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K145 is a selective inhibitor of sphingosine kinase 2 (SPHK2; Ki = 6.4 µM) with IC50 values of 4.3 and >10 µM for human recombinant SPHK2 and SPHK1, respectively.1 It inhibits SPHK2, but not SPHK1, activity in U937 cells when used at a concentration of 10 µM. In vivo, K145 (15 mg/kg, i.p.) inhibits tumor growth in a U937 mouse xenograft model. It also improves glucose tolerance and regulates gluconeogenesis by stimulating insulin-dependent Akt/FoxO1 signaling in a mouse model of insulin resistance induced by dexamethasone (Item No. 11015) when administered at a dose of 30 mg/kg.2
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1. Biological characterization of 3-
2. 3-