TLR7/8-IN-1

TLR7 8-IN-1, a crystalline TLR7 TLR8 inhibitor from patent WO2019220390 (compound 2b), is a valuable compound for autoimmune disease research.

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.

3M-011, a potent dual toll-like receptor TLR7 8 agonist and cytokine inducer, serves as a powerful adjuvant to radiotherapy, eliciting significant local and systemic immune responses. Additionally, it effectively inhibits H3N2 influenza viral replication in the nasal cavity and exhibits strong antitumor activity[1][2][3].

BI1543673 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4). It can diminish inflammatory responses in human lung tissue stimulated by TLR4 and TLR7 8. Additionally, BI1543673 reduces inflammatory signaling in a mouse lung inflammation model induced by LPS.

Gardiquimod (hydrochloride) is an imidazoquinoline class TLR7 8 agonist. It can inhibit HIV-1 infection in macrophages and activated peripheral blood mononuclear cells (PBMCs). At concentrations below 10 μM, Gardiquimod (hydrochloride) specifically activates TLR7.

TLR7 8 antagonist 2 (Compound 15) is a highly potent and orally active agonist of TLR7 8 with IC50 values of 4.9 nM for TLR7 and 0.6 nM for TLR8, making it a promising candidate for treating and investigating autoimmune diseases like lupus erythematosus, which involves inappropriate activation of TLR7 and TLR8. Consequently, TLR7 8 antagonist 2 is a valuable tool for autoimmune disease research [1].

TLR7 8 Antagonist 1 (Compound 16c), an imidazoquinoline derivative, is a potent TLR7 8 agonist with IC50 values of 3.91 and 2.19 μM for TLR7 and TLR8, respectively. rel-O-2050 (TLR-2050) is a key target for drug development in infectious diseases, cancer, and autoimmune diseases.

HE-S2, an antibody-drug conjugate, elicits a potent antitumor immune response by inhibiting the PD-1 PD-L1 interaction and stimulating the Toll-like receptor 7 8 (TLR7 8) signaling pathway, resulting in significant antitumor activity [1].

TLR7 8 agonist 8 (compound 24m) is a potent dual agonist for toll-like receptors 7 and 8 (TLR7 8), exhibiting half-maximal effective concentrations (EC50s) of 27 nM for human TLR7 (hTLR7) and 12 nM for human TLR8 (hTLR8). This compound enhances the efficacy of PD-1 PD-L1 inhibitors in antitumor activity [1].

TLR7 8 agonist 9 (Compound 25a), with EC50 values of 40 nM for hTLR7 and 23 nM for hTLR8, demonstrates anti-tumor properties and enhances the efficacy of PD-1 PD-L1 blockade treatments, making it valuable for cancer immunotherapy research [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.