TLR

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.

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

TLR7/8-IN-1, a crystalline TLR7/TLR8 inhibitor, is a valuable compound for autoimmune disease research[1].

Imiquimod (R 837) is an immune response modifier that acts as a toll-like receptor 7 agonist.

Resiquimod (R848) is a Toll-like receptor 7 8 (TLR7 TLR8) agonist that induces cytokine upregulation. Resiquimod is an immunomodulator with antitumor and antiviral activity.

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.

Chloroquine phosphate (Aralen phosphate) is an aminoquinoline antimalarial and also is widely used as an autophagy inhibitor. Chloroquine also is an inhibitor of toll-like receptors (TLRs).

A natural, noncaloric sweetener with a potency 300 times more than that of regular sucrose. Exhibits transepithelial p-aminohippurate transport via organic anion transport system interference.

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.

Chloranil (tetrachloro-p-benzoquinone) triggers inflammation and neurological dysfunction through Toll-like receptor 4 signaling and can be used to model inflammation in mice.

RS09 2TFA (1449566-36-2 free base) is a TLR4 agonist. Promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. It acts as an adjuvant in vivo and enhances X-15 specific antibody serum concentrations.

Rabeximod is a potent immunomodulator that reduces the severity of autoimmune diseases in rat models. Rabeximod inhibits arthritis in a time-dependent manner by stimulating TLR2 and TLR4 downstream to block the activation of inflammatory cells, most likely macrophages. Rabeximod effectively reduces brain antigen presentation in mice during anti-inflammatory therapy for traumatic brain injury.

VB 201 is an oxidized phospholipid small molecule with anti-inflammatory activity that inhibits CD14 and Toll-like receptor 2-dependent innate cell activation and limits atherosclerosis, and can be used to study atherosclerosis.

Isatoribine(ANA245) free base is a potent TLR7 receptor agonist with anti-hepatitis C virus infection activity for the study of HCV infection.

TLR7 8 9 antagonist 2 is an orally active and highly bioavailable vTLR7 8 9 antagonist. It inhibits HEK hTLR7, HEK hTLR8, and HEK hTLR9 with IC50s of 0.011 μM, 0.029 μM, and 0.052 μM, respectively. TLR7 8 9 antagonist 2 can be used to study auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis.

ABR-238901 is an oral, active S100A8 A9 blocker that inhibits the interaction of S100A8 A9 with its receptors RAGE(receptor for advanced glycation end products) and TLR4 (toll-like receptor 4). ABR-238901 has potential as a compound for the treatment of myocardial infarction (MI).

AZD8848 is a selective antedrug agonist of toll-like receptor 7 (TLR7). It is developed for the research of asthma and allergic rhinitis.

CU-115 is a selective and potent TLR8 antagonist with IC50 of 1.04 µM and =>50 µM for TLR8 and TLR7, respectively. CU-115 decreases production of TNF-α and IL-1β activated by R-848 in THP-1 cells.

Selgantolimod is an effective and selective toll-like receptor 8 agonists for the treatment of the hepatitis B virus and human immunodeficiency virus infection.

Enpatoran is an inhibitor of TLR7(IC50 = 11.1 nM) and TLR8(IC50 = 24.1 nM). Enpatoran was found to be inactive against TLR3, TLR4, and TLR9 in vitro and in vivo.

CU-CPD107 is a selective agonist of toll-like receptor 8 (TLR8) and also shows activation activity against ssRNA ligands. CU-CPD107 acts as an inhibitor of TLR8 signaling in the presence of R848 (IC50=13.7 μM). CU-CPD107 exhibited coagonist activity in the presence of ssRNA, while CU-CPD107 alone could not affect TLR8 signal transduction.

CL264, a selective agonist of TLR7, can be used in studies about innate immune signals.

DSR-6434 is a selective agonist of TLR7 with antitumor effect. DSR-6434 exhibits EC50s of 7.2 nM and 4.6 nM for human and mouse.

CU-CPT-9a is a potent TLR8 inhibitor (IC50 : 0.5 nM), that suppresses TLR8-mediated proinflammatory signaling in various cell lines and human primary cells-

Polygalasaponin F has anti-neuroinflammatory activity, can inhibit the release of inflammatory cytokines TNF-α and NO induced by lipopolysaccharides (LPS) and reduce the expression of inducible nitric oxide synthases. Polygalasaponin F can significantly i

1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide-I significantly sensitizes the res

Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) has antioxidant and anticancer activity.

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

E6446 inhibits Toll-like receptor (TLR)7 and 9 signaling. E6446 works in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro. When administered to mice, this compound suppress responses to challenge doses of cytidine-phosphate-guanidine (CpG)-containing DNA, which stimulates TLR9.

CU-CPT9b (TLR8-specific antagonist 1) is an antagonist of toll-like receptor 8 (TLR8; Kd = 21 nM). It inhibits activation of NF- B induced by the TLR8 agonist R-848 in TLR8-overexpressing HEK-Blue cells with an IC50 value of 0.7 nM.

Polyinosinic-polycytidylic acid (Poly(I:C)) is a double-stranded RNA (dsRNA) and a TLR3 agonist. Polyinosinic-polycytidylic acid induces natural immunity in mammals.

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

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

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.

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.

Motolimod (VTX-378) (VTX-2337) is an effective and specific Toll-like receptor (TLR) 8 agonist (EC50: 100 nM), > 50-fold selectivity over TLR7.

Bropirimine (U-54461) (U-54461) is a biological response modifier that is thought to act through the induction of lymphokines.

TLR7 8 9-IN-1 is a potent inhibitor of Toll-like receptors 7, 8, and 9 (TLR7 8 9) with an IC50 of 43 nM.

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.

Leonurine hydrochloride (SCM-198 hydrochloride) , a major alkaloid compound extracted from Leonurus japonicas Houtt. (Labiatae), is considered to have antitumor roles.

TLR3-IN-1 (CU CPT 4a) is a selective TLR3 inhibitor (IC50: 3.44 μM in RAW 264.7 cells). It can inhibit TLR3/dsRNA complex-mediated downstream signaling pathways and inhibit the production of TNF-α and IL-1β in whole cells.

Gardiquimod is a TLR7/8 agonist. When used at concentrations below 10 μM, Gardiquimod specifically activates TLR7. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells.

TLR7 8 agonist 3 is a potent activator of TLR7 and TLR8.

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

Protosappanin A (PTA) has anti-oxidative nitrative activities on brain immune and neuroinflammation through regulation of CD14 TLR4-dependent IKK IκB NF-κB inflammation signal pathway; it exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway. Protosappanin A and protosappanin B have antimicrobial activity, they show both alone activities and resistance reversal effects of amikacin and gentamicin against MRSA. Protosappanin A shows strong effect against HIV-1 IN with an IC50 value of 12.6 uM.

Procyanidin B1, isolated from commonly eaten fruits, binds to the TLR4/MD-2 complex and has anti-inflammatory activity.

SM-276001 is a potent, selective agonist of TLR7 and an orally active interferon (IFN) inducer.

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

1. Isofraxidin (Phytodolor) protects leukemia cells from radiation-induced apoptosis via ROS/mitochondria pathway in a p53-independent manner. 2. Isofraxidin has a protective effect against LPS-induced ALI, and the protective effect of Isofraxidin seems to result from the inhibition of COX-2 protein expression in the lung, which regulates the production of PGE2. 3. Isofraxidin possesses significant analgesic and anti-inflammatory activities that may be mediated through the regulation of pro-inflammatory cytokines, TNF-α and the phosphorylation of p38 and ERK1/2.