HS-243 是一种有效且选择性的 IRAK-4 和 IRAK-1 抑制剂，IC₅₀ 为 20 和 24 nM。HS-243 对 TAK1 (转化生长因子 β 活化激酶 1) 有微弱的抑制活性，IC₅₀ 为 0.5 μM。HS-243 具有抗炎和抗癌活性。

HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC 50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC 50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity.

Solid

IRAK4 20 nM (IC50) IRAK-1 24 nM (IC50

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).
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.
HS-243 shows minimal to no percentage of inhibition against IRAK-4 Y262T or Y262A mutants at 0.3 and 1 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 41.67 mg/mL (128.48 mM; Need ultrasonic)配制储备液