Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic double-stranded RNA (dsRNA), which is a Toll-like receptor 3 (TLR3) agonist. Polyinosinic-polycytidylic acid presents in some viruses, and is therefore commonly used to model the actions of extracellular dsRNA.
Okanin, effective constituent of the flower tea Coreopsis tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/NF-κB signaling pathways[1].
A potent TLR7/8 agonist and cytokine inducer; stimulates type I interferon (IFN) and other cytokines such as TNF-alpha, IL-12, and IFN-gamma from rat peripheral blood mononuclear cells; induces IL-12 and COX-2 expression in mDC from HIV+ and HIV- individuals, and inhibits H3N2 influenza viral replication in the nasal cavity; potentiates NK cytotoxicity, and shows antitumor effects in scid/B6 mice and scid/NOD mice.
MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189 μM for the recombinant human MD2 (rhMD2).
SM-276001 is a potent selective TLR7 agonist that can induce antitumor immune responses. SM-276001 is an orally active interferon (IFN) inducer[1][2].
ODN 2336 is a A-Class CpG ODN (oligodeoxynucleotides), is a potent TLR9 agonist. ODN 2336 induces the production of IFN-α. ODN 2336 up-regulates the expression of IP-10 mRNA and IL-18 mRNA. ODN 2336 can be used as adjuvant of vaccines[1][2][3].
Loxoribine (7-Allyl-8-oxoguanosine) is a guanosine analog with anti-viral and anti-tumor activities. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist[1][2][3].
Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.
Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling[1].
Selgantolimod (GS-9688; GS9688) is a novel toll-like receptor TLR8 modulator for the treatment of HIV infection.
Mumefural is a bioactive component of the processed fruit of Prunus mume Sieb. Mumefural inhibits platelet aggregation. Mumefural shows anti-thrombotic effects and ameliorates cognitive impairment[1][2].
ODN M326 (CpG-ODN M326) is a potent TLR9 agonist. ODN M326 induces the production of TNF. ODN M326 can be used as a vaccine adjuvant[1].
Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 also activates iNOS expression and NO production in mouse macrophages[1][2][3].
Polyinosinic acid is a single stranded homonucleic acid, which is a Toll-like Receptor 3 (TLR3) agonist. Polyinosinic acid enhances cellular immune response through TLR3 and TRIF. Polyinosinic acid has potential applications in immune regulation[1].
Toll-like receptor modulator is a modulator of TLR7/8, which modulates immune function.
TLR9-IN-1 is a potent and selective TLR9 inhibitor with an IC50 value of 7 nM for human TLR9. TLR9-IN-1 can be used for researching diseases associated with undesirable immune response[1].
Imiquimod is an immune response modifier and a toll-like receptor 7 agonist.
Cobitolimod sodium is a DNA oligonucleotide agonist of TLR-9 with anti-inflammatory activity. Cobitolimod sodium inhibits Th17 cells and induces anti-inflammatory FoxP3 and IL-10 expression, inhibiting the IL-17 signaling pathway[1].
TLR7 agonist 14 (compound 17b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 14 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations[1].
Polygalasaponin F, an oleanane-type triterpenoid saponin extracted from Polygala japonica, decreases the release of the inflammatory cytokine tumor necrosis factor a (TNFa). Polygalasaponin F reduces neuroinflammatory cytokine secretion through the regulation of the TLR4-PI3K/AKT-NF-kB signaling pathway [1].
Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α.
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis[1][2].
TLR7 agonist 5 (compound IIb-11) is an TLR7 agonist with an EC50 value of ~4 nM[1].
M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis[1].
ODN 21158 is a potent G-modified TLR3 andTLR9inhibitor. ODN 21158 shows no cytotoxic. ODN 21158 nhibits IFN-α secretion in a dose dependent manner[1].
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect[1][2].
TLR7 agonist 16 (compound 16d) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 16 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations[1].
Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) 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 sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis[1][2].
CpG ODN 10101, a synthetic oligodeoxynucleotide (ODN), is a toll-like receptor 9 (TLR9) agonist. CpG ODN 10101 is a potent inducer of cytokine/chemokine expression ex vivo when used in combination with HH2(VQLRIRVAVIRA-NH2). CpG ODN 10101 induces IFN- secretion from dendritic cells (DCs) and stimulates B-cells.CpG ODN 10101 has antiviral and immunomodulatory properties that can influence chronic infection with HCV[1][2].
Guignardone L is a metabolite isolated from the endophytic fungus Guignardia mangiferae with toll-like receptor 3 regulating activity[1].