PD-L1

Anti-Mouse PD-L1 Antibody (10F.9G2) is an IgG-class antibody against mouse PD-L1.

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.

Human PD-L1 Inhibitor V is a peptide that binds to the human PD-1 protein with an affinity characterized by a dissociation constant (Kd) of 3.32 μM, effectively inhibiting the hPD-1/hPD-L1 interaction [1].

PD-L1-IN-3 (Compound 4a) functions as an inhibitor of the PD-1/PD-L1 axis, with an IC50 value of 4.97 nM for PD-L1 inhibition and an EC50 value of 2.70 μM for Jurkat T cell modulation. It antagonizes the PD-1/PD-L1 interaction by binding to the PD-L1 dimer, obstructing PD-1 signaling. This compound is utilized in research pertaining to lung cancer and melanoma [1].

Human membrane-bound PD-L1 polypeptide serves as an antigen for inducing the production of PD-L1 antibodies [1].

Human PD-L1 inhibitor IV is a polypeptide compound that competitively inhibits the human PD-1 protein. It has a Kd value of 1.38 μM and effectively blocks the interaction between hPD-1 and hPD-L1.

Human PD-L1 inhibitor III [Human PD-L1 inhibitor] is a bioactive compound designed to inhibit the programmed death-ligand 1 (PD-L1) protein in humans.

Human PD-L1 inhibitor II, a potent PD-L1 inhibitor, exhibits strong anti-cancer activity.

Human PD-L1 inhibitor I is a peptide ligand that specifically inhibits the interaction between human PD-L1 and human PD-1, exhibiting a KD value of 3.39 μM, indicating its binding affinity. The presence of Human PD-L1 inhibitor I disrupts their binding, thereby attenuating their respective functions.

BMS-1 (PD-1/PD-L1 inhibitor 1) is an inhibitor of the PD1-PD-L1 protein-protein interaction. It also acts as an immunomodulator. Programmed death ligand 1 (PD-L1) is a protein in humans that is encoded by the CD274 gene and the upregulation of PD-L1 allows Ys to evade the host immune system. High tumor expression of PD-L1 was associated with increased tumor aggressiveness and a 4.5-fold increased risk of death.

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.

PD-1/PD-L1-IN-NP19, a PD-1/PD-L1 inhibitor, exhibits an IC50 of 12.5 nM against the human PD-1/PD-L1 interaction, potentially activating the tumor immune microenvironment and contributing to its antitumor effects[1].

PD-1/PD-L1-IN-26 (Compound II-14) is a potent PD-1/PD-L1 inhibitor with an IC50 of 0.0380 μM. It enhances the immune microenvironment by promoting CD4+ T cell infiltration into tumor tissues, suggesting its potential application in cancer research [1].

PD-1/PD-L1-IN-27 is a potent inhibitor of PD-1/PD-L1, with an IC50 of 134 nM, and demonstrates antitumor effects with minimal T cell cytotoxicity. It activates CD8+ T cells and mitigates T cell exhaustion [1].

PD-L1-IN-2, a Naamidine J derivative, serves as a promising antineoplastic immunomodulator by hindering PD-L1 activity. In vivo studies indicate that it suppresses PD-L1 expression and amplifies tumor-infiltrating T-cell response, thus exerting anticancer effects. This compound is particularly utilized in the investigation of colorectal cancer [1].

PD-1/PD-L1-IN-31 is a potent inhibitor of PD-1/PD-L1 (IC50=2.2 nM) that enhances IFN-γ secretion and activates the immune response of peripheral blood mononuclear cells (PBMCs), leading to the inhibition of tumor cells [1].

PD-1/PD-L1-IN-34 (Compound (1S,2S)-A25) effectively inhibits the PD-1/PD-L1 interaction (IC50 = 0.029 μM) and demonstrates selective binding affinity to PD-L1 (KD = 0.1554 μM), resulting in the activation of the immune microenvironment and suppression of tumor growth [1].

PD-1/PD-L1-IN-32 (compound A56) is a potent inhibitor of PD-1/PD-L1 with an IC50 value of 2.4 nM, demonstrating significant anticancer activity. It effectively suppresses tumor growth in the hPD-L1 MC38 humanized mouse model and exhibits negligible toxicity to the normal functions of the mice [1].

PD-1/PD-L1-IN-33 (Compound N11), a PD-1/PD-L1 inhibitor with an IC50 of 6.3 nM, effectively impedes the interaction between PD-1 and PD-L1. It enhances T-cell proliferation, activation, and infiltration within tumor environments, thereby exhibiting immunomodulatory and anticancer properties [1].

PD-1/PD-L1-IN-10 is an orally available PD-1/PD-L1 inhibitor (IC50 value of 2.7 nM) that shows anti-tumor activity.

PROTAC PD-L1 degrader-2, an orally administered compound, targets HPK1 and boosts the efficacy of PD-L1 antibody therapy.

PD-L1 ligand 1 is classified as a PROTAC-targeted protein ligand, primarily utilized as a degradation agent for PD-L1.

PD-L1/VISTA-IN-1 (Compound P17) is an orally active dual inhibitor targeting PD-L1 and VISTA. It effectively hinders the PD-1/PD-L1 interaction (IC50: 0.1492 μM) and the VISTA pathway (KD: 0.2723 μM), leading to the reactivation of T cells. Additionally, PD-L1/VISTA-IN-1 exhibits antitumor activity.

PD-L1/HDAC-IN-1 (Compound 14) is an inhibitor of PD-L1 and HDAC, effectively blocking PD-1/PD-L1 interaction as well as HDAC2 and HDAC3 with IC50 values of 88.10, 27.98, and 14.47 nM, respectively. It exhibits mild cytotoxicity in MCF-7 cells (IC50=19.34 μM) and enhances the expression of PD-L1 and CXCL10, promoting antitumor immune responses by recruiting T cell infiltration into the tumor microenvironment (TME).