Triciribine

Triciribine is an Akt activation inhibitor and a prodrug form of triciribine phosphate (Item No. 37985).^1,2 It reduces levels of phosphorylated Akt1, -2, and -3 in Akt-overexpressing NIH3T3 cells when used at a concentration of 1 µM.¹ Triciribine is selective for Akt1, -2, and -3 over a panel of seven other Akt-activating kinases at 1 µM. It reduces the proliferation of L1210 mouse leukemia cells when used at concentrations of 0.05, 0.2, and 1 µM.² Triciribine (1 µM) induces cell cycle arrest at the G₁ phase in L1210 cells.¹ It reduces viral plaque formation in CEM-SS cells and human foreskin fibroblasts (HFFs) infected with HIV-1 and human cytomegalovirus (CMV), respectively (IC₅₀s = 0.02 and 2 µM, respectively).³ It inhibits tumor proliferation in an OVCAR-3 ovarian cancer mouse xenograft model when administered at a dose of 1 mg/kg per day.¹

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1. Yang, L., Dan, H.C., Sun, M., et al. Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumor activity in cancer cells overexpressing Akt. Cancer Res. 64(13), 4394-4399 (2004).

2. Wotring, L.L., Passiatore, J.E., Roti Roti, J.L., et al. Effects of the tricyclic nucleoside 6-amino-4-methyl-8-(β-D-ribofuranosyl)- pyrrolo[4,3,2-de]pyrimido[4,5-c]pyridazine on the viability and cell cycle distribution of L1210 cells in vitro. Cancer Res. 45(12 Pt 1), 6355-6361 (1985).

3. Kucera, L.S., Iyer, N.P., Puckett, S.H., et al. Activity of triciribine and triciribine-5'-monophosphate against human immunodeficiency virus types 1 and 2. AIDS Res. Hum. Retroviruses 9(4), 307-314 (1993).