Catalog No.
Product Name
Application
Product Information
Citations
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TLR7 agonist
Imiquimod (Aldara) is a a heterocyclic imidazoquinoline amide that acts as an immune response modifier.- David Diaz-Carballo, .et al. , Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Kunishita Y, .et al. , Front Immunol, 2020, Feb 7;11:98 PMID: 32117252
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TLR7/8 Agonist
Resiquimod is an immune response modifier that acts as a potent TLR 7/8 agonist. Phase 2.- Honglin Huang, .et al. , Acta Pharmaceutica Sinica B, 2023, Ocb,26 PMID: 38486995
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TLR Inhibitor
TLR2-IN-C29 is an inhibitor of TLR2/1 and TLR2/6 signaling.- Sholihah, I.A., .et al. , BioNanoSci, 2026, 16, 396
- Qian-Lu Wang, .et al. , Mol Immunol, 2021, Oct;138:99-109 PMID: 34365196
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TLR8 agonist
VTX-2337 is a small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities.- Yinwen Cheng, .et al. , Sci Rep, 2021, Jan 15;11(1):1535 PMID: 33452311
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TLR7 agonist
GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7.- Yu-Geun Ji, .et al. , J Pharm Biomed Anal, 2019, 12 November, 112987 PMID: 31761376
- Zhikuan Zhang, .et al. , Cell Reports, 2018, 25(12): 3371-3381.e5 PMID: 30566863
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TLR-3 Agonist
Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA that serves as an agonist for toll-like receptor 3 (TLR3) and RIG-I-like receptors, including RIG-I and MDA5. This compound enhances both innate and adaptive immune responses, making it valuable in vaccine development as an adjuvant. Additionally, Poly(I:C) influences the tumor microenvironment and can directly induce apoptosis in cancer cells, highlighting its potential applications in cancer immunotherapy and research. -
PROTAC CSK Degrader
DB-3-291 is a potent and selective PROTAC degrader targeting the protein CSK, exhibiting a Kd of 1 nM. This compound facilitates the degradation of CSK through its specific interaction with the E3 ligase, enabling in-depth studies of CSK-related biological pathways and providing insights into potential therapeutic strategies. It is valuable for researchers investigating targeted protein degradation and cancer biology. -
TLR4 Agonist
GlcNAc-MurNAc is a disaccharide that acts as a TLR4 agonist, exhibiting a binding affinity (Kd) of 383 μM for murine TLR4. This compound directly interacts with TLR4, subsequently activating the downstream NF-κB and IRF signaling pathways. Research indicates that GlcNAc-MurNAc ameliorates dextran sulfate sodium salt (DSS)-induced colitis in mice via a TLR4-dependent mechanism, making it a valuable tool for the investigation of inflammatory bowel disease. -
TLR3 Agonist
Polyinosinic-polycytidylic acid sodium is a synthetic analogue of double-stranded RNA and acts as an agonist for toll-like receptor 3 (TLR3) and RIG-I-like receptors. It serves as a potent immunomodulator, enhancing both innate and adaptive immune responses, making it valuable for vaccine development. Additionally, Poly(I:C) sodium can influence the tumor microenvironment and directly induce apoptosis in cancer cells, thus providing significant potential in cancer research and therapy. -
TLR9 Agonist
ODN 1826 is a class B CpG oligodeoxynucleotide that acts as an agonist for Toll-like receptor 9 (TLR9). It stimulates the production of nitric oxide (NO) and inducible nitric oxide synthase (iNOS), promoting apoptosis and enhancing immune surveillance. This compound is also associated with increased aortic atherosclerotic plaque size and exhibits antitumor activity against various cancer types, including lung cancer, glioma, and melanoma. ODN 1826 is valuable for researching immune response mechanisms and potential cancer therapies. -
TLR7/8 Antagonist
Afimetoran is a selective and highly bioavailable antagonist of Toll-like receptors 7 and 8 (TLR7/8). It effectively inhibits TLR7/8-mediated activation of the NF-κB signaling pathway and can reverse TLR7-induced resistance to steroid-driven apoptosis in plasmacytoid dendritic cells. This compound is particularly relevant for research into inflammation and autoimmune diseases, including systemic lupus erythematosus. -
