Home Immunology & Inflammation IRAK inhibitor HS-243 For research use only.

HS-243

HS-243 is a highly potent interleukin-1 receptor-associated kinase (IRAK) inhibitor with IC50 of 24 nM, 20 nM and 0.5 μM for IRAK-1, IRAK-4 and TAK1, respectively.

HS-243 Chemical Structure

HS-243 Chemical Structure

CAS No. 848249-10-5

Purity & Quality Control

HS-243 Related Products

Biological Activity

Description HS-243 is a highly potent interleukin-1 receptor-associated kinase (IRAK) inhibitor with IC50 of 24 nM, 20 nM and 0.5 μM for IRAK-1, IRAK-4 and TAK1, respectively.
Targets
IRAK-4 [1]
(Cell-free assay)		 IRAK-1 [1]
(Cell-free assay)		 TAK1 [1]
(Cell-free assay)
20 nM 24 nM 0.5 μM
In vitro
In vitro

HS-243 has exquisite selectivity toward both IRAK-1 (IC50 = 24 nM) and IRAK-4 (IC50 = 20 nM), with only minimal TAK1-inhibiting activity (IC50 = 0.5 μM). Using HS-243 and takinib, we evaluates the consequences of cytokine/chemokine responses after selective inhibition of IRAK-1/4 or TAK1 in response to lipopolysaccharide challenge in human rheumatoid arthritis fibroblast-like synoviocytes. HS-243 specifically inhibits intracellular IRAKs without TAK1 inhibition and these kinases have distinct, nonredundant signaling roles.[1]
Kinase Assay Activity of purified IRAK-4 protein
In brief, IRAK-4 (20 ng/well) is incubated with 2 mM ATP containing radiolabeled [32P]ATP in the presence of 300 μM substrate peptide in a final volume of 40 μl in the presence of buffer and HS-243. The reaction is terminated at 20 min with 10 μl of 1 M H3PO4. The remaining activity is measured using a scintillation counter. Dose–response curves are repeated two times and averaged.
Cell Research Cell lines RA-FLS cells, THP-1 cells
Concentrations 10 μM
Incubation Time 24 h
Method

RA-FLS cells or THP-1 cells are treated with 10 μM HS-243 or vehicle (DMSO), and 24 h after treatment, supernatant is added to human cytokine XL proteome array in accordance with the manufacturer’s protocol. Chemiluminescence is used to visualize protein quantities.

Chemical Information & Solubility

Molecular Weight 324.33 Formula

C17H16N4O3
CAS No. 848249-10-5 SDF --
Smiles CCCN1C(NC2=CC=CC=C12)=NC(=O)C3=CC(=CC=C3)[N+]([O-])=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 16 mg/mL ( (49.33 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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