1. Cell Cycle/DNA Damage PI3K/Akt/mTOR Anti-infection
  2. DNA/RNA Synthesis Akt HIV
  3. Triciribine

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

Cat. No.: HY-15457 Purity: 98.59%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Triciribine Chemical Structure

Triciribine Chemical Structure

CAS No. : 35943-35-2

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 117 In-stock
Solution
10 mM * 1 mL in DMSO USD 117 In-stock
Solid
5 mg USD 106 In-stock
10 mg USD 168 In-stock
50 mg USD 502 In-stock
100 mg USD 778 In-stock
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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of Triciribine:

Top Publications Citing Use of Products

    Triciribine purchased from MedChemExpress. Usage Cited in: Stem Cell Res Ther. 2018 Mar 1;9(1):52.  [Abstract]

    Signaling protein expression detected by western blotting and quantified by densitometry with or without Triciribine.

    Triciribine purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290.  [Abstract]

    Inhibition of pAkt by API-2 effectively prevents K145 induced increasing phosphorylation of FoxO1 in response to insulin. API-2 also significantly reverses K145 suppressed PEPCK and G6Pase mRNA and protein expression.

    Triciribine purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290.  [Abstract]

    API-2 apparently inhibits insulin induced phosphorylation of Akt S473 in a dose dependent manner.

    View All Akt Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    IC50 & Target[1][2][3]

    DNA synthesis

     

    HIV-1

    0.02-0.46 μM (IC50)

    HIV-2

    0.02-0.46 μM (IC50)

    Akt

    130 nM (IC50, cell assay)

    In Vitro

    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.

    In Vivo

    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.

    Clinical Trial
    Molecular Weight

    320.30

    Formula

    C13H16N6O4

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to khaki

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (312.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.1221 mL 15.6104 mL 31.2207 mL
    5 mM 0.6244 mL 3.1221 mL 6.2441 mL
    View the Complete Stock Solution Preparation Table

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (7.81 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.81%

    References
    Cell Assay
    [2]

    The human SF295 and U87MG GBM lines and the mouse K1861-10, KR158, and KR130G astrocytoma lines are plated at a density of 2500 cells/100 µL complete media in 96-well plates. Mouse primary astrocytes are plated at 5000 cells/100 µL. Cells are treated in triplicate with serial dilutions of inhibitors (The inhibitors tested are PI-103, Triciribine and Rapamycin) ranging from µM to pM. Cell proliferation is measured after 3 days using the Alamar Blue assay on a Novostar plate reader. Values for 50% inhibitory concentration (IC50) and 50% growth inhibitory concentration (GI50) are calculated using standard procedures in GraphPad Prism v4 and Microsoft Excel[2].

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

    Animal Administration
    [4]

    Mice[4]
    Akt1+/+ and Akt1−/− mice are subjected to normoxia or hypoxia (10% O2) for 7 and 14 days (n=2-6 mice per group). Noteworthy, high mortality is observed in Akt1−/− mice exposed to hypoxia longer than 14-16 days. For pharmacological inhibition studies, Akt1+/+ mice, subjected to normoxia or chronic hypoxia for 14 days, received daily i.p. injection of saline, Triciribine (0.5 mg/kg per day) or Rapamycin (1.5 mg/kg per day) for 7 days, and the total continuous exposure to hypoxia or normoxia is 21 days (n=6-8 mice per group). Pharmacological inhibitors are administered daily while the mice are maintained in the hypoxia chamber to minimize exposure to air and spontaneous reversal of pulmonary remodelling.

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

    References

    Complete Stock Solution Preparation Table

    * 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.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1221 mL 15.6104 mL 31.2207 mL 78.0518 mL
    5 mM 0.6244 mL 3.1221 mL 6.2441 mL 15.6104 mL
    10 mM 0.3122 mL 1.5610 mL 3.1221 mL 7.8052 mL
    15 mM 0.2081 mL 1.0407 mL 2.0814 mL 5.2035 mL
    20 mM 0.1561 mL 0.7805 mL 1.5610 mL 3.9026 mL
    25 mM 0.1249 mL 0.6244 mL 1.2488 mL 3.1