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Isoform-selective Products

TLR7 TLR8 TLR9 TLR4 TLR2 TLR3 TLR1 TLR6

TLR Products

All (50)
TLR Inhibitors (19)
TLR Antibodies (3)
TLR Activators (3)
TLR Antagonists (6)
TLR Agonists (14)
TLR Modulators (2)
New TLR Products

Catalog No.	Product Name	Information	Product Use Citations
S4157	Chloroquine diphosphate	Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).	Nat Commun, 2024, 15(1):1642 Cancer Lett, 2024, 604:217258 Phytomedicine, 2024, 135:156053
S6999	Chloroquine	Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.	Signal Transduct Target Ther, 2025, 10(1):26 Cell Discov, 2025, 11(1):15 Cell Metab, 2025, S1550-4131(25)00149-4
S4430	Hydroxychloroquine (HCQ) 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.	iScience, 2025, 28(4):112054 Int J Mol Sci, 2025, 26(2)588 Exp Cell Res, 2025, 446(2):114473
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. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.	Carbohydr Polym, 2025, 350:122980 J Neuroinflammation, 2025, 22(1):38 Phytomedicine, 2025, 142:156645
S8133	Resiquimod (R-848)	Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.	Int J Nanomedicine, 2024, 19:3589-3605 Front Immunol, 2024, 15:1331480 J Inflamm Res, 2024, 17:9757-9771
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).	Cancer Cell, 2024, S1535-6108(24)00135-1 J Exp Clin Cancer Res, 2023, 42(1):172 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	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.	Cell Rep, 2025, 44(5):115625 Gen Physiol Biophys, 2025, 44(1):81-92 Int Immunopharmacol, 2024, 137:112426
S3924	Ginsenoside Rb1	Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.	J Biol Chem, 2024, 300(8):107542 J Ethnopharmacol, 2021, S0378-8741(21)00169-0 J Biol Chem, 2021, S0021-9258(21)00790-0
S8562	IRAK4-IN-2	IRAK4-IN-2 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades.	Cancer Lett, 2021, 503:75-90 Cancer Lett, 2021, 503:75-90
S2979	CU-T12-9	CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.	Nat Commun, 2025, 16(1):2743 Biomedicine & Pharmacotherapy, 2023, 114638 Biomed Pharmacother, 2023, 162:114638
S0716	E6446	E6446 is an inhibitor of Toll-like receptor (TLR) 7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.	Cancer Cell, 2024, S1535-6108(24)00135-1 Front Immunol, 2024, 15:1354055 JCI Insight, 2023, 8(22)e171054
S0822	TLR4-IN-C34	TLR4-IN-C34 (TLR4-C34, C34, TLR4-C34-IN) is a potent and selective antagonist of Toll-like receptor 4 (TLR4). TLR4-IN-C34 reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.	Protein Cell, 2025, pwaf020 Mol Med Rep, 2025, 32(1)177 Exp Mol Med, 2024, 56(2):408-421.
F2122^New	TLR4 mAb	TLR4,Toll-like Receptor 4
F0360^New	Rig-I Rabbit mAb	Rig-I,RIG-I/DDX58
F2506^New	TLR7 Rabbit mAb	TLR7,Toll-like Receptor 7
S0494	SM 324405	SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.
E4998^New	Polyinosinic-polycytidylic acid sodium	Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic double-stranded RNA (dsRNA) analogue that activates the MDA-5 receptor in the cytoplasm and TLR3 in endosomal compartments. This activation promotes the production of type I interferons and induces apoptosis in cancer cells, particularly those that lack protective anti-apoptotic mechanisms like Bcl-xL.
S0002	IAXO-102	IAXO-102 is an antagonist of TLR4 targeting both MD-2 and CD14 co-receptors. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and downregulates the expression of TLR4 dependent proinflammatory proteins. IAXO-102 inhibits experimental abdominal aortic aneurysm (AAA) development.
E6040^New	Imiquimod maleate	Imiquimod maleate (R 837 maleate) is a small-molecule salt derivative of maleic acid, isolated from the Imiquimod free base and is an 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.
