| Bioactivity | AQX-016A is an orally active and potent SHIP1 agonist. AQX-016A can activate recombinant SHIP1 enzyme in vitro and stimulate SHIP1 activity. AQX-016A also can inhibit the PI3K pathway and TNFa production, can be useful for various inflammatory diseases research[1][2]. | ||||||||||||
| Invitro | AQX-016A (5 μg/mL, 30 min) inhibits the PI3K-mediated increase in intracellular PIP3 levels, and reduces PIP3 levels through activation of a 5 'phosphatase enzyme[1].AQX-01 6A (0-5 μg/mL, 30 min) inhibits LPS-induced PKB phosphorylation in a SHIP dependent manner[1].AQX-016A (0-5 μg/mL, 2 h) significantly inhibits TNFa in both J774 and peritoneal macrophages at both 1 and 5 μg/mL[1].AQX-016A (0-6 μg/mL, 30 min) requires SHIP to maximally inhibit TNFa production in BMDM, selectively inhibits TNF production from SHIP1+/+ but not SHIP1-/- macrophages[1].AQX-016A (0-5 μg/mL, 0-90 min) inhibits TNFa translation[1].AQX-016A (0-15 μM, 30 min) increases SHIP1 enzyme activity in vitro and in intact cells, inhibits macrophage and mast-cell activation[2].AQX-016A (15 μM, 30 min) inhibits immune cell activation, and inhibits PI3K-dependent macrophage and mast-cell responses in a SHIP-dependent manner[2]. Western Blot Analysis Cell Line: | ||||||||||||
| In Vivo | AQX-016A (20 mg/kg, Orally, once) significantly inhibits plasma TNFa levels, and inhibits inflammation in a mouse model endotoxemia[1][2]. | ||||||||||||
| Name | AQX-016A | ||||||||||||
| CAS | 849669-54-1 | ||||||||||||
| Formula | C22H32O2 | ||||||||||||
| Molar Mass | 328.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. [1]Yau, Tien Yin. Novel strategies for antagonizing the phosphatidylinositol-3-kinase pathway in disease. University of British Columbia. 2010. [2]. Ong CJ, et al. Small-molecule agonists of SHIP1 inhibit the phosphoinositide 3-kinase pathway in hematopoietic cells. Blood. 2007 Sep 15;110(6):1942-9. |