PD-1/PD-L1

PD-1/PD-L1-IN-10 is an orally active PD-1/PD-L1 inhibitor (IC50 of 2.7 nM) with potent anticancer efficacy.

Nivolumab (anti-PD-1) is a genetically engineered fully human immunoglobulin Ig) G4 monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed death-1PD-1PCD-1) with immune checkpoint inhibitory and antineoplastic activities.

Pembrolizumab 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 (anti-PD-L1) is a fully humanized IgG1 monoclonal antibody that blocks the interaction of PD-L1 with both PD-1 and B7.1 but not the interaction of PD-L2 with PD-1.

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.

PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor(IC50 of 92.3 nM).

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.

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.

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.

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

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-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-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.

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

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.

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

Anti-Mouse PD-L1 Antibody is a rat-derived IgG2b monoclonal antibody that inhibits mouse PD-L1.

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

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

Eciskafusp alfa, a cis-targeted IL2v immunocytokine, acts on programmed cell death 1 (PDCD1, commonly known as PD-1), preferentially targeting antigen-specific stem-like PD-1+ TCF-1+ CD8+ T cells to differentiate into a more effective effector population. This compound is applicable in the study of cancer and chronic infections [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

Pidilizumab (CT-011), a humanized IgG1κ anti-PD-1 monoclonal antibody, serves as a DLL1 antagonist with potential applications in researching hematologic malignancies [1].

Lipustobart is an IgG4-kappa humanized monoclonal antibody targeting PDCD1 (programmed cell death 1, PD1, PD-1, CD279), with immunostimulant and antineoplastic activity [1].

Danburstotug (IMC-001), an immunostimulant and antineoplastic [1], is a humanized IgG1-lambda monoclonal antibody targeting CD274 (PDL1, B7 homologue 1, B7H1).

Visugromab, a GDF-15 neutralizing IgG4 monoclonal antibody (mAb), demonstrates potent efficacy in treating PD-1/PD-L1 relapsed/refractory metastatic solid tumors [1].

Sasanlimab (PF-06801591), a humanized IgG4-κ antibody, selectively targets PD-1 and is primarily produced in Chinese Hamster Ovary (CHO) cells [1].

Spartalizumab (PDR001) is a humanized immunoglobulin 4 monoclonal antibody that selectively binds to PD-1 at low concentrations and shows high activity. Spartalizumab blocks the interaction with PD-L1 and PD-L2, and can be used to study undifferentiated thyroid cancer (ATC).

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.

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.

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.

PD-1/PD-L1-IN-32 (compound A56) is a potent inhibitor of PD-1/PD-L1, displaying pronounced anticancer activity with an IC50 value of 2.4 nM. It effectively suppresses tumor growth in the hPD-L1 MC38 humanized mouse model and exhibits negligible toxicity to the mice's normal functions [1].

PD-1/PD-L1-IN-27 is a potent inhibitor of PD-1/PD-L1, exhibiting an IC50 of 134 nM and demonstrating antitumor effects with minimal T cell cytotoxicity. It activates CD8+ T cells and mitigates T cell exhaustion [1].

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, effectively impedes the interaction between PD-1 and PD-L1 with an IC50 of 6.3 nM. By doing so, it enhances T-cell proliferation, activation, and infiltration within tumor environments, exhibiting immunomodulatory and anticancer properties [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), resulting in the inhibition of tumor cells [1].

PD-1/PD-L1-IN-26 (Compound II-14) is a potent PD-1/PD-L1 inhibitor, demonstrating an IC50 of 0.0380 μM. It enhances the immune microenvironment by facilitating CD4+ T cell infiltration into tumor tissues, indicating potential use in cancer research [1].

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.

PD-L1-IN-3 is a selective and potent PD-1/PD-L1 inhibitor with antitumor activity that blocks PD-1 signaling by preventing PD-1 from binding to PD-L1.PD-L1-IN-3 is used in the study of neoplasms and immune diseases.

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

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

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.

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

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.

Acrixolimab is a humanized IgG4-κ monoclonal antibody that selectively targets PD-1 [1] [2].

PD-L1-IN-2, a Naamidine J derivative, serves as a promising antineoplastic immunomodulator by hindering PD-L1 activity. In vivo studies indicate that it suppresses PD-L1 expression and amplifies tumor-infiltrating T-cell response, thus exerting anticancer effects. This compound is particularly utilized in the investigation of colorectal cancer [1].

SWS1, a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM), displays anticancer activity by augmenting tumor-infiltrating lymphocytes and demonstrating anti-tumor efficacy, as evidenced by a 66.1% tumor growth inhibition (TGI=66.1%) in the B16-F10 mouse model [1].

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].

Spartalizumab (anti-PD-1) is a useful organic compound for research related to life sciences and the catalog number is T35396.