BC-1618

FBXO48抑制剂；3µM时对FBXO48的选择性优于FBXO30；0.5-10µM时可增加表达人类FBXO48的HEK293T细胞中的pAMPK和pACC水平；诱导BEAS-2B细胞中的线粒体裂变和表达GFP标记LC3的HEK293A细胞中的自噬；抑制报告分析中THP-1细胞中LPS诱导的NF-κB激活和分离的人类PBMCs中的细胞因子释放；20mg/kg时可增加高脂饮食诱发的肥胖小鼠模型中的胰岛素敏感性。An inhibitor of FBXO48; selective for FBXO48 over FBXO30 at 3 µM; increases the levels of pAMPK and pACC in HEK293T cells expressing human FBXO48 at 0.5-10 µM; induces mitochondrial fission in BEAS-2B cells and autophagy in HEK293A cells expressing GFP-tagged LC3; inhibits LPS-induced activation of NF-κB in THP-1 cells in a reporter assay and cytokine release in isolated human PBMCs; increases insulin sensitivity in a mouse model of high-fat diet-induced obesity at 20 mg/kg.分子式C24H24F3NO2分子量415.5FC(F)(C1=CC=C(C=C1)OCC(CN(CC2=CC=CC=C2)CC3=CC=CC=C3)O)F