1. Signaling Pathways
  2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system. They are single, membrane-spanning, non-catalytic receptors usually expressed in sentinel cells such as macrophages and dendritic cells, that recognize structurally conserved molecules derived from microbes. Once these microbes have breached physical barriers such as the skin or intestinal tract mucosa, they are recognized by TLRs, which activate immune cell responses. The TLRs include TLR1, TLR2, TLR3, TLR4, TLR5, TLR6, TLR7, TLR8, TLR9, TLR10, TLR11, TLR12, and TLR13. Toll-Like Receptors (TLRs) play a critical role in the early innate immune response to invading pathogens by sensing microorganism and are involved in sensing endogenous danger signals. TLRs are evolutionarily conserved receptors are homologues of the Drosophila Toll protein, discovered to be important for defense against microbial infection. TLRs recognize highly conserved structural motifs known as pathogen-associated microbial patterns (PAMPs), which are exclusively expressed by microbial pathogens.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-110353
    CU-T12-9
    Agonist 98.94%
    CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
    CU-T12-9
  • HY-109137
    Selgantolimod
    Agonist 98.23%
    Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.
    Selgantolimod
  • HY-U00435
    Neoseptin 3
    Agonist 99.57%
    Neoseptin 3 is a Toll-like receptor 4/myeloid differentiation factor 2 (mTLR4/MD-2) agonist with an EC50 of 18.5 μM.
    Neoseptin 3
  • HY-107202A
    Poly (I:C):Kanamycin (1:1)
    Poly (I:C):Kanamycin (1:1) is a mixture of poly (I:C) and kanamycin. Poly(I:C) is a synthetic double-stranded RNA (dsRNA), which is a Toll-like receptor 3 (TLR3) agonist. Kanamycin is positively charged (poly-NH3) and can thus neutralize the negative charge of Poly I:C and thereby stabilized the molecule.
    Poly (I:C):Kanamycin (1:1)
  • HY-150751
    ODN TTAGGG
    Antagonist 99.87%
    ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.
    ODN TTAGGG
  • HY-N0703
    Schaftoside
    Inhibitor 99.67%
    Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
    Schaftoside
  • HY-134581A
    Enpatoran hydrochloride
    Inhibitor 99.33%
    Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research.
    Enpatoran hydrochloride
  • HY-128799
    CL097
    Agonist 99.89%
    CL097, a potent TLR7 and TLR8 agonist, induces pro-inflammatory cytokines in macrophages. CL097 induces NADPH oxidase priming, resulting in an increase of the fMLF-stimulated ROS production.
    CL097
  • HY-N0774
    Isofraxidin
    Inhibitor 99.00%
    Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
    Isofraxidin
  • HY-103698A
    TLR7/8 agonist 1 dihydrochloride
    Agonist 99.89%
    TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.
    TLR7/8 agonist 1 dihydrochloride
  • HY-117066
    CL075
    Agonist 99.25%
    CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.
    CL075
  • HY-150726
    ODN 1668
    Agonist ≥99.0%
    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’.
    ODN 1668
  • HY-116213
    Sparstolonin B
    Antagonist 99.54%
    Sparstolonin B acts as a selective TLR2 and TLR4 antagonist and selectively blocks TLR2- and TLR4-mediated inflammatory signaling. Sparstolonin B has anti-HIV and anticancer activities.
    Sparstolonin B
  • HY-N1346
    Robinin
    Inhibitor 98.77%
    Robinin is a flavonoid that can be extracted from the leaves of purple cowpea, inhibiting TGF-β, TLR4/NF-κB and TLR2-PI3k-AKT signaling pathways. Robinin exerts anti-inflammatory and anti-tumor effects. The combination of Robinin and Methotrexate (HY-14519) reduces inflammation in experimental arthritis, Robinin can decrease the Doxorubicin (HY-15142A) induced cardiac toxicity effect.
    Robinin
  • HY-150738
    ODN 2088
    Antagonist
    ODN 2088 is a potent TLR3, TLR7 and TLR9 inhibitor. ODN 2088 shows no cytotoxic. ODN 2088 inhibits the release of IFN-α and IL-6.
    ODN 2088
  • HY-103697A
    Gardiquimod diTFA
    Agonist ≥99.0%
    Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
    Gardiquimod diTFA
  • HY-N6949
    Juglone
    Inhibitor
    Juglone (5-hydroxy-1,4-naphthalenedione) is a yellow dye that can be extracted from Juglans regia. Juglone induces apoptosis through the mitochondrial pathway. Juglone has antibacterial and antitumor activity .
    Juglone
  • HY-N0795
    Procyanidin B1
    Antagonist 99.28%
    Procyanidin B1 is a polyphenolic flavonoid isolated from commonly eaten fruits, binds to TLR4/MD-2 complex, and has anti-inflammatory activity.
    Procyanidin B1
  • HY-P2036A
    FSL-1 TFA
    Agonist 99.76%
    FSL-1 TFA, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection. FSL-1 TFA induces MMP-9 production through TLR2 and NF-κB/AP-1 signaling pathways in monocytic THP-1 cells.
    FSL-1 TFA
  • HY-P1439A
    RS 09 TFA
    Agonist 99.81%
    RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
    RS 09 TFA
Cat. No. Product Name / Synonyms Species Source
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