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.