HS-243

For research use only.

Catalog No.S9701

HS-243 Chemical Structure

CAS No. unknown

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.

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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

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]

Protocol

Kinase Assay:

[1]

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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:

[1]

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  • 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.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 65 mg/mL (200.41 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 324.33
Formula

C17H16N4O3

CAS No. unknown
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID