2. Protein Tyrosine Kinase/RTK
  3. Itk
  4. 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。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

ITK-IN-6 Chemical Structure

ITK-IN-6 Chemical Structure

CAS No. : 2616666-32-9

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

ITK-IN-6 相关抗体

Top Publications Citing Use of Products

  • 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.

ITK-IN-6 相关抗体:

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

ITK-IN-6 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

ITK-IN-62616666-32-9ItkInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseAsthmainflammationITKTCR signalingJurkat cellsCD4? T cellsC57BL/6JInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
ITK-IN-6
目录号：
HY-174903
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z