A cell surface receptor called Programmed Death-1 (PD-1) serves as a T cell checkpoint and is crucial in controlling T cell exhaustion. PDL-1 or PDL-2 engagement with PD-1 causes it to become active. When the PD-1 receptor binds to its ligands, PD-L1 and PD-L2, which are expressed on cancer cells and antigen-presenting cells, it sends inhibitory checkpoint signals to activated T cells. This suppresses T-cell effector function and allows tumor immune evasion. An appealing approach for tumor immunotherapy is to block the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) pathway.
Activated T cells, B cells, monocytes, dendritic cells, regulatory T cells, and natural killer T cells all express PD-1. It belongs to a group of immunoglobulin domain (Ig) co-receptors that affect how the T cell receptor responds when activated by an antigen-presenting cell (APC) or an infected target cell. In contrast to PD-L2, which is only and inducibly expressed on professional APCs, PD-L1 is widely expressed and constitutively on both hematopoietic and nonhematopoietic cells, including naive T and B cells, vascular endothelial cells, and pancreatic islet cells.
Structure | Cat No. | Product Name | CAS No. | Product Description |
---|---|---|---|---|
V3676 | (-)-JQ-1 | 1268524-71-5 | JQ-1 is the (R)-Enantiomer of JQ1 or the stereoisomer of (+)-JQ1. | |
V77385 | (D)-PPA 1 TFA | (D)-PPA 1 TFA is a hydrolytic D-peptide antagonist. | ||
V88733 | Antitumor agent-169 | Antitumor agent-169 (Compound B3) is a dual inhibitor of PD-1/PD-L1 interaction and PARP7 with IC50 of 0.426 μM and 2.50 nM, respectively. | ||
V88725 | Antitumor agent-170 | Antitumor agent-170 (Compound C6) exhibits inhibitory activity against PD-1/PD-L1 interaction and PARP7 with IC50 of 0.342 μM and 7.05 nM, respectively. | ||
V3096 | AUNP-12 | 1353563-85-5 | AUNP-12 (also known as Aur-012, Aurigene-012, and Aurigene NP-12), a novel and potent immune checkpoint modulator developed by Aurigene Discovery Technologies, is an inhibitor of thePD-1 signalling pathway with an EC50 of 0.72 nM in the inhibition of binding PD1 to PD-L2 using hPDL2expressing HEK293 cells, and an EC50 of 0.41 nM in a rat peripheral blood mononuclearcells (PBMC) proliferation assay using hPDL1 expressing MDA-MB231 cells. | |
V77227 | AUNP-12 TFA (NP-12 TFA) | AUNP-12 (NP-12) TFA is a bioactive peptide antagonist of the PD-1 signaling pathway and has equivalent antagonistic effects on PD-L1 and PD-L2 in inhibiting lymphocyte proliferation and effector functions. | ||
V86965 | Benzosceptrin C | 1204605-36-6 | Benzosceptrin C is a programmed cell death ligand 1 (PD-L1) inhibitor that promotes the degradation of PD-L1 through the lysosomal pathway, enhances T cell cytotoxicity and exhibits anti-tumor activity. | |
V3097 | BMS-1 | 1675201-83-8 | BMS-1(also known as PD1-PDL1-IN1, or PD1/PD-L1 inhibitor 1) isa novel and highly potent small molecule inhibitor ofPD-1/PD-L1 protein/protein interactionwith an IC50of 6 nM. | |
V3674 | BMS-1001 | 2113650-03-4 | BMS-1001 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value of 2.25 nM in cell free assays. | |
V3675 | BMS-1166 | 1818314-88-3 | BMS-1166 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value of 1.6 nM in cell free assays. | |
V60028 | BMS-1233 | 2447065-99-6 | BMS-1233 (BMS1233) is novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with an IC50 of<100 nM in the HTRF assay. | |
V3678 | BMS-200 | 1675203-82-3 | BMS-200 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value of 80 nM in cell free assays. | |
V3677 | BMS-242 | 1675204-51-9 | BMS-242 is a novel and potent small molecule inhibitor of the PD-1/PD-L1 protein protein interaction with IC50 value in the range of 6-100 nM in cell free assays. | |
V3256 | BMS-8 | 1675201-90-7 | BMS-8is a novel small molecule inhibitor of the PD-1 (Programmed death-1)/PD-L1 (Programmed death-ligand 1) protein/protein interaction with potential anticancer activities. | |
V86960 | BMS-986189 | 1629665-96-8 | BMS-986189 is a macrocyclic peptide PD-L1 inhibitor (IC50: 1.03 nM) for cancer research. | |
V77194 | BMSpep-57 hydrochloride | BMSpep-57 HCl is a potent macrocyclic peptide inhibitor that can suppress PD-1/PD-L1 interaction with IC50 of 7.68 nM. | ||
V78692 | CD24/Siglec-10 blocking peptide, CSBP | CD24/Siglec-10 blocking peptide, CSBP can not only block the interaction of CD24/Siglec-10, but also block PD-1/PD-L1. | ||
V36345 | CP21 | CP21is a bifunctional immunomodulatory small molecule targeting PD-L1 and CXCL12 with high affinities. | ||
V86964 | CVRARTR | 2349354-64-7 | CVRARTR is an antagonist of programmed cell death ligand 1 (PD-L1) with a KD of 281 nM. | |
V78968 | CYP51/PD-L1-IN-1 | 3032386-49-2 | CYP51/PD-L1-IN-1 (compound L11) is a quinazoline compound with antifungal activity. |