tlr9

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.

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.

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 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.

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).

Pixatimod (also known as PG-545) is a synthetic carbohydrate-modified heparan sulfate mimetic and a Toll-like receptor 9 (TLR9) agonist. It exhibits potential immunostimulatory, antitumor, and antiviral effects. Pixatimod effectively inhibits SARS-CoV-2 by disrupting the spike protein-ACE2 interaction. Additionally, it blocks various cancer-promoting processes such as cell proliferation, invasion, metastasis, angiogenesis, and epithelial-mesenchymal transition. These effects have demonstrated significant efficacy in numerous mouse cancer models, including about 30 xenograft models and 20 syngeneic models. Pixatimod has been tested in combination with several approved anticancer compounds, showing clinical potential when used with gemcitabine, paclitaxel, sorafenib, platinum compounds, and anti-PD-1 antibodies.

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.

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.

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.

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

ODN 2088 is a potent inhibitor of TLR3, TLR7 and TLR9 that is non-cytotoxic and shows inhibition of the release of IFN-α and IL-6.

ODN 21158 is a potent, non-cytotoxic inhibitor of G-modified TLR3 and TLR9. ODN 21158 dose-dependently inhibits IFN-α secretion.

BMS-986122 is a IRAK4 Inhibitor. BMS-986126 attenuates Disease in Murine Lupus Models and Demonstrates Steroid Sparing Activity. BMS-986126 inhibited TLR7- and TLR9-dependent responses using cells derived from lupus patients, suggesting that inhibition of IRAK4 has the potential for therapeutic benefit in treating lupus.

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.

CpG ODN 10101 (CPG 10101) is a novel potent and selective Toll-like receptor 9 (TLR9)-containing oligodeoxynucleotide agonist with antiviral activity for the treatment of chronic infections.

ODN 1668 is an immunostimulatory class B CpG oligodeoxynucleotide (ODN) containing an intact thio backbone of one or more CpG dinucleotides, which is primarily used as an agonist for Toll-like receptor 9 (TLR9), and also upregulates the level of IgM and induces an antimicrobial immune response via a CaTLR9-dependent pathway.

ODN 2395, a class C oligodeoxynucleotide and TLR9 agonist, serves as a vaccine adjuvant. Its sequence is 5'-tcgtcgttttcggcgc:gcgccg-3' [1].

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.

FITC-labeled ODN 1018 (sodium), a TLR-9 agonist oligodeoxynucleotide, enables the evaluation of CpG ODN cellular uptake and localization via confocal laser-scanning microscopy [excitation 495 nm, emission 520 nm] or flow cytometry.

Biotin-labeled Agatolimod (sodium), a class B CpG ODN (oligodeoxynucleotide) and TLR9 agonist, facilitates the assessment of cellular uptake and localization of CpG ODNs through a biotin detection system with light microscopy.