1. Signaling Pathways
  2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)
  4. Toll-like Receptor (TLR) Inhibitors

Toll-like Receptor (TLR) Inhibitors

TLR3

TLR8

TLR9

TLR2

TLR4

TLR7

TLR1

TLR6

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Toll-like Receptor (TLR) Inducers, Inhibitors, Agonists, Antagonists & Activators
Product Name TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6 Purity
Lipopolysaccharides, from E. coli O55:B5        
TLR4
     
Resiquimod  
TLR8
     
TLR7
    99.95%
Resatorvid        
TLR4
      99.95%
Imiquimod          
TLR7
    99.96%
C29      
TLR2
        ≥98.0%
Hydroxychloroquine sulfate    
TLR9
   
TLR7
    99.99%
Pam3CSK4 TFA      
TLR2
   
TLR1
  99.66%
CU-CPT 4a
TLR3, IC50: 3.44 μM (in RAW 264.7 cells)
              99.34%
Enpatoran  
TLR8, IC50: 24.1 nM (in HEK293 cells)
TLR8, IC50: 620 nM (in peripheral blood mononuclear cells (PBMCs))
TLR8, IC50: 120 nM ( in whole blood (WB) cells)
     
TLR7, IC50: 11.1 nM (in HEK293 cells)
TLR7, IC50: 68.3 nM (in peripheral blood mononuclear cells (PBMCs))
TLR7, IC50: 2.2 nM ( in whole blood (WB) cells)
    99.77%
ODN 1826    
TLR9
         
Agatolimod sodium    
TLR9
         
Diprovocim      
TLR2
   
TLR1
  98.35%
Imiquimod hydrochloride          
TLR7
    99.77%
Agatolimod    
TLR9
         
ODN 1826 sodium    
TLR9
          99.51%
CU-CPT22      
TLR2
   
TLR1
  ≥99.0%
TLR4-IN-C34        
TLR4
      99.90%
Telratolimod  
TLR8
     
TLR7
    98.98%
Polyinosinic-polycytidylic acid sodium
TLR3
              99.40%
Motolimod  
TLR8
            98.12%
Physcion        
TLR4
      99.10%
Atractylenolide I    
TLR9
   
TLR7
    99.94%
ODN 2216    
TLR9
         
AT791    
TLR9, IC50: 0.04 μM
   
TLR7, IC50: 3.33 μM
    98.77%
Schaftoside        
TLR4
      99.67%
ODN 1018    
TLR9
         
CU-T12-9      
TLR2, EC50: 52.9 nM (in HEK-Blue cells)
   
TLR1, EC50: 52.9 nM (in HEK-Blue cells)
  98.94%
Selgantolimod  
TLR8
            98.23%
MMG-11      
TLR2
        99.11%
ODN 2395    
TLR9
          98.39%
Enpatoran hydrochloride  
TLR8, IC50: 24.1 nM
     
TLR7, IC50: 11.1 nM
    99.33%
Neoseptin 3        
TLR4, EC50: 18.5 μM
      99.57%
CL097  
TLR8
     
TLR7
    99.89%
CL075  
TLR8
            99.25%
Sparstolonin B      
TLR2
TLR4
      99.54%
FSL-1 TFA      
TLR2
     
TLR6
99.65%
Okanin        
TLR4
      99.98%
ODN 1668    
TLR9
         
D-Glucuronic acid        
TLR4
     
ODN 2395 sodium    
TLR9
         
TLR9-IN-1    
human TLR9, IC50: 7 nM
          99.80%
TLR7/8-IN-1  
TLR8
     
TLR7
    99.92%
Robinin      
TLR2
TLR4
      98.77%
Gardiquimod diTFA  
TLR8
     
TLR7
    ≥99.0%
Isofraxidin        
TLR4
      99.00%
ODN 1668 sodium    
TLR9
          ≥99.0%
Gardiquimod  
TLR8
     
