SH2 domain-containing inositol 5’-phosphatase 2 (SHIP2) negatively regulates the insulin signaling pathway by hydrolyzing phosphatidylinositol-3,4,5-trisphosphate.¹ Its activity has been implicated in the pathogenesis of insulin resistance and type 2 diabetes.² AS-1949490 is a small molecule inhibitor of SHIP2 (IC₅₀s = 0.62 and 0.34 µM for human and mouse, respectively; K_i = 0.44 µM for hSHIP2).³ 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).³ AS-1949490 has been shown to dose-dependently increase insulin-induced phosphorylation of Akt and to activate glucose metabolism.³ 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.³

≥98%

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1.Batty, I.H.,Van der Kaay, J.,Gray, A., et al. The control of phosphatidylinositol 3,4-bisphosphate concentrations by activation of the Src homology 2 domain containing inositol polyphosphate 5-phosphatase 2, SHIP2. Biochemistry Journal 407, 255-266 (2007).

2.Sleeman, M.W.,Wortley, K.E.,Lai, K.M.V., et al. Absence of the lipid phosphatase SHIP2 confers resistance to dietary obesity. Nature Medicine 11(2), 199-205 (2005).

3.Suwa, A.,Yamamoto, T.,Sawada, A., et al. Discovery and functional characterization of a novel small molecule inhibitor of the intracellular phosphatase, SHIP2. British Journal of Pharmacology 158, 879-887 (2009).