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

Toll-like Receptor (TLR)

Toll-like Receptor (TLR)

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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.

Toll-like Receptor (TLR) Isoform Specific Products:

Toll-like Receptor (TLR) Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-135748A
    Poly (I:C):Kanamycin (1:1) sodium
    		Agonist 99.0%
    Poly (I:C):Kanamycin (1:1) sodium is an isometric complex of Poly (I:C) (HY-135748) and Kanamycin (HY-16566). Poly(I:C) sodium, a synthetic analog of double-stranded RNA, is a TLR3 and retinoic acid-inducible gene I receptor (RIG-I and b>MDA5) agonist. Poly(I:C) sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses and induce apoptosis in cancer cells. Kanamycin is an orally active antibacterial agent (Gram-negative/positive bacteria) that inhibits translocation and causes miscoding by binding to the 70S ribosomal subunit. Kanamycin shows good inhibitory activity against Mycobacterium tuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia.
    Poly (I:C):Kanamycin (1:1) sodium
  • HY-110120
    DSR-6434
    		Agonist 99.32%
    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.
    DSR-6434
  • HY-131952
    TLR7/8/9-IN-1
    		Antagonist 98.51%
    TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC50 = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).
    TLR7/8/9-IN-1
  • HY-103483
    MD2-IN-1
    		Inhibitor 99.88%
    MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189 μM for the recombinant human MD2 (rhMD2).
    MD2-IN-1
  • HY-120149
    Inotodiol
    		Inhibitor 98.29%
    Inotodiol activates p53 signaling pathway, inhibits MMP-2/9, and exhibits antitumor activity in cancer cell HeLa. Inotodiol inhibits the generation of ROS and exhibits antioxidant and neuroprotective effects. Inotodiol inhibits the activation of MAPK and NF-κB signaling pathway, and exhibits anti-inflammatory activity. Inotodiol inhibits TLR-4 mediated TNF-α production (IC50s in BMMC and BMDM is 0.7 μM and 3.0 μM), inhibits the degranulation in mast cell, exhibits anti-allergic activity. Inotodiol is orally active.
    Inotodiol
  • HY-P10586A
    Macrophage-activating lipopeptide 2 TFA
    		Activator 99.83%
    Macrophage-activating lipopeptide 2 TFA is an agonist of Toll like receptors TLR-2/TLR-6. Macrophage-activating lipopeptide-2 enhances endothelial nitric oxide synthase (eNOS) phosphorylation and endothelial cell release of NO, thereby improving vasodilation. Macrophage-activating lipopeptide-2 enhances endothelial adhesion of white blood cells and improve perfusion recovery and collateral growth in the hind limbs of hypercholesterolemic Apoe deficient mice undergoing experimental femoral artery ligation (FAL).
    Macrophage-activating lipopeptide 2 TFA
  • HY-107202GL
    Polyinosinic-polycytidylic acid (GMP Like)
    		Agonist
    Polyinosinic-polycytidylic acid (Poly(I:C)) (GMP Like) is the GMP Like class Polyinosinic-polycytidylic acid (HY-107202), and can be used as pharmaceutical excipients. 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.
    Polyinosinic-polycytidylic acid (GMP Like)
  • HY-N2110
    Phellopterin
    		Inhibitor 99.94%
    Phellopterin, an orally active furocoumarin with multiple biological activities. Phellopterin is a partial agonist of the central benzodiazepine receptors. Phellopterin exerts anti-inflammatory effects by upregulating SIRT1, downregulating ICAM-1 (reducing chronic inflammation, aiding diabetic ulcer healing), inhibiting STAT3 phosphorylation (easing atopic dermatitis inflammation), regulating Akt/PKC pathways (lowering TNF-α-induced VCAM-1 to block monocyte adhesion), and inhibiting TLR4/NF-κB pathway and macrophage M2 polarization (alleviating colitis-related cancers). Phellopterin suppresses ovarian cancer progression via inhibiting the PU.1/CLEC5A/PI3K-AKT loop (inducing cell cycle arrest, apoptosis, DNA damage). Phellopterin alleviates murine diabetes by promoting adipocyte differentiation and increasing PPARγ. Phellopterin also has anti-HSV-1 activity. Phellopterin can be used for studying anti-inflammation, anti-cancer (e.g., ovarian cancer, colitis cancer), blood glucose lowering, anti-diabetes, and anti-virus.
    Phellopterin
  • HY-B0012A
    Pamidronate disodium
    		Inhibitor 98.0%
