IN-NP19, a PD-1 PD-L1 inhibitor, exhibits an IC50 of 12.5 nM against the human PD-1 PD-L1 interaction, potentially activating the tumor immune microenvironment and contributing to its antitumor effects[1].

PD-1/PD-L1-IN 3 TFA inhibits the binding of human PD-1 to PD-Ll with an IC50 of 9 nM.

PD-1 PD-L1-IN-47 (MolPort-001-742-690) is a pH-selective inhibitor of the PD-1 PD-L1 signaling pathway, demonstrating significant affinity for PD-L1 under acidic conditions and lower toxicity. It is utilized in the study of tumors.

PD-1 PD-L1-IN-48 (compound HD10) is an effective inhibitor of the PD-1 PD-L1 interaction, exhibiting an IC50 of 3.1 nM. It plays a vital role in cancer research.

PD-1 PD-L1-IN-28, an inhibitor of the PD-1 PD-L1 signaling pathway (IC 50 = 0.744 µM), demonstrates promising research potential in tumor immunity. This immune checkpoint inhibitor effectively blocks the interaction within the pathway, offering insights into cancer treatment strategies.

PD-1 PD-L1-IN-22, a small molecule inhibitor (IC50: 0.732 μM), blocks PD-1 PD-L1 protein-protein interactions and can be utilized to study cancer, infectious diseases, and autoimmune diseases.

PD-1 PD-L1-IN-17 (Compound P20) is a potent PD-1 PD-L1 inhibitor (IC50: 26.8 nM) and a promising lead compound for the development of inhibitors of PD-1 PD-L1 interactions, with potential applications in cancer disease research.

PD-1 PD-L1-IN-14 (compound 17) is an inhibitor of PD-1 PD-L1 interaction (IC50=27.8 nM) that promotes PD-L1 dimerization, endocytosis, and degradation.

PD-1 PD-L1-IN 5 is a potent inhibitor of the PD-1 PD-L1 protein protein interaction (IC50 ≤ 100 nM).

PD-1 PD-L1-IN-23 is a potent, orally active ester prodrug of L7, a benzooxadiazole derivative, that functions as an inhibitor of PD-1 PD-L1. It has undergone biological evaluation for its inhibitory effects on PD-L1, showing significant antitumor effects in both syngeneic tumor models and PD-L1 humanized mice.