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124017

Sigma-Aldrich

InSolution Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2

The InSolution Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):
InSolution Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2
Empirical Formula (Hill Notation):
C34H29N7O
Molecular Weight:
551.64

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

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This Item
124030124029124034
form

liquid

form

solid

form

solid

form

powder

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

OK to freeze

shipped in

wet ice

shipped in

ambient

shipped in

ambient

shipped in

ambient

storage temp.

−70°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°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
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.

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 - (Dimethylsulfoxide)

Flash Point(C)

87 °C - (Dimethylsulfoxide)


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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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