Human PD-L1 inhibitor III is a human PD-L1 inhibitor.
PD-1/PD-L1-IN-13 (Compound 43) is a potent immune checkpoint PD-1/PD-L1 inhibitor with an IC50 value of 10.2 nM. PD-1/PD-L1-IN-13 promots CD8+ T cell activation and delays the tumor growth in the Hepa1-6 syngeneic mouse model[1].
SWS1 is a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM) with anticancer activity. SWS1 can increase the number of tumor-infiltrating lymphocytes and exhibit anti-tumor efficacy in the B16-F10 mouse model (TGI=66.1%)[1].
Sulfamethizole is a sulfathiazole antibacterial agent.Target: AntibacterialSulfamethizole is a sulfathiazole antibacterial agent. Sulfamethizole is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is necessary in these organisms for the synthesis of folic acid. Sulfamethizole, an inhibitor of dihydropteroate synthetase and the formation of folic acid, inhibited bioluminescence more than growth [1]. Treatment with sulfamethizole resulted in a significant reduction in bacterial counts in all samples from a susceptible strain (MIC, 128 micro g/ml) and a resistant strain (MIC, 512 micro g/ml). Infection with a sulII gene-positive strain (MIC, >2,048 micro g/ml) could not be treated with sulfamethizole, as no effect could be demonstrated in the urine, bladder, or kidneys [2].
Tuvonralimab (PSB-205; QL1706) is a dual immune checkpoint blockade containing a mixture of anti-PD-1 IgG4 and anti-CTLA-4 IgG1 antibodies, Iparomlimab and Tuvonralimab[1].
SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research[1].
Sintilimab (IBI308) is a fully human IgG4 monoclonal antibody that binds to PD-1, thereby blocking the interaction of PD-1 with its ligands (PD-L1 and PL-L2) and consequently helping to restore the endogenous antitumour T-cell response. Sintilimab can be used for the research of classical Hodgkin's lymphoma, non-small cell lung cancer and oesophageal cancer[1].
L-Lysine6-13C (dihydrochloride) is a 13C-labeled Sulfamethoxypyridazine.
Atorolimumab (P3x22914G4) is a monoclonal antibody used for immunotherapies targeting programmed death-1 (PD-1)[1].
Pimivalimab (JTX-4014) is a PD-1 inhibitor. Pimivalimab can be used for the research of solid tumor[1].
Adebrelimab (SHR-1316) is a humanized IgG4 monoclonal PD-L1 (PD-1/PD-L1) antibody. Adebrelimab has promising antitumor activity in solid tumors including extensive-stage small-cell lung cancer (SCLC)[1][2].
Benmelstobart is an IgG1κ antibody targeting PD-L1/CD274, derived from mice[1].
PD-1/PD-L1-IN-33 (Compound N11) is a PD-1/PD-L1 inhibitor. PD-1/PD-L1-IN-33 inhibits PD-1 and PD-L1 interaction with an IC50: 6.3 nM. PD-1/PD-L1-IN-33 promotes T-cell proliferation, activation, and infiltration into tumor spheres. PD-1/PD-L1-IN-33 has immunomodulatory and anticancer activity[1].
Opucolimab is an anti-PD-L1 recombinant human monoclonal antibody. Opucolimab can be used to synthesis antibody drug conjugates. Opucolimab can be used for the research of advanced solid tumors[1].
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively[1].
PD-1/PD-L1-IN-21 (Example 22) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-21 blocks PD-1/PD-L1 with the IC50 of 4.99 μM. PD-1/PD-L1-IN-21 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
Latikafusp (AMG 256) is a bifunctional fusion protein comprising a PD-1-targeting antibody and IL-21 mutein designed to deliver IL-21 pathway stimulation to PD-1+ cells. Latikafusp is designed to prime and extend the activity of cytotoxic and memory T cells and induce anti-tumor immunity. Latikafusp has the potential for solid tumors research[1][2].
NP-12 is a peptide antagonist of the PD-1 signaling pathway, which acts as an immunomodulatory agent for cancer therapy[1].
PD-1/PD-L1-IN 5 is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM[1].
Geptanolimab (CBT-501) is a humanized IgG4k monoclonal antibody against programmed death-1 (PD-1). Siplizumab inhibits the binding of PD-L1/L2 to PD-1 through a competitive action. Siplizumab can be used in research of cancer[1].
PD-1/PD-L1-IN 5 is a PD-1/PD-L1 protein/protein interaction inhibitor extracted from patent WO2017222976A1, compound Example 1, has an IC50 of ≤100 nM[1].
Zeluvalimab (AMG-404) is a monoclonal antibody targeting the PD-1 receptor that can be used for the research of cancer[1].
PD-1/PD-L1-IN 6 (compound A13) is a potent PD-1/PD-L1 interaction inhibitor, with an IC50 of 132.8 nM. PD-1/PD-L1-IN 6 exhibits outstanding immunoregulatory activity. PD-1/PD-L1-IN 6 significantly elevates interferon-γ secretion in a Hep3B/OS-8/hPD-L1 and CD3 T cell co-culture model, without significant toxic effect. PD-1/PD-L1-IN 6 restores the immune response in a T cell-tumor co-culture model[1].
ASC-69 (APY69)is a potent and promising?PD-1/PD-L1 small-molecule inhibitor[1].
Izuralimab is a bispecific IgG1 antibody targeting inducible T-cell costimulator (ICOS/CD278) and PD-1[1].
Cosibelimab (CK-301; TG-1501) is a high-affinity, fully human PD-L1-blocking monoclonal antibody that binds PD-L1 and blocks its interaction with PD-1. Cosibelimab has a functional Fc domain and is capable of inducing ADCC and complement-dependent cytotoxicity (CDC)-mediated killing of PD-L1+ cell lines, including lymphoma cells[1].
Cadonilimab (AK104) is a targeting PD1/CTLA4 IgG1 scaffold Fc-engineered humanized antibody. Cadonilimab can be used for researching metastatic cervical cancer[1][2].
Tislelizumab, a monoclonal antibody with high binding affinity to the PD-1 receptor, minimizes Fcγ receptor binding on macrophages, thereby abrogating antibody-dependent phagocytosis, a mechanism of T cell clearance and potential resistance to anti-PD-1 therapy. Tislelizumab can be used for the research of advanced squamous non-small-cell lung cancer[1].
PD-1/PD-L1-IN-20 (Example 21) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-20 blocks PD-1/PD-L1 with the IC50 of 5.29 nM. PD-1/PD-L1-IN-20 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
PD-1/PD-L1-IN-30 (Compound (1S,2S)-A25) inhibits PD-1/PD-L1 interaction (IC50=0.029 μM), with a selected binding affinity with PD-L1 (KD=0.1554 μM). PD-1/PD-L1-IN-30 inhibits tumor growth by activating the immune microenvironment[1].