SMU-Z1 is a potent, specific small molecule agonist of TLR1/2, specifically activates TLR2 through its association with TLR1, induces NF‐κB activation in HEK‐Blue hTLR2 cells with EC50 of 4.88 nM.
SMU‐Z1 specifically activates TLR1/2 but not TLR2/6 signaling.
SMU‐Z1 (10-1,000 nM) stimulates a strong TNF‐α and IL‐1β production in a dose‐response manner in both mouse cells and human PBMC cultures, significantly increases IL‐6 mRNA level in human PBMC, upregulates IL‐6 synthesis about 100 fold.
SMU‐Z1 specifically simulates TLR1 and TLR2 through the NF‐κB pathway to trigger the synthesis of proinflammatory cytokines, such as TNF‐α, IL‐1β, IL‐6 and nitric oxide.
SMU‐Z1 promotes splenocyte proliferation, up‐regulates the expression of CD8+ T, NK and DC cells, which in turn resulted in antitumor immunity against leukemia in vivo.
SMU-Z1 can both enhance HIV-1 transcription and promote NK cell-mediated inhibition of HIV-1-infected autologous CD4+ T cells.