CD80-IN-3 is a potent CD80 inhibitor and inhibits CD80/CD28 interaction (Kd: 125 nM; EC50: 630 nM).

Davoceticept (ALPN-202; CD80 vIgD-Fc), a monoclonal antibody that targets CTLA-4, is comprised of the (1-107) fragment of CD80 fused to the IGHG1 Fc domain through a peptidyl linker. It is commonly produced in CHO (Chinese Hamster Ovary) cells [1].

Durvalumab (MEDI 4736) is a humanized monoclonal antibody targeting PD-L1. It can block the interaction of PD-L1 with PD-1 and CD80, with IC50 values of 0.1 and 0.04 nM, respectively. Durvalumab is often used in combination with platinum-based compounds for the treatment of non-small cell lung cancer and advanced hepatocellular carcinoma cells.

Cyclic di-IMP (sodium salt) (c-di-IMP) is a synthetic second messenger structurally related to the bacterial second messengers cyclic di-GMP and cyclic di-AMP . C-di-IMP has adjuvant properties when co-administered with antigens in vitro and by mucosal routes in vivo. C-di-IMP enriches the population of MHC class I and II, CD80, CD86, CD40, and CD54 positive dendritic cells derived from murine bone marrow. It also stimulates macrophages at 500 ng/ml. Mice immunized with β-galactosidase (β-gal) plus c-di-IMP through the intranasal route show a humoral immune response, evidenced by an increase in IgG titers up to 2-fold compared to mice immunized with β-gal alone. Mice immunized with β-gal plus c-di-IMP also exhibit a Th1/Th2 response, indicating that the adjuvant activity of c-di-IMP leads to a cellular immune response as well.

M04 acts as a stimulator of interferon genes (STING) agonist, effectively inducing IFN reporter gene expression in HEK293T cells equipped with wild-type human STING. Its activity is specific, not affecting HEK293T cells with the R71H-G230A-R293Q (HAQ) human STING variant or mouse RAW 264.7 cells, showcasing allelic- and species-dependent effects at a concentration of 75 µM. This compound also stimulates the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At 50 µM, M04 enhances human monocyte-derived dendritic cells' expression of HLA-DR (MHC class II receptor) and co-stimulatory molecules CD40, CD80, and CD86, improving T cell cross-priming in an ex vivo assay.

ODN D-SL03, a class C CpG oligonucleotide, effectively stimulates peripheral blood mononuclear cells (PBMCs) to produce high levels of IFN-α. It activates human B cells, NK cells, and mononuclear cells, elevating the expression of CD80, CD86, and HLA-DR on PBMC subsets' surface. Additionally, ODN D-SL03 impedes tumor growth. Its sequence: 5'-tcgcgaacgttcgccgcgttcgaacgcgg-3' [1].

PD-1/PD-L1-IN 3 TFA, a macrocyclic peptide, serves as a potent and selective inhibitor of PD-1/PD-L1 interaction. This compound disrupts PD-L1's binding with PD-1 and CD80 by directly binding to PD-L1, exhibiting IC50 values of 5.60 nM and 7.04 nM, respectively. It is utilized in the research of numerous illnesses, such as cancer and infectious diseases [1].

Galiximab (IDEC 114), a primatized IgG1 lambda monoclonal antibody, targets the CD80 antigen. It combines primatized (cynomologous monkeys) variable regions with human constant regions. This compound is utilized in the study of B-cell lymphoma [1].

Macluraxanthone (3-Hydroxyblancoxanthone) has many biological activities including anticholinesterase, antioxidant, anticancer, antimalarial, anti-inflammatory and immunomodulatory effects. macluraxanthone promotes the polarization of M1-like pro-inflammatory macrophages by increasing the percentage of macrophages expressing CD86 while decreasing their expression of CD14, CD11b and CD80. Macluraxanthone significantly reduced the production of TNF-α and IL-10 cytokines in the presence of the pro-inflammatory stimulant lipopolysaccharide.

LCC-12, a derivative of the biguanide metformin, acts as a copper (II) chelator. It efficiently forms a monomeric bond with copper (II) and at 20 µM, it mitigates hydrogen peroxide-induced oxidation from NADH to NAD+. At a concentration of 10 µM, LCC-12 significantly reduces the secretion of cytokines IL-1β, IL-2, IL-6, IL-8, and TNF-α, along with the downregulation of JAK2, STAT2, and IL-1 receptor-associated kinase 4 (IRAK4) in primary human cytokine-activated monocyte-derived macrophages (MDMs). Additionally, it decreases the presence of CD80+ and CD86+ within these macrophages at 10 µM. When administered at 0.3 mg/kg per day, LCC-12 enhances survival rates in mouse models exposed to sepsis, triggered either by lipopolysaccharide (LPS) or cecal ligation and puncture.