HS-276 是一种口服有效且高选择性的TAK1抑制剂，Ki值为 2.5 nM。HS-276 对 TAK1、CLK2、GCK、ULK2、MAP4K5、IRAK1、NUAK、CSNK1G2、CaMKKβ-1 和 MLK1 具有显著抑制作用，IC50值分别为 8.25、29、33、63、125、264、270、810、1280 和 5585 nM。HS-276 可用于类风湿关节炎 (RA) 研究。

HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a K i of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC 50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 can be used for rheumatoid arthritis (RA) research [1].

HS-276 reduces expression of TNF, IL-6, and IL-1β in a dose-dependent manner, with IC 50 values of 138, 201, and 234 nM, respectively [1].

HS-276 (CIA mouse model of inflammatory arthritis, 50 mg/kg, IP, daily for 6 days) reduces inflammation, pannus, cartilage damage (CD), bone resorption (BR), and periosteal bone formation (PBF) histological manifestations [1]. HS-276 (CD-1 mice, 30 mg/kg, Oral gavage, once) shows excellent bioavailability in mice with a C max of 3.68 μM and %F of 98.1% [1].

2767422-72-8

C24H29N5O2

419.52

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years