tlr 1

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

CU-T12-9 is a potent TLR1/2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay). It acts by activating the NFkB pathway, upregulating proinflammatory cytokines, and enhancing TLR1 and TLR2 dimerization.CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 binds at the interface of TLR1 and TLR2 (IC50 = 0.58 μM). It competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 (Ki: 0.41 μM).

TLR7 agonist 1 is a selective and oral TLR7 agonist (IC50: 90 nM).

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.

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 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.

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

TLR4-IN-1 (compound 3k) demonstrates potent inhibition of RAW264.7 cell viability with an IC 50 value of 1.02 μM. Additionally, it suppresses the release of cytokines TNF-α, IL-1β, and IL-6, and shows anti-inflammatory effectiveness in rat models of rheumatoid arthritis.

TLR4/NF-κB-IN-1 (Compound 7x) is an orally bioavailable inhibitor targeting the TLR4/NF-κB signaling pathway, with anti-inflammatory properties and the ability to cross the blood-brain barrier. It can alleviate LPS-induced acute neuroinflammation in mice and downregulate the protein expression of TLR4, P-NF-κB, and P-IκB-α.

TLR8 antagonist 1 (Compound 10) is a selective antagonist that can inhibit TLR8 mediated inflammation and signaling pathways. TLR8 antagonist 1 reduces MyD88 recruitment and inhibits NF - κ B and IRF pathways, exhibiting certain anti-inflammatory activity.

P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.

TLR7-IN-1 (compound 16-A) is a TLR7 inhibitor with an EC50 value of 0.001 µM.

TLR2antagonist-1 is a selective antagonist of Toll-like receptor 2 (TLR2). It effectively inhibits excessive activation of TLR2, with an IC50 value of 11.41 μM, and reduces the production of inflammatory factors. TLR2antagonist-1 exhibits metabolic stability, with a half-life (T1/2) of 16.67 minutes in mouse liver microsomes. This compound is useful for research in inflammation, immunology, and neurological disorders.

NOD2/TLR4 agonist-1 (Compound 2) is a dual agonist for NOD2 and TLR4. It does not possess immunostimulatory activity, making it a significant negative control in research studies.

TLR9-IN-1 (compound 29) is an effective and selective TLR9 inhibitor with an IC50 of 7 nM in human B cells, suitable for autoimmune diseases and inflammation.

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

TLR7/8 agonist 1 is a toll-like receptor TLR7/TLR8 agonist with anticancer and antiviral activities and can be used to study immune-related diseases.

Tri(TLR4-IN-C34-C2-amide-PEG1)-amide-C3-COOH is a chemical linker with the TLR4 inhibitor TLR4-IN-C34, which inhibits TLR4 in enterocytes and macrophages, reducing systemic inflammation in mouse models of endotoxemia and necrotizing enterocolitis [1].

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

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

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].