tlr

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

TLR7 agonist 2 (TLR7-IN-1) is a specific and effective Toll-like Receptor 7 (TLR7) agonist (LEC=0.4 μM).

TLR7/8 agonist 1 dihydrochloride (TLR7/8 agonist-5d) is a TLR7/8 agonist which shows prominent immunostimulatory activities.

MD2-TLR4-IN-1 is a myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex inhibitor.

IAXO-102 is a TLR4 antagonist that negatively regulates TLR4 signaling by inhibiting MAPK and p65 NF-κB phosphorylation, as well as the expression of TLR4-dependent proinflammatory proteins. It also prevents the development of experimental abdominal aortic aneurysm.

Resiquimod (R848) is an agonist of Toll-like receptors 7 and 8 (TLR7/TLR8) that induces the upregulation of cytokines including TNF-α, IL-6, and IFN-α. It possesses immunomodulatory, antitumor, and antiviral activities, and can be used to induce models of myocarditis and systemic lupus erythematosus (SLE).

Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.

Resatorvid (TAK-242), a selective Toll-like receptor 4 (TLR4) inhibitor, binds directly to Cys747 to prevent TLR4-TIRAP interaction, thereby blocking downstream signaling. Resatorvid exhibits antitumor, anti-inflammatory, and neuroprotective activities.

Imiquimod (R 837) is an immune response modifier and a toll-like receptor 7 (TLR7) agonist with antiviral and antitumor effects. It is used in the study of external genital warts, perianal warts, cancer, and COVID-19, and is commonly employed to induce psoriasis models.

Chloroquine phosphate (Aralen phosphate) is an antimalarial and anti-inflammatory agent widely used for malaria and rheumatoid arthritis. Chloroquine phosphate acts as an inhibitor of autophagy and toll-like receptors, effectively suppressing SARS-CoV-2 (COVID-19) infection (EC50 = 1.13 μM). Chloroquine phosphate can be utilized in research on autophagy, lysosomal function, and tumor diseases.

Hydroxychloroquine sulfate (Acidum iopanoicum) inhibits plasmodial heme polymerase. It is a chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa.

Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5).

Hydroxychloroquine (2-[[4-[(7-Chloroquinolin-4-yl)amino]pentyl](ethyl)amino]ethanol) (HCQ) is an alkalinizing lysosomatropic drug that acts by inducing apoptosis of renal cancer cells in vitro and inhibiting TLR7/9. It is a medication used to prevent and treat malaria, and it's also being studied as an experimental treatment for COVID-19.

SM-324405 is an agonist of TLR7.

1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist known for its anti-tumor properties.

Pam3CSK4 TFA (Pam3Cys-Ser-(Lys)4 TFA) is a Toll-like receptor 1/2 agonist with EC₅₀ of 0.47 ng/mL for human TLR1/2.

CU-CPT17e is a potent agonist of TLR(TLR3, TLR8, and TLR9).

CU-T12-9 is a potent TLR1/2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay). It acts by activating the NFkB pathway, upregulating proinflammatory cytokines, and enhancing TLR1 and TLR2 dimerization.CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 binds at the interface of TLR1 and TLR2 (IC₅₀ = 0.58 μM). It competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 (Ki: 0.41 μM).

Loxoribine (RWJ 21757) is a guanosine analog. Loxoribine is an orally bioavailable and selective Toll-like receptor (TLR) 7 agonist. It has anti-viral and anti-tumor activities.Loxoribine is a potent new immunostimulant with a relatively broad spectrum of immunobiological activities.

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

Telratolimod (MEDI9197) is a toll-like receptors 7/8 agonist. It has an antitumor activity.

Robinin (NSC-9222) belongs to natural products, serving as a TLR2 inhibitor with cell permeability. Robinin exerts anti-inflammatory and antitumor activities through inhibiting the TLR2-PI3K-AKT pathway, and can be used for experimental research related to pancreatic cancer.

C29 is a novel inhibitor of TLR2/1 and TLR2/6 signaling induced by synthetic and bacterial TLR2 agonists in human HEK-TLR2 and THP-1 cells, but only TLR2/1 signaling in murine macrophages.