TLR Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
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
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
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
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.	Mol Ther Nucleic Acids, 2025, 36(4):102743 Cancer Cell, 2024, S1535-6108(24)00135-1 Front Immunol, 2024, 15:1354055
S6719	E6446 Dihydrochloride	E6446 dihydrochloride is a specific Toll-like receptor 9 inhibitor.	Int J Biol Sci, 2025, 21(13):5762-5781 Cell Death Dis, 2025, 16(1):60 Diabetes, 2025, 74(3):409-415
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
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 Letters, 2021, 75-90 Cancer Lett, 2021, 503:75-90
E5812	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.
E7077	DSRM-3716	DSRM-3716 (5-Iodoisoquinoline, Compound 6) is a potent and selective inhibitor of SARM1 with an IC50 of 75 nM. It robustly blocks axonal degeneration by preventing cADPR elevation following axotomy or mitochondrial stress.
E5922^New	Enpatoran	Enpatoran is a potent, selective inhibitor of Toll-like receptors 7 and 8 (TLR7/8), with IC50 of 11.1 nM and 24.1 nM, respectively, in HEK293 cells. It also demonstrates potential for treating autoimmune diseases.
E2758^New	Robinin	Robinin is a flavonoid that acts by inhibiting TLR4/NF-κB and TLR2-PI3k-AKT signaling pathways. Robinin reduces oxidized-LDL-induced TLR2 and TLR4 expression at the mRNA level and prevents NF-κB p65 nuclear translocation by regulating TLR-NF-κB signaling. Robinin exhibits anti-inflammatory and anti-tumor effects.
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). This compound 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.
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
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).	Front Vet Sci, 2025, 12:1587391 Nat Commun, 2024, 15(1):1642 Cancer Lett, 2024, 604:217258
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
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. This compound, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. It also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. This chemical 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
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. This compound blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. It significantly reduces the mRNA expression of TLR2 and TLR4. This chemical also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.	Int J Mol Sci, 2025, 26(18)8816 International Journal of Molecular Sciences, 2025, 8816 Journal of Inflammation Research, 2024, 153-170
S9234	Schaftoside	Schaftoside, a bioactive compound found in the Herba Desmodii Styracifolii, exhibits pancreatic lipase inhibitory activity. This compound inhibits the expression of TLR4 and Myd88. It 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.
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.