Triciribine

Triciribine is an adenosine analog that targets protein kinase B (Akt) with an IC₅₀ value of 130nM and has antitumor activity^{[1, 2]}. Triciribine is a DNA synthesis inhibitor of HIV-1 with an IC₅₀ value of 20nM^[3].

In vitro, treatment of prostate cancer PC-3 cells with Triciribine (10μM) for 24h enhanced apoptosis induced by TNF-related apoptosis-inducing ligand (TRAIL) and anti-CD95^[4]. Treatment of bovine cumulus-oocyte complex (COC) with Triciribine (1μM) for 22h resulted in an increase in the rate of blastocyst formation and increased the in vitro yield of bovine embryos^[5].

In vivo, treatment of C57BL/6 J mice with Triciribine (1, 2mg/kg/day) by intraperitoneal injection for 2 weeks significantly increased the level of low-density lipoprotein receptor (LDLR) in the liver of mice^[6]. Triciribine (1mg/kg/day) was intraperitoneally injected into mice inoculated with GFP⁺ Huh7 cells for 14 days, which significantly inhibited the growth of tumors in mice and exerted a synergistic effect when combined with rosiglitazone^[7].

References:
[1] Barrichon M, Hadi T, Wendremaire M, et al. EXPRESSION OF CONCERN: Dose‐dependent biphasic leptin‐induced proliferation is caused by non‐specific IL‐6/NF‐κB pathway activation in human myometrial cells[J]. British Journal of Pharmacology, 2015, 172(12): 2974-2990.
[2] Garrett C R, Coppola D, Wenham R M, et al. Phase I pharmacokinetic and pharmacodynamic study of triciribine phosphate monohydrate, a small-molecule inhibitor of AKT phosphorylation, in adult subjects with solid tumors containing activated AKT[J]. Investigational new drugs, 2011, 29: 1381-1389.
[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[J]. AIDS research and human retroviruses, 1993, 9(4): 307-314.
[4] Dieterle A, Orth R, Daubrawa M, et al. The Akt inhibitor triciribine sensitizes prostate carcinoma cells to TRAIL‐induced apoptosis[J]. International journal of cancer, 2009, 125(4): 932-941.
[5] Curcio A G, Ribeiro T I S, Gomes H F, et al. Increased in vitro production of bovine embryos resulting from oocyte maturation in the presence of triciribine, a specific inhibitor of AKT[J]. Theriogenology, 2025, 231: 222-227.
[6] Bjune K, Wierød L, Naderi S. Triciribine increases LDLR expression and LDL uptake through stabilization of LDLR mRNA[J]. Scientific Reports, 2018, 8(1): 16174.
[7] Liu L, Yang Z, Xu Y, et al. Inhibition of oxidative stress-elicited AKT activation facilitates PPARγ agonist-mediated inhibition of stem cell character and tumor growth of liver cancer cells[J]. PloS one, 2013, 8(8): e73038.