tlr1/2

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).

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.

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

Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma model. 1.Morin, M.D., Wang, Y., Jones, B.T., et al.Diprovocims: A new and exceptionally potent class of toll-like receptor agonistsJ. Am. Chem. Soc.140(43)14440-14454(2018) 2.Wang, Y., Su, L., Morin, M.D., et al.Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in miceProc. Natl. Acad. Sci. U.S.A.115(37)E8698-E8706(2018)

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, 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.

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 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.

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).