5.06081
Foxo1 Inhibitor, AS1842856
InSolution, ≥98%, 50 mM in DMSO, A cell-permeable oxodihydroquinoline
Synonym(s):
InSolution Foxo1 Inhibitor, AS1842856, 5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
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About This Item
Empirical Formula (Hill Notation):
C18H22FN3O3
Molecular Weight:
347.38
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
liquid
Storage condition:
OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light
Quality Segment
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
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
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)
Storage Class
10 - Combustible liquids
wgk
WGK 1
flash_point_f
188.6 °F - (refers to pure substance)
flash_point_c
87 °C - (refers to pure substance)
Certificates of Analysis (COA)
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