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344355 Foxo1 Inhibitor, AS1842856 - CAS 836620-48-5 - Calbiochem

Foxo1 Inhibitor, AS1842856, is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 (IC₅₀ = 33 nM). Directly binds to the active Foxo1, but not the Ser256-phosphorylated form.

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Synonymes: 5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

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344355
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Tableau de caractéristiques principal

CAS #Empirical Formula
836620-48-5C₁₈H₂₂FN₃O₃

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      Description
      OverviewA cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 (IC50 = 33 nM) over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in HepG2-based reporter assays; [AS184256] = 100 nM) via direct binding of the active Foxo1, but not the Ser256-phosphorylated/inactive form of Foxo1. Shown to inhibit gluconeogenesis in rat heptoma Fao cultures (IC50 = 43 nM against glucose production) in vitro and in liver of both non-diabetic and diabetic mice during a 26-hour fasting period (100 mg/kg/8 h p.o.) in vivo. Also available as a 50 mM solution in DMSO (Cat. No. 506081).
      Catalogue Number344355
      Brand Family Calbiochem®
      Synonyms5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
      References
      ReferencesNagashima, T., et al. 2010. Mol. Pharmacol. 78, 961.
      Product Information
      CAS number836620-48-5
      FormOff-white to tan to yellow solid
      Hill FormulaC₁₈H₂₂FN₃O₃
      Chemical formulaC₁₈H₂₂FN₃O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Regulatory Review
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      344355-10MG 07790788059712

      Documentation

      Foxo1 Inhibitor, AS1842856 - CAS 836620-48-5 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Foxo1 Inhibitor, AS1842856 - CAS 836620-48-5 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      344355

      Références bibliographiques

      Aperçu de la référence bibliographique
      Nagashima, T., et al. 2010. Mol. Pharmacol. 78, 961.

      Brochure

      Titre
      New Products: Volume 3, 2012
      Fiche technique

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision09-September-2016 JSW
      Synonyms5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
      DescriptionA 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.
      FormOff-white to tan to yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number836620-48-5
      Chemical formulaC₁₈H₂₂FN₃O₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Regulatory Review
      ReferencesNagashima, T., et al. 2010. Mol. Pharmacol. 78, 961.