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

Akt 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),

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 1,3-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

Primary Target: Akt1, Akt2, Akt3
124018
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Overview

Key Spec Table

CAS #Empirical Formula
612847-09-3C₃₄H₂₉N₇O

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Catalogue NumberPackaging Qty/Pack
124018-1MG Plastic ampoule 1 mg
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124018-5MG 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
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