E5778^New	CU-CPT 4a	CU-CPT 4a (TLR3-IN-1) is a potent small molecule antagonist of TLR3 with an IC50 of 3.44 µM that also inhibits TLR3/dsRNA-mediated signaling, including TNF-α and IL-1β expression. It is a valuable tool for studying protein-RNA complexes.
S9937	CU-CPD107	CU-CPD107 is a selective, dual-activity small-molecule which demonstrated differential activity against the TLR8 agonists and ssRNA ligands. In the presence of R848, CU-CPD107 acts as a TLR8 signaling inhibitor (IC50=13.7 μM). In the presence of ssRNA, CU-CPD107 shows synergistic agonist activities, while CU-CPD107 alone is unable to influence TLR8 signaling.
S8428	FSL-1	FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.
S9234	Schaftoside	Schaftoside, a bioactive compound found in the Herba Desmodii Styracifolii, exhibits pancreatic lipase inhibitory activity. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
E3193	Saponaria Officinalis Extract	Saponaria Officinalis Extract is extracted from Saponaria Officinalis, which reduces downstream inflammatory responses by disrupting the TLR4/MD2 complex and blocking MyD88-dependent inflammatory signaling.
E4864^New	Pentamidine	Pentamidine (MP-601205) is an aromatic diamidine drug, an antagonist of TLR4.It also inhibits PI3K/AKT signaling pathway and reduce the expression of MMP-2 and MMP-9. It exhibits anti- protozoal, anti-inflammatory, and anti-tumor activities and is used as an agent for treating African trypanosomiasis, antimony resistant leishmaniasis and Pneumocystis carinii pneumonia.
E5812^New	AT791	AT791 is a potent and orally bioavailable inhibitor of TLR7 and TLR9 with an IC50 of 3.33 μM and 0.04 μM, respectively, in human embryonic kidney cells and also inhibits DNA-TLR9 interaction in vitro.
S0078	1V209 (TLR7 agonist T7)	1V209 (T7, TLR7 agonist T7) is an agonist of Toll-like receptor 7 (TLR7) with anti-tumor effects. 1V209 can be used as vaccine adjuvants, enhances antigen specific humoral and cellular immune responses.	Acta Pharm Sin B, 2024, 14(10):4577-4590
E3625	Cnidii Fructus Extract	Cnidii Fructus Extract is extracted from Cnidii Fructus, the dry ripe fruit of Cnidium monnieri (L.)Cuss.. Chinese herbal medicine Cnidii Fructus has an outstanding effect on chronic lumbar pain and impotence, also has been used against osteoporosis with high frequency.
S9623	Telratolimod	Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.
S6934	AMG-9810	AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.
S9931	Enpatoran Hydrochloride	Enpatoran (M5049) hydrochloride is a potent, orally active, and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM, respectively, in HEK293 cells.
S0139	MD2-TLR4-IN-1	MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively.
E0639	TLR7/8 agonist 1 dihydrochloride	TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.TLR7/8 agonist 1 retains TLR7-agonistic activity with an EC50 of 20 nM.
A2696	Anti-TLR3 / CD283 (CNTO5429)	Anti-TLR3 / CD283 (CNTO5429) is a novel antibody that binds to the extracellular domain of TLR3 and inhibit poly(I:C)-induced inflammation. MW: 145.3 KD.
E1134	ABR-238901	ABR-238901 is a novel S100A8/A9 blocker that potently inhibits S100A8/A9 interaction with its receptors RAGE (receptor for advanced glycation endproducts) and TLR4 (toll-like receptor 4).
E3594	Radix tetrastigme Extract	Radix Tetrastigme Extract is extracted from Tetrastigma hemsleyanum, which can modulate TLR4/COX-2/NF-κB signaling pathway.
E6039^New	Imiquimod hydrochloride	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.
E7472^New	Pam3CSK4	Pam3CSK4 (Pam3Cys-Ser-(Lys)4) is a synthetic triacylated lipopeptide that serves as a ligand for the Toll-like receptor 2/1 (TLR2/1) heterodimer. It is an agonist of toll-like receptor 1/2 (TLR1/2) with an EC50 of 0.47 ng/mL in human TLR1/2.
