pd-1/pd-l1-in-9

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.

SF-9-2 is a PD-L1/PD-1 binding inhibitor with an IC50 of 24.9 nM. It suppresses epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, while also inducing apoptosis and causing cell cycle arrest. SF-9-2 blocks PD-L1-induced growth of SK-N-SH cells via the MAPK signaling pathway. It restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. In the SK-N-SH NOG mouse model, SF-9-2 inhibits tumor growth without notable toxicity. Additionally, SF-9-2 acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function and is applicable to neuroblastoma research.

TLR7/8 agonist 9 (Compound 25a), with EC50 values of 40 nM for hTLR7 and 23 nM for hTLR8, demonstrates anti-tumor properties and enhances the efficacy of PD-1/PD-L1 blockade treatments, making it valuable for cancer immunotherapy research [1].

DGKζ-IN-1 (compound 9) is a DGKζ inhibitor with potential applications in cancer research, particularly for studying immunocyte activation and resistance to anti-PD-1/anti-PD-L1 antibody therapies [1].

Opamtistomig is a humanized monoclonal antibody immunoglobulin (H-γ1-scFv-L-κ) dimer targeting human programmed death-ligand 1 (PD-L1), CD274, and tumor necrosis factor receptor superfamily member 9 (TNFRSF9). It is anticipated for use in research on various solid tumors and hematologic malignancies.

PD-1/PD-L1-IN 3 TFA inhibits the binding of human PD-1 to PD-Ll with an IC50 of 9 nM.