Chemical Name:1,5-Dihydro-5-methyl-1-b-D-ribofuranosyl-1,4,5,6,8-pent
aazaacenaphthylen-3-amine
Biological Activity:
Selective inhibitor of Akt (protein kinase B)
signalling; displays minimal inhibition of PKC, PKA, SGK and p38 pathways.
Inhibits phosphorylation and activation of downstream targets of Akt including
Bad, GSK-3β
and AFX. In vitro, induces apoptosis and growth arrest preferentially in human
cancer cells with elevated levels of Akt. In mice, potently and selectively
inhibits growth of Akt-overexpressing tumours. Inhibits DNA synthesis and
displays antiviral activity against HIV-1 and -2.
Wotring et al (1990) Dual mechanisms of inhibition
of DNA synthesis by triciribine. Cancer Res. 50 4891. Ptaket al (1998) Phosphorylation of triciribine is necessary for activity
against HIV type 1. AIDS Res.Hum.Retroviruses. 14 1315. Yanget al (2004) Akt/protein kinase B signaling inhibitor-2, a selective
small molecule inhibitor of Akt signaling with antitumour activity in cancer
cells overexpressing Akt. Cancer Res. 64 4394.