E5909^New	CL075	CL075 (3M002) is a selective agonist of TLR8 with immunomodulatory properties. It primes human neutrophils by activating signaling pathways, including p47phox phosphorylation and p38MAPK, leading to enhanced reactive oxygen species (ROS) production and contributing to immune defense.
E0694	Okanin	Okanin, a chalcone found in the flower tea Coreopsis tinctoria, effectively reduces LPS-induced microglial activation by inhibiting the TLR4/NF-κB signalling pathways. It also reduces LPS-induced nitric oxide (NO) production and iNOS expression by increasing HO-1 expression. It exhibits a potential as a nutritional preventive measure for neurodegenerative disorders.
S4461	CU-CPT-8m	CU-CPT-8m (CPD1578) is a specific antagonist of toll-like receptor 8(TLR8) with IC50 of 67 nM and Kd of 220 nM.	Nat Commun, 2024, 15(1):5678
P1246^New	ODN 1826 sodium	ODN 1826 sodium (CpG 1826 sodium) is a synthetic CpG oligodeoxynucleotide and agonist of TLR9 signaling pathway, that induces G1-phase arrest and apoptosis in A20 lymphoma cells while stimulating NO and iNOS production in mouse models, as part of its immunostimulatory activity.
A2757	Anti-TLR7	Anti-TLR7 is a monoclonal antibody against Toll-like receptor 7 (TLR7) with the potential to treat autoimmune disease. MW: 145.04 KD.
S6719	E6446 dihydrochloride	E6446 dihydrochloride is a specific Toll-like receptor 9 inhibitor.	Cell Death Dis, 2025, 16(1):60 Diabetes, 2025, 74(3):409-415 Antioxidants (Basel), 2024, 13(10)1265
A2333	Tomaralimab (Anti-TLR2 / CD282)	Tomaralimab (Anti-TLR2 / CD282) is a humanized immunoglobulin (Ig) G4 monoclonal antibody directed against toll-like receptor type 2 (TLR2) with potential anti-inflammatory and antineoplastic activities. It has the potential for research on Myelodysplastic Syndromes (MDS). MW : 145.5 KD.
S9730	CU-CPT9a	CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.	Nat Commun, 2024, 15(1):5678 J Gen Virol, 2023, 104(5)001858
S4157	Chloroquine diphosphate	Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).	Nat Commun, 2024, 15(1):1642 Cancer Lett, 2024, 604:217258 Phytomedicine, 2024, 135:156053
S6999	Chloroquine	Chloroquine is an antimalarial drug and autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective agianst SARS-CoV-2 (COVID-19) infection with EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.	Signal Transduct Target Ther, 2025, 10(1):26 Cell Discov, 2025, 11(1):15 Cell Metab, 2025, S1550-4131(25)00149-4
S4430	Hydroxychloroquine (HCQ) 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.	iScience, 2025, 28(4):112054 Int J Mol Sci, 2025, 26(2)588 Exp Cell Res, 2025, 446(2):114473
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. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy.	Carbohydr Polym, 2025, 350:122980 J Neuroinflammation, 2025, 22(1):38 Phytomedicine, 2025, 142:156645
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).	Cancer Cell, 2024, S1535-6108(24)00135-1 J Exp Clin Cancer Res, 2023, 42(1):172 J Exp Clin Cancer Res, 2023, 42(1):172
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
S3924	Ginsenoside Rb1	Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.	J Biol Chem, 2024, 300(8):107542 J Ethnopharmacol, 2021, S0378-8741(21)00169-0 J Biol Chem, 2021, S0021-9258(21)00790-0
S8562	IRAK4-IN-2	IRAK4-IN-2 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades.	Cancer Lett, 2021, 503:75-90 Cancer Lett, 2021, 503:75-90
S0716	E6446	E6446 is an inhibitor of Toll-like receptor (TLR) 7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro.	Cancer Cell, 2024, S1535-6108(24)00135-1 Front Immunol, 2024, 15:1354055 JCI Insight, 2023, 8(22)e171054
S9234	Schaftoside	Schaftoside, a bioactive compound found in the Herba Desmodii Styracifolii, exhibits pancreatic lipase inhibitory activity. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
E3193	Saponaria Officinalis Extract	Saponaria Officinalis Extract is extracted from Saponaria Officinalis, which reduces downstream inflammatory responses by disrupting the TLR4/MD2 complex and blocking MyD88-dependent inflammatory signaling.
