Triciribine  (Synonyms: API-2; NSC 154020; TCN)

Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC₅₀ of 130 nM, and 0.02-0.46 μM, respectively.

The nucleoside analog Triciribine (TCN) is a purine analog which is initially shown to inhibit DNA synthesis. Triciribine selectively inhibits the phosphorylation and activation of all three Akt isoforms. At a concentration of 10 μM Triciribine Akt phosphorylation is inhibited at both Thr308 and Ser473. Triciribine effectively inhibits the phosphorylation and consequently the catalytic activity of Akt in PC-3 cells^[1]. The Akt inhibitor Triciribine (TCN) does not effectively inhibit the human cell line U87MG but inhibits other astrocytoma cell lines in a grade-dependent manner. The WHO II K1861-10 line is incompletely inhibited (69% maximum inhibition) with a GI₅₀ value of 1.7 μM for Triciribine. Triciribine exhibits maximum growth inhibition around 1-10 μM and inhibits phosphorylation of Akt, as well as downstream p70S6K, to basal levels at 100 μM (IC₅₀=130 nM) in KR158 cells^[2]. Triciribine (TCN) is a novel tricyclic compound with known antitumor activity. Using a syncytial plaque assay, Triciribine is active against HIV-1 at 0.01-0.02 μM. Using a microtiter XTT assay, Triciribine is active against a panel of HIV-1 and HIV-2 strains at IC₅₀ values ranging from 0.02 to 0.46 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Triciribine (TCBN) treatment, administered for 7 days after 14 days of hypoxia until 21 days of hypoxia is reached, reversed the vascular thickening as shown by immunohistochemistry and Western analyses. On the other hand, Rapamycin treatment did not prevent hypoxia-induced pulmonary alveolar haemorrhage and congestion. Triciribine partially inhibits progressive pruning of the vasculature^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

320.30

C₁₃H₁₆N₆O₄

35943-35-2

Solid

Light yellow to khaki

OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)N2C3=NC=NC4=C3C(C(N)=NN4C)=C2

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Dieterle A, et al. The Akt inhibitor triciribine sensitizes prostate carcinoma cells to TRAIL-induced apoptosis. Int J Cancer. 2009 Aug 15;125(4):932-41.  [Content Brief]

  [2]. Gürsel DB, et al. Control of proliferation in astrocytoma cells by the receptor tyrosine kinase/PI3K/AKT signaling axis and the use of PI-103 and TCN as potential anti-astrocytoma. Neuro Oncol. 2011 Jun;13(6):610-21  [Content Brief]

  [3]. Kucera LS, et al. Activity of triciribine and triciribine-5'-monophosphate against human immunodeficiency virus types 1 and 2. AIDS Res Hum Retroviruses. 1993 Apr;9(4):307-14.  [Content Brief]

  [4]. Abdalla M, et al. The Akt inhibitor, triciribine, ameliorates chronic hypoxia-induced vascular pruning and TGFβ-induced pulmonary fibrosis. Br J Pharmacol. 2015 Aug;172(16):4173-88.  [Content Brief]