PD-1/PD-L1

RMP1-14 is an IgG1-like immunoglobulin and anti-Mouse PD-1 antibody that blocks PD-1 PD-L1 signaling.

Pembrolizumab (MK-3475) is a humanized monoclonal antibody inhibiting the PD-1 receptor and the first in the class of agents called the HER2 dimerization inhibitors that impairs the ability of HER2 to bind to other members of the HER family.

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.

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.

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.

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

Camrelizumab (SHR-1210) is a human IgG4-κ monoclonal antibody with high affinity directed against PD-1, binding PD-1 with an affinity of up to 3 nM and inhibiting PD-1 PD-L1 with an IC50 of 0.70 nM. Camrelizumab exhibits anti-tumor activity and is well tolerated in cancers, including NSC-LC, ESCC, Hodgkin's lymphoma, and advanced HCC.

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-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-IN-10 is an orally available PD-1 PD-L1 inhibitor (IC50 value of 2.7 nM) that shows anti-tumor activity.

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.

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.

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

INCB086550 (PD-1/PD-L1-IN-8) (example 24) is a PD-1/PD-L1 inhibitor, with an IC50 <= 10 nM.

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

AUNP-12 acetate is a polypeptide inhibitor of PD-1 that is equivalent to PD-1 and PD-2 in inhibiting lymphocyte proliferation and effector fuction, in addition to immune activation and antitumor activity.

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.

Sintilimab (IBI308) is a humanized IgG4 monoclonal antibody with significant anti-tumor activity that restores endogenous anti-tumor T-cell responses by binding to PD-1 and thereby blocking the interaction of PD-1 with its ligands (PD-L1 and PL-L2).Sintilimab is used in combination with other compounds for the treatment of classical Hodgkin's lymphoma, non-cellular lung cancer and esophageal cancer. Sintilimab is used in combination with other compounds to treat classical Hodgkin's lymphoma, non-small cell lung cancer and esophageal cancer.

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.

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.

Tislelizumab (BGB-A317) is an IgG4 class monoclonal antibody targeting human programmed death receptor-1 (PD-1) with antitumor activity that inhibits the binding of Fcγ receptor to macrophages and can be used to study advanced squamous non-small cell lung cancer.

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.

LSD1-IN-27 is a potent LSD1 inhibitor with an IC50 value of 13 nM.LSD1-IN-27 inhibited the stemness and migration of gastric cancer cells.LSD1-IN-27 inhibited the expression of PD-L1 in BGC-823 and MFC cells.LSD1-IN-27 potentiated the T-cell immune response against gastric cancer.

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-L1-IN-3 (Compound 4a) functions as an inhibitor of the PD-1 PD-L1 axis, with an IC50 value of 4.97 nM for PD-L1 inhibition and an EC50 value of 2.70 μM for Jurkat T cell modulation. It antagonizes the PD-1 PD-L1 interaction by binding to the PD-L1 dimer, obstructing PD-1 signaling. This compound is utilized in research pertaining to lung cancer and melanoma [1].

CAY10678 is an mPGES-1 inhibitor that inhibits PD-1.CAY10678 reduces collagen deposition and T-cell depletion, and may be used to study melanoma.CASHIPS

Evixapodlin (PD-1/PD-L1-IN 7) is a human PD-1/PD-L1 protein/protein interaction inhibitor (IC50: 0.213).Evixapodlin has anticancer and antiviral activities.

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.

PDL-1 cpd 10 is a novel small molecule PD-L1 inhititor.

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-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.

BMS-1001 is a potent inhibitor of PD-1 PD-L1 interaction(IC50 : 2.25 nM, in a homogenous time-resolved fluorescence binding assay).

Nofazinlimab (CS1003) is a human anti-PD-1 IgG4 monoclonal antibody used to study unresectable hepatocellular carcinoma (uHCC) and metastatic colorectal cancer.

Ezabenlimab (BI-754091) is a humanized monoclonal antibody targeting programmed cell death protein-1 with antitumor activity that blocks the interaction of PD-1 with PD-L1 and PD-L2, inhibits tumor growth in vivo, and can be used to study advanced solid tumors.

Latikafusp (AMG 256) is a fusion protein that is a PD-1 blocker and IL-21R agonist with antitumor activity.Latikafusp initiates and prolongs cytotoxicity and memory T-cell activity and induces the generation of immunogenicity-mediated responses.

Feladilimab (GSK3359609) is an IgG4 monoclonal antibody that is an ICOS agonist. Feladilimab binds to ICOS-expressing T cells, induces IFNγ, and increases PD-1 L1 expression. Feladilimab has anti-tumor activity and can be used to study cancer.

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-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 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].

ASC-69 (APY69) is a promising potent inhibitor of the PD-1/PD-L1 signaling pathway, classified as a small-molecule compound [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].

Rezilimab is a bispecific antibody that targets PD-1/PD-L1 and mediates antibody-dependent cell cytotoxicity (ADCC) in cancer research [1] [2].

LP23, a non-arylmethylamine PD-1/PD-L1 inhibitor (IC 50: 16.7 nM), exhibits anti-tumor activity through the restoration of immune cell function in HepG2/Jurkat T cells and induction of HepG2 cell death. Additionally, LP23 demonstrates in vivo efficacy in the B16-F10 tumor model (TGI=88.6% at 30 mg/kg) [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].