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TLR
TLR Products
- All (38)
- TLR Inhibitors (18)
- TLR Antibodies (3)
- TLR Activators (2)
- TLR Antagonists (4)
- TLR Agonists (9)
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- New TLR Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| 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). |
|
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| 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. | ||
| 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. |
|
|
| 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. | ||
| 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. | ||
| 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. | ||
| 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). | ||
| S7221 | Vesatolimod (GS-9620) | Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7. | ||
| S6597 | TLR2-IN-C29 | TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling. | ||
| S6573 | MD2-IN-1 | MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S0494 | SM 324405 | SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. |
||
| 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). |
|
|
| 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. | ||
| 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. |
|
|
| 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. | ||
| 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). | ||
| S6597 | TLR2-IN-C29 | TLR2-IN-C29 (C29) is a Toll-like receptor 2 (TLR2) inhibitor that inhibits TLR2/1 and TLR2/6 signaling. | ||
| S6573 | MD2-IN-1 | MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD value of 189 μM. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S9730 | CU-CPT9a | CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM. |
||
| 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. | ||
| 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. | ||
| S7221 | Vesatolimod (GS-9620) | Vesatolimod (GS-9620) is a potent and selective orally active small molecule agonist of Toll-like receptor 7. | ||
| 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. | ||
| S0494 | SM 324405 | SM 324405 (compound 9e) is a potent and selective Toll-like receptor 7 (TLR7) agonist with EC50 of 50 nM. | ||
| 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. | ||
| 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. | ||
| 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. |
Choose Selective TLR Inhibitors
Tags: TLR inhibitor|TLR agonist|TLR activator|TLR inducer|TLR antagonist|TLR signaling pathway|TLR assay kit
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