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124018 Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 - CAS 612847-09-3 - Calbiochem

124018
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Key Spec Table

Empirical FormulaCAS #
C₃₄H₂₉N₇O612847-09-3

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124018-5MGCN
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      Description
      OverviewA cell-permeable and reversible quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition appears to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo. A 10 mM (1 mg/181 µl) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124017) in DMSO is also available.
      Catalogue Number124018
      Brand Family Calbiochem®
      Synonyms1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one, Akti-1/2
      References
      ReferencesCalleja, V., et al. 2009. PLoS Biol. 7, e17.
      Logie, L., et al. 2007. Diabetes 56, 228.
      Barnett, S.F., et al. 2005. Biochem. J. 385, 399.
      DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271.
      Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905.
      Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761.
      Product Information
      CAS number612847-09-3
      ATP CompetitiveN
      FormYellow solid
      Hill FormulaC₃₄H₂₉N₇O
      Chemical formulaC₃₄H₂₉N₇O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ200
      Applications
      ApplicationAkt Inhibitor VIII, Isozyme-Selective, Akti-1/2, CAS 612847-09-3, is a cell-permeable, reversible & selective inhibitor of Akt1/Akt2 (IC50 = 58 nM and 210 nM for Akt1 & Akt2, respectively),
      Biological Information
      Primary TargetAkt1, Akt2, Akt3
      Primary Target IC<sub>50</sub>58 nM, 210 nM, 2.12 µM against Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      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 Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 - CAS 612847-09-3 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 - CAS 612847-09-3 - Calbiochem Certificates of Analysis

      TitleLot Number
      124018

      References

      Reference overview
      Calleja, V., et al. 2009. PLoS Biol. 7, e17.
      Logie, L., et al. 2007. Diabetes 56, 228.
      Barnett, S.F., et al. 2005. Biochem. J. 385, 399.
      DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271.
      Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905.
      Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761.

      Brochure

      Title
      Akt
      Data Sheet

      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.

      Revision22-September-2012 JSW
      Synonyms1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one, Akti-1/2
      DescriptionA cell-permeable, reversible, potent, and selective inhibitor of Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition is reported to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number612847-09-3
      Chemical formulaC₃₄H₂₉N₇O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
      Toxicity Standard Handling
      ReferencesCalleja, V., et al. 2009. PLoS Biol. 7, e17.
      Logie, L., et al. 2007. Diabetes 56, 228.
      Barnett, S.F., et al. 2005. Biochem. J. 385, 399.
      DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271.
      Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905.
      Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761.