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Merck

124020

Akt Inhibitor X

The Akt Inhibitor X, also referenced under CAS 925681-41-0, controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonyme(s) :

Akt Inhibitor X, 10-(4ʹ-(N-diethylamino)butyl)-2-chlorophenoxazine, HCl, 10-NCP

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A propos de cet article

Formule empirique (notation de Hill) :
C20H25ClN2O · xHCl
Numéro CAS:
925681-41-0
Poids moléculaire :
344.88 (free base basis)
MDL number:
MFCD09038570
UNSPSC Code:
12352200
NACRES:
NA.77

Principaux documents

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SMILES string

[Cl-].Clc1cc2c(cc1)Oc3c(cccc3)N2CCCC[N+H](CC)CC

InChI

1S/C20H25ClN2O.ClH/c1-3-22(4-2)13-7-8-14-23-17-9-5-6-10-19(17)24-20-12-11-16(21)15-18(20)23;/h5-6,9-12,15H,3-4,7-8,13-14H2,1-2H3;1H

InChI key

SVKSJUIYYCQZEC-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

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

color

white

solubility

water: 1 mg/mL

shipped in

ambient

Quality Level

100

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Catégories apparentées

General description

A cell-permeable, reversible, and selective inhibitor of the phosphorylation of Akt and its in vitro kinase activity (complete inhibition <5 M) with minimal effect on PI 3-K, PDK1, or SGK1. Shown to suppress growth of Rh (rhabdomyosarcoma) cell lines (IC50 = 2-5 M), inhibit IGF-I-stimulated nuclear translocation of Akt, and prevent phosphorylation of the downstream targets, mTOR, p70S6 kinase, and S6 ribosomal protein. Unlike Akti1/2 (Cat. No. 124018), the mode of inhibition is not PH domain-dependent. Also shown to induce neuronal autophagy in an Akt- and mTOR-independent manner and enhances the clearance of misfolded protein. Also available as a 20 mM solution in H2O(Cat. No. 124039).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Akt
Product does not compete with ATP.
Reversible: yes
Secondary Target
Rn cell lines (IC₅₀ = 2-5 µM)
Target IC50: <5 µM against Akt ; 2-5 µM against growth of Rh (rhabdomyosarcoma) cell lines

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Tsvetkov, A.S., et al. 2010. Proc. Natl. Acad. Sci. USAin press.
Thimmaiah, K.N., et al. 2005. J. Biol. Chem.280, 31924.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Irritant (B)

Classe de stockage

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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Uncoupling protein 2 (UCP2), a mitochondrial protein, is known to be upregulated in pancreatic islets of patients with type 2 diabetes (T2DM); however, the pathological significance of this increase in UCP2 expression is unclear. In this study, we highlight the

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