Skip to Content
Merck
All Photos(1)

Key Documents

5.06081

Sigma-Aldrich

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

Sign Into View Organizational & Contract Pricing

Select a Size


Select a Size

Change View

About This Item

Empirical Formula (Hill Notation):
C18H22FN3O3
Molecular Weight:
347.38
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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
Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

A 50 mM (5 mg/288 µL) sterile-filtered solution of Foxo1 Inhibitor, AS1842856 (Cat. No. 344355) in DMSO.

Reconstitution

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

Storage Class Code

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)

    Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

    Already Own This Product?

    Find documentation for the products that you have recently purchased in the Document Library.

    Visit the Document Library

    Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

    Contact Technical Service