PD-1

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-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.

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.

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.

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

Anti-Mouse PD-L1 Antibody (10F.9G2) is an IgG-class antibody against mouse PD-L1.

Atezolizumab is an antibody inhibitor, a humanized monoclonal antibody, IgG1, which targets PD-L1 and blocks the interaction of PD-L1 with PD-1. Atezolizumab has antitumor activity and promotes T-cells to attack tumor cells.

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

Nivolumab is a monoclonal antibody, a humanized IgG4 antibody to PD-1. Nivolumab has antitumor activity and is used in the treatment of melanoma, non-small cell lung cancer, renal cell carcinoma and others.

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.

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.

Sulfamethoxypyridazine (CL 13494) is a sulfanilamide antibacterial agent.