Uses
HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 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].
Biological Activity
HS-276 is an orally activepotent and selective TGF-β-activated kinase-1 (TAK-1; TAK1) inhibitor (Ki = 2.5 nM; IC50 = 8.25 nM) th at significantly reduced cytokines production in THP-1 human macrophages upon LPS/IFNγ treatment (IC50 = 138 nM/TNF201 nM/IL-6and 234 nM/IL-1β). HS-276 effectively attenuates arthritic-like symptoms in the CIA mouse rheumatoid arthritis (RA) model (10-30 mg/kg/d p.o. or 25 mg/kg/d i.p.).
