トリシリビン

化学的特性

Off-White Solid

使用

Triciribine is an antitumor tricyclic nucleoside. Triciribine acts as a potent, small-molecule inhibitor of AKT phosphorylation in subjects with solid tumors contining activated AKT. Triciribine is al so a selective inhibitor of HIV-1 and HIV-2, including strains known to be resistant to AZT or TIBO.

生物活性

Selective inhibitor of Akt (protein kinase B) signaling; displays minimal inhibition of PKC, PKA, SGK and p38 pathways. Inhibits phosphorylation and activation of downstream targets of Akt including Bad, GSK-3 β 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 tumors. Inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2.