TLR3

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.

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).

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

Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic double-stranded RNA (dsRNA) analog and an agonist of TLR3 as well as retinoic acid-inducible gene I (RIG-I) and melanoma differentiation-associated protein 5 (MDA5). It can induce innate immune responses in mammals and serve as a vaccine adjuvant to enhance both innate and adaptive immunity, while modulating the tumor microenvironment and directly inducing apoptosis in cancer cells. Poly(I:C) is commonly used to establish acute respiratory distress syndrome (ARDS) animal models for studying immune responses and disease mechanisms.

Anti-TLR3/CD283 Antibody (CNTO5429) is a CHO-expressed human antibody designed to target TLR3/CD283. It features a huIgG2 heavy chain and a huκ light chain, with an estimated molecular weight (MW) of 145.42 kDa. For its isotype control, refer to HumanIgG4kappa, Isotype Control.

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.

R1-ICR-5 is a selective PROTAC degrader targeting serine/threonine-protein kinase 1 (RIPK1). Mediated by VHL, R1-ICR-5 promotes the degradation of RIPK1, disrupting the TNFR1 and TLR3/4 signaling hubs, enhancing NF-κB, MAPK, and IFN signal output, and facilitating RIPK3 activation and necroptosis induction. R1-ICR-5 holds potential for research in cancer and inflammatory diseases.

SMU-14a is a TLR3 inhibitor with an IC50 of 0.18 µM. It suppresses IL-6 secretion in mouse peritoneal macrophages and downregulates TNF-α in human peripheral blood mononuclear cells. The compound exerts anti-inflammatory effects by reducing the phosphorylation of p65, ERK, and TBK1 via the NF-κB, MAPK, and IRF3 signaling pathways, and by lowering serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST). SMU-14a is applicable in acute hepatitis research.

M199, a novel inhibitor of TLR3/9 activation, induces secretion of IL-6, IL-8 and TNFalpha in human PBMCs.

SMU127 is an agonist of the toll-like receptor 1/2 (TLR1/2) heterodimer.

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.

Poly(I:C):Kanamycin (1:1) is an equimolar mixture of Poly(I:C) and kanamycin. Poly(I:C) is a synthetic double-stranded RNA analogue and TLR3 agonist commonly used as a vaccine adjuvant; kanamycin enhances Poly(I:C) stability.

Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium), a synthetic double-stranded RNA analog, serves as an agonist for toll-like receptor 3 (TLR3) and retinoic acid-inducible gene I (RIG-I)-like receptors (RIG-I and MDA5), offering applications in immunotherapy. Its sodium variant enhances both innate and adaptive immune responses when used as a vaccine adjuvant and is instrumental in modifying the tumor microenvironment. Additionally, Poly(I:C) potassium can directly induce apoptosis in cancer cells [1] [2] [3].

Poly(I:C):Kanamycin (1:1) sodium is a complex.Poly(I:C) is a synthetic double-stranded RNA analogue and a TLR3 and RIG-I/MDA5 agonist that enhances immunity and promotes apoptosis in cancer cells.Kanamycin is an antimicrobial agent that is effective against both Gram-negative and positive bacteria which is able to bind the 70S ribosomal subunit.

Polyinosinic acid, a single-stranded homonucleic acid and a Toll-like Receptor 3 (TLR3) agonist, enhances the cellular immune response through TLR3 and TRIF. It holds potential applications in immune regulation [1].

Guignardone L, a metabolite extracted from the endophytic fungus Guignardia mangiferae, possesses toll-like receptor 3 (TLR3) regulating activity [1].

Biotin-labeled ODN 2088 (sodium) is a potent inhibitor of TLR3, TLR7, and TLR9, used to evaluate cellular uptake and localization of CpG ODN via a biotin detection system in conjunction with light microscopy.

FITC-labeled ODN 2088 (sodium) is a potent inhibitor of TLR3, TLR7, and TLR9, used to assess CpG ODN cellular uptake and localization via confocal laser-scanning microscopy (excitation 495 nm, emission 520 nm) or flow cytometry.

CRAMP (140-173) (mouse), the ortholog of the human LL-37 antimicrobial peptide, inhibits LPS-induced responses and does not colocalize with TLR3 in BEAS-2B cells [1].

NCI 126224, a toll-like receptor 4 (TLR4) antagonist, demonstrates selective inhibition of nitric oxide (NO) production in RAW 264.7 macrophages, triggered by the TLR4 agonist LPS (IC50 = 0.31 µM), as opposed to minimal effects on NO production induced by agonists for TLR7/8 (R-848), TLR1/2 (Pam3CSK4), and TLR3 (poly(I:C)). Nevertheless, it also effectively inhibits NO production initiated by the TLR2/6 agonist FSL-1 at an IC50 of 0.6 µM in the same cell line. Moreover, NCI 126224 suppresses LPS-induced NF-κB activity in BV-2 microglial cells and reduces LPS-triggered increases in IL-1β and TNF-α levels in RAW 264.7 macrophages with IC50 values of 5.92, 0.42, and 1.54 µM, respectively.

Polyinosinic Acid Sodium, the sodium variant of Polyinosinic Acid, is a single-stranded homonucleic acid that acts as a Toll-like Receptor 3 (TLR3) ligand. By engaging TLR3 and TRIF, it bolsters cellular immune response, showing promise for immune regulation applications [1].

CRAMP (140-173) (mouse) TFA is a homolog of the human LL-37 antimicrobial peptide. It inhibits LPS-induced responses and does not colocalize with TLR3 in BEAS-2B cells.