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124036 Akt Inhibitor XVIII, SC66 - Calbiochem

124036
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Replacement Information

Tableau de caractéristiques principal

Empirical Formula
C₁₈H₁₆N₂O

Prix & Disponibilité

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124036-25MG
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      Description
      OverviewA cell-permeable pyridine compound that selectively targets Akt, but not PLCδ, PH domain, preventing Akt membrane localization/activation and rendering Akt in a conformation susceptible to ubiquitination and subsequent proteasomal degradation. Akti-1/2 (Cat. Nos. 124017 & 124018) competes for Akt PH domain binding and blocks SC66-induced Akt ubiquitination and proteasomal degradation. Effectively inhibits HEK293T growth both in vitro (>99 inhibition at 0.4 µM) and in mice in vivo (84% of control tumor size with twice weekly i.p. dose of 30 mg/kg), Synergizes with LY294002 (Cat. Nos. 440202 & 440204) in cell death induction in HeLa and HS-Sultan cultures in vitro.
      Catalogue Number124036
      Brand Family Calbiochem®
      Synonyms(2E,6E)-2,6-bis(4-Pyridylmethylene)cyclohexanone
      References
      ReferencesJo, H., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 6486.
      Product Information
      FormPale yellow solid
      Hill FormulaC₁₈H₁₆N₂O
      Chemical formulaC₁₈H₁₆N₂O
      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 1 month at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Akt Inhibitor XVIII, SC66 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Jo, H., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 6486.
      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.

      Revision03-April-2012 JSW
      Synonyms(2E,6E)-2,6-bis(4-Pyridylmethylene)cyclohexanone
      DescriptionA cell-permeable pyridine compound that represses Akt activation by allosterically disrupting Akt-PH domain binding to PIP3 and directly facilitating Akt ubiquitination with little proteasomal or deubiquitination activity. Blocks phosphorylations of Akt-Ser473 and downstream targets TSC, FOXO and PRAS40 in HEK293T cells at 8 µg/ml with minimal effect on pAkt-Thr450. Shown to be highly efficacious towards PI 3-K inhibitor resistant Akt1-E17K mutant and exert synergistic apoptotic activity with LY 294002 (Cat. No. 440202) against HeLa cells. Suppresses tumor growth in a mouse HEK293T-xenograft model (30 mg/kg, s.c., twice per week).
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₈H₁₆N₂O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (25 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
      Toxicity Regulatory Review
      ReferencesJo, H., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 6486.