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.

• Synonym(e): Akt-Inhibitor X, 10-(4ʹ-(N-Diethylamino)butyl)-2-chlorphenoxazin, HCl, 10-NCP
• Empirische Formel (Hill-System): C₂₀H₂₅ClN₂O · xHCl
• CAS-Nummer: 925681-41-0
• Molekulargewicht: 344.88 (free base basis)
• MDL number: MFCD09038570
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥95% (HPLC)
• Form: solid
• Storage condition: OK to freeze, desiccated (hygroscopic), protect from light

Eigenschaften

• Quality Segment: 100
• 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
• storage temp.: 2-8°C
• 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

Beschreibung

General description

Ein zellpermeabler, reversibler und selektiver Inhibitor der Phosphorylierung von Akt und seiner In-vitro-Kinaseaktivität (vollständige Hemmung <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

Primärziel
Akt

Produkt konkurriert nicht mit ATP.

Reversibel: ja

Sekundärziel
Rn-Zelllinien (IC₅₀ = 2–5 µmol/l)

Zellpermeabel: ja

Ziel-IC₅₀: <5 µmol/l gegen Akt; 2–5 µmol/l gegen das Wachstum von Rh(Rhabdomyosarkom)-Zelllinien

Packaging

Verpackt unter inertem Gas

Preparation Note

Nach der Rekonstitution in Aliquote aufteilen und einfrieren (-20 °C). Stammlösungen sind bei -20 °C bis zu 3 Monate haltbar.

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

Toxizität: Reizstoff (B)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable