HS-243 is an inhibitor of IRAK-4 and IRAK-1 with IC50s of 20 and 24 nM. HS-243 shows anti-inflammatory and anticancer activity.
HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 (0-10 μM) inhibits cell survival by 21% for AN3-CA pancreatic cancer cells, and 13% for SKOV-3 ovarian cancer cells. HS-243 (10 μM) potently reduces the pro-inflammatory response of RA cells and macrophages and 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].