pd1-pdl1 inhibitor 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.

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.

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.

Sulfamethoxypyridazine (CL 13494) is a sulfanilamide antibacterial agent.

Tomivosertib (eFT508) is a potent and highly selective MNK1 and MNK2 inhibitor with an IC50 value of 1-2 nM.

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.

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

LTB is a prodrug formed through the conjugation of the glycolysis inhibitor (Lonidamine) and the PD1 PDL1 blocker (BMS-1) via a thioketal bond. LTB can encapsulate the photosensitizer Chlorin e6 (Ce6), constructing a co-delivery photodynamic nanoplatfform through self-assembly (LTB-6 NPs).

BMS-8 is a novel inhibitor of the PD-1 PD-L1 interaction (IC50: 7.2 μM) by binding directly to PD-L1 and inducing the formation of PD-L1 homodimers.

BMS202 hydrochloride (1675203-84-5(free base)) (PD-1 PD-L1 inhibitor 2 hydrochloride) is a small-molecule PD-1 PD-L1 interaction inhibitor (IC50: 18 nM). Biophysical studies demonstrate that BMS202 binds directly to PD-L1. Binding of BMS202 promotes PD-L1 dimerisation and blocks the PD-L1 PD1 interaction.

BMS-1166 is a potent inhibitor of the PD-1 PD-L1 interaction.

1. Fraxinellone significantly reduced weight loss and diarrhea in mice and alleviated the macroscopic and microscopic signs of the disease. 2. Fraxinellone exhibited a variety of insecticidal activities including feeding-deterrent activity, inhibition of growth, and larvicidal activity. 3. Fraxinellone has effect in the midgut metabolism of Mythimna separata (M. separata), via protease (especially the weak alkaline trypsin-like enzyme), carboxylesterase and glutathione S-transferase.

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

PD1-PDL1-IN 2 (ZE132) is a potent, selective inhibitor of PD-1/PD-L1, exhibiting significant anti-tumor activity in vivo. It enhances cytotoxic T-cell tumor infiltration and stimulates IL-2 expression, while also strongly inhibiting TGF-β [1] mRNA expression, showcasing its comprehensive immunotherapeutic potential.

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.