1. Immunology/Inflammation
  2. IRAK
  3. IRAK4-IN-21

IRAK4-IN-21 

Cat. No.: HY-151363
Handling Instructions

IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 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-21 Chemical Structure

IRAK4-IN-21 Chemical Structure

CAS No. : 2170694-04-7

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Description

IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 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].

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

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 0.17 and 0.51 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 0.20 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 0.47 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].

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 54% inhibition of IL-6, plasma concentrations was 2877 ng/mL at 0.5 h and 496 ng/mL at 2 h.
Molecular Weight

513.57

Formula

C28H28FN7O2

CAS No.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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IRAK4-IN-21
Cat. No.:
HY-151363
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