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

TLR7/8/9 antagonist 2 is an orally active and highly bioavailable vTLR7/8/9 antagonist. TLR7/8/9 antagonist 2 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.

TLR1 is a cell-penetrating Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop mimic and inhibits IL-1 receptor-mediated responses.

TLR4 agonist-1 (TEA, compound 17a) is a potent activator of Toll-like Receptor 4 (TLR4) and prompts the production of MIP-1β in RAW 264.7 and MM6 cells [1].

TLR4 agonist-1 (compound 17a) serves as a potent activator of Toll-like Receptor 4 (TLR4) and stimulates the production of MIP-1β in RAW 264.7 and MM6 cells [1].

TLR7/8 agonist 4 hydroxy-PEG6-acid, a Drug-Linker Conjugate for ADCs, comprises the TLR7/8 agonist 4 and a hydroxy-PEG6-acid linker, suitable for the synthesis of antibody-drug conjugates (ADCs) [1].

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

TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugate employed in antibody-drug conjugates (ADC). This compound exhibits remarkable antitumor activity by utilizing TLR7/8 agonist 4, which acts as a potent activator of TLR7/8. The TLR7/8 agonist 4 is linked to hydroxy-PEG10-acid, the ADC linker, via a cleavable bond. Overall, it demonstrates promising pharmaceutical potential in the context of ADC-based therapeutics.

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

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

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

TLR7/8 agonist 4 TFA (compound 41) is a highly potent TLR7/8 agonist that exhibits significant anti-cancer activity.

TLR7/8 agonist 4 hydroxy-PEG10-acid hydrochloride (compound 9) is a drug-linker conjugate used in antibody-drug conjugates (ADCs) with high efficacy against tumors. It consists of TLR7/8 agonist 4, a potent TLR7/8 agonist, linked to the ADC linker hydroxy-PEG10-acid which can be cleaved.

TLR7 agonist 3 (Compound 2), a potent activator of toll-like receptor 7 (TLR7), plays a critical role in initiating immune responses, positioning it as a promising target for immunomodulator development.

TLR7/8 agonist 6 (Compound 4), an imidazoquinoline derivative, is a potent TLR7/8 agonist with IC50 values of 0.18 and 5.34 μM for TLR7 and TLR8, respectively. TLR7/8 Antagonist

TLR8 agonist 2 hydrochloride is a highly potent and selective agonist for human TLR8, exhibiting an EC50 of 3 nM. However, its activity towards human TLR7 is considerably weaker, with an EC50 of 33.33 μM.

MD2-TLR4-IN-1 is a myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex inhibitor.

TLR4-IN-C34-C2-COO is a linker compound that incorporates TLR4 inhibitor TLR4-IN-C34. It effectively inhibits TLR4 activity in enterocytes and macrophages. Moreover, it demonstrates a notable ability to mitigate systemic inflammation in murine models of endotoxemia and necrotizing enterocolitis.

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

TLR8 agonist 2 is a highly effective and specific compound that activates TLR8, possessing an EC 50 of 3 nM in human TLR8. Notably, TLR8 agonist 2 demonstrates lower activity towards human TLR7, with an EC 50 of 33.33 μM.

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.

TLR7/8 agonist-7d is a useful organic compound for research related to life sciences and the catalog number is T64606.

Compound 17b, a TLR7 agonist also known as TLR7 agonist 14, exhibits high potency with an EC50 of 18 nM. It effectively activates mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) at low-nanomolar concentrations [1].

TLR7/8 agonist 9 (Compound 25a), exhibiting EC50 values of 40 nM and 23 nM for hTLR7 and hTLR8 respectively, demonstrates anti-tumor properties and enhances the efficacy of PD-1/PD-L1 blockade treatments. This compound is utilized in cancer immunotherapy research [1].

Compound A, a potent TLR8 agonist, exhibits an EC50 of 0.052 µM and promotes the production of IL-12p40 in human PBMCs with an EC50 of 0.031 µM. This compound is applicable for research in virus resistance, infection resistance, autoimmunity, and tumor studies [1].

TLR7/8 agonist 4 (compound 41) is a potent agonist of TLR7/8 with anti-cancer activity [1].

