2. Immunology/Inflammation NF-κB MAPK/ERK Pathway Stem Cell/Wnt Apoptosis
  3. Toll-like Receptor (TLR) MyD88 IKK p38 MAPK ERK TNF Receptor Interleukin Related
  4. SMU-L11-R

SMU-L11-R 是一种选择性 TLR7 激动剂，对人 TLR7 的 EC50 为 0.012 μM。SMU-L11-R 特异性激活 TLR7，募集 MyD88，并触发  MAPK/NF-κB 通路，从而导致小鼠和人外周血单核细胞分泌 TNF-α/IL-1β/IL-6。SMU-L11-R 促进 M1 样巨噬细胞极化。SMU-L11-R 与 PD-L1 抑制剂具有优异的协同抗肿瘤作用，可通过上调 CD8+T 细胞发挥作用。SMU-L11-R 在结直肠癌研究中显示出潜力。

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SMU-L11-R

SMU-L11-R Chemical Structure

CAS No. : 3040320-18-8

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SMU-L11-R 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits  MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8+T cells. SMU-L11-R shows potential in colorectal cancer studies[1].

IC50 & Target[1]

human TLR7

0.024 μM (EC50)

TLR8

2.56 μM (EC50)

体外研究
(In Vitro)

SMU-L11-R (0-100 μM；24 小时；HEK-Blue hTLR7 细胞) 没有明显的毒性效应[1]。
SMU-L11-R (0-100 μM；24 小时；B16-F10 细胞) 在最高浓度 100 μM 时显示细胞毒性效应[1]。
SMU-L11-R (0, 0.1, 1, 5, 10 μM; 24 小时; 腹腔巨噬细胞) 显示 M1 型巨噬细胞随剂量增加而增加[1][1]。
SMU-L11-R (1 μM；15-120 min；BMDCs) 可通过 MyD88 蛋白激活 TLR7 下游信号通路，包括 NF-κB 和 MAPK 信号通路[1]。
SMU-L11-R (0, 0.01, 0.1, 1, 10 μM；24 小时；HEK-Blue hTLR7 细胞) 显示 TLR7 蛋白剂量依赖性增加[1]。
SMU-L11-R (0-10 μM；24 小时；Raw 264.7 细胞) 显示出 TNF-α 和 IL-6 的显著增加[1]。
SMU-L11-R (0-10 μM；24 小时；人 PBMCs) 显示出剂量依赖性的 TNF-α 和 IL-1β 增加[1]。
SMU-L11-R (0-10 μM；24 小时；小鼠 BMDCs) 显示出 IL-6 的显著增加[1]。
SMU-L11-R (0, 0.1, 1, 10 μM；24 小时；腹腔巨噬细胞) 显示出 NO 生成的浓度依赖性增加[1]。
随着浓度的增加，SMU-L11-R 也显示出对 TLR8 的激活作用（EC50 = 2.56 μM），但其激活作用比 TLR7 低 156 倍。 SMU-L11-R 诱导 HEK-Blue 细胞中 hTLR2、hTLR3 或 hTLR4 的激活作用可以忽略不计[1]。

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

SMU-L11-R 相关抗体:

Cell Viability Assay[1]

Cell Line: HEK-Blue hTLR7 cells
Concentration: 0.26 μM, 0.52 μM, 1.04 μM, 2.08 μM, 4.17 μM, 8.33 μM, 16.67 μM, 33.33 μM, 100 μM
Incubation Time: 24 h
Result: Showed no obvious toxic effect.

Cell Viability Assay[1]

Cell Line: MC38 cells
Concentration: 0.02 μM, 0.05 μM, 0.14 μM, 1.23 μM, 11.11 μM, 33.33 μM, 100 μM
Incubation Time: 24 h
Result: Showed cytotoxic effect at a high testing concentration (100 μM).

Cell Viability Assay[1]

Cell Line: B16-F10 cells
Concentration: 0.26 μM, 0.52 μM, 1.04 μM, 2.08 μM, 4.17 μM, 8.33 μM, 16.67 μM, 33.33 μM, 100 μM
Incubation Time: 24 h
Result: Showed cytotoxic effect at a high testing concentration (100 μM).

Western Blot Analysis[1]

Cell Line: HEK-Blue hTLR7 cells
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Showed dose-dependent increase in TLR7 protein.

Western Blot Analysis[1]

Cell Line: BMDCs
Concentration: 1 μM
Incubation Time: 15 min, 30 min, 60 min, 90 min, 120 min
Result: Showed significant induction of the phosphorylation of IKK α/ β, p65, p38 and ERK1/2 in BMDCs.

ELISA Assay[1]

Cell Line: Raw 264.7 cells
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Showed significant increase in TNF-α and IL-6.

ELISA Assay[1]

Cell Line: Mouse BMDCs
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Showed significant increase in IL-6.

ELISA Assay[1]

Cell Line: Human PBMCs
Concentration: 0, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: Showed dose-dependent increase in TNF-α and IL-1β.
体内研究
(In Vivo)

SMU-L11-R (5-10 mg/kg；IP；每隔 2 天；15 天) 抑制小鼠 MC38 肿瘤生长，并且与 PD-L1 抑制剂联合使用时增强抗肿瘤效果[1]。

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

Animal Model: C57/BL6 wild-type male mice (6-8 weeks old) were injected subcutaneousely with 2 x 105 MC38 cells[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: IP; every 2 days; 15 days
Result: Significantly inhibited tumor growth and exhibited excellent synergistic anti-tumor effects when combined with PD-L1 inhibitors by upregulating CD8+ T cells.
分子量

324.42

Formula

C19H24N4O
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

SMU-L11-R 相关分类

  • 摩尔计算器

  • 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.

Keywords:

SMU-L11-R3040320-18-8Toll-like Receptor (TLR)MyD88IKKp38 MAPKERKTNF ReceptorInterleukin RelatedIκB kinaseI kappa B kinase Extracellular signal regulated kinasesTumor Necrosis Factor ReceptorTNFRILInflammatory cytokinesTLR7 agonistCD8(+)T cellsCancer immunotherapyPD-L1Inhibitorinhibitorinhibit

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