AS 1949490

Biological Activity

AS 1949490 is a selective SHIP2 (SH2 domain-containing inositol 5'-phosphatase 2) inhibitor (IC₅₀ values are 0.34 μM and 0.62 μM for mouse and human respectively); displays approximately 30-fold affinity for SHIP2 over SHIP1. Increases insulin-induced phosphorylation of Akt in L6 myotubules. Stimulates activation of glucose metabolism; regulates gluconeogenesis in vitro and in vivo and exhibits antidiabetic effects. Also promotes increased BDNF mRNA levels in cultured cortical neurons and has memory enhancing and antidepressant effects in vivo.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Phosphatidylinositol 3,4-bisphosphate regulates neurite initiation and dendrite morphogenesis via actin aggregation
   SX Zhang, LH Duan, SJ He, GF Zhuang, X Yu
   Cell Res, 2017;0(0):.
2. Endophilin marks and controls a clathrin-independent endocytic pathway.
   Boucrot E, Ferreira A, Almeida-Souza L, Debard S, Vallis Y, Howard G, Bertot L, Sauvonnet N, McMahon H
   Nature, 2015;517(7535):460-5.
3. AS1949490, an inhibitor of 5'-lipid phosphatase SHIP2, promotes protein kinase C-dependent stabilization of brain-derived neurotrophic factor mRNA in cultured cortical neurons.
   Tsuneki et al.
   Eur.J.Pharmacol., 2019;
4. Glucose metabolism activation by SHIP2 inhibitors via up-regulation of GLUT1 gene in L6 myotubes.
   Suwa et al.
   Eur.J.Pharmacol., 2010;642:177

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