Toll-like Receptors

Toll-like receptors (TLRs) are single transmembrane cell-surface receptors, which have a key role in the innate immune system. TLRs generally exist as homodimers (heterodimers have been reported) and are found on immune cells; macrophages, B lymphocytes and mast cells.

Pathways (1)
Gene Data

Toll-like Receptor Agonists

Cat. No. Product Name / Activity
6142 CL 075
TLR8 agonist
5414 CU-T12-9
Potent TLR1/2 agonist
4809 DSR 6434
Potent TLR7 agonist
3700 Imiquimod
Toll-like receptor 7 (TLR7) agonist
4637 Pam2CSK4
TLR2/6 agonist; induces TNF-α production
4633 Pam3CSK4
TLR1/2 agonist; induces cytokine production
4287 Poly(I:C)
TLR3 agonist
4536 Resiquimod
Toll-like receptor 7 (TLR7) agonist
5445 SM 324405
Potent TLR7 agonist

Toll-like Receptor Antagonists

Cat. No. Product Name / Activity
6858 MMG 11
TLR2 antagonist

Toll-like Receptor Inhibitors

Cat. No. Product Name / Activity
5373 C34
TLR4 inhibitor
4884 CU CPT 22
Selective TLR1/2 inhibitor
4883 CU CPT 4a
Selective TLR3 inhibitor
6479 CU CPT 9a
Highly potent TLR8 inhibitor
5648 Hydroxychloroquine sulfate
TLR9 inhibitor; also Autophagy inhibitor
5705 M62812
TLR-4 inhibitor
6587 TAK 242
TLR4 signaling inhibitor


Cat. No. Product Name / Activity
7414 DSRM-3716
Potent and reversible SARM1 NAD hydrolase inhibitor
3270 GIT 27
Interferes with TLR4, TLR2/6 signaling

Related Targets

Toll-like receptors (TLRs) are single transmembrane cell-surface receptors, which have a key role in the innate immune system. TLRs generally exist as homodimers (although TLR2-TLR6 heterodimers have been reported) and are found on immune cells such as macrophages, B lymphocytes and mast cells.

Toll-like receptors are activated by molecules associated with biological threat and are highly specific towards evolutionarily conserved entities on microbes, such as bacterial cell-surface lipopolysaccharides, flagella and unmethylated CpG islands. It has been suggested that some toll-like receptors may have endogenous ligands, such as Hsp60 and fibrinogen, and this has promoted speculation that endogenous toll-like receptor activators may have a pathological role in autoimmune disease.

Activation of toll-like receptors initiates downstream signaling cascades, initially via the adapter molecules MyD88, Trap, Trif and Tram, which converge on the PI3K and NF-κB pathways and regulate intracellular kinases and gene expression. This can stimulate an inflammatory and/or antigen-specific immune response. The signaling cascade coupled to toll-like receptor activation is very similar to that of interleukin-1 receptor (IL-1R) activation.

External sources of pharmacological information for Toll-like Receptors :

    Pathways for Toll-like Receptors

    Toll-like Receptor Signaling Pathway

    Toll-like Receptor Signaling Pathway

    TLR signaling is involved in the cellular response to threatening molecules such as bacteria and viruses. It results in an inflammatory and immmunological response.

    Toll-like Receptor Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    TLR1 Human TLR1 NM_003263 Q15399
    Mouse Tlr1 NM_030682 Q9EPQ1
    Rat Tlr1 XM_223421 -
    TLR2 Human TLR2 NM_003264 O60603
    Mouse Tlr2 NM_011905 Q9QUN7
    Rat Tlr2 NM_198769 Q6YGU2
    TLR3 Human TLR3 NM_003265 O15455
    Mouse Tlr3 NM_126166 Q99MB1
    Rat Tlr3 NM_198791 Q7TNI8
    TLR4 Human TLR4 NM_138554 Q9UK78
    Mouse Tlr4 NM_021297 Q9QUK6
    Rat Tlr4 NM_019178 Q9QX05
    TLR5 Human TLR5 NM_003268 O60602
    Mouse Tlr5 NM_016928 Q9JLF7
    Rat Tlr5 XM_223016 Q80Z87
    TLR6 Human TLR6 NM_006068 Q9Y2C9
    Mouse Tlr6 NM_011604 Q9EPW9
    Rat Tlr6 NM_207604 Q6P690
    TLR7 Human TLR7 NM_016562 Q9NYK1
    Mouse Tlr7 NM_133211 P58681
    Rat Tlr7 NM_001097582 XP_228909
    TLR8 Human TLR8 NM_016610 Q9NR97
    Mouse Tlr8 NM_133212 P58682
    Rat Tlr8 NM_001101009 XP_001070405
    TLR9 Human TLR9 NM_017442 Q9NR96
    Mouse Tlr9 NM_031178 Q9EQU3
    Rat Tlr9 NM_198131 Q80VG6
    TLR10 Human TLR10 NM_030956 Q9BXR5
    Rat Tlr10 XM_223422 XP_223422
    TLR11 Mouse Tlr11 NM_205819 Q6R5P0
    Rat Tlr11 XM_573751 XP_573751
    TLR12 Mouse Tlr12 NM_205823 Q6QNU9
    Rat Tlr12 NM_001108682 XP_342923
    TLR13 Mouse TLR13 NM_205820 Q6R5N8