Toll-like Receptors

Imiquimod (Aldara) is a a heterocyclic imidazoquinoline amide that acts as an immune response modifier.

Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases.

PF-4878691 (3M-852A) is a potent, orally active, and selective Toll-like receptor 7 (TLR7) agonist modelled to dissociate its antiviral and inflammatory activities.

VGX-1027 displays immunomodulatory and anti-inflammatory activities by inhibiting toll-like receptor 4 (TLR4) signaling.

Toll-Like Receptor 7 Ligand II is a cell-permeable hydroxyadenine compound which acts as a potent and highly specific TLR7 (toll-like receptor 7) agonist without any detectable activity towards TLR2/3/5/8/9. It is shown to be 10-times more potent than R848 in stimulating the production of TLR7-dependent cytokines in cultures in vitro .

VTX-2337 is a small-molecule Toll-like receptor 8 (TLR8) agonist with potential immunostimulating and antineoplastic activities.

MD2-IN-1 is an inhibitor of Myeloid differentiation protein 2 (MD2) with a KD of 189 ?μM for the recombinant human MD2 (rhMD2).

GS-9620 is a potent and selective orally active small molecule agonist of Toll-like receptor 7.

Hydroxychloroquine 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.

Isatoribine is a novel guanosine analogue showing immunostimulatory activity both in vivo and in vitro.

S enantiomer of TAK-242. TAK-242 (Resatorvid), a small-molecule inhibitor of Toll-like receptor (TLR) 4 signaling. TAK-242 is in treatment of sepsis and septic shock.

Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system.

Resiquimod is an immune response modifier that acts as a potent TLR 7/8 agonist. Phase 2.

TLR7-agonist-1 is a potent and selective Toll-like Receptor 7 (TLR7) agonist with a LEC of 0.4 μM.

Gardiquimod is a chemical compound which acts selectively at both mouse and human forms of toll-like receptor 7 (TLR7). It functions as an immune response modifier. CAS: 1159840-61-5 (TFA) 1020412-43-4 (free base)

E6446 dihydrochloride is a robust antagonist for TLR7 and TLR9, with potential applications in studying harmful inflammatory responses. Additionally, it acts as a significant inhibitor of SCD1 with a KD of 4.61 μM. This compound can notably suppress adipogenic differentiation and liver lipogenesis via the SCD1-ATF3 pathway. Studies have indicated that E6446 dihydrochloride can enhance liver pathology in mice on a high-fat diet, making it a potential candidate for researching non-alcoholic fatty liver disease (NAFLD).

TLR2-IN-C29 is an inhibitor of TLR2/1 and TLR2/6 signaling.

MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.

IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein.

TLR7 agonist 1 is a potent, selective and oral TLR7 agonist with an IC50 of 90 nM.

CU-CPT9b is a specific TLR8 antagonist, with an IC50 of 0.7 nM. CU-CPT9b shows high binding affinity towards TLR8 with a Kd of 21 nM.

CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67 nM.

CU-CPT17e is a potent multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.

CU-CPT-9a is a specific TLR8 antagonist, with an IC50 of 0.5 nM.

LHC-165 is a TLR7 agonist. Has potential to treat solid tumors.

CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor.

MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity.

Telratolimod is a toll like receptors 7/8 (TLR7/8) agonist, with antitumor activity.

AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.

TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.

TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.

E6446 is an inhibitor os Toll-like receptor (TLR)7 and 9 signaling.

TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM.