[CAS NO. 35943-35-2]  Triciribine

The nucleoside analog Triciribine (TCN) is a purine analog which is initially shown to inhibit DNA synthesis. Triciribine selectively inhibits the phosphorylation and activation of all three Akt isoforms. At a concentration of 10 μM Triciribine Akt phosphorylation is inhibited at both Thr308 and Ser473. Triciribine effectively inhibits the phosphorylation and consequently the catalytic activity of Akt in PC-3 cells ^[1] . The Akt inhibitor Triciribine (TCN) does not effectively inhibit the human cell line U87MG but inhibits other astrocytoma cell lines in a grade-dependent manner. The WHO II K1861-10 line is incompletely inhibited (69% maximum inhibition) with a GI ₅₀ value of 1.7 µM for Triciribine. Triciribine exhibits maximum growth inhibition around 1-10 µM and inhibits phosphorylation of Akt, as well as downstream p70S6K, to basal levels at 100 µM (IC ₅₀ =130 nM) in KR158 cells ^[2] . Triciribine (TCN) is a novel tricyclic compound with known antitumor activity. Using a syncytial plaque assay, Triciribine is active against HIV-1 at 0.01-0.02 μM. Using a microtiter XTT assay, Triciribine is active against a panel of HIV-1 and HIV-2 strains at IC ₅₀ values ranging from 0.02 to 0.46 μM ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.