HS-276 (C09-1138-586)

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) researchIn VitroHS-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoHS-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 . 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% . MCE has not independently confirmed the accuracy of these methods. They are for reference only.IC50& Target:IRAK1 264 nM (IC 50 ) IRAK4 2500 nM (IC 50 ). Specifications and Purity: 10mM in DMSO. Molecular Formula: C24H29N5O2. Molecular Weight: 419.52.