1. Protein Tyrosine Kinase/RTK
  2. Itk
  3. ITK-IN-6

ITK-IN-6 是一种高效的有选择性的 ITK 抑制剂 (Kd = 387 nM)。ITK-IN-6 直接结合到 ITK 激酶结构域。ITK-IN-6 阻止促炎细胞因子释放以及 Th2 和 Th17 细胞的活化与分化。ITK-IN-6 通过减轻炎症细胞浸润、减少黏液和 IgE 生成来改善哮喘进展。ITK-IN-6 显著抑制气道炎症,用于哮喘研究。

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ITK-IN-6 Chemical Structure

ITK-IN-6 Chemical Structure

CAS No. : 2616666-32-9

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ITK-IN-6 is a highly potent and selective ITK inhibitor (Kd = 387 nM). ITK-IN-6 directly binds to the ITK kinase domain. ITK-IN-6 blocks the release of pro-inflammatory cytokines and the activation and differentiation of Th2 and Th17 cells. ITK-IN-6 improves asthma progression by reducing inflammatory cell infiltration, mucus and IgE production. ITK-IN-6 significantly inhibits airway inflammation and is used in asthma research[1].

体外研究
(In Vitro)

ITK-IN-6 (Compound C-161) (24 h) 在 Jurkat-NFAT-Luc 稳定细胞系抑制 ITK 下游转录活性,抑制率62.27 %[1]

ITK-IN-6 (0.07-5 μM, 12 h) 在 CD4+ T 细胞中有效剂量下安全性良好,并在体外减弱 Th2 和 Th17 分化[1]

ITK-IN-6 (0.15-2.5 μM, 12 h) 在 Jurkat 细胞中阻断 T 细胞活化关键因子,抑制 T 细胞表面活化标志物[1]

ITK-IN-6 (0.625-2.5 μM, 12 h) 在 Jurkat T细胞中特异性抑制 ITK 并阻断 T 细胞受体近端信号传导的细胞和分子激活的潜力,且 CD69 的表达受到显著抑制[1]

ITK-IN-6 (0.15-2.5 μM) 在 Jurkat 细胞中处理以剂量依赖的方式在转录和蛋白质水平上抑制 IL-2 表达,IC50 为 494 nM[1]

ITK-IN-6 (0.625-2.5 μM, 30 min) 处理 Jurkat 细胞可显著降低抗 cD3 诱导的细胞内 Ca2+ 通量[1]

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

Western Blot Analysis[1]

Cell Line: Jurkat T cells
Concentration: 0.625 μM, 1.25 μM, 2.5 μM
Incubation Time: 12 h
Result: Inhibited the phosphorylation of p-PLCγ1, p-IκBα, p-NF-κB, and p-ERK in a dose-dependent manner by C-161, whereas the phosphorylation of upstream ZAP70 remained unchanged.

Cell Differentiation Assay[1]

Cell Line: CD4⁺ T cells
Concentration: 0.07 μM, 0.15 μM, 0.3 μM, 1.25 μM, 2.5 μM, 5 μM
Incubation Time: 4 days (Th2); 3 days (Th17)
Result: Inhibited IL-4 production by Th2 cells in a dose-dependent manner, and no cytotoxic effect was observed.
Significantly reduced the percentage of cells producing IL-17A at a relatively high concentration (1.25 μM), but was accompanied by mild cytotoxicity.
Inhibited the differentiation of naive CD4+ T cells into Th2 cells and significantly reduced the percentage of cells producing IL-17A.
体内研究
(In Vivo)

ITK-IN-6 (Compound C-161) (10 mg/kg, i.p, 7至11天每日一次) 通过抑制 Th2/Th17 分化和细胞因子产生,显著缓解屋尘螨诱导的 C57BL/6J 小鼠气道炎症,且安全性良好[1]

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

Animal Model: HDM-induced asthma C57BL/6J mice model (6-8 weeks, 18-20 g)[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), 7 to 11 days after HDM sensitization, once a day, one hour before HDM challenge.
Result: Reduced the total number of inflammatory cells, eosinophils (EOS), neutrophils (NEU), and B cells in BALF, alleviated inflammatory infiltration and mucus secretion in lung tissue, and decreased serum total IgE and HDM-specific IgE levels.
Reduced CD3⁺ T cell infiltration in lung tissue, decreased the proportion and number of CD4⁺ T cells in the lung, and downregulated the mRNA and protein levels of Th2/Th17-related cytokines (IL-4/IL-5/IL-13/IL-17A) in lung tissue.
Caused no weight loss or death in mice, and resulted in no abnormalities in organ indexes, serum biochemical indicators, or tissue pathology.
分子量

451.32

Formula

C20H16Cl2N2O4S

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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产品名称:
ITK-IN-6
目录号:
HY-174903
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