AS 1949490, 10 mg

AS 1949490 is a potent and selective inhibitor of SHIP2. Inhibitory activity was tested using human and mouse SHIP2 resulting in IC50 values of 0.62 and 0.34 µM respectively. An approximately 30 fold higher IC50 was detected for structural related SHIP1 whereas no inhibition was found for other phosphatases (PTEN, synaptojanin and myotubularin, used concentration range: up to 50 µM AS 1949490). Inhibition of SHIP2 results in an increased phosphorylation of insulin signalling-related molecules, including Akt which in turn leads to activation of glucose metabolism and the reduction of gluconeogenesis. Chronic treatment of diabetic db/db mice with AS 1949490 considerably improved hyperglycaemia and glucose intolerance.

Chemical name:     3-[(4-Chlorophenyl)methoxy]-N-[(1S)-1-phenylethyl]thiophene-2-        carboxamide
CAS No.                1203680-76-5
Formula:                 C20H18ClNO2S
Molecular Weight:  371.88 g/mol
Long Term Storage:     4 °C
Preparation of solutions:     We recommend that stock solutions, once prepared, are stored aliquoted in tightly sealed vials at -20° C or below and used within 1 month. Wherever possible solutions should be made up and used on the same day.
Purity:                     99 %
Solubility:                Soluble to 100 mM in DMSO / ethanol

Product specific litertaure:

• Suwa A, Yamamoto T, Sawada A, Minoura K, Hosogai N, Tahara A, Kurama T, Shimokawa T, Aramori I. (2009) "Discovery and functional characterization of a novel small molecule inhibitor of the intracellular phosphatase, SHIP2." Br J Pharmacol. 2009; 158(3):879-87.

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.