(D)-PPA 1 is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy[1].
Spartalizumab (PDR001) is a humanized immunoglobulin 4 monoclonal antibody that binds PD-1 with subnanomolar activity and blocks interaction with PD-L1 and PD-L2. Spartalizumab can be used for the research of anaplastic thyroid carcinoma (ATC)[1].
PD-1/PD-L1-IN-32 (compound A56) is a potent PD-1/PD-L1 inhibitor (IC50=2.4 nM), with anticancer activity. PD-1/PD-L1-IN-32 significantly inhibits tumor growth in hPD-L1 MC38 humanized mouse model, without obvious toxicity against mouse normal ability[1].
Reozalimab is a bispecific antibody targeting to PD-1/PD-L1. Reozalimab mediates antibody-dependent cell cytotoxicity in cancer research[1][2].
Sulindac (sodium) (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac (sodium) is used to reduce pain, swelling, and joint stiffness from arthritis. Sulindac is also used for the research of arthritis of the spine, gouty arthritis. Sulindac (sodium), as an immunomodulatory agent, can downregulate PD-L1 through the blockade of NF-κB signaling and modulates the response of pMMR colorectal cancer (CRC) to anti-PD-L1 immunotherapy, inhibits the development and progression of colorectal cancer CRC. Sulindac (sodium) also inhibits TGF-β1- induced epithelial-mesenchymal transition (EMT) and suppresses lung cancer cell migration and invasion via downregulation of SIRT1[1][2].
BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM.
Lipustobart is an IgG4-kappa, anti-PDCD1 (programmed cell death 1, PD1, PD-1, CD279) humanized monoclonal antibody. Lipustobart shows immunostimulant and antineoplastic activity[1].
BMS-1166 hydrochloride is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
Tebotelimab (MGD-013) is a human IgG4κ bispecific PD-1/LAG-3 dual-affinity re-targeting (DART) antibody. Tebotelimab binds cell-surface expressed PD-1 and LAG-3 with EC50s of 1.65 nM and 0.41 nM in NS0 cells, respectively. Tebotelimab blocks PD-1/PD-L1, PD-1/PD-L2 and LAG-3/HLA (MHC-II) interactions and PD-1 signaling. Tebotelimab restores exhausted T-cell responses and and enhances antitumour immunity[1][2][3].
A potent PD-1/PD-L1 interaction inhibitor with IC50 of 2.25 nM in a homogenous time-resolved fluorescence binding assay.
PD-1/PD-L1-IN-29 (S4-1) is a potent PD-1/PD-L1 inhibitor with an IC50 value of 6.1 nM. PD-1/PD-L1-IN-29 binds PD-L1 and disrupts PD-1/PD-L1 interactions, induces PD-L1 dimerization and internalization, improves its localization to the endoplasmic reticulum, and promotes PD-L1 entry into the endoplasmic reticulum. PD-1/PD-L1-IN-29 has anticancer activity[1].
BMS-8 inhibits the PD-1/PD-L1 interaction with IC50 of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1[1].
Ivonescimab (AK112) is a PD-1/VEGF Bispecific Antibody. Ivonescimab can be used for cancer research[1][2][3].
PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester prodrug of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice[1].
Fidasimtamab (IBI-315; BH2950) is a recombinant human IgG1 bispecific antibody that targets, binds and inhibits both HER2 and PD-1 and their downstream signalling pathways, and links PD-1 expressing T cells to HER2 expressing tumour cells. Fidasimtamab has potential immunosuppressive and antitumor activity[1].
Pidilizumab (CT-011) is a humanized IgG1k anti-PD-1 monoclonal antibody. Pidilizumab acts as a DLL1 antagonist. Pidilizumab has the potential for hematologic malignancies research[1].
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1[1].
Gilvetmab is a potent caninized antiPD-1 monoclonal antibody. gilvetmab blocks the interaction between PD-1 and its ligand PDL-1[1].
Onvatilimab (JNJ-61610588) is a human IgG1κ anti-VISTA (V-domain Ig Suppressor of T-cell Activation) monoclonal antibody. Onvatilimab has an anti-tumor activity[1].
LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor with IC50 = 0.247 μM. LSD1-IN-24 can mediate the expression of PD-L1, enhance T cell killing response, and can be used in cancer research[1].
PD-1-IN-17 is a programmed cell death- 1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM[1].
Toripalimab is the first domestic anti-tumor PD-1 antibody in China. Toripalimab is a selective, recombinant, humanized monoclonal antibody against PD-1. Toripalimab is able to bind to PD-1 and block the interaction with its ligands. Toripalimab has exhibited primary anti-tumor effects in tumors such as melanoma, lung cancer, digestive tract tumors, hepatobiliary and pancreatic tumors, neuroendocrine neoplasms, nasopharyngeal carcinoma and urothelial carcinoma[1].
Serplulimab is humanized monoclonal anti-PD-1 antibody[1].
Retifanlimab is an anti-programmed cell death protein 1 (anti-PD-1) monoclonal antibody (mAb). Retifanlimab can be used for the research of gastroesophageal adenocarcinoma (GEA)[1].
Manelimab is a monoclonal antibody that inhibits programmed death-ligand 1 (PD-L1)[1].
Pacmilimab (CX-072) is a potent PD-L1 inhibitor. Pacmilimab shows antitumor activity[1].
PD-1/PD-L1-IN-28 (compound 3) is an immune checkpoint inhibitor of PD-1/PD-L1 signaling pathway (IC50=0.744 µM). PD-1/PD-L1-IN-28 shows good research potential in tumor immunity[1].
PD-1/PD-L1-IN-22 (Example 2) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-22 blocks PD-1/PD-L1 with the IC50 of 0.732 μM. PD-1/PD-L1-IN-22 can be used for the research of cancers, infectious diseases and autoimmune diseases[1].
Budigalimab (ABBV 181; PR 1648817) is a humanized IgG1 monoclonal antibody targeting programmed cell death 1 (PD-1) receptor. Budigalimab is Fc mutated thus to reduce Fc receptor interactions and limit effector function[1].
Acasunlimab (GEN1046) is a bispecific antibody (bsAb) targeting PD-L1 and 4-1BB. Acasunlimab enhances T-cell and NK-cell function through conditional 4-1BB stimulation while constitutively blocking the PD-1/PD-L1 inhibitory axis. Acasunlimab can be used in research of cancer[1][2].