TLR9 Agonist
Agatolimod is a Toll-like receptor 9 (TLR9) agonist and immunomodulator with an EC50 of 180 nM. It activates TLR9 and upregulates TLR6 expression, initiating downstream signaling through IRAK4, IRF5, and IRF7. Agatolimod enhances Th1-type immune responses and promotes the activation of various immune cells, leading to increased antigen presentation, antibody regulation, cytokine secretion, apoptosis, and enhanced cytotoxicity. This compound is relevant for research into COVID-19, breast cancer, lung adenocarcinoma, HPV-related tumors, melanoma, and salmonellosis. -
TLR2/4 Inhibitor
Robinin is a flavonoid that acts as an inhibitor of Toll-like receptors 2 and 4 (TLR2/4), modulating the TGF-β, TLR4/NF-κB, and TLR2-PI3k-AKT signaling pathways. This compound demonstrates significant anti-inflammatory and anti-tumor properties. Additionally, Robinin has been shown to enhance the anti-inflammatory effects of Methotrexate in experimental arthritis models and may mitigate cardiac toxicity induced by Doxorubicin. These attributes make Robinin a valuable reagent for research applications in inflammation and cancer therapy. -
COX-2/MMP-7/TLR4 Inhibitor
Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex. -
TLR1/2 agonist
CU-T12-9 is a specific and potent agonist of the Toll-like receptor 1/2 (TLR1/2) heterodimer, with an EC₅₀ of 52.9 nM in the HEK-Blue hTLR2 SEAP assay. It selectively activates TLR1/2 without affecting TLR2/6 and stimulates both innate and adaptive immune responses. CU-T12-9 signals through the NF-κB pathway, leading to elevated expression of downstream effectors such as TNF-α, IL-10, and iNOS, making it a valuable tool for immunological and inflammatory research. -
TLR7 Agonist
SMU-L11-R is a selective TLR7 agonist that demonstrates an EC50 of 0.012 μM for human TLR7. This compound specifically activates TLR7, recruits MyD88, and initiates the MAPK/NF-κB signaling pathways, resulting in the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6 in both mouse and human peripheral blood mononuclear cells. Additionally, SMU-L11-R promotes M1-like macrophage polarization and exhibits synergistic anti-tumor effects in combination with PD-L1 inhibitors through the upregulation of CD8+ T cells, making it a valuable tool for research in colorectal cancer. -
TLR2 Agonist
Pam2CSK4 is a TLR2 agonist that activates immune signaling pathways, leading to the expression of inducible nitric oxide synthase (iNOS) and nitric oxide (NO) in macrophage cell lines through TBK1 and MyD88. This compound stimulates the NF-κB and Bruton's tyrosine kinase pathways in platelets, enhancing interactions between platelets and endothelial cells. Pam2CSK4 promotes the expansion of myeloid-derived suppressor cells (MDSCs) and can suppress anti-tumor immune responses in the tumor microenvironment. Its applications span various diseases, including thromboinflammatory conditions, sepsis, atherosclerosis, and certain cancers, making it a valuable tool in immunological and therapeutic research. -
PI3K/Akt/mTOR signaling pathway Inhibitor, TLR4 signaling Inhibitor
25(R,S)-Ruscogenin is a potent inhibitor of the PI3K/Akt/mTOR and TLR4 signaling pathways. This compound effectively suppresses hepatocellular carcinoma (HCC) metastasis by decreasing the expression of matrix metalloproteinases (MMP-2 and MMP-9), uPA, VEGF, and HIF-1α. Additionally, 25(R,S)-Ruscogenin mitigates LPS-induced apoptosis in pulmonary endothelial cells, highlighting its potential for applications in cancer research and inflammatory disease studies. -
Selective Intranasal TLR7 Agonist
GSK2245035 maleate is a selective intranasal agonist of Toll-Like receptor 7 (TLR7), exhibiting potent Type-1 interferon (IFN) stimulating activity with pEC50 values of 9.3 for IFNα and 6.5 for TNFα. This compound effectively reduces allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 maleate is primarily utilized in research focused on asthma and other Th2-mediated allergic responses. -
TLR Inhibitor
