SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.{22158} Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.{12707} AS-1949490 is a small molecule inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2).{28682} It is not as potent an inhibitor of SHIP1, demonstrating inhibitory values 30-fold higher than that of SHIP2, and shows little effect against the phosphatases PTEN, synaptojanin, and myotubularin (IC50s >50 µM).{28682} AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.{28682} It has also been shown to suppress gluconeogenesis through reduced expression of PEPCK and G6Pase mRNA in normal mice and to decrease plasma glucose in diabetic db/db mice.{28682}
产品描述
A selective inhibitor of SHIP2 (IC50s = 0.62 and 0.34 µM for human and mouse, respectively; Ki = 0.44 µM for hSHIP2); dose-dependently increases insulin-induced phosphorylation of Akt and activates glucose metabolism