TLR7
    99.91%
IAXO-102        
TLR4
      ≥98.0%
Loxoribine          
TLR7
    99.64%
MD2-IN-1        
TLR4
      99.89%
TLR7/8 agonist 1  
TLR8
     
TLR7
   
NecroX-7        
TLR4
      99.69%
E6446 dihydrochloride    
TLR9
   
TLR7
    99.96%
CU-CPT-8m  
TLR8, IC50: 67 nM
            99.98%
CpG ODN 10101    
TLR9
         
L48H37        
TLR4
     
Monophosphoryl lipid A        
TLR4
      ≥99.0%
CU-CPT-9a  
TLR8, IC50: 0.5 nM
            99.36%
CAY10614        
TLR4, IC50: 1.675 μM (in HEK293 cells)
      98.04%
TLR7/8 agonist 3  
TLR8
     
TLR7
    99.96%
CU-CPT17e
TLR3
TLR8
TLR9
          99.00%
CL264          
TLR7
    98.63%
DSR-6434          
TLR7, EC50: 7.2 nM (Human)
TLR7, EC50: 4.6 nM (Mice)
    99.55%
Procyanidin B3        
TLR4
      99.63%
TLR7 agonist 3          
TLR7
    99.90%
GSK2245035          
TLR7
    99.85%
ODN M362    
TLR9
         
ODN 20844    
TLR9
   
TLR7
   
Kaempferol 3-O-sophoroside      
TLR2
TLR4
      99.84%
AN-3485
TLR3
   
TLR2
TLR4
     
Imiquimod maleate          
TLR7
    99.25%
L6H21        
TLR4
      99.46%
LHC-165          
TLR7
    ≥98.0%
Fosfenopril        
TLR4
      99.89%
CU-115  
TLR8, IC50: 1.04 μM
     
TLR7, IC50: 50 μM
    99.55%
TLR7/8 agonist 4  
TLR8
     
TLR7
    99.04%
CU-CPT9b  
TLR8, IC50: 0.7 nM
TLR8, Kd: 21 nM
            99.03%
E6446    
TLR9
   
TLR7
    ≥98.0%
ssRNA40 sodium  
TLR8
     
TLR7
   
1V209          
TLR7
    99.67%
Polygalasaponin F        
TLR4
      99.85%
RKH acetate        
TLR4
      99.45%
Resiquimod (GMP)  
TLR8
     
TLR7
   
AZD8848          
TLR7
    99.14%
PF-4878691          
TLR7
    99.89%
Chloranil        
TLR4
      98%
TLR7 agonist 6          
TLR7, EC50: ~4 nM
    98.08%
MAPK-IN-1        
TLR4
     
Resiquimod-d5  
TLR8
     
TLR7
    99.84%
TLR7 agonist 1          
TLR7, IC50: 90 nM
    98.95%
MMG-11 quarterhydrate      
TLR2
        99.09%
ODN 24987    
TLR9
         
SM-324405          
human TLR7, pEC50: 7.3
Rat TLR7, pEC50: 6.6
TLR7, EC50: 50 nM
    98.52%
FAM-labeled ODN 1826 sodium    
TLR9
          98.03%
CL097 hydrochloride  
TLR8
     
TLR7
    99.51%
TLR4-IN-C34-C2-amide-C6-OH        
TLR4
      99.62%
BBIQ          
TLR7, EC50: 59.1 nM (Human TLR7)
    99.85%
Kdo2-Lipid A ammonium        
TLR4
      99.00%
ORN 06 sodium          
TLR7
   
SMU-L11          
TLR7, EC50: 0.024 μM
    99.64%
Diprovocim-X      
TLR2
   
TLR1
  98.64%
TMX-201          
TLR7
   
ODN M326 sodium    
TLR9
         
MC-Val-Cit-PAB-Amide-TLR7 agonist 4  
TLR8
     
TLR7
    99.39%
TLR7 agonist 4          
TLR7, EC50: 4.3 nM
    98.87%
AXC-715 hydrochloride  
TLR8
     