E5812^New	AT791	AT791 is a potent and orally bioavailable inhibitor of TLR7 and TLR9 with an IC50 of 3.33 μM and 0.04 μM, respectively, in human embryonic kidney cells and also inhibits DNA-TLR9 interaction in vitro.
S6934	AMG-9810	AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.
S9931	Enpatoran Hydrochloride	Enpatoran (M5049) hydrochloride is a potent, orally active, and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM, respectively, in HEK293 cells.
S0139	MD2-TLR4-IN-1	MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively.
E1134	ABR-238901	ABR-238901 is a novel S100A8/A9 blocker that potently inhibits S100A8/A9 interaction with its receptors RAGE (receptor for advanced glycation endproducts) and TLR4 (toll-like receptor 4).
E0694	Okanin	Okanin, a chalcone found in the flower tea Coreopsis tinctoria, effectively reduces LPS-induced microglial activation by inhibiting the TLR4/NF-κB signalling pathways. It also reduces LPS-induced nitric oxide (NO) production and iNOS expression by increasing HO-1 expression. It exhibits a potential as a nutritional preventive measure for neurodegenerative disorders.
S6719	E6446 dihydrochloride	E6446 dihydrochloride is a specific Toll-like receptor 9 inhibitor.	Cell Death Dis, 2025, 16(1):60 Diabetes, 2025, 74(3):409-415 Antioxidants (Basel), 2024, 13(10)1265
A2696	Anti-TLR3 / CD283 (CNTO5429)	Anti-TLR3 / CD283 (CNTO5429) is a novel antibody that binds to the extracellular domain of TLR3 and inhibit poly(I:C)-induced inflammation. MW: 145.3 KD.
A2757	Anti-TLR7	Anti-TLR7 is a monoclonal antibody against Toll-like receptor 7 (TLR7) with the potential to treat autoimmune disease. MW: 145.04 KD.
A2333	Tomaralimab (Anti-TLR2 / CD282)	Tomaralimab (Anti-TLR2 / CD282) is a humanized immunoglobulin (Ig) G4 monoclonal antibody directed against toll-like receptor type 2 (TLR2) with potential anti-inflammatory and antineoplastic activities. It has the potential for research on Myelodysplastic Syndromes (MDS). MW : 145.5 KD.
S7850	Lipopolysaccharides	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.	Cell Rep, 2025, 44(5):115625 Gen Physiol Biophys, 2025, 44(1):81-92 Int Immunopharmacol, 2024, 137:112426
E4998^New	Polyinosinic-polycytidylic acid sodium	Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic double-stranded RNA (dsRNA) analogue that activates the MDA-5 receptor in the cytoplasm and TLR3 in endosomal compartments. This activation promotes the production of type I interferons and induces apoptosis in cancer cells, particularly those that lack protective anti-apoptotic mechanisms like Bcl-xL.
S9937	CU-CPD107	CU-CPD107 is a selective, dual-activity small-molecule which demonstrated differential activity against the TLR8 agonists and ssRNA ligands. In the presence of R848, CU-CPD107 acts as a TLR8 signaling inhibitor (IC50=13.7 μM). In the presence of ssRNA, CU-CPD107 shows synergistic agonist activities, while CU-CPD107 alone is unable to influence TLR8 signaling.
S0822	TLR4-IN-C34	TLR4-IN-C34 (TLR4-C34, C34, TLR4-C34-IN) is a potent and selective antagonist of Toll-like receptor 4 (TLR4). TLR4-IN-C34 reduces systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis.	Protein Cell, 2025, pwaf020 Mol Med Rep, 2025, 32(1)177 Exp Mol Med, 2024, 56(2):408-421.
