PD-L1-IN-1

PD-L1-IN-1, a powerful PD-L1 inhibitor, demonstrated an IC50 of 115 nM. By forming a robust bond with the PD-L1 protein, PD-L1-IN-1 effectively suppressed tumor growth by enhancing the antitumor immune activity of peripheral blood mononuclear cells in co-cultures with PD-L1 expressing cancer cells (PC9 and HCC827 cells). It significantly elevated the release of interferon γ and induced apoptosis in cancer cells, while exhibiting minimal cytotoxicity in healthy cells [1].

CYP51/PD-L1-IN-1 (compound L11), a quinazoline with antifungal properties, inhibits CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM), induces early apoptosis in the fungal cell cycle, decreases intracellular IL-2, NLRP3, and NF-κBp65 protein levels, causes mitochondrial damage and ROS accumulation, leading to fungal lysis and cell death [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-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-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-13 is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM for PD-1/PD- L1 interaction.PD-1/PD-L1-IN-13 promotes CD8+ T-cell activation and delays tumour growth in a Hepa1-6 homozygous mouse model.

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.

PD1-PDL1-IN 1 is a potent inhibitor of programmed cell death 1 (PD-1),and used as immune modulator.

PD1-PDL1-IN 1 TFA (compound 16) is a potent inhibitor of programmed cell death 1 (PD-1), functioning as an immune modulator [1].

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.

Pembrolizumab (MK-3475) is a highly selective humanized monoclonal antibody that antagonizes PD-1. It can block the PD-1 protein on T cells and prevent their interaction with PD-L1 on cancer cells.

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.

ARB-272572 is a potent inhibitor of programmed cell death ligand 1 (PD-L1) signaling that induces PD-L1 homodimer interactions and produces immunostimulatory activity in human primary cells.

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.

BMS-1001 hydrochloride is an orally active inhibitor of human PD-1/PD-L1 immune checkpoint with low-toxicity in cells.BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes.

Durvalumab (MEDI 4736) is a humanized monoclonal antibody targeting PD-L1. It can block the interaction of PD-L1 with PD-1 and CD80, with IC50 values of 0.1 and 0.04 nM, respectively. Durvalumab is often used in combination with platinum-based compounds for the treatment of non-small cell lung cancer and advanced hepatocellular carcinoma cells.

CA-170 is an orally bioavailable dual inhibitor of VISTA and PD-L1 that selectively restores T-cell proliferation and effector function suppressed by immune checkpoint signaling, while demonstrating minimal off-target activity across a broad receptor and enzyme panel, making CA-170 a valuable compound for immuno-oncology research and immune checkpoint modulation studies.

PD-1/PD-L1-IN 5 is an inhibitor of PD-1/PD-L1 protein-protein interaction with an IC50 of ≤100 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.

LSD1-IN-35 (Compound Z-1) is a selective inhibitor of LSD1, exhibiting an IC50 of 108 nM. This compound inhibits the demethylation of H3K4me1/2 and acts as an immunomodulator. Additionally, LSD1-IN-35 enhances the responsiveness of gastric cancer cells to T-cell killing by reducing PD-L1 expression, thereby weakening the PD-1/PD-L1 interaction.

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%.