protac pd 1/pd l1 degrader 1

PROTAC PD-1/PD-L1 degrader-1, a Cereblon E3 ligand-based compound, is a PD-1/PD-L1 PROTAC that effectively inhibits the PD-1/PD-L1 interaction with an IC50 of 39.2 nM. It restores the suppressed immune response in a co-culture model of Hep3B/OS-8/hPD-L1 cells and CD3 T cells and moderately decreases PD-L1 protein levels through a lysosome-dependent mechanism.

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

Pomalidomide-amido-C3-piperazine-N-Boc is a synthetic E3 ligase ligand-linker conjugate that includes a cereblon ligand based on Pomalidomide and a linker. It is utilized in the synthesis of PROTAC PD-1/PD-L1 degrader-1.

N-Boc-piperazine-C3-COOH is a PROTAC linker used in the synthesis of PROTACPD-1/PD-L1 degrader-1.

PROTACPD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with significant PD-L1 protein degradation capacity. It demonstrates strong PD-L1 degradation activity in 4T1 cells, with a DC50 of 0.609 μM. This compound is applicable to breast cancer research.

BMS-1166-N-piperidine-COOH is a chemical compound that functions as the BMS-1166-based moiety. It binds to the E3 ligase ligand through a linker, leading to the formation of PROTAC PD-1/PD-L1 degrader-1, which facilitates the degradation of PD-1/PD-L1. BMS-1166 demonstrates potent inhibition of PD-1/PD-L1 interaction, with an IC 50 of 1.4 nM. By antagonizing the inhibitory effect of the PD-1/PD-L1 immune checkpoint on T cell activation, BMS-1166 promotes T cell activation.

BMS-1166-N-piperidine-CO-N-piperazine is a chemical compound containing a PD-1/PD-L1 immune checkpoint ligand and a PROTAC linker. It is used in synthesizing [PROTAC PD-1/PD-L1 degrader-1], which effectively inhibits the PD-1/PD-L1 interaction with an IC50 value of 39.2 nM.

Br-C3-methyl ester is an alkyl/ether-based PROTAC linker utilized for the synthesis of PROTAC PD-1/PD-L1 degrader-1.