2. Immunology/Inflammation
  3. IRAK
  4. IRAK4-IN-22

IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis.

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

IRAK4-IN-22 Chemical Structure

IRAK4-IN-22 Chemical Structure

CAS No. : 2170694-05-8

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Based on 1 publication(s) in Google Scholar

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Description

IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis[1].

In Vitro

IRAK4-IN-21 (a 4-fold serial dilution from 10 µM; 1 h) decreases the levels of IL-23 (in THP-1 and DC cells), IL-6 (in HUVEC cells) and MIP-1β (in human whole blood)[1].

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

IRAK4-IN-22 Related Antibodies

Cell Viability Assay[1]

Cell Line: THP-1, DC cells (are primed with IFN-γ)
Concentration: 10 µM (a 4-fold serial dilution from 10 µM)
Incubation Time: 1 h (pre-incubate)
Result: Inhibited the levels of IL-23 in the supernatant of THP-1 and DC cells with IC50 of 0.10 and 0.11 µM, respectively.

Cell Viability Assay[1]

Cell Line: HUVEC cells (IL-1β-stimulated)
Concentration: 10 µM (a 4-fold serial dilution from 10 µM)
Incubation Time: 1 h (pre-incubate)
Result: Inhibited the level of IL-6 in the supernatant of HUVEC cells with an IC50 of 0.11 µM.

Cell Viability Assay[1]

Cell Line: Human whole blood (IL-1β-stimulated)
Concentration: 10 µM (a 4-fold serial dilution from 10 µM)
Incubation Time: 1 h (pre-incubate)
Result: Inhibited the level of MIP-1β in the human whole blood with an IC50 of 0.51 µM.
In Vivo

IRAK4-IN-21 (75 mg/kg; p.o.; single) shows moderate efficacy in acute animal model studies for the inhibition of IL-6 production[1].

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

Animal Model: BALB/c mice (acute mouse model; IL-1β-stimulated)[1].
Dosage: 75 mg/kg
Administration: Oral administration; single (pre-treat).
Result: Showed 64% inhibition of IL-6, plasma concentrations was 6817 ng/mL at 0.5 h and 700 ng/mL at 2 h.
Molecular Weight

513.57

Formula

C28H28FN7O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1[C@@H](C2)C=C[C@@H]2[C@H]1NC3=NC(NC4=CC=CC(C(N5CCCC5)=O)=C4)=NC=C3C6=CC(F)=NC=C6)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (194.72 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 1.9472 mL 9.7358 mL 19.4715 mL
5 mM 0.3894 mL 1.9472 mL 3.8943 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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.
Calculation results:
Working solution concentration: mg/mL
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 1.9472 mL 9.7358 mL 19.4715 mL 48.6789 mL
5 mM 0.3894 mL 1.9472 mL 3.8943 mL 9.7358 mL
10 mM 0.1947 mL 0.9736 mL 1.9472 mL 4.8679 mL
15 mM 0.1298 mL 0.6491 mL 1.2981 mL 3.2453 mL
20 mM 0.0974 mL 0.4868 mL 0.9736 mL 2.4339 mL
25 mM 0.0779 mL 0.3894 mL 0.7789 mL 1.9472 mL
30 mM 0.0649 mL 0.3245 mL 0.6491 mL 1.6226 mL
40 mM 0.0487 mL 0.2434 mL 0.4868 mL 1.2170 mL
50 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9736 mL
60 mM 0.0325 mL 0.1623 mL 0.3245 mL 0.8113 mL
80 mM 0.0243 mL 0.1217 mL 0.2434 mL 0.6085 mL
100 mM 0.0195 mL 0.0974 mL 0.1947 mL 0.4868 mL
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IRAK4-IN-22 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:

IRAK4-IN-222170694-05-8IRAKInterleukin-1 receptor associated kinaseIL-1R associated kinaseplaque psoriasispsoriatic arthritisTHP-1DCHUVECInhibitorinhibitorinhibit

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