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TLR

Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system. They are single-pass membrane-spanning receptors usually expressed on sentinel cells such as macrophages and dendritic cells, that recognize structurally conserved molecules derived from microbes.

  • Chloroquine
    T868954-05-7
    Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.
    • $54
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  • Resatorvid
    TQ0181243984-11-4
    Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.
    • $45
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  • Polyinosinic-polycytidylic acid
    T2317124939-03-5
    Polyinosinic-polycytidylic acid (Poly(I:C)) is a double-stranded RNA (dsRNA) and a TLR3 agonist. Polyinosinic-polycytidylic acid induces natural immunity in mammals.
    • $45
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  • Pam3CSK4 TFA (112208-00-1 free base)
    TP1067112208-01-2
    Pam3CSK4 TFA (Pam3Cys-Ser-(Lys)4 TFA) is a Toll-like receptor 1 2 agonist with EC50 of 0.47 ng mL for human TLR1 2.
    • $128
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  • ABR-238901
    T391151638200-22-2In house
    ABR-238901 is an oral, active S100A8 A9 blocker that inhibits the interaction of S100A8 A9 with its receptors RAGE(receptor for advanced glycation end products) and TLR4 (toll-like receptor 4). ABR-238901 has potential as a compound for the treatment of myocardial infarction (MI).
    • $125
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  • Schaftoside
    T389851938-32-0
    Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) has antioxidant and anticancer activity.
    • $40
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  • TLR7/8-IN-1
    T380782205095-75-4
    TLR7 8-IN-1, a crystalline TLR7 TLR8 inhibitor from patent WO2019220390 (compound 2b), is a valuable compound for autoimmune disease research.
    • $189
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  • Telratolimod
    T170321359993-59-1
    Telratolimod (MEDI9197) is a toll-like receptors 7 8 agonist. It has an antitumor activity.
    • $175
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  • Pepinh-TRIF TFA
    T76089
    Pepinh-TRIF TFA is a 30 aa peptide associated with the immune system that blocks TRIF signaling by interfering with TLR-TRIF interaction (TLR-TRIF interaction ).
    • $128
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  • Resiquimod
    T6964144875-48-9
    Resiquimod (R848) is a Toll-like receptor 7 8 (TLR7 TLR8) agonist that induces cytokine upregulation. Resiquimod is an immunomodulator with antitumor and antiviral activity.
    • $30
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  • Afimetoran
    T396542171019-55-7
    Afimetoran (BMS-986256) is a toll-like receptor antagonist. Afimetoran can be used in the research of inflammatory and autoimmune diseases.
    • $84
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  • Robinin
    T2S0265301-19-9
    Flavone glycoside from Robinia with antibacterial and diuretic properties; derived from kaempferol.The ability of robinin to reverse the multidrug resistance of the human colon cancer cell line Colo 320 expreβing MDR1 LRP was explored by monitoring their uptake of Rhodamine 123, but was shown to have minimal effect. Robinin (NSC-9222) was detected in lysates of the human breast cancer cell line MCF-7 using liquid chromatography-tandem maβ spectrometry.
    • $68
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  • Enpatoran
    T95702101938-42-3In house
    Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.
    • $122
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  • CU-CPD107
    T353492573912-32-8In house
    CU-CPD107 is a selective agonist of toll-like receptor 8 (TLR8) and also shows activation activity against ssRNA ligands. CU-CPD107 acts as an inhibitor of TLR8 signaling in the presence of R848 (IC50=13.7 μM). CU-CPD107 exhibited coagonist activity in the presence of ssRNA, while CU-CPD107 alone could not affect TLR8 signal transduction.
    • $64
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  • 1V209
    T83161062444-54-5
    1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist known for its anti-tumor properties.
    • $32
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  • C29
    T3502363600-92-4
    C29 is a novel inhibitor of TLR2 1 and TLR2 6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2 1 signaling in murine macrophages.
    • $47
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  • Polyinosinic-polycytidylic acid sodium
    T1251642424-50-0
    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).
    • $38
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  • CpG ODN 10101
    T748741234402-77-7
    CpG ODN 10101 (CPG 10101) is a novel potent and selective Toll-like receptor 9 (TLR9)-containing oligodeoxynucleotide agonist with antiviral activity for the treatment of chronic infections.
