Chemical Name:10-[4'-(N,N-Diethylamino)butyl]-2-chlorophenoxazine
hydrochloride
Biological Activity:
Selective
inhibitor of Akt/PKB. Inhibits IGF-1-stimulated phosphorylation and activation
of Akt (complete inhibition at 2.5 μM), suppressing downstream activation
of mTOR, p70 S6 kinase and S6 ribosomal protein. Shows no activity at PDK1,
SGK1 or PI 3-kinase. Inhibits cell growth (IC50 ~ 2-6 μM) and induces apoptosis in
rhabdomyosarcoma cells.
Thimmaiahet al (1992) Synthesis and
chemical characterization of N-substituted phenoxazines directed toward
reversing vinca alkaloid resistance in multidrug-resistant cancer cells.
J.Med.Chem. 35 3358. Thimmaiahet al (2005)
Identification of N10-substituted phenoxazines as potent and
specific inhibitors of Akt signaling. J.Biol.Chem. 36 31924.