TLR7
    99.46%
E104          
TLR7
   
Hydroxychloroquine sulfate (Standard)    
TLR9
   
TLR7
   
Pam3CSK4      
TLR2
   
TLR1
 
TLR7 agonist 20 hydrochloride  
TLR8, EC50: 17.21 μM
     
TLR7, EC50: 0.23 μM
    99.86%
ODN 24888    
TLR9
   
TLR7
   
PVP-037.2  
TLR8
     
TLR7
   
TLR7/8 agonist 8  
TLR8, EC50: 12 nM
     
TLR7, EC50: 27 nM
   
(S)-Hydroxychloroquine    
TLR9
   
TLR7
   
Guretolimod          
TLR7
   
(R)-Hydroxychloroquine    
TLR9
   
TLR7
   
TLR8 agonist 2 hydrochloride  
TLR8, EC50: 3 nM
     
TLR7, EC50: 33.33 μM
   
TLR8 agonist 2  
TLR8, EC50: 3 nM
     
TLR7, EC50: 33.33 μM
   
TLR7/8 agonist 4 TFA  
TLR8
     
TLR7
   
UC-1V150          
TLR7
   
Mumefural        
TLR4
     
TLR7 agonist 17          
human TLR7, EC50: 12 nM
mTLR7, EC50: 17 nM
   
ORN 06          
TLR7
   
Eritoran        
TLR4
     
WYJ-2      
TLR2
       
RC529-MDP        
TLR4
     
TLR7 agonist 20  
TLR8, EC50: 17.21 μM
     
TLR7, EC50: 0.23 μM
   
TLR7-IN-1          
TLR7, IC50: 0.001 μM
   
Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH        
TLR4
     
BI1543673  
TLR8
   
TLR4
TLR7
   
TLR7 agonist 7          
TLR7, EC50: ~4 nM
   
Polyinosinic-polycytidylic acid potassium
TLR3
             
TLR7 agonist 21  
TLR8, EC50: 5932 nM
     
human TLR7, EC50: 17.53 nM
mTLR7, EC50: 41.7 nM
   
TLR7 agonist 24          
TLR7, EC50: 3.72 μM
   
TLR7 agonist 9          
TLR7
   
TLR8 agonist 7  
TLR8
           
NF-κB-IN-14        
TLR4
     
ORN 02  
TLR8
           
FSL-1      
TLR2
     
TLR6
Vidutolimod    
TLR9
         
TLR7 agonist 27          
TLR7, EC50: 238.1 nM
   
Macrophage-activating lipopeptide 2      
TLR2
     
TLR6
TLR8 agonist 8  
TLR8
           
Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH        
TLR4
     
Pam3CSK4-Biotin      
TLR2
   
TLR1
 
TLR7 agonist 5          
TLR7, EC50: ~4 nM
   
ODN M326    
TLR9
         
TLR8 agonist 9  
TLR8
           
TLR7/8 agonist 11  
TLR8, EC50: 13.1 nM
     
human TLR7, EC50: 31.1 nM
   
TLR2 agonist 1      
hTLR2, EC50: 116 pM
       
Xanthine oxidase-IN-6        
TLR4
     
ORN 02 sodium  
TLR8
           
3M-011  
TLR8
     
TLR7
   
MTT5          
TLR7
   
M199
TLR3
 
TLR9
         
Rabeximod      
TLR2
TLR4
     
TLR7 agonist 8          
TLR7, EC50: ~4 nM
   
TLR7/8 agonist 9  
TLR8
     
TLR7
   
TLR7 agonist 26          
TLR7, EC50: 225.5 nM
   
Cholesterol oxidase, rhodococcus sp      
TLR2
       
TLR7 agonist 14          
TLR7, IC50: 18 nM
   
UM-3006  
TLR8
     
TLR7
   
Isatoribine          
TLR7
   
AYK004-B1          
TLR7, EC50: 0.2265 nM