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Tricirbine Triciribine is a potent AKT inhibitor and a cell-permeable tricyclic nucleoside molecule with potential antineoplastic activity. Akt-1, -2, and -3 are serine/threonine protein kinases in the phosphatidylinositol (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival. Following recruitment of Akt to the plasma membrane, phosphorylation at threonine 308 and serine 473 (Akt-1 numbering) by phosphoinositide-dependent kinases (PDK) 1 and 2 results in full activation of the enzyme. Triciribine is a cell-permeable tricyclic nucleoside that inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3. It does not inhibit phosphatidylinositol 3 (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 effectively inhibits growth of Akt-overexpressing human cancer cell lines in vitro with 50% inhibition at ~5-10 μM. It also inhibit growth of tumor xenografts in mice by greater than 80% at a dose of 1 mg/kg/day. Group: Pharmaceutical. Alternative Names: VQD-002; VQD 002; VQD002; API-2; Akt Inhibitor V; Pentaazacentopthylene; Tricyclic nucleoside; 1,5-Dihydro-5-methyl-1-beta-D-ribofuranosyl-1,4,5,6,8-pentaazaacenaphthylen-3-amine. CAS No. 35943-35-2. Pack Sizes: 100 mg. Product ID: B1370-090988. Molecular formula: C13H16N6O4. Mol BOC Sciences
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