pd-l1/pd-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.

PD-1/PD-L1 antagonist 1 (Compound A5) is an inhibitor of the interaction between programmed cell death protein 1 (PD-1) and programmed death-ligand 1 (PD-L1), with an IC50 value of 23.78 nM.

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.

Compound 8j, also known as PD-L1/PD-1-IN-1, is a potent inhibitor of the PD-L1/PD-1 interaction, demonstrating an IC50 value of less than 1 nM. It is significant in the field of anti-tumor research [1].

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.

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) /PD-Ll (Programmed death-ligand 1) protein/protein interaction.

D18 is an immune modulator that acts as a dual agonist for TLR7/8 (with EC50 values of 24 nM for hTLR7 and 10 nM for hTLR8, respectively). It enhances the expression of PD-L1 through epigenetic regulation, thereby increasing the sensitivity of tumors to PD-1/PD-L1 blockade. Additionally, D18 functions as a cytotoxin for ADC synthesis, specifically for the ADC HE-S2 [1].

Avelumab, a fully human IgG1 anti-PD-L1 monoclonal antibody, exhibits potential antibody-dependent cell-mediated cytotoxicity.

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.

BMS-1166-n-piperidine-co-n-piperazine dihydrochloride, a resorcinol di-Ph ether scaffold-based programmed cell death-1 (PD-1)/programmed cell death ligand 1 (PD-L1) inhibitor, inhibits the PD-1/PD-L1 interaction with an IC50 of 39.2 nM. It contains the target protein PD-1/PD-L1 ligand and PROTAC linker, which can be used to synthesize PROTAC PD-1/PD-L1 degrader-1 and has anticancer activity. Additionally, it serves as a diluent for the preparation of tablets for direct compression.

IMMH 010 maleate (YPD-30 maleate) is an orally available programmed cell death ligand 1 inhibitor with potential antitumor activity for the study of neurological disorders and advanced malignant solid tumors.

ARB-272572 hydrochloride is a small molecule PD-L1 inhibitor with an IC50 value of 400 pM for PD-1/PD-L1 HTRF.ARB-272572 hydrochloride inhibits PD-1/PD-L1 cell signaling by inducing homologous interactions with PD-L1 proteins.

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.

Sulfamethoxypyridazine (CL 13494) is a sulfanilamide antibacterial agent.

LSD1-IN-24 is a selective and potent LSD1 inhibitor with an IC50 value of 0.247 μM.LSD1-IN-24 induces PD-L1 expression and enhances the T cell killing response, and can be used in cancer-related diseases.

AXC-715 trihydrochloride (T785 trihydrochloride) is a TLR7/TLR8 dual agonist for the synthesis of antibody-adjuvanted immunocouplings. The couplings are mostly programmed death ligand 1 (PD-L1) attached to one or more antibody structures of the adjuvant.

N-deacetylated BMS-202 is an inhibitor of PD-1/PD-L1 interactions and has potential anticancer activity for cancer research.

Motixafortide (BKT140 4-fluorobenzoyl) is an antagonist of CXCR4 (IC50: 1 nM). BMS-1166 hydrochloride is an inhibitor of PD-1/PD-L1 interaction (IC50: 1.4 nM). BMS-1166 rivalries the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.

ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.

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.