| Bioactivity | AS1949490 is a potent, orally active, selective SHIP2 phosphatase inhibitor with IC50 values of 0.34, 0.62, 13, >50, >50, and >50 µM for Mouse SHIP2, Human SHIP2, Human SHIP1, Human PTEN, Human synaptojanin, and Human myotubularin, respectively. AS1949490 increases the phosphorylation of Akt, glucose consumption and glucose uptake. AS1949490 activates intracellular insulin signalling pathways. AS1949490 can be used for research of diabetes[1][2]. | |||||||||
| Target | IC50: 0.34 nM (Mouse SHIP2), 0.62 nM (Human SHIP2), 13 nM (Human SHIP1), >50 nM (Human PTEN), >50 nM (Human synaptojanin), and >50 µM (Human myotubularin). | |||||||||
| Invitro | AS1949490 (0-16 µM; 15 min; L6 myotubes) increases insulin-induced phosphorylation of Akt[1].AS1949490 (0-10 µM; 48 h) activates glucose metabolism and stimulates glucose uptake activity in L6 myotubes[1].AS1949490 (0-10 µM; 24 h; L6 myotubes) decreases the level of insulin-induced gluconeogenesis[1].AS1949490 (10 µM; 48 h) activates glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[2]. Western Blot Analysis[1] Cell Line: | |||||||||
| In Vivo | AS1949490 (300 mg/kg; p.o.; twice daily, for 7 or 10 d) decreases plasma glucose and activates intracellular insulin signalling in diabetic mice[1].AS1949490 (300 mg/kg; p.o.; once, for 8 h; male ICR mice) suppresses gluconeogenesis and the expression of related genes[1]. Animal Model: | |||||||||
| Name | AS1949490 | |||||||||
| CAS | 1203680-76-5 | |||||||||
| Formula | C20H18ClNO2S | |||||||||
| Molar Mass | 371.88 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Suwa A, et, al. Discovery and functional characterization of a novel small molecule inhibitor of the intracellular phosphatase, SHIP2. Br J Pharmacol. 2009 Oct;158(3):879-87. [2]. Suwa A, et, al. Glucose metabolism activation by SHIP2 inhibitors via up-regulation of GLUT1 gene in L6 myotubes. Eur J Pharmacol. 2010 Sep 10;642(1-3):177-82. |
AS1949490
CAS: 1203680-76-5 F: C20H18ClNO2S W: 371.88
AS1949490 is a potent, orally active, selective SHIP2 phosphatase inhibitor with IC50 values of 0.34, 0.62, 13, >50, >50
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