生化机理 |
Triciribine, also known as API-2, suppresses the phosphorylation level and kinase activity of Akt. Triciribine is a cell-permeable tricyclic nucleoside that inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3. Triciribine does not inhibit PI3-Kinase or PDK1, the direct upstream activators of Akt, nor does it inhibit PKC, PKA, ERK1/2, serum- and glucocorticoid-inducible kinase, p38, STAT3, or JNK signalling pathways. Triciribine induces apoptosis and growth arrest in vitro, preferentially in human cancer cells with elevated levels of Akt. Triciribine potently and selectively inhibits growth of Akt-overexpressing tumors in mice. Triciribine also inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2. |
别名 |
6-Amino-4-methyl-8-(β-D-ribofuranosyl)-4H,8H-pyrrolo[4,3,2-de]pyrimido[4,5-c]pyridazine;6-Amino-4-methyl-8-(β-D-ribofuranosyl)-4H,8H-pyrrolo[4,3,2-de]pyrimido[4,5-c]pyridazine |