TLR7/8 agonist 1 is a toll-like receptor ( TLR7 )/ TLR8 dual-agonistic imidazoquinoline.

Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a chemical linker featuring the TLR4 inhibitor TLR4-IN-C34, known for inhibition of TLR4 in enterocytes and macrophages, thereby diminishing systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis [1].

TLR7 agonist 12 (example 20), a purine nucleoside analog, functions as a TLR7 agonist with broad antitumor activity, particularly against indolent lymphoid malignancies. Its anticancer mechanisms include DNA synthesis inhibition, apoptosis induction, among others [1] [2].

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.

TLR7/8 agonist 4 hydroxy-PEG6-acid hydrochloride, a Drug-Linker Conjugate for ADC synthesis, is the hydrochloride variant of TLR7/8 agonist 4 hydroxy-PEG6-acid, comprising the TLR7/8 agonist 4 component attached to the hydroxy-PEG6-acid linker [1].

TLR7 agonist 15 (compound 16b) is a potent activator of mouse macrophages and hPBMCs, demonstrating an EC50 of 18 nM. It induces robust responses at low-nanomolar concentrations [1].

Tri(TLR4-IN-C34-C2-amide-C3-amide-PEG1)-amide-C3-COOH, a chemical compound, serves as a linker incorporating TLR4 inhibitor TLR4-IN-C34. This compound effectively inhibits TLR4 in both enterocytes and macrophages, significantly reducing systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis [1].

TLR7/8 agonist 7, a compound that functions as a TLR7/8 agonist, plays a pivotal role in activating various immune cells and is instrumental in the synthesis of immune-stimulating antibody conjugate (ISAC) molecules. This compound holds significant potential for research in immunology.

TLR7 agonist 4 (Compound 1.2) is a TLR7 agonist (EC50: 4.3 nM).

Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH is a chemical linker incorporating the TLR4 inhibitor, TLR4-IN-C34, which suppresses TLR4 activity in enterocytes and macrophages, consequently diminishing systemic inflammation observed in mouse models of endotoxemia and necrotizing enterocolitis [1].

TLR8 Agonist 5, exhibiting potent efficacy as a TLR8 agonist, demonstrates an EC50 of 20 nM in HEK-Blue hTLR8, effectively activating the immune response.

TLR4/NF-κB/MAPK-IN-1 is a novel antineuroinflammatory agent that functions by inhibiting the TLR4/NF-κB/MAPK pathways.

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 has been shown to enhance the efficacy of PD-1/PD-L1 inhibitors in antitumor activity [1].

TLR4-IN-C34-C2-amide-C6-OH, a chemical compound, serves as a linker encompassing the TLR4 inhibitor TLR4-IN-C34. This inhibitor is known to target TLR4 in enterocytes and macrophages, effectively reducing systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis [1].

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.

TLR7 agonist 13 is a useful organic compound for research related to life sciences. The catalog number is TNU1350 and the CAS number is 2389988-70-7.

TLR7 agonist 16 (compound 16d) is a potent activator of TLR7 with an EC50 value of 18 nM. It effectively triggers the activation of both mouse macrophages and human peripheral blood mononuclear cells (hPBMCs) at low-nanomolar levels [1].

MC-Val-Cit-PAB-Amide-TLR7 agonist 4 (example 15) is a conjugate that acts as an immune agonist targeting both HER2-TLR7 and HER2-TLR8 pathways [1].

TLR7/8 antagonist 2 (Compound 15) is a highly potent and orally active agonist of TLR7/8, exhibiting IC50 values of 4.9 and 0.6 nM for TLR7 and TLR8, respectively. Its strong affinity for these receptors makes it a promising candidate for the treatment and investigation of autoimmune diseases, including lupus erythematosus, which is associated with inappropriate activation of TLR7 and TLR8. Consequently, TLR7/8 antagonist 2 represents a valuable tool for research in the field of autoimmune diseases [1].

TLR8 agonist 4 was effective in inhibiting both wild-type and drug-resistant (lamivudine and entecavir) HBV strains with their IC50 values of 0.15 and 0.10 μM, respectively.

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.

Paquinimod (ABR 25757) is a S100A9 inhibitor preventing S100A9 binding to TLR-4.

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).

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