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AKT protein kinase inhibitor VIII, 5 mg  

AKT protein kinase inhibitor VIII, 5 mg

1-(1-(phenyl-1H-imidazo[4,5-g]quinoxalin-6-yl)benzyl)piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one

Akt Inhibitor VIII is a non-ATP competitive inhibitor of Akt isoforms 1 and 2

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PKI-AKTIN8-005

Availability: within 3 days

182,00 €

Background: Akt Inhibitor VIII is a non-ATP competitive inhibitor of Akt isoforms 1 (PKB alpha) and 2 (PKB beta) (IC50 values 58 nM and 210 nM for Akt1 and Akt2, respectively). Moreover, the Akt inhibitor efficiently inhibits Ca2+/CaM-dependent protein kinase (CaMKIα) activity (IC50 value 3.99 μM) and prevents TCDD induced nuclear translocation of aryl hydrocarbon receptor (AhR) in MCF-7 cells. Akti-1/2 inhibitory effects towards CaMKIα and TCDD-induced EROD activity in function of Akti-1/2 concentrations were quite similar (IC50 ± SD, 3.99 ± 0.82 μM and 5.86 ± 1.85 μM, respectively).

Chemical formula: C34H29N7O
Molecular weight: 551.64 g/mol
Purity: 98 %
Appearance: Off-white solid
Solubility: Soluble in 0.1N HCl(aq) and DMSO
CAS Number: 612847-09-3

Manufacturer:  Axon Medchem BV

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.  

References

D. Gilot et al. Akti-1/2, an allosteric inhibitor of Akt 1 and 2, efficiently inhibits CaMKIα activity and aryl hydrocarbon receptor pathway. Chem Biol Interact. 2010 Dec 5;188(3):546-52.
 
C.W. Lindsley et al. Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. Bioorg Med Chem Lett. 2005 Feb 1;15(3):761-4.

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