For research use only. Not for therapeutic Use.
HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity[1].
HS-243 (0-10 μM, 24 h) inhibits cell survival by 21% for AN3-CA (pancreatic cancer cell), and 13% for SKOV-3 (ovarian cancer cell)[1].
HS-243 (10 μM, 24 h) potently reduces the proinflammatory response of RA cells and macrophages, significantly reduces the secretion of 15 cytokines, including IL-8, CD14, GRO-α, MIP-1a, MIP-3a, uPAR, Osteopontin, MMP-9, MCP-1, I-TAC, TIM-3, IP-10, GDF-15, and RANTES[1].
HS-243 shows minimal to no percentage of inhibition against IRAK-4 Y262T or Y262A mutants at 0.3 and 1 μM[1].
| Catalog Number | I028893 |
| CAS Number | 848249-10-5 |
| Synonyms | 3-nitro-N-(1-propylbenzimidazol-2-yl)benzamide |
| Molecular Formula | C17H16N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C17H16N4O3/c1-2-10-20-15-9-4-3-8-14(15)18-17(20)19-16(22)12-6-5-7-13(11-12)21(23)24/h3-9,11H,2,10H2,1H3,(H,18,19,22) |
| InChIKey | JLLIANWHDQWCMY-UHFFFAOYSA-N |
| SMILES | CCCN1C2=CC=CC=C2N=C1NC(=O)C3=CC(=CC=C3)[N+](=O)[O-] |
| Reference | [1]. Scarneo SA, et al. A highly selective inhibitor of interleukin-1 receptor-associated kinases 1/4 (IRAK-1/4) delineates the distinct signaling roles of IRAK-1/4 and the TAK1 kinase. J Biol Chem. 2020 Feb 7;295(6):1565-1574. |
