AQX-016A

• CAT Number: I022363
• CAS Number: 849669-54-1
• Molecular Formula: C22H32O2
• Molecular Weight: 328.49
• Purity: ≥95%
• Synonyms: (4aS,6aR,11aR,11bS)-4,4,6a,7,11b-pentamethyl-1,2,3,4a,5,6,11,11a-octahydrobenzo[a]fluorene-9,10-diol
• InChI: InChI=1S/C22H32O2/c1-13-11-15(23)19(24)14-12-17-21(4)9-6-8-20(2,3)16(21)7-10-22(17,5)18(13)14/h11,16-17,23-24H,6-10,12H2,1-5H3/t16-,17+,21-,22+/m0/s1
• InChIKey: DTFQQAANPRPMBC-DEVSCXNHSA-N
• SMILES: CC1=CC(=C(C2=C1C3(CCC4C(CCCC4(C3C2)C)(C)C)C)O)O

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].
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].
AQX-016A (20 mg/kg, Orally, once) significantly inhibits plasma TNFa levels, and inhibits inflammation in a mouse model endotoxemia[1][2].

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.
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