Targeted Pattern Recognition Receptor-Type Adjuvants

Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis.

Vadimezan (DMXAA), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan is unable to activate human STING. Vadimezan has anti-influenza virus H1N1-PR8 activities.

2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP is produced in mammalian cells in response to DNA in the cytoplasm.

diABZI STING agonist-1 is a tautomerism of diABZI STING agonist-1 tautomerism (HY-112921). diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

ODN 1826 is a class B CpG ODN (oligodeoxynucleotide) and TLR9 agonist. ODN 1826 induces NO and iNOS production and enhances Apoptosis. ODN 1826 enhances immune surveillance. ODN 1826 increases aortic atherosclerotic plaque size. ODN 1826 has antitumor activity against lung cancer, glioma and melanoma.

2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP sodium binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP sodium is produced in mammalian cells in response to DNA in the cytoplasm.

2’3’-c-di-AM(PS)2 (Rp,Rp) (ADU-S100), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.

2’3’-c-di-AM(PS)2 (Rp,Rp) disodium salt (ADU-S100 disodium salt) is an activator of stimulator of interferon genes (STING).

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist, with EC₅₀s of 130, 186 nM for human and mouse, respectively.

cGAMP (Cyclic GMP-AMP) functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.

ODN 1826 sodium is a class B CpG ODN (oligodeoxynucleotide) and TLR9 agonist. ODN 1826 sodium induces NO and iNOS production and enhances Apoptosis. ODN 1826 sodium enhances immune surveillance. ODN 1826 sodium increases aortic atherosclerotic plaque size. ODN 1826 sodium has antitumor activity against lung cancer, glioma and melanoma.

Agatolimod sodium (ODN 2006) is a class B CpG ODN and is a TLR9 agonist. Agatolimod sodium can be used as vaccine adjuvant. Agatolimod sodium can be used for the research of cancer. Sequence: 5’-TCGTCGTTTTGTCGTTTTGTCGTT-3’.

2’3’-c-di-AM(PS)2 (Rp,Rp) ammonium salt (ADU-S100 ammonium salt), an activator of stimulator of interferon genes (STING), leads to potent and systemic tumor regression and immunity.

Agatolimod ((ODN 2006; PF-3512676; CpG 7909)) is a TLR9 agonist and immunomodulator with an EC₅₀ of 180 nM against human TLR9. Agatolimod activates and upregulates the expression of both TLR9 and TLR6, and mediates downstream signaling pathways via IRAK4, IRF5, IRF7. Agatolimod induces Th1-type innate and adaptive immune responses, activates various immune cells and promotes antigen presentation, regulates antibody levels and immune cell infiltration, upregulates the secretion of multiple cytokines, induces apoptosis and cell cycle arrest, enhances cytotoxicity, and clears intracellular Salmonella. Agatolimod is applicable to research on COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis.

c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.

ODN 2216 sodium is a type A CpG oligodeoxynucleotide vaccine adjuvant and a TLR9 agonist. ODN 2216 sodium interacts with TLR9 in the lysosomes of CD4⁺ T cells and activates feedback-dependent signaling pathways. ODN 2216 sodium induces the production of type I interferons, IL-6 and TGF-β via the IRAK4/IRF7 axis, while increasing intracellular ATP levels. ODN 2216 sodium not only induces the differentiation of CD4⁺ T cells into anti-inflammatory Th3-like regulatory phenotypes to inhibit autologous proliferation, but also enhances the specific CD8⁺ T cell-mediated cytotoxicity against Mammaglobin-A in breast cancer cells. ODN 2216 sodium is widely used in studies related to breast cancer and systemic lupus erythematosus.

ODN 2216 is a type A CpG oligodeoxynucleotide vaccine adjuvant and a TLR9 agonist. ODN 2216 interacts with TLR9 in the lysosomes of CD4⁺ T cells and activates feedback-dependent signaling pathways. ODN 2216 induces the production of type I interferons, IL-6 and TGF-β via the IRAK4/IRF7 axis, while increasing intracellular ATP levels. ODN 2216 not only induces the differentiation of CD4⁺ T cells into anti-inflammatory Th3-like regulatory phenotypes to inhibit autologous proliferation, but also enhances the specific CD8⁺ T cell-mediated cytotoxicity against Mammaglobin-A in breast cancer cells. ODN 2216 is widely used in studies related to breast cancer and systemic lupus erythematosus.

Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research.

ISD sodium is an interferon-stimulatory DNA, a 45 bp non-CpG double-stranded oligonucleotide derived from the genome of Listeria monocytogenes. ISD sodium potently induces type I interferon production via the cGAS‑STING‑TBK1‑IRF3 pathway.

ODN 1018 (1018 ISS) sodium is a TLR9 agonist and immune modulator. ODN 1018 sodium exhibits adjuvant activity and augments CD8+ T cell responses with LNP-encapsulated OVA peptides. ODN 1018 sodium triggers sustained suppression of allergic airway inflammation. ODN 1018 sodium can be used for the research of allergic asthma and systemic lupus erythematosus.