tlr1

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).

Pam3CSK4 TFA (Pam3Cys-Ser-(Lys)4 TFA) is a Toll-like receptor 1/2 agonist with EC50 of 0.47 ng/mL for human TLR1/2.

a15:0-i15:0 PE is a dia-cyl phosphatidylethanolamine with two branched chains. It functions as an atypical TLR2-TLR1 heterodimer agonist and is immunogenic. This compound activates T cell and dendritic cell (DC) signaling, exhibiting anti-inflammatory properties. Additionally, a15:0-i15:0 PE induces the production of TNFα and IL-6. It is a major component of the A. muciniphila lipid membrane, constituting approximately 50%.

SMU-C68 is a highly selective small molecule agonist of the TLR1/2 heterodimer (EC50=0.009 μM). It activates the NF-κB and MAPK pathways, leading to the release of pro-inflammatory cytokines such as TNF-α and IL-1β. SMU-C68 holds potential for cancer research applications.

ETI60 is an orally active selective TLR inhibitor that targets the nucleoside-binding sites I of TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM) without affecting surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4, and TLR5). It demonstrates nanomolar activity in cell-based, biophysical, and in vivo assays, effectively inhibiting endosomal TLR-mediated pro-inflammatory signaling. ETI60 modulates the expression of genes related to inflammation and significantly improves symptoms in mouse models of psoriasis and systemic lupus erythematosus (SLE). ETI60 is applicable in studies related to autoimmune and inflammatory diseases.

ETI41 is an orally active selective TLR inhibitor that targets the nucleoside-binding site I of TLR7 (IC50= 0.63 μM) and TLR9 (IC50= 0.16 μM), without affecting surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4, and TLR5). It demonstrates nanomolar activity in cell-based, biophysical, and in vivo studies, effectively inhibiting endosomal TLR-mediated pro-inflammatory signaling. ETI41 suppresses the expression of inflammation-related genes and significantly improves symptoms in mouse models of psoriasis and systemic lupus erythematosus (SLE). ETI41 is applicable in research related to autoimmune and inflammatory diseases.

TLR2/9 antagonist 1 (Compound 24) is a reversible covalent antagonist of TLR2, with an IC₅₀ of 0.5 μM for TLR2/TLR6 and 0.6 μM for TLR2/TLR1, as well as TLR9, with an IC₅₀ of 0.32 μM. This compound does not significantly affect other TLR subtypes and is utilized for studying central nervous system diseases and malignancies caused by inflammation.

SMU-C409 is a TLR1/2 agonist with an EC50 of 65 nM in HEK-Blue hTLR2 cells. It activates the TLR1/2–MyD88–NF-κB pathway, inducing TNF-α/IL-1β secretion and strongly activating immune cells, resulting in antitumor immunomodulatory effects. Exhibiting low toxicity in vitro, SMU-C409 is useful for cancer immunology research.

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

Diprovocim-1 is a highly potent, small-molecule TLR1/TLR2 dual agonist with an EC₅₀ of 110 pM for human TLR1/TLR2. Diprovocim-1 can be used in research on immunological adjuvants and anticancer vaccines.

Diprovocim-X (compound 35), a robust TLR1/TLR2 (toll-like receptor 1/2) agonist, exhibits EC 50 values of 0.14 nM for hTLR1/TLR2 and 0.75 nM for mTLR1/TLR2. As a potent in vivo adjuvant in mice, it effectively stimulates the adaptive immune response [1].

NCI 126224 is a Toll-like receptor 4 (TLR4) antagonist that selectively inhibits nitric oxide production induced by the TLR4 agonist LPS in RAW 264.7 macrophages (IC50 = 0.31 µM), while exhibiting weaker effects against the TLR7/8 agonist R-848, TLR1/2 agonist Pam3CSK4, and TLR3 agonist poly(I:C). NCI 126224 also inhibits FSL-1-induced NO production at 0.6 µM and suppresses LPS-induced NF-κB activity in BV-2 glial cells, while reducing IL-1β and TNF-α levels in RAW 264.7 cells (IC50s of 5.92 and 1.54 µM, respectively). 0.42, and 1.54 µM, respectively), demonstrating its significant value in studies of inflammatory and innate immune signaling pathways.

WYJ-2, a selective agonist for toll-like receptor 2/1 (TLR2/1), demonstrates an EC50 of 18.57 nM in HEK 293T cells transiently co-transfected with human TLR2 and TLR1. It induces pyroptosis and has shown anticancer activity against non-small cell lung cancer (NSCLC) [1].

TLR2 Agonist1 (Compound R-7d) serves as an activator for human toll-like receptor 2 (TLR 2) with an EC50 of 116 pM. It enhances the activation of the NF-κB promoter via the TLR2/TLR1 heterodimer.

Pam3CSK4-Biotin is a biotinylated derivative of Pam3CSK4, functioning as a Toll-like receptor 1/2 (TLR1/2) agonist.

Pam3CSK4-Biotin (Pam3Cys-Ser-(Lys)4-Biotin) TFA is the biotinylated version of Pam3CSK4. It acts as an agonist for Toll-like receptor 1/2 (TLR1/2).