PD-1

Anti-Mouse PD-1 Antibody (RMP1-14) is an IgG2a antibody inhibitor against mouse PD-1 and can block PD-1/PD-L1 signaling.

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-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].

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

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-IN-17 is an inhibitor of programmed cell death-1 (PD-1). PD-1-IN-17 inhibits 92% splenocyte proliferation at 100 nM.

PD-1-IN-22 is a potent inhibitor of the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction, with an IC50 of 92.3 nM.

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.

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-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%.

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-40 (Compound EP16) is a PD-1/PD-L1 inhibitor. It effectively suppresses the production of exosomal PD-L1 with an IC50 of 0.108 μM. PD-1/PD-L1-IN-40 serves as a lead compound for the elimination of exosomal PD-L1 and is applicable in cancer research.

PD-1/PD-L1-IN-39 (X 14) is an orally active PD-1/PD-L1 inhibitor with an IC50 value of 15.73 nM. It exhibits strong binding affinity to human and mouse PD-L1, with KD values of 14.62 and 392 nM, respectively. PD-1/PD-L1-IN-39 also demonstrates antitumor activity.

PD-1/PD-L1-IN-41 (Compound 5c) is an inhibitor of PD-L1 and PD-1 with an IC50 value of 10.2 nM.