For research use only.
CAS No. 848249-10-5
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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|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.|
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.
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.
|In vitro||DMSO||65 mg/mL (200.41 mM)|
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