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

124018
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Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₃₄H₂₉N₇O 612847-09-3

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124018-1MG
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      Plastic ampoule 1 mg
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      124018-5MG
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          Glass bottle 5 mg
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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
          New Research Tools for Signal Transduction and Life Science Research
          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.