S0002	IAXO-102	IAXO-102 is an antagonist of TLR4 targeting both MD-2 and CD14 co-receptors. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and downregulates the expression of TLR4 dependent proinflammatory proteins. IAXO-102 inhibits experimental abdominal aortic aneurysm (AAA) development.
E5778^New	CU-CPT 4a	CU-CPT 4a (TLR3-IN-1) is a potent small molecule antagonist of TLR3 with an IC50 of 3.44 µM that also inhibits TLR3/dsRNA-mediated signaling, including TNF-α and IL-1β expression. It is a valuable tool for studying protein-RNA complexes.
E4864^New	Pentamidine	Pentamidine (MP-601205) is an aromatic diamidine drug, an antagonist of TLR4.It also inhibits PI3K/AKT signaling pathway and reduce the expression of MMP-2 and MMP-9. It exhibits anti- protozoal, anti-inflammatory, and anti-tumor activities and is used as an agent for treating African trypanosomiasis, antimony resistant leishmaniasis and Pneumocystis carinii pneumonia.
S4461	CU-CPT-8m	CU-CPT-8m (CPD1578) is a specific antagonist of toll-like receptor 8(TLR8) with IC50 of 67 nM and Kd of 220 nM.	Nat Commun, 2024, 15(1):5678
S9730	CU-CPT9a	CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.	Nat Commun, 2024, 15(1):5678 J Gen Virol, 2023, 104(5)001858
S8133	Resiquimod (R-848)	Resiquimod (R-848, S28463) is an immune response modifier that acts as a potent TLR 7/TLR 8 agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. Resiquimod reduces hepatitis C virus (HCV) infection. Phase 2.	Int J Nanomedicine, 2024, 19:3589-3605 Front Immunol, 2024, 15:1331480 J Inflamm Res, 2024, 17:9757-9771
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
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
S2979	CU-T12-9	CU-T12-9 is a specific agonist of Toll-like receptor (TLR) 1/2 with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.	Nat Commun, 2025, 16(1):2743 Biomedicine & Pharmacotherapy, 2023, 114638 Biomed Pharmacother, 2023, 162:114638
S0494	SM 324405	SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM.
E6040^New	Imiquimod maleate	Imiquimod maleate (R 837 maleate) is a small-molecule salt derivative of maleic acid, isolated from the Imiquimod free base and is an 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.
S8428	FSL-1	FSL-1, a bacterial-derived toll-like receptor 2/6 (TLR2/6) agonist, enhances resistance to experimental HSV-2 infection.
S0078	1V209 (TLR7 agonist T7)	1V209 (T7, TLR7 agonist T7) is an agonist of Toll-like receptor 7 (TLR7) with anti-tumor effects. 1V209 can be used as vaccine adjuvants, enhances antigen specific humoral and cellular immune responses.	Acta Pharm Sin B, 2024, 14(10):4577-4590
S9623	Telratolimod	Telratolimod (3M-052, MEDI9197) is an agonist of toll-like receptor 7 (TLR-7) and toll-like receptor 8 (TLR-8) with antitumor activity.
E0639	TLR7/8 agonist 1 dihydrochloride	TLR7/8 agonist 1 dihydrochloride is a toll-like receptor TLR7/TLR8 dual-agonistic imidazoquinoline.TLR7/8 agonist 1 retains TLR7-agonistic activity with an EC50 of 20 nM.
E6039^New	Imiquimod hydrochloride	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.
E7472^New	Pam3CSK4	Pam3CSK4 (Pam3Cys-Ser-(Lys)4) is a synthetic triacylated lipopeptide that serves as a ligand for the Toll-like receptor 2/1 (TLR2/1) heterodimer. It is an agonist of toll-like receptor 1/2 (TLR1/2) with an EC50 of 0.47 ng/mL in human TLR1/2.
