Information 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. Targets IRAK-4 (Cell-free assay); IRAK-1 (Cell-free assay); TAK1 (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. Cell Research(from reference) Cell lines：RA-FLS cells, THP-1 cells Concentrations：10 μM Incubation Time：24 h
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HS-243
CAS number：848249-10-5 molecular formula：C17H16N4O3
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| Chinese alias | - | ||
| English alias | (E)-3-nitro-N-(1-propyl-1H-benzo[d]imidazol-2(3H)-ylidene)benzamide | ||
| CAS number | 848249-10-5 | molecular formula | C17H16N4O3 |
| molecular weight | 324.33 g/mol | Exact mass | ≥98% |
| PSA | 92.700 Ų | logp | 3.374 |
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