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.

For research use only. We do not sell to patients.

ITK-IN-6 Chemical Structure

ITK-IN-6 Chemical Structure

CAS No. : 2616666-32-9

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

ITK-IN-6 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

ITK-IN-6 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
ITK-IN-6
Cat. No.:
HY-174903
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

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.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

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