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

Overview

Key Spec Table

CAS #Empirical Formula
612847-09-3C₃₄H₂₉N₇O

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124018-1MG
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      124018-5MG
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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
          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
          Global Trade Item Number
          Catalogue Number GTIN
          124018-1MG 07790788048006
          124018-5MG 04055977205718