2. Immunology/Inflammation NF-κB Apoptosis
  3. Toll-like Receptor (TLR) MyD88 NF-κB TNF Receptor Interleukin Related
  4. SMU-C409

SMU-C409 是一种 TLR1/2 激动剂，在 HEK-Blue hTLR2 细胞中的 EC50 值为 65 nM。SMU-C409 可激活 TLR1/2–MyD88–NF-κB 通路，诱导 TNF-α/IL-1β 分泌，并强烈激活免疫细胞，从而发挥抗肿瘤免疫调节作用。SMU-C409 在体外表现出较低的毒性，可用于癌症免疫的研究。

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SMU-C409

SMU-C409 Chemical Structure

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SMU-C409 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-C409 is a TLR1/2 agonist with an EC50 of 65 nM in HEK-Blue hTLR2 Cells. SMU-C409 activates the TLR1/2–MyD88–NF-κB pathway, inducing TNF-α/IL-1β secretion and robust immune cell activation for antitumor immunomodulation. SMU-C409 shows low toxicity in virto. SMU-C409 can be used for cancer immunotherapy research[1].

体外研究
(In Vitro)

SMU-C409 (0-100 nM) 在 HEK-Blue hTLR2 细胞中能选择性激活 hTLR2 信号通路，而对其他 TLR 亚型 (hTLR3/4/7/8) 无明显活性[1]。
SMU-C409 在 HEK-Blue hTLR2 细胞中特异性靶向 TLR1/2，其 EC50 值为 65 nM[1]。
SMU-C409 (0-100 μM，24 小时) 在 HEK-Blue hTLR2 细胞、PBMC、B16-F10 细胞及 MCF-7 细胞中表现出低毒性[1]。
SMU-C409 (0-50 μM，0-24 小时) 在 HEK-Blue hTLR2 及 THP-1 细胞中特异性靶向并激活 TLR2[1]。
SMU-C409 (0-100 μM，0-700 分钟) 以 Kd 值为 72.4 nM 的亲和力与 hTLR2 蛋白结合[1]。
SMU-C409 (0-20 μM，0-120 分钟) 激活 TLR1/2 异源二聚体，在 THP-1 (Phorbol 12-myristate 13-acetate (HY-18739 ) PMA 分化) 细胞中通过募集 MyD88 触发下游信号传导，进而促进 MyD88-NF-κB 通路组分的磷酸化及抑制性蛋白的解离[1]。
SMU-C409 (0.01-10 μM，24 小时) 通过 NF-κB 通路刺激下游细胞因子产生，在炎症信号传导中发挥关键作用，且其信号效应在 THP-1 细胞 (PMA 分化)、PBMC、小鼠腹腔巨噬细胞及小鼠 RAW264.7 细胞等不同免疫细胞类型与信号轴中均表现出保守的物种特异性[1]。
SMU-C409 (0-10 μM，48 小时) 在 CD3+ 细胞、CD4+ 细胞、CD8+ 细胞、单核细胞、B 细胞及 NK 细胞中均展现出了一定程度的免疫激活活性[1]。
SMU-C409 (1-20 μM，24 小时) 可增强免疫细胞介导的 SJSA-1 细胞凋亡诱导作用，显示出潜在的抗肿瘤免疫活性[1]。
SMU-C409 (8 小时) 在大鼠血浆中表现出显著改善的血浆稳定性，其降解速率常数 (k) 为 0.0003 min-1[1]。

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

SMU-C409 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HEK-Blue hTLR2 cells, PBMC, B16−F10 cells and MCF-7 cells
Concentration: 0, 0.14, 0.41, 1.23, 3.7, 11.11, 33.3 and 100 μM
Incubation Time: 24 h
Result: Showed no obvious toxicity to HEK-BluehTLR2 cells, peripheral blood mononuclear cells (PBMC), B16−F10 cells or MCF-7 cells at a high concentration of 100 μM.

Western Blot Analysis[1]

Cell Line: HEK-Blue TLR2 cells or THP-1 cells
Concentration: 0, 0.01, 0.1, 1, 10, or 50 μM
Incubation Time: 0, 15, 30, 60, 90, or 120 min
Result: Showed SMU-C409 dose dependently upregulated TLR2 expression in both HEK-Blue hTLR2 cells and PMA-differentiated THP-1 cells.

ELISA Assay[1]

Cell Line: Wild-type THP-1 cells and TLR2 knockdown THP-1 cells
Concentration: 20, 40 μM
Incubation Time: 24 h
Result: Induced TNF-α in wild-type cells but not inTLR2-knockdown cells.

Western Blot Analysis[1]

Cell Line: THP-1(PMA differentiated) cells
Concentration: 0, 10 and 20 μM
Incubation Time: 0, 15, 30, 60, 90, 120 min and 24 h
Result: Upregulated TLR1 and TLR2 protein expression after 24 h stimulation at 20 μM.
Induced time-dependent phos phorylation of IKKα/β, p65, and p38 (evident by 15 min, with peak dynamics varying by protein) and progressive IκBα dissociation in THP-1 cells, coupled with subsequent IκBα recovery by 120 min.

ELISA Assay[1]

Cell Line: THP-1 cells (PMA-differentiated), PBMC cells, mouse peritoneal macrophages and mouse RAW264.7 cells.
Concentration: 0, 0.01, 0.1, 1, 5 and 10 μM
Incubation Time: 24 h
Result: Induced dose dependent secretion of TNF-α and IL-1β in both freshly isolated human PBMCs and PMA-differentiated THP-1 cells.
Showed no significant effect on TNF-α and IL-6 secretion in murine peritoneal macrophages.
Failed to elicit concentration-dependent NO activation in mouse RAW264.7 cells.

Apoptosis Analysis[1]

Cell Line: SJSA-1 (GFP labeled), Jurkat T cells, and PMA-differentiated THP-1 cells
Concentration: 0, 0.01, 0.1, 1, 5 and 10 μM
Incubation Time: 24 h
Result: Resulted the spontaneous apoptosis rate (4.91%) of SJSA-1 cells.
Resulted an increase apoptosis rate from 7.69 to 13.77%. in SJSA-1 cells cocultured with Jurkat T and PMA-differentiated THP-1 cells.
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat[1] 20 mg/kg p.o. Tmax 0.63 h
Rat[1] 2 mg/kg i.v. Tmax 0.03 h
Rat[1] 20 mg/kg p.o. T1/2 6.07 h
Rat[1] 2 mg/kg i.v. T1/2 3.06 h
Rat[1] 2 mg/kg i.v. Cmax 1406810.39 μg/L
Rat[1] 20 mg/kg p.o. Cmax 364528.03 μg/L
Rat[1] 2 mg/kg i.v. AUC0-t 261976.59 μg/L·h
Rat[1] 20 mg/kg p.o. AUC0-t 219790.73 μg/L·h
Rat[1] 2 mg/kg i.v. AUC0-∞ 262353 μg/L·h
Rat[1] 20 mg/kg p.o. AUC0-∞ 221255.84 μg/L·h
Rat[1] 20 mg/kg p.o. F 8.39 %
分子量

395.54

Formula

C21H21N3OS2
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-C409 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-C409Toll-like Receptor (TLR)MyD88NF-κBTNF ReceptorInterleukin RelatedNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILTLR1/2agonistimmune cellimmunomodulationcancerInhibitorinhibitorinhibit

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