| S8133 |
Resiquimod (R-848)
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Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist, inducing the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. This compound reduces hepatitis C virus (HCV) infection. Phase 2.
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Nature, 2025, 644(8078):1058-1068
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J Virol, 2025, e0128025.
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Int J Nanomedicine, 2024, 19:3589-3605
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| S8428 |
FSL-1
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FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.
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| S4430 |
HCQ (Hydroxychloroquine) Sulfate
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Hydroxychloroquine (HCQ) 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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EMBO J, 2025, 10.1038/s44318-025-00581-3
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iScience, 2025, 28(4):112054
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Int J Mol Sci, 2025, 26(2)588
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| E6039 |
Imiquimod hydrochloride
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Imiquimod hydrochloride (R 837 hydrochloride) is a small-molecule immune response modifier, a potent and selective agonist of toll like receptor 7 (TLR7), an antagonist of adenosine A₂A receptor with a Ki of 2.16 μM, and an inhibitor of adenylyl cyclase activity, inducing antiviral proteins like cystatin A. It exhibits strong antitumoral and antiviral efficacy, making it effective for conditions such as COVID 19, HPV warts, molluscum contagiosum, actinic keratosis, basal and squamous cell carcinoma, Bowen's disease, and vulvar intraepithelial neoplasia.
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Chemotherapy, November 29, 2021, 1-12
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The FASEB Journal, January 2020, 208-221
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Journal of Neuroinflammation, 2022, 315
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| S7455 |
Resatorvid (TAK-242)
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Resatorvid (TAK-242, CLI-095) is a small-molecule-specific inhibitor of Toll-like receptor (TLR) 4 signaling, blocking LPS-induced production of NO, TNF-α and IL-6 in macrophages with IC50 of 1.8 nM, 1.9 nM and 1.3 nM, respectively. This compound downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF, and it also inhibits autophagy.
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EMBO J, 2025, 10.1038/s44318-025-00515-z
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Carbohydr Polym, 2025, 350:122980
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J Neuroinflammation, 2025, 22(1):38
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| S6597 |
TLR2-IN-C29
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TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling.
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Mol Oral Microbiol, 2026, 10.1111/omi.70030
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Protein Cell, 2025, pwaf020
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J Neuroinflammation, 2025, 22(1):38
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| S7850 |
Lipopolysaccharides (LPS)
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Lipopolysaccharides (LPSs, Endotoxin,LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria. Lipopolysaccharides consists of an antigen O-specific chain, a core oligosaccharide and lipid A. Lipopolysaccharides is a pathogenic associated molecular pattern (PAMP) that activates the immune system. Lipopolysaccharides activates TLR-4 on immune cells. Lipopolysaccharides induces secretion of cell migrasome.
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PLoS One, 2026, 21(2):e0341867
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Immun Inflamm Dis, 2026, 14(3):e70348
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J Immunother Cancer, 2025, 13(7)e010898
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| S7161 |
Motolimod
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Motolimod is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.
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ImmunoHorizons, February 24, 2020, 93-107
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Journal of Leukocyte Biology, 2025, qiaf036
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J Leukoc Biol, 2025, 117(5)qiaf036
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| S8677 |
CU-CPT22
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CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM while no significant inhibition to TLR2/6. It demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4).
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EMBO Rep, 2025, 10.1038/s44319-025-00558-7
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Cancer Cell, 2024, S1535-6108(24)00135-1
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J Exp Clin Cancer Res, 2023, 42(1):172
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| S0822 |
TLR4-IN-C34
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TLR4-IN-C34 (TLR4-C34, C34, TLR4-C34-IN) is a potent and selective antagonist of Toll-like receptor 4 (TLR4). This compound reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.
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Carbohydr Polym, 2026, 373:124618
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Mol Oral Microbiol, 2026, 10.1111/omi.70030
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Protein Cell, 2025, pwaf020
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