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 In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . 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 )
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HS-276
CAS number：2767422-72-8(DMSO) molecular formula：C24H29N5O2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2767422-72-8(DMSO) | molecular formula | C24H29N5O2 |
| molecular weight | 419.52 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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