SMU-Z1 is a TLR1/2 heterodimer agonist with an EC 50 of 4.88 nM. SMU-Z1 activates the NF-κB pathway, triggers pro-inflammatory cytokine production, and induces the generation of TNF-α, IL-1β, IL-6 and NO. SMU-Z1 promotes splenocyte proliferation and upregulates the expression of CD8 + T cells, NK cells and dendritic cells. SMU-Z1 exhibits significant anti-tumor effects in mouse leukemia models. SMU-Z1 can be used for leukemia-related research [1].
In Vivo, SMU-Z1 (0.3 mg; intraperitoneal injection; once every 5 days; D7-D32) reduces tumor volume in leukemia xenograft mouse models, while increasing the frequencies of CD8+ T cells, NK cells and DC cells infiltrating the spleen and tumors[1]. SMU-Z1 (0.1 mg; intraperitoneal injection; single dose) increases the frequencies of splenic CD8+ T cells and CD3+CD8+TLR2+ T cells in normal mice[1].
In Vitro, SMU-Z1 specifically activates the TLR1/2 heterodimer in HEK-Blue hTLR2 cells, with an EC50 of 4.88 × 10-9 M[1]. SMU-Z1 (0-10 μM; 24 h) dose-dependently stabilizes the TLR2 protein in HEK-Blue hTLR2 cells[1]. SMU-Z1 (0-5 μM; 24 h) dose-dependently activates the NF-κB signaling pathway in stably transfected human macrophage U937 cells[1]. SMU-Z1 (0-10 μM; 24 h) dose-dependently stimulates the production of TNF-α and IL-1β in Raw 264.7 mouse macrophages[1]. SMU-Z1 (0-10 μM; 24 h) dose-dependently stimulates the production of TNF-α and IL-1β in human peripheral blood mononuclear cells (PBMC)[1]. SMU-Z1 (0-1000 nM; 24 h) stimulates Raw 264.7 mouse macrophages to produce NO[1]. SMU-Z1 (0-10 μM; 24 h) upregulates the mRNA expression of IL-6 and IL-8 in PBMC[1]. SMU-Z1 (0-5 μM; 24-72 h) promotes the proliferation of primary splenocytes from C57Bl/6 mice[1]. SMU-Z1 (0-1000 nM; 48-72 h) dose-dependently activates the proliferation of naive T cells isolated from C57Bl/6 mice[1].
References:
[1]. Cen X, et al. TLR1/2 Specific Small-Molecule Agonist Suppresses Leukemia Cancer Cell Growth by Stimulating Cytotoxic T Lymphocytes. Adv Sci (Weinh). 2019;6(10):1802042. Published 2019 Mar 27.
In Vivo, SMU-Z1 (0.3 mg; intraperitoneal injection; once every 5 days; D7-D32) reduces tumor volume in leukemia xenograft mouse models, while increasing the frequencies of CD8+ T cells, NK cells and DC cells infiltrating the spleen and tumors[1]. SMU-Z1 (0.1 mg; intraperitoneal injection; single dose) increases the frequencies of splenic CD8+ T cells and CD3+CD8+TLR2+ T cells in normal mice[1].
In Vitro, SMU-Z1 specifically activates the TLR1/2 heterodimer in HEK-Blue hTLR2 cells, with an EC50 of 4.88 × 10-9 M[1]. SMU-Z1 (0-10 μM; 24 h) dose-dependently stabilizes the TLR2 protein in HEK-Blue hTLR2 cells[1]. SMU-Z1 (0-5 μM; 24 h) dose-dependently activates the NF-κB signaling pathway in stably transfected human macrophage U937 cells[1]. SMU-Z1 (0-10 μM; 24 h) dose-dependently stimulates the production of TNF-α and IL-1β in Raw 264.7 mouse macrophages[1]. SMU-Z1 (0-10 μM; 24 h) dose-dependently stimulates the production of TNF-α and IL-1β in human peripheral blood mononuclear cells (PBMC)[1]. SMU-Z1 (0-1000 nM; 24 h) stimulates Raw 264.7 mouse macrophages to produce NO[1]. SMU-Z1 (0-10 μM; 24 h) upregulates the mRNA expression of IL-6 and IL-8 in PBMC[1]. SMU-Z1 (0-5 μM; 24-72 h) promotes the proliferation of primary splenocytes from C57Bl/6 mice[1]. SMU-Z1 (0-1000 nM; 48-72 h) dose-dependently activates the proliferation of naive T cells isolated from C57Bl/6 mice[1].
References:
[1]. Cen X, et al. TLR1/2 Specific Small-Molecule Agonist Suppresses Leukemia Cancer Cell Growth by Stimulating Cytotoxic T Lymphocytes. Adv Sci (Weinh). 2019;6(10):1802042. Published 2019 Mar 27.