pd-1/pd-l1

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 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.

BMS-1 (PD-1/PD-L1 inhibitor 1) is an inhibitor of the PD1-PD-L1 protein-protein interaction. It also acts as an immunomodulator. Programmed death ligand 1 (PD-L1) is a protein in humans that is encoded by the CD274 gene and the upregulation of PD-L1 allows Ys to evade the host immune system. High tumor expression of PD-L1 was associated with increased tumor aggressiveness and a 4.5-fold increased risk of death.

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.

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-IN-49 (compound 1c) is a potent inhibitor of PD-1/PD-L1 with an IC50 of 77 nM. This compound can activate Jurkat T cells and effectively block the PD-1/PD-L1 immune checkpoint.

PD-1/PD-L1-IN-55 (compound D6) is a potent PD-1/PD-L1 inhibitor with an IC50 of 4.8 nM. It enhances IFN-γ secretion and decreases the proportion of late apoptosis due to PD-L1.

PD-1/PD-L1-IN-57 (Compound J29) is a PD-1/PD-L1 inhibitor with an IC50 value of 5.5 nM. It demonstrates potent immunomodulatory activity, significantly promoting T cell proliferation and restoring the ability to kill tumor cells. PD-1/PD-L1-IN-57 is applicable to research in tumor immunotherapy.

PD-1/PD-L1-IN-59 (Compound MZ51) is a PD-1/PD-L1 inhibitor with an IC50 of 183 nM, suitable for research in triple-negative breast cancer (TNBC).

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

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-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-25, an inhibitor of PD-1/PD-L1 interaction (IC50: 16.17 nM), effectively activates anti-tumor immunity in T cells within PBMCs and can be utilized in cancer research.

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-15 is a potent PD-1/PD-L1 inhibitor (IC50: 60.1 nM) with demonstrated investigational potential for tumor immunotherapy.

PD-1/PD-L1-IN-16, a potent inhibitor of PD-1/PD-L1 (IC50: 53.2 nM), has demonstrated research potential for tumor immunotherapy.

PD-1/PD-L1-IN-20 is a small molecule inhibitor of PD-1/PD-L1 protein-protein interaction, blocking the interaction with an IC50 of 5.29 nM. PD-1/PD-L1-IN-20 can be used to study cancer, infectious diseases, and autoimmune diseases.

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-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.

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-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-29 (S4-1) is a potent inhibitor of the PD-1/PD-L1 interaction with an IC50 value of 6.1 nM. It effectively binds to PD-L1, promoting its dimerization and internalization, enhancing its localization to the endoplasmic reticulum, and demonstrating anticancer activity.