849669-54-1
849669-54-1 structure
- Name: AQX-016A
- Chemical Name: AQX-016A
- CAS Number: 849669-54-1
- Molecular Formula: C22H32O2
- Molecular Weight: 328.49
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphatase
- Create Date: 2021-05-22 17:10:21
- Modify Date: 2024-04-05 19:27:35
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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].
| Name | AQX-016A |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
TNFα PI3K |
| In Vitro | 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: SHIP1+/+ and SHIP1-/- mast cells[2] Concentration: 0, 3, 6, 15, 30 μM Incubation Time: 30 min Result: Inhibited PIP3-regulated intracellular signal transduction events in SHIP-expressing hematopoietic cells, but not in SHIP-deficient hematopoietic or nonhematopoietic cells. Preferentially inhibited, in a dose-dependent manner, LPS-stimulated PKB phosphorylation in SHIP1+/+ but not in SHIP1-/-macrophages, and inhibited the phosphorylation of PKB, p38MAPK and extracellular signal-regulated kinase (ERK) in SHIP1+/+ but not in SHIP1-/- mast cells. |
| In Vivo | AQX-016A (20 mg/kg, Orally, once) significantly inhibits plasma TNFa levels, and inhibits inflammation in a mouse model endotoxemia[1][2]. |
| References |
| Molecular Formula | C22H32O2 |
|---|---|
| Molecular Weight | 328.49 |