1. Immunology/Inflammation NF-κB Apoptosis
  2. Toll-like Receptor (TLR) NF-κB TNF Receptor Interleukin Related
  3. SMU-Z1

SMU-Z1 是一种 TLR1/2 异二聚体激动剂,EC50 为 4.88 nM。SMU-Z1 可激活 NF-κB 通路,触发促炎细胞因子生成,并诱导 TNF-αIL-1βIL-6NO 的产生。SMU-Z1 可促进脾细胞增殖,上调 CD8+T 细胞、NK 细胞和树突状细胞的表达。SMU-Z1 在小鼠白血病模型中展现出显著的抗肿瘤效果。SMU-Z1 可用于白血病的相关研究。

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SMU-Z1

SMU-Z1 Chemical Structure

CAS No. : 2410782-66-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SMU-Z1 is a TLR1/2 heterodimer agonist with an EC50 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].

体外研究
(In Vitro)

SMU-Z1 可在 HEK-Blue hTLR2 细胞中特异性激活 TLR1/2 异源二聚体,其 EC50 为 4.88 × 10-9 M[1]
SMU-Z1 (0-10 μM; 24 h) 可在 HEK-Blue hTLR2 细胞中呈剂量依赖性地稳定 TLR2 蛋白[1]
SMU-Z1 (0-5 μM; 24 h) 可在稳定转染的人巨噬细胞 U937 中剂量依赖性激活 NF-κB 信号通路[1]
SMU-Z1 (0-10 μM; 24 h) 可在 Raw 264.7 小鼠巨噬细胞中呈剂量依赖性地刺激 TNF-α 和 IL-1β 的产生[1]
SMU-Z1 (0-10 μM; 24 h) 可呈剂量依赖性地刺激人外周血单个核细胞 (PBMC) 产生 TNF-α 和 IL-1β[1]
SMU-Z1 (0-1000 nM; 24 h) 刺激 Raw 264.7 小鼠巨噬细胞产生 NO[1]
SMU-Z1 (0-10 μM; 24 h) 上调 PBMC 中 IL-6 和 IL-8 mRNA 的表达[1]
SMU-Z1 (0-5 μM; 24-72 h) 促进 C57Bl/6 小鼠原代脾细胞的增殖[1]
SMU-Z1 (0-1000 nM; 48-72 h) 可呈剂量依赖性激活分离自 C57Bl/6 小鼠的初始 T 细胞增殖[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HEK-Blue hTLR2 cells
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Increased TLR2 protein stability in a dose-dependent manner, with higher TLR2 protein levels observed as concentrations increased from 0.01 to 10 μM.

ELISA Assay[1]

Cell Line: Raw 264.7 mouse leukemic monocyte macrophage cells
Concentration: 0.0007, 0.002, 0.006, 0.018, 0.036, 0.12, 0.4, 1 μM (TNF-α); 0.0015, 0.0043, 0.0133, 0.04, 0.12, 0.4, 1.2, 3.6, 10 μM (IL-1β)
Incubation Time: 24 h
Result: Stimulated dose-dependent production of TNF-α and IL-1β.
Increased TNF-α levels from ~2000 pg/mL at 0.006 μM to ~4000 pg/mL at 1 μM.
Increased IL-1β levels from ~50 pg/mL at 0.0043 μM to ~550 pg/mL at 10 μM.

Cell Proliferation Assay[1]

Cell Line: C57Bl/6 mouse primary splenocytes
Concentration: 0, 0.1, 0.5, 1, 5 μM
Incubation Time: 0, 24, 48, 72 h
Result: Dependently promoted proliferation of C57Bl/6 mouse primary splenocytes, with a 3-5-fold increase observed at 5 μM after 48 h of incubation.
体内研究
(In Vivo)

SMU-Z1 (0.3 mg;腹腔注射;每 5 天 1 次;D7-D32) 可将白血病异种移植小鼠模型的肿瘤体积降低,同时可提高脾脏及肿瘤浸润 CD8+ T 细胞、NK 细胞和 DC 细胞的频率[1]
SMU-Z1 (0.1 mg;腹腔注射;单次) 在正常小鼠中可提升脾脏 CD8+ T 细胞频率、 CD3+CD8+TLR2+ T 细胞频率[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (8-week-old male, 17-19 g, subcutaneous inoculation of 5 × 105 syngeneic murine FBL3 leukemia cancer cells)[1]
Dosage: 0.3 mg
Administration: i.p.; once every 5 days
Result: Reduced mean tumor volume to 386 mm3 on day 35 (vs. 2370 mm3 in PBS controls).
Induced complete tumor disappearance in 3 out of 7 treated mice after three administrations.
Increased splenic CD3+ T cells to 25.7% (vs. 11.6% in controls).
Increased splenic CD8+ T cells to 19.4% (vs. 10.6% in controls).
Increased splenic CD8/CD4 ratio to 0.28 (vs. 0.13 in controls).
Increased splenic NK cells to 10.5% (vs. 4.64% in controls).
Increased splenic DC cells to 3.87% (vs. 1.54% in controls).
Increased tumor tissue CD3+ T cells to 37.0%.
Increased tumor tissue CD8+CD3+ T cells to 28.1%.
Increased tumor tissue NK cells to 3.66%.
Increased tumor tissue DC cells to 4.12%.
Caused no significant change in mouse body weight relative to controls.
Animal Model: C57BL/6 (8-10-week-old male)[1]
Dosage: 0.1 mg
Administration: i.p.; single administration
Result: Increased splenic CD8+ T cells to 27.4% after 7 days (vs. 17.1% in PBS controls).
Increased splenic CD8+ T cells to 21.3% after 5 days (vs. 16.7% in PBS controls).
Increased splenic CD3+CD8+TLR2+ T cells to 6.3% after 5 days (vs. 2.6% in PBS controls).
Increased splenic CD3+CD8+TLR2+ T cells to 6.7% after 7 days (vs. 2.6% in PBS controls).
Reduced splenic CD4+ T cells to 55.6% (vs. 69.5% in PBS controls).
Increased the splenic CD8/CD4 ratio.
Caused no significant change in splenic CD19+ B cell frequencies.
分子量

378.31

Formula

C17H13F3N4O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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