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Triciribine, also known as API-2, NSC 154020, is a cell-permeable tricyclic nucleoside that inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3. Akt-1, -2, and -3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival. Triciribine induced autophagy, which could be interpreted as a defensive mechanism, because an autophagy inhibitor (chloroquine) increased triciribine-induced apoptosis. In vitro, Triciribine (API-2) significantly inhibits Akt-overexpressing human cancer cell lines growth with 50% inhibition at ~5-10 µM. It also inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2. Combinations of triciribine with classic inhibitors targeting other molecules of the PI3K-AKT-pathway led to synergistic anti-proliferative effects.
| Cell Experiment | |
|---|---|
| Cell lines | LNCaP, PC-3, OVCAR3, OVCA8, PANC1, MDA-MB-468, and WM35 cells line |
| Preparation method | Screening for Inhibition of Akt-Transformed Cell Growth. AKT2 transformed NIH3T3 cells or LXSN vector-transfected NIH3T3 control cells (4) were plated into 96-well tissue culture plate. After treatment with 5 μM NCI Diversity Set compound, cell growth was detected with CellTier 96 One Solution Cell Proliferation kit (Promega). Compounds that inhibit growth in AKT2-transformed but not LXSN-transfected NIH3T3 cells were considered as candidates of Akt inhibitor and subjected to additional analysis. |
| Concentrations | 0~20 μM |
| Incubation time | 24 and 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Nude Mouse Tumor Xenograft Model |
| Formulation | 20% DMSO |
| Dosages | 1 mg/kg/day |
| Administration | i.p. |
| Molecular Weight | 320.3 |
| Formula | C13H16N6O4 |
| CAS Number | 35943-35-2 |
| Solubility (25°C) | DMSO 54 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Akt Products |
|---|
| (E)-Akt inhibitor-IV
(E)-Akt inhibitor-IV is a PI3K-Akt inhibitor, with potent cytotoxic. |
| K-80003
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth. |
| FPA-124
FPA-124, a cell-permeable copper complex, is a selective Akt inhibitor with an IC50 of 0.1 μM. |
| SPOP-IN-1
SPOP-IN-1 is a selective SPOP E3 ubiquitin ligase inhibitor. |
| 10-DEBC hydrochloride
10-DEBC hydrochloride is a selective Akt inhibitor, with an IC50 of 1.28 μM. |
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