PD-1/PD-L1 Ligand

Besufetamig is a bispecific antibody targeting programmed cell death 1 (PD-1) and CD3ε chain. Besufetamig modulates the activity of immune cells, exerting immunosuppressive and antineoplastic activities. Besufetamig is promising for research of cancers.

BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 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.

2-Methylbiphenyl-oxadiazole-NH-Ph-CHO is the PD-L1 ligand part of AUTAC PD-L1 degrader-3 (HY-169363). 2-Methylbiphenyl-oxadiazole-NH-Ph-CHO can be utilized in AUTAC synthesis.

LGT-1 is a PD-L1 ligand. LGT-1 labeled with ¹⁸F has an excellent specific uptake in B16-F10 tumor cells, and shows a high tumor uptake but a low liver uptake with good stability in B16-F10 tumor-bearing mice model. LGT-1 can be used as a radiotracer for PET imaging of PD-L1 expression in tumors.

2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc is the PD-L1 ligand-linker conjugate part of AUTAC PD-L1 degrader-3 (HY-169363). 2-Methylbiphenyl-oxadiazole-NH-Ph-NH-PEG3-C2-NH-Boc can be utilized in AUTAC synthesis.

NOTA-WL12 is a conjugate of WL12 (HY-P3440) (peptide targeting PD-L1) and NOTA (HY-134418) (chelate). NOTA-WL12 shows high binding affinity to the PD-L1 (K_D = 3.012 nM). NOTA-WL12 can be labeled with radioactive isotopes for tumor imaging.

N-(8-Carboxyoctanoyl)-deacetyl BMS-202 is a target protein ligand-linker conjugate. N-(8-Carboxyoctanoyl)-deacetyl BMS-202 contains the target protein PD-1/PD-L1 ligand and a PROTAC linker. N-(8-Carboxyoctanoyl)-deacetyl BMS-202 can be used for the synthesis of PROTAC PD-L1 Degrader-3 (HY-182959).