Art. -Nr.: HY-174903

ITK-IN-6

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ITK-IN-6 is a highly potent and selective ITK inhibitor (K_d = 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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Reinheit: 99.02%
CAS. Nr.: 2616666-32-9
Formel: C₂₀H₁₆Cl₂N₂O₄S
Molecular Weight:451.32

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

ITK-IN-6 Chemical Structure

CAS. Nr.: 2616666-32-9

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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.

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.

Chemical Information

CAS. Nr. 2616666-32-9
Appearance Solid
Molecular Weight 451.32
Formel C₂₀H₁₆Cl₂N₂O₄S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2157 mL

11.0786 mL

22.1572 mL

5 mM

0.4431 mL

2.2157 mL

4.4314 mL

10 mM

0.2216 mL

1.1079 mL

2.2157 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhaoxi Guo, et al. A Novel Small Molecule ITK Inhibitor Suppresses Th2/Th17 Differentiation and Attenuates Airway Inflammation in a Mouse Model of HDM-Induced Asthma. Immunology. 2025 Jun 12. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ITK-IN-6

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ITK-IN-6 Related Classifications

HY-174903 Related Classifications