tlr9

TLR9-IN-1 is a selective and potent TLR9 inhibitor that acts on human TLR9 (IC50: 7 nM). TLR9-IN-1 can be used in the study of adverse immune response-related diseases.

TLR9-IN-18 is a potent and selective TLR9 antagonist. TLR9-IN-18 suppresses the production of the proinflammatory cytokine IL-6 in a CpG-induced mouse model.

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.

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).

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.

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

BMS-905 is a potent dual inhibitors of TLR7 and TLR8 with good selectivity against TLR9 and other family members. BMS-905 can be used in studies about the treatment of diseases such as psoriasis, arthritis, and lupus.

Pixatimod (also known as PG-545) is a synthetic modified heparan sulfate mimetic and an agonist of Toll-like receptor 9 (TLR9), showcasing potential immunostimulatory, antitumor, and antiviral properties. It effectively inhibits SARS-CoV-2 by disrupting the interaction between the spike protein and ACE2. Moreover, Pixatimod blocks cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These activities have demonstrated significant efficacy across various murine cancer models, including approximately 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, underscoring its clinical potential, with drugs like gemcitabine, paclitaxel, sorafenib, platinum-based compounds, and an anti-PD-1 antibody.

ODN 1826 is a 20-mer DNA strand, a TLR9 agonist and an immunostimulant, with anti-tumor and cardioprotective effects, promoting apoptosis, and stimulating the production of NO and iNOS. ODN 1826 is a CpG DNA mimetic that can be used as an adjuvant for synthetic vaccines.

Biotin-labeled ODN TTAGGG (sodium) is an inhibitory oligonucleotide (ODN) that antagonizes TLR9, AIM2, and cGAS, serving as a tool for assessing cellular uptake and localization of CpG ODN using biotin detection systems and light microscopy.

FITC-labeled ODN 2395 (sodium), a class C oligodeoxynucleotide and TLR9 agonist, facilitates the assessment of CpG ODN cellular uptake and localization via confocal laser-scanning microscopy [excitation 495 nm, emission 520 nm] or flow cytometry.

FITC-labeled ODN 1585 (sodium) effectively induces IFN and TNFα production and serves to assess CpG ODN cellular uptake and localization via confocal laser-scanning microscopy [excitation 495 nm, emission 520 nm] or flow cytometry.

FITC-labeled ODN TTAGGG (sodium) is an inhibitory oligonucleotide that antagonizes TLR9, AIM2, and cGAS, aiding in assessing CpG ODN cellular uptake and localization through confocal laser-scanning microscopy (excitation at 495 nm, emission at 520 nm) or flow cytometry.

Tylogenin, a steroidal aglycone generated by acid hydrolysis from two seasonal glycosides occurring in Tylophora sylvatica, inhibits IgE-induced basophil mediator release for allergic reactions. In the rabbit basophil-dependent serotonin release (BDSR) assay system, the inhibitory activity of tylogenin was significantly greater than that of its parent glycosides, tylophoroside and acetyltylophoroside, and that of dexamethasone. The activity of tylogenin was found to increase with the incubation time. In the human leukocyte-dependent histamine release test model, the glycosides had only a minimal activity. In contrast, tylogenin, with a geom mean IC50 = 49 microM, exerted a significantly greater potency than dexamethasone. These results suggest that tylogenin could represent a new class of antiallergic agents.

E6446 dihydrochloride is a novel synthetic antagonist for nucleic acid-sensing TLRs; potently suppressed DNA stimulation of HEK:TLR9 cells with IC50 of 10 nM.

AT791 is an orally available TLR7 and TLR9 inhibitor, suppressing TLR7 and TLR9 signaling, used in autoimmune lupus research.

TIC10g is a dual inhibitor of Toll-like receptors 7 and 9 (TLR7 and TLR9), effectively suppressing the release of TNF-α mediated by TLR7 and TLR9 in mouse macrophages (with IC50 values of 14.5 μM and 6.5 μM, respectively) and in human B lymphocytes (with IC50 values of 7.69 μM and 11.5 μM, respectively). TIC10g inhibits the activation of NF-κB and MAPK, exhibiting anti-inflammatory activity useful in treating conditions such as systemic lupus erythematosus and rheumatoid arthritis.

FITC-labeled Agatolimod (sodium), a class B CpG ODN (oligodeoxynucleotide) and TLR9 agonist, enables the evaluation of CpG ODN cellular uptake and localization using confocal laser-scanning microscopy (excitation 495 nm, emission 520 nm) or flow cytometry.

AJ2-30 is an SLCl5A4 inhibitor that inhibits TLR9-mediated B cell activation and inhibits MDP transporter.AJ2-30 inhibits endogenous NOD signaling in human and mouse macrophages.AJ2-30 can be used for the study of inflammation.

Tilsotolimod sodium, a synthetic Toll-like receptor 9 (TLR9) agonist, has shown antitumor activity in preclinical models.

ODN 4084-F, a class B ('broadly-active') inhibitory ODN, is a potent inhibitor of TLR9-induced B cells and macrophages.

Biotin-labeled ODN 1018 (sodium), a TLR-9 agonist oligodeoxynucleotide, is used to evaluate cellular uptake and localization of CpG ODNs via biotin detection systems and light microscopy.