E5909^New	CL075	CL075 (3M002) is a selective agonist of TLR8 with immunomodulatory properties. It primes human neutrophils by activating signaling pathways, including p47phox phosphorylation and p38MAPK, leading to enhanced reactive oxygen species (ROS) production and contributing to immune defense.
P1246^New	ODN 1826 sodium	ODN 1826 sodium (CpG 1826 sodium) is a synthetic CpG oligodeoxynucleotide and agonist of TLR9 signaling pathway, that induces G1-phase arrest and apoptosis in A20 lymphoma cells while stimulating NO and iNOS production in mouse models, as part of its immunostimulatory activity.
E3625	Cnidii Fructus Extract	Cnidii Fructus Extract is extracted from Cnidii Fructus, the dry ripe fruit of Cnidium monnieri (L.)Cuss.. Chinese herbal medicine Cnidii Fructus has an outstanding effect on chronic lumbar pain and impotence, also has been used against osteoporosis with high frequency.
E3594	Radix tetrastigme Extract	Radix Tetrastigme Extract is extracted from Tetrastigma hemsleyanum, which can modulate TLR4/COX-2/NF-κB signaling pathway.
F2122^New	TLR4 mAb	TLR4,Toll-like Receptor 4
F0360^New	Rig-I Rabbit mAb	Rig-I,RIG-I/DDX58
F2506^New	TLR7 Rabbit mAb	TLR7,Toll-like Receptor 7
E4998^New	Polyinosinic-polycytidylic acid sodium	Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic double-stranded RNA (dsRNA) analogue that activates the MDA-5 receptor in the cytoplasm and TLR3 in endosomal compartments. This activation promotes the production of type I interferons and induces apoptosis in cancer cells, particularly those that lack protective anti-apoptotic mechanisms like Bcl-xL.
E6040^New	Imiquimod maleate	Imiquimod maleate (R 837 maleate) is a small-molecule salt derivative of maleic acid, isolated from the Imiquimod free base and is an 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.
E5778^New	CU-CPT 4a	CU-CPT 4a (TLR3-IN-1) is a potent small molecule antagonist of TLR3 with an IC50 of 3.44 µM that also inhibits TLR3/dsRNA-mediated signaling, including TNF-α and IL-1β expression. It is a valuable tool for studying protein-RNA complexes.
E4864^New	Pentamidine	Pentamidine (MP-601205) is an aromatic diamidine drug, an antagonist of TLR4.It also inhibits PI3K/AKT signaling pathway and reduce the expression of MMP-2 and MMP-9. It exhibits anti- protozoal, anti-inflammatory, and anti-tumor activities and is used as an agent for treating African trypanosomiasis, antimony resistant leishmaniasis and Pneumocystis carinii pneumonia.
E5812^New	AT791	AT791 is a potent and orally bioavailable inhibitor of TLR7 and TLR9 with an IC50 of 3.33 μM and 0.04 μM, respectively, in human embryonic kidney cells and also inhibits DNA-TLR9 interaction in vitro.
E6039^New	Imiquimod hydrochloride	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.
E7472^New	Pam3CSK4	Pam3CSK4 (Pam3Cys-Ser-(Lys)4) is a synthetic triacylated lipopeptide that serves as a ligand for the Toll-like receptor 2/1 (TLR2/1) heterodimer. It is an agonist of toll-like receptor 1/2 (TLR1/2) with an EC50 of 0.47 ng/mL in human TLR1/2.
E5909^New	CL075	CL075 (3M002) is a selective agonist of TLR8 with immunomodulatory properties. It primes human neutrophils by activating signaling pathways, including p47phox phosphorylation and p38MAPK, leading to enhanced reactive oxygen species (ROS) production and contributing to immune defense.
P1246^New	ODN 1826 sodium	ODN 1826 sodium (CpG 1826 sodium) is a synthetic CpG oligodeoxynucleotide and agonist of TLR9 signaling pathway, that induces G1-phase arrest and apoptosis in A20 lymphoma cells while stimulating NO and iNOS production in mouse models, as part of its immunostimulatory activity.

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