1. Immunology/Inflammation
  2. IRAK
  3. IRAK inhibitor 4

IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.

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

IRAK inhibitor 4 Chemical Structure

IRAK inhibitor 4 Chemical Structure

CAS No. : 1012104-68-5

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE IRAK inhibitor 4

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.

In Vitro

Lack of IRAK-4 impairs the production of proinflammatory mediators by macrophages and DCs in response to M. bovis and M. tuberculosis. IRAK-4-/- cells stimulated with E. coli LPS display delayed activation kinetics of all signaling proteins analyzed, and exhibit dramatically reduced p65 phosphorylation[1]. IRAK1/4 (20 μM) has an inhibitory effect on LPS mediated IL-6 production. IRAK1/4 inhibitor do not decrease p38 phosphorylation in AMs. Combination of IRAK1/4 and Rip2 inhibitors inhibits TLR2-mediated cytokine production in sarcoidosis PBMCs and AMs[2]. IRAK4 is overexpressed and activated in T-ALL. IRAK4 mRNA level is elevated in T-ALL cells from patients compared with the levels detected in thymic T cells or T cells from peripheral blood[3].

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

In Vivo

IRAK-4-/- mice exhibit a greatly reduced survival rate following aerosol infection compared with IRAK-4+/+ or IRAK-4+/- mice. IRAK-4-/- mice show increased bacterial burden in all organs at 15, 30, and 60 d postinfection[1]. MCL1, but not BCL-xL, overrides the therapeutic effects of combinatorial IRAK1/4 inhibitor and ABT-737 therapy in vivo[3].

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

Molecular Weight

620.66

Formula

C33H35F3N6O3

CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

OC1CCC(N2C3=C(C=C(C=C3)C(NCCC(C)C)=O)N=C2NC4=NNC5=C4C=C(C=C5)C6=CC=CC=C6OC(F)(F)F)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (20.14 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 1.6112 mL 8.0559 mL 16.1119 mL
5 mM 0.3222 mL 1.6112 mL 3.2224 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (2.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 1.25 mg/mL (2.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
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

Purity: 99.77%

References
Cell Assay
[1]

THP-1 cells are grown in RPMI 1640 medium supplemented with 2 mM L-glutamine, 10% heat-inactivated FBS, 100 U/mL penicillin, and 100 μg/mL streptomycin. For monocytic differentiation, cells are seeded in 24-well flat-bottom culture plates at a density of 5×105 cells/well and allowed to adhere and differentiate for 48 h at 37°C in the presence of 100 nM PMA. THP-1 cells are incubated with 0.1 or 1 μM IRAK-4 inhibitor (IRAK inhibitor 1) for 45 min and then stimulated with M. bovis BCG Moreau (MOI 5:1) or E. coli LPS (1 μg/mL). Culture supernatants are collected after 24 h of stimulation and assayed for the concentrations of human TNF-α or IL-12/23p40 by ELISA. For Western blot analysis, cells are incubated with IRAK-4 inhibitor, in the same concentrations described above, for 45 min and then stimulated with M. bovis BCG Moreau (MOI 5:1) or E. coli LPS (1 μg/mL) for 30 min. The cells are then processed for Western blot assay, as described below.

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

Animal Administration
[1]

To evaluate IRAK-4 involvement in mycobacterial infection, IRAK-4+/+ (wild-type), IRAK-4+/- (heterozygous), and IRAK-4-/- (IRAK-4-knockout) mice are used. Eight-week-old mice are infected i.v. with 1×106 CFU of M. bovis strain Moreau. The bacterial loads in the spleens, livers, and lungs are determined at 15, 30, and 60 d postinfection. Briefly, the organs are collected aseptically and homogenized in distilled water that contained 0.05% Tween 80. Serial dilutions of the resulting suspensions are plated on Middlebrook 7H11 agar medium supplemented with 10% oleic acid-albumin-dextrose-catalase, and CFU are counted following a 21-d incubation at 37°C and 5% CO2.

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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6112 mL 8.0559 mL 16.1119 mL 40.2797 mL
5 mM 0.3222 mL 1.6112 mL 3.2224 mL 8.0559 mL
10 mM 0.1611 mL 0.8056 mL 1.6112 mL 4.0280 mL
15 mM 0.1074 mL 0.5371 mL 1.0741 mL 2.6853 mL
20 mM 0.0806 mL 0.4028 mL 0.8056 mL 2.0140 mL
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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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IRAK inhibitor 4
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HY-13278
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