Triciribine Phosphate

Triciribine phosphate is an Akt activation inhibitor and an active metabolite of the prodrug triciribine (Item No. 10010237).^1,2 Upon entry into cells, triciribine is metabolized to triciribine phosphate by adenosine kinase (AK).² It binds to the Pleckstrin homology (PH) domain of Akt and prevents its recruitment to the plasma membrane in MDA-MB-468 cells.¹ Triciribine phosphate reduces the proliferation of A1847 and A2780 ovarian cancer cells (IC₅₀s = 1.6 and 18 µM, respectively).³ It inhibits HIV-1 reverse transcriptase activity in CEM-SS cells (IC₅₀ = 0.04 µM), as well as herpes simplex virus 1 (HSV-1) replication in BS-C-1 cells and human cytomegalovirus (CMV) plaque formation in HFF-1 IRR cells (IC₅₀s = 20 and 0.8 µM, respectively).⁴

WARNING This product is not for human or veterinary use.

1. Berndt, N., Yang, H., Tinczek, B., et al. The Akt activation inhibitor TCN-P inhibits Akt phosphorylation by binding to the PH domain of Akt and blocking its recruitment to the plasma membrane. Cell Death Differ. 17(11), 1795-1804 (2010).

2. Plagemann, P.G.W. Transport, phosphorylation, and toxicity of a tricyclic nucleoside in cultured Novikoff rat hepatoma cells and other cell lines and relase of its monophosphate by the cells. J. Natl. Cancer Inst. 57(6), 1283-1295 (1976).

3. Behrens, B.C., Hamilton, T.C., Louie, K.G., et al. Activity of tricyclic nucleoside 5'-phosphate in model systems of human ovarian cancer. Invest New Drugs 4(4), 295-304 (1986).

4. Porcari, A.R., Ptak, R.G., Borysko, K.Z., et al. Deoxy sugar analogues of triciribine: Correlation of antiviral and antiproliferative activity with intracellular phosphorylation. J. Med. Chem. 43, 2438-2448 (2000).