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).
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.
Toll-like receptor modulator is a modulator of TLR7/8, which modulates immune function.
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].
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis[1][2].
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].
Guignardone L is a metabolite isolated from the endophytic fungus Guignardia mangiferae with toll-like receptor 3 regulating activity[1].
E6446 is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses.
Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM[1][2].
UC-1V150 is a specific TLR7 (Toll-like receptor) agonist that stimulates cellular immune responses and has anti-tumor activity. UC-1V150 can be used to synthesize ISAC (Immune-Stimulating Antibody Conjugates) molecule[1][2].
Chloroquine (diphosphate) is an antimalarial and anti-inflammatory drug widely used to treat malaria and rheumatoid arthritis. Chloroquine is an inhibitor of autophagy and toll-like receptors (TLRs).
Cavrotolimod is an immunostimulatory spherical nucleic acid (SNA) modified with type B CpG oligonucleotides designed to agonize TLR9 and elicit immune responses useful in oncology applications.
TLR7 agonist 15 (compound 16b) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 15 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations[1].
TLR7/8 agonist 7 (compound 10) is a TLR7/8 agonist. TLR7/8 agonist 7 activates a variety of immune cells and it can be used to synthesize immune stimulating antibody conjugate (ISAC) molecules. TLR7/8 agonist 7 can be used for the research of immunity[1].
Agatolimod (ODN 2006), a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. Agatolimod is also an optimal CpG sequence for humans. Agatolimod stimulates very strong production of NO2 and IL-6 in HD11 cells. Agatolimod can be used for breast cancer research. Sequence: 5'-tcgtcgttttgtcgttttgtcgtt-3'[1][2].
Monophosphoryl lipid A (Glucopyranosyl lipid A) is a toll-like receptor 4 agonist. Monophosphoryl lipid A is derived from the cell wall of nonpathogenic Salmonella. Monophosphoryl lipid A can be used for the research of immunization and vaccine[1].
TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8[1].
Eritoran is a Toll-like receptor 4 (TLR4) antagonist. Eritoran protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran inhibits pathogenesis of filovirus infection[1].
Imiquimod maleate is an immune response modifier that acts as a toll-like receptor 7agonist.
ODN 1668, a class B CpG ODN (oligodeoxynucleotide), is a TLR-9 agonist. ODN 1668 is an immunostimulatory sequence and can be used as vaccine adjuvant. Sequence: 5'-tccatgacgttcctgatgct-3’[1][2].
Imiquimod hydrochloride is an immune response modifier that acts as a toll-like receptor 7agonist.
Agatolimod sodium (ODN 7909) 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’[1][2].
L6H21, a derivative of chalcone, is an orally active and potent MD-2 (myeloid differentiation factor 2) inhibitor. L6H21 inhibits TLR4-NF-κB signaling and NLRP3 inflammasome activation in macrophages. L6H21 inhibits EtOH + LPS-induced apoptosis and mitochondrial damage in RAW264.7 cells. L6H21 effectively inhibits EtOH + LPS-induced hepatic fat accumulation and liver injury. L6H21 shows neuroprotective effect in a model of prediabetes[1][2].
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively[1].