    • $297
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  • Atractylenolide I
    T5S016773069-13-3
    1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res
    • $36
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  • Corilagin
    T379523094-69-1
    Corilagin has anti-inflammatory activity. Corilagin has a significant antitumour potential and lower toxicity in normal cells in vitro.Corilagin can enhance the cytotoxicity of both cisplatin and doxorubicin on the Hep3B hepatoma cells.Corilagin has antiviral activity, reduces the cytotoxicity induced by EV71 or CA16 on Vero cells with and IC50 value of 5.6 and 32.33 μg mL, respectively. Corilagin shows the potential to protect against HSV-1-induced encephalitis, and the beneficial effects may be mediated by inhibiting TLR2 signaling pathways.Corilagin has antifibrotics property and is potentiated in treating idiopathic pulmonary fibrosis(IPF), attenuates bleomycin-induced epithelial injury and fibrosis via inactivation of oxidative stress, proinflammatory cytokine release and NF-κB and TGF-β1 signaling. Solvent:Pyridine, Methanol, Ethanol, etc.
    • $43
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  • Okanin
    TN2008484-76-4
    Okanin shows significant activities on both linoleic acid peroxidation inhibition and DPPH radical scavenging effect.
    • $80
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  • E6446 dihydrochloride
    T40681345675-25-3
    E6446 dihydrochloride is a novel synthetic antagonist for nucleic acid-sensing TLRs; potently suppressed DNA stimulation of HEK:TLR9 cells with IC50 of 10 nM.
    • $109
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  • Imiquimod hydrochloride
    T2209199011-78-6
    Imiquimod hydrochloride (R 837 hydrochloride), a selective toll-like receptor 7 (TLR7) agonist, functions as an immune response modifier with in vivo antiviral and antitumor properties, and is utilized in researching external genital and perianal warts, cancer, and COVID-19 [1] [2].
    • $33
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  • Loxoribine
    T15777121288-39-9
    Loxoribine (RWJ 21757) is a guanosine analog. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist. It has anti-viral and anti-tumor activities.Loxoribine is a potent new immunostimulant with a relatively broad spectrum of immunobiological activities.
    • $31
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  • TLR3-IN-1
    T226981279713-77-7
    TLR3-IN-1 (CU CPT 4a) is a selective TLR3 inhibitor (IC50: 3.44 μM in RAW 264.7 cells). It can inhibit TLR3/dsRNA complex-mediated downstream signaling pathways and inhibit the production of TNF-α and IL-1β in whole cells.
    • $48
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  • Sophocarpine
    T66776483-15-4
    Sophocarpine, a major ingredient of Sophora alopecuroides, has a wide range of pharmacological effects.
    • $45
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  • Kdo2-Lipid A ammonium
    T386351246298-62-3
    Kdo2-Lipid A ammonium (KLA) is a selective and potent TLR4 agonist, a lipopolysaccharide.Kdo2-Lipid A ammonium induces the release of TNF and PGE2.
    • $1,245
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  • Hydroxychloroquine sulfate
    T0951747-36-4
    Hydroxychloroquine sulfate (Acidum iopanoicum) inhibits plasmodial heme polymerase. It is a chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa.
    • $48
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  • PF-4878691
    T16506532959-63-0
    PF-4878691 (3M-852A) is a potent and selective Toll-like receptor 7 agonist, designed to dissociate its antiviral and inflammatory activities.
    • $40
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  • TLR4-IN-C34
    T850340592-88-9
    TLR4-IN-C34 is an inhibitor of TLR4, and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis
    • $38
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  • ODN 1826
    T74509202668-42-6
    ODN 1826 is a 20-mer DNA strand, a TLR9 agonist and an immunostimulant, with anti-tumor and cardioprotective effects, promoting apoptosis, and stimulating the production of NO and iNOS. ODN 1826 is a CpG DNA mimetic that can be used as an adjuvant for synthetic vaccines.
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  • Chloroquine phosphate
    T019450-63-5
    Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).
    • $42
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  • Stevioside
    T291157817-89-7
    A natural, noncaloric sweetener with a potency 300 times more than that of regular sucrose. Exhibits transepithelial p-aminohippurate transport via organic anion transport system interference.
    • $35
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  • E6446
    T42061219925-73-1
    E6446 inhibits Toll-like receptor (TLR)7 and 9 signaling. E6446 works in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro. When administered to mice, this compound suppress responses to challenge doses of cytidine-phosphate-guanidine (CpG)-containing DNA, which stimulates TLR9.
    • $84
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  • CU-CPT17e
    T108992109805-75-4
    CU-CPT17e is a potent agonist of TLR(TLR3, TLR8, and TLR9).
    • $213
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  • Gardiquimod
    T153711020412-43-4
    Gardiquimod is a TLR7/8 agonist. When used at concentrations below 10 μM, Gardiquimod specifically activates TLR7. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells.
    • $30
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  • Imiquimod
    T013499011-02-6
    Imiquimod (R 837) is an immune response modifier that acts as a toll-like receptor 7 agonist.
    • $37
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  • CL097
    T384231026249-18-2
    CL097 is an effective agonist of TLR7 and TLR8. CL097 induces pro-inflammatory cytokines in macrophages and NADPH oxidase priming, thereby increasing the fMLF-stimulated ROS production.
    • $58
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  • CU-T12-9
    T150171821387-73-8
    CU-T12-9 is a potent TLR1 2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay). It acts by activating the NFkB pathway, upregulating proinflammatory cytokines, and enhancing TLR1 and TLR2 dimerization.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.
    • $108
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  • Hydroxychloroquine
    T9287118-42-3
    Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol) (HCQ) is an alkalinizing lysosomatropic drug that acts by inducing apoptosis of renal cancer cells in vitro and inhibiting TLR7 9. It is a medication used to prevent and treat malaria, and it's also being studied as an experimental treatment for COVID-19.
    • $30
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  • CU-CPT22
    T150201416324-85-0
    CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 binds at the interface of TLR1 and TLR2 (IC50 = 0.58 μM). It competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1 2 (Ki: 0.41 μM).
    • $44
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  • Semapimod tetrahydrochloride
    T35593164301-51-3
    Semapimod tetrahydrochloride (CPSI-2364 tetrahydrochloride) is a synthetic ornithine mitogen-activated protein kinase blocker and pro-inflammatory cytokine production inhibitor that interferes with macrophage and microglia function. Sematimod tetrahydrochloride inhibits TLR4 signaling, TNF-α, IL-1β, and IL-6, and is used in the study of Crohn's disease and other inflammatory conditions.
    • $99
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  • Sparstolonin B
    T382611259330-61-4
    Sparstolonin B, a selective TLR2 and TLR4 antagonist, is an isocoumarin compound isolated from the tubers of Sparganium stoloniferum and Scirpus yagara with anti-HIV, anticancer, antitumour and anti-inflammatory activities, inhibits selective Toll-like receptors, inhibits free fatty acids It inhibits selective Toll-like receptors, inhibits free fatty acid palmitate-induced chondrocyte inflammation and attenuates post-traumatic arthritis in obese mice, and inhibits lipopolysaccharide-induced inflammation in 3T3-L1 adipocytes, which can be used for validation and mammary carcinoma studies.
    • $97
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  • TH1020
    T87271841460-82-9
    TH1020 is a novel Inhibitor of Toll-Like Receptor 5 (TLR5) Flagellin Complex with promising activity (IC50 =0.85±0.12 μm) and specificity.
    • $38
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  • MyD88-IN-1
    T773532911609-80-6
    MyD88-IN-1 is a potent MyD88 inhibitor with anti-inflammatory activity, inhibiting downstream pathways such as the NF-κB pathway of the Toll-like receptor (TLR) and interleukin-1 (IL-1) receptor family. MyD88-IN-1 may be used in the study of cancer and inflammation treatment.
    • $48
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  • IAXO-102
    T115981115270-63-7
    IAXO-102 is a TLR4 antagonist that negatively regulates TLR4 signaling by inhibiting MAPK and p65 NF-κB phosphorylation, as well as the expression of TLR4-dependent proinflammatory proteins. It also prevents the development of experimental abdominal aortic aneurysm.
    • $89
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  • Protosappanin A
    TJS1779102036-28-2
    Protosappanin A (PTA) has anti-oxidative nitrative activities on brain immune and neuroinflammation through regulation of CD14 TLR4-dependent IKK IκB NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.
    • $89
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  • MD2-IN-1
    T4231111797-22-9
    MD2-IN-1 is a Myeloid differentiation protein 2 (MD2) inhibitor with a KD of 189  μM for the recombinant human MD2 (rhMD2).
    • $54
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  • CU-CPT-9a
    T73172165340-32-7
    CU-CPT-9a is a potent TLR8 inhibitor (IC50 : 0.5 nM), that suppresses TLR8-mediated proinflammatory signaling in various cell lines and human primary cells-
    • $34
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  • Vesatolimod
    T68461228585-88-3
    Vesatolimod (GS-9620) is an effective and specific orally active agonist of Toll-like receptor 7.
    • $45
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