124017
Akt Inhibitor VIII, Akti-1/2
InSolution, ≥95%, Isozyme-Selective
Synonym(s):
InSolution Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2
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About This Item
Empirical Formula (Hill Notation):
C34H29N7O
Molecular Weight:
551.64
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
≥95% (HPLC)
form
liquid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
shipped in
wet ice
storage temp.
−70°C
General description
A cell-permeable, 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Akt1, Akt2, Akt3
Akt1, Akt2, Akt3
Product does not compete with ATP.
Reversible: yes
Target IC50: 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays
Packaging
Packaged under inert gas
Please refer to vial label for lot-specific concentration.
Warning
Toxicity: Irritant (B)
Physical form
A 10 mM (1 mg/181 µl) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124018) in DMSO.
Reconstitution
Following initial thaw, aliquot and freeze (-70°C).
Other Notes
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
10 - Combustible liquids
WGK
WGK 2
Flash Point(F)
188.6 °F - closed cup - (Dimethylsulfoxide)
Flash Point(C)
87 °C - closed cup - (Dimethylsulfoxide)
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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Sarah J Russell et al.
The Journal of biological chemistry, 295(45), 15292-15306 (2020-09-02)
Muscle atrophy is regulated by the balance between protein degradation and synthesis. FOXO1, a transcription factor, helps to determine this balance by activating pro-atrophic gene transcription when present in muscle fiber nuclei. Foxo1 nuclear efflux is promoted by AKT-mediated Foxo1
Enrico Desideri et al.
Autophagy, 19(1), 152-162 (2022-04-19)
Impaired degradation of the transcriptional coactivator YAP1 and IL6ST (interleukin 6 cytokine family signal transducer), two proteins deregulated in liver cancer, has been shown to promote tumor growth. Here, we demonstrate that YAP1 and IL6ST are novel substrates of chaperone-mediated
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