    Pamidronate disodium (CGP 23339A), the second-generation nitrogen-containing bisphosphonate, is an inhibitor of bone loss. Pamidronate disodium significantly inhibits subchondral bone loss in early osteoarthritis by upregulating the expression of osteoprotegerin in cartilage and subchondral bone, and inhibiting the expression of RANKL and MMP-9 in both tissues, as well as TLR-4 in cartilage, thereby alleviating cartilage degeneration. Additionally, Pamidronate disodium can inhibit the signaling of Wnt and β-catenin, and is applicable for research on osteoporosis and osteosarcoma.
    Pamidronate disodium
  • HY-P10227
    Xelafaslatide
    		Inhibitor 99.88%
    Xelafaslatide (ONL-1204) is a Fas receptor antagonist. Xelafaslatide blocks the Fas receptor signaling pathway and inhibits downstream apoptosis and inflammatory pathways. Xelafaslatide suppresses neuroinflammation and microglial activation in glaucoma models, protects retinal ganglion cells and prevents axonal degeneration. Xelafaslatide is applicable to relevant research on glaucoma.
    Xelafaslatide
  • HY-150750
    ODN M362
    		Agonist
    ODN M362, a class C oligodeoxynucleotide, is a TLR-9 agonist and can be used as a vaccine adjuvant. ODN M362 induces cancer cell apoptosis.
    ODN M362
  • HY-128598
    MD2-TLR4-IN-1
    		Inhibitor 98.16%
    MD2-TLR4-IN-1 is a myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex antagonist. MD2-TLR4-IN-1 inhibits Lipopolysaccharides (HY-D1056) (LPS)-induced expression of TNF-α and IL-6 in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively. MD2-TLR4-IN-1 can be used for the study of acute lung injury (ALI).
    MD2-TLR4-IN-1
  • HY-128799A
    CL097 hydrochloride
    		Agonist 99.96%
    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 hydrochloride
  • HY-159747
    Aluminum hydroxide adjuvant aluminum : 4~6 mg/mL
    		Activator
    Aluminum hydroxide adjuvant (aluminum : 4~6 mg/mL) is a micron level water-based aluminum hydroxide adjuvant. The aluminum content is 4 - 6 mg/ml. It has a strong adsorption capacity for negatively charged antigens, a significant sustained-release effect, no stress response, high safety, and can effectively induce immune responses in the body. It is suitable for various veterinary vaccines, including inactivated vaccines or gene-engineered subunit vaccines for bacterial and viral diseases of livestock and poultry.
    Aluminum hydroxide adjuvant aluminum : 4~6 mg/mL
  • HY-W082785A
    L6H21
    		Inhibitor 99.19%
    L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a high affinity and low KD value of 33.3 μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research.
    L6H21
  • HY-N2055
    Kaempferol 3-O-sophoroside
    		Inhibitor 99.41%
    Kaempferol 3-O-sophoroside is an orally active derivative of Kaempferol. It exhibits anti-inflammatory, analgesic, and antidepressant effects. Kaempferol 3-O-sophoroside is an inhibitor of the cell surface receptor toll-like receptor (TLR) 2/4 for High mobility group box 1 (HMGB1), and it also exerts anti-inflammatory effects by blocking the activation of NF-κB expression and the production of TNF-α. Kaempferol 3-O-sophoroside promotes the production of brain-derived neurotrophic factor (BDNF) and enhances autophagy by binding to AMP-activated protein kinase (AMPK), thereby exerting antidepressant effects. Kaempferol 3-O-sophoroside holds promise for research in the fields of inflammation and neurodegenerative diseases.
    Kaempferol 3-O-sophoroside
  • HY-N1508
    Ecliptasaponin A
    		Inhibitor 99.81%
    Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors.
    Ecliptasaponin A
  • HY-150745A
    ODN 24987 sodium
    		99.08%
    ODN 24987 sodium is a Guanine-modified inhibitory oligonucleotides (ODN), targeting TLR9. ODN 24987 can inhibit IL-6 and IFN-α release. ODN 24987 sodium can be used for research immune disorders. ODN 24987 sequence: 5’-C-C-T-G-G-C-c7G-G-G-G-3’.
    ODN 24987 sodium
  • HY-150217A
    CpG ODN 10101 sodium
    		Agonist 98.84%
    CpG ODN 10101 sodium, a synthetic oligodeoxynucleotide (ODN), is a toll-like receptor 9 (TLR9) agonist. CpG ODN 10101 sodium is a potent inducer of cytokine/chemokine expression ex vivo when used in combination with HH2(VQLRIRVAVIRA-NH2). CpG ODN 10101 sodium induces IFN- secretion from dendritic cells (DCs) and stimulates B-cells.CpG ODN 10101 sodium has antiviral and immunomodulatory properties that can influence chronic infection with HCV.
    CpG ODN 10101 sodium
  • HY-18976
    UF010
    		99.83%
    UF010 is a selective inhibitor of class I HDAC. UF010 has cytotoxicity to cancer cells and reduces neuroinflammation in the hippocampus. UF010 can be used for the research of neurological diseases.
    UF010
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Toll-like Receptor (TLR) Isoform Comparison

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