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TLR inhibitors/agonists

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Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S8133 Resiquimod (R-848) 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.
Nature, 2025, 644(8078):1058-1068
J Virol, 2025, e0128025.
Int J Nanomedicine, 2024, 19:3589-3605
S8428 FSL-1 FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.
S4430 HCQ (Hydroxychloroquine) Sulfate 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.
EMBO J, 2025, 10.1038/s44318-025-00581-3
iScience, 2025, 28(4):112054
Int J Mol Sci, 2025, 26(2)588
Verified customer review of HCQ (Hydroxychloroquine) Sulfate
S7455 Resatorvid (TAK-242) 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.
EMBO J, 2025, 10.1038/s44318-025-00515-z
Carbohydr Polym, 2025, 350:122980
J Neuroinflammation, 2025, 22(1):38
S7161 Motolimod Motolimod is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.
J Leukoc Biol, 2025, 117(5)qiaf036
J Pharmacol Exp Ther, 2024, 388(3):751-764
Cell Rep, 2021, 35(7):109143
S8677 Cu-CPT22 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).
EMBO Rep, 2025, 10.1038/s44319-025-00558-7
Cancer Cell, 2024, S1535-6108(24)00135-1
J Exp Clin Cancer Res, 2023, 42(1):172
S7221 Vesatolimod (GS-9620) Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7.
PLoS Pathog, 2022, 18(3):e1010354
J Pharm Biomed Anal, 2020, 179:112987
Stem Cell Res Ther, 2019, 10(1):387
S6597 TLR2-IN-C29 TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling.
Protein Cell, 2025, pwaf020
J Neuroinflammation, 2025, 22(1):38
Int J Biol Macromol, 2025, 284(Pt 2):138092
S6573 MD2-IN-1 MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM.
Life Sci Alliance, 2023, 6(3)e202201636
Front Immunol, 2022, 13:995791
Br J Pharmacol, 2021, 10.1111/bph.15412
S7850 Lipopolysaccharides (LPS) 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.
J Immunother Cancer, 2025, 13(7)e010898
Cell Rep, 2025, 44(5):115625
Biomedicines, 2025, 13(6)1320