ETI60 is a selective Toll-like receptor (TLR) inhibitor that primarily targets the nucleoside-binding Site I on TLR7 and TLR9, with IC50 values of 0.68 μM and 0.12 μM, respectively. This compound effectively inhibits endosomal TLR-mediated pro-inflammatory signaling, demonstrating nanomolar activity in cellular, biophysical, and in vivo assays. ETI60 modulates the expression of inflammation-related genes and has shown efficacy in alleviating symptoms in mouse models of psoriasis and systemic lupus erythematosus (SLE). This reagent is valuable for research involving autoimmune and inflammatory diseases. -
TLR Inhibitor
ETI41 is a selective Toll-like receptor (TLR) inhibitor that targets the nucleoside-binding Site I on TLR7 and TLR9, demonstrating IC50 values of 0.63 μM and 0.16 μM, respectively, while sparing surface TLRs. This compound effectively inhibits endosomal TLR-mediated pro-inflammatory signaling, displaying potent nanomolar activity across cellular, biophysical, and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and improves symptoms in murine models of psoriasis and systemic lupus erythematosus (SLE). It is valuable for research into autoimmune and inflammatory diseases. -
TLR9 Antagonist
TLR9 antagonist 1 is a selective toll-like receptor 9 (TLR9) antagonist that exhibits an IC50 of 0.1 nM for human TLR9, demonstrating a significant preference over TLR2, TLR4, TLR5, TLR7, and TLR8. This compound is known to exacerbate symptoms in systemic lupus erythematosus (SLE) mouse models by increasing levels of anti-dsDNA and anti-Sm antibodies. TLR9 antagonist 1 is valuable for research in inflammatory and autoimmune diseases, particularly in the study of disorders such as lupus and arthritis. -
TLR3/9 Inhibitor
M199 is a selective inhibitor of TLR3 and TLR9 signaling pathways. This compound effectively induces the secretion of pro-inflammatory cytokines, including IL-6, IL-8, and TNFα, in human peripheral blood mononuclear cells (PBMCs). M199 is utilized in research to investigate immune response modulation and the role of TLR signaling in various biological processes. -
Selective Intranasal TLR7 Agonist
GSK2245035 is a selective intranasal agonist for Toll-Like Receptor 7 (TLR7), exhibiting potent Type-1 interferon (IFN) stimulation, with pEC50 values of 9.3 for IFNα and 6.5 for TFNα. This compound demonstrates efficacy in suppressing allergen-induced Th2 cytokine production in human peripheral blood cell cultures, making it a valuable tool for asthma research. Its unique mechanism of action highlights its potential in studying immune responses and therapeutic applications in allergic conditions. -
TLR4 Activator
Kdo2-Lipid A ammonium is a selective TLR4 activator known for its potent endotoxin activity comparable to that of lipopolysaccharide (LPS). It effectively stimulates the release of pro-inflammatory mediators, including tumor necrosis factor (TNF) and prostaglandin E2 (PGE2). This compound is widely utilized in immunological research to investigate TLR4 signaling pathways and the associated inflammatory responses. -
TLR1/TLR2 Agonist
Diprovocim is a potent TLR1/TLR2 agonist that activates immune responses by inducing full agonist activity in human THP-1 cells, with an EC50 of 110 pM. This compound effectively stimulates TNF-α release from mouse macrophages at an EC50 of 1.3 nM. By activating downstream signaling pathways, including MAPK and NF-κB, Diprovocim demonstrates significant adjuvant activity in mice, enhancing cellular immune responses and making it a valuable tool for immunological research. -
HER2-TLR7/8 Conjugate
MC-Val-Cit-PAB-Amide-TLR7 Agonist 4 is a HER2-targeted TLR7 and TLR8 immune agonist conjugate. This compound activates Toll-like receptors, enhancing immune responses through the stimulation of both innate and adaptive immunity. It is primarily utilized in research applications aimed at cancer immunotherapy, particularly in enhancing the immune system's ability to target HER2-expressing tumors. -
TLR8 Agonist
TLR8 Agonist 4 is a potent agonist targeting Toll-like receptor 8 (TLR8), demonstrating efficacy against both wild-type and drug-resistant HBV strains, including those resistant to lamivudine and entecavir. The compound exhibits IC50 values of 0.15 μM and 0.10 μM, respectively, highlighting its potential for use in antiviral research and therapeutic development against Hepatitis B virus. -
TLR7 Agonist
TLR7 Agonist 12 is a potent TLR7 agonist and a purine nucleoside analog. This compound demonstrates significant antitumor activity, particularly against indolent lymphoid malignancies. Its anticancer mechanisms are mediated through the inhibition of DNA synthesis and the induction of apoptosis, making it valuable for research applications in cancer therapeutics and immune modulation studies. -
TLR7 Agonist
SMU-L11 is a selective TLR7 agonist with an EC50 of 0.024 μM, which engages the MyD88 adapter protein to activate downstream NF-κB and MAPK signaling pathways. This compound significantly enhances immune cell activation in murine models, promoting the proliferation of CD4+ T and CD8+ T cells, leading to direct tumor cell lysis and inhibition of tumor growth. SMU-L11 is a valuable reagent for cancer research and can also be utilized for investigations into immune system-related diseases. -
TLR4/HCN Inhibitor
HCN-IN-1 is a TLR4 inhibitor and modulator of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels, specifically targeting HCN2 and HCN4. It effectively inhibits TLR4-mediated signaling, evidenced by reduced alkaline phosphatase activity. HCN-IN-1 modulates HCN2 currents by shifting the voltage-dependent activation to hyperpolarized potentials and slowing activation kinetics, while also blocking currents through HCN4 channels. This compound demonstrates significant analgesic, anti-inflammatory, and anti-anginal properties, making it valuable for research into inflammatory pain, neuropathic pain, heart failure, and related inflammatory conditions. -
Fas receptor Antagonist
Xelafaslatide is a Fas receptor antagonist that effectively inhibits Fas receptor signaling, thereby blocking downstream apoptosis and inflammatory pathways. This compound demonstrates significant potential in suppressing neuroinflammation and microglial activation in glaucoma models, offering protection to retinal ganglion cells and preventing axonal degeneration. Xelafaslatide is relevant for research focused on glaucoma and related neurodegenerative conditions. -
TLR7 Ligand
Toll-Like Receptor 7 Ligand II is a cell-permeable hydroxyadenine compound which acts as a potent and highly specific TLR7 (toll-like receptor 7) agonist without any detectable activity towards TLR2/3/5/8/9. It is shown to be 10-times more potent than R848 in stimulating the production of TLR7-dependent cytokines in cultures in vitro . -
TLR4 inhibitor
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases. -
TLR7 agonist
PF-4878691 (3M-852A) is a potent, orally active, and selective Toll-like receptor 7 (TLR7) agonist modelled to dissociate its antiviral and inflammatory activities. - Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
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TLR7 agonist
Isatoribine is a novel guanosine analogue showing immunostimulatory activity both in vivo and in vitro. -
TLR7 agonist
TLR7-agonist-2 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.
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TLR7 agonist
Gardiquimod is a chemical compound which acts selectively at both mouse and human forms of toll-like receptor 7 (TLR7). It functions as an immune response modifier. CAS: 1159840-61-5 (TFA) 1020412-43-4 (free base) -
TLR/SCD inhibitor
E6446 dihydrochloride is a robust antagonist for TLR7 and TLR9, with potential applications in studying harmful inflammatory responses. Additionally, it acts as a significant inhibitor of SCD1 with a KD of 4.61 μM. This compound can notably suppress adipogenic differentiation and liver lipogenesis via the SCD1-ATF3 pathway. Studies have indicated that E6446 dihydrochloride can enhance liver pathology in mice on a high-fat diet, making it a potential candidate for researching non-alcoholic fatty liver disease (NAFLD).
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MD2-TLR4 inhibitor
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. -
TLR7/8 agonist
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline. -
TLR4 inhibitor
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.
