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

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.

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ITK-IN-6

ITK-IN-6 Chemical Structure

CAS No. : 2616666-32-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

ITK-IN-6 Related Antibodies

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Description

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].

In Vitro

ITK-IN-6 (Compound C-161) (24 h) inhibits ITK downstream transcriptional activity in Jurkat-NFAT-Luc stable cell line with an inhibition rate of 62.27 %[1].

ITK-IN-6 (0.07-5 μM, 12 h) C-161 has good safety at effective doses in CD4+ T cells, attenuates Th2 and Th17 differentiation in vitro[1].

ITK-IN-6 (0.15-2.5 μM, 12 h) blocks key factors for T cell activation and inhibits T cell surface activation markers in Jurkat cells[1].

ITK-IN-6 (0.625-2.5 μM, 12 h) specifically inhibits ITK in Jurkat T cells and blocks the cellular and molecular activation potential of T cell receptor proximal signaling, and the expression of CD69 is significantly suppressed[1].

ITK-IN-6 (0.15-2.5 μM) inhibits IL-2 expression at both the transcriptional and protein levels in a dose-dependent manner, with an IC50 of 494 nM in Jurkat cells[1].

ITK-IN-6 (0.625-2.5 μM, 30 min) treatment of Jurkat cells significantly reduces intracellular Ca2+ flux induced by anti-CD3[1].

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

ITK-IN-6 Related Antibodies

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.
In Vivo

ITK-IN-6 (Compound C-161) (10 mg/kg, i.p, Once daily for 7 to 11 days) significantly alleviates airway inflammation in C57BL/6J mice induced by house dust mites (HDM) by inhibiting Th2/Th17 differentiation and cytokine production, with good safety[1].

MedChemExpress (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.
Molecular Weight

451.32

Formula

C20H16Cl2N2O4S
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

OC1=C(NS(=O)(C)=O)C=C(NC(C2=CC=C(C3=C(Cl)C(Cl)=CC=C3)C=C2)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (221.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2157 mL 11.0786 mL 22.1572 mL
5 mM 0.4431 mL 2.2157 mL 4.4314 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2157 mL 11.0786 mL 22.1572 mL 55.3931 mL
5 mM 0.4431 mL 2.2157 mL 4.4314 mL 11.0786 mL
10 mM 0.2216 mL 1.1079 mL 2.2157 mL 5.5393 mL
15 mM 0.1477 mL 0.7386 mL 1.4771 mL 3.6929 mL
20 mM 0.1108 mL 0.5539 mL 1.1079 mL 2.7697 mL
25 mM 0.0886 mL 0.4431 mL 0.8863 mL 2.2157 mL
30 mM 0.0739 mL 0.3693 mL 0.7386 mL 1.8464 mL
40 mM 0.0554 mL 0.2770 mL 0.5539 mL 1.3848 mL
50 mM 0.0443 mL 0.2216 mL 0.4431 mL 1.1079 mL
60 mM 0.0369 mL 0.1846 mL 0.3693 mL 0.9232 mL
80 mM 0.0277 mL 0.1385 mL 0.2770 mL 0.6924 mL
100 mM 0.0222 mL 0.1108 mL 0.2216 mL 0.5539 mL
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ITK-IN-6 Related Classifications

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

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