- 商品介绍
- 规格参数
- 包装参数
General description
A cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in HepG2-based reporter assays; [AS184256] = 100 nM) in a dose-dependent manner (IC50 = 33 nM) via direct binding of the non-Ser256-phosphorylated/active Foxo1, but not the Ser256-phosphorylated/inactive form of Foxo1. Shown to inhibit gluconeogenesis in rat heptoma Fao cultures (IC50 = 37 and 130 nM against PEPCK and G6Pase mRNA level; IC50 = 43 nM against glucose production) in vitro and in murine liver of both normoglycemic ICR mice (60% and 45% inhibition of hepatic G6Pase and PEPCK mRNA level, respectively; three 100 mg/kg p.o. dosages at 0, 12, 24 h) and diabetic db/db mice (86%, 70%, 56%, 48%, 35%, and 31% inhibition of hepatic G6Pase, ABCG8, ABCG5, PEPCK, IL-1β, and apoCIII mRNA level, respectively; three 100 mg/kg p.o. dosages at 0, 12, 24 h) during a 26-hour fasting period in vivo.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Foxo1
Reversible: yes
Packaging
Packaged under inert gas
Physical form
A 50 mM (5 mg/288 µL) sterile-filtered solution of Foxo1 Inhibitor, AS1842856 (Cat. No. 344355) in DMSO.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.
Other Notes
Nagashima, T., et al. 2010. Mol. Pharmacol.78, 961.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,avoid repeated freeze/thaw cycles,desiccated (hygroscopic),protect from light |
| storage temp. | −70°C |
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¥ 1683.78
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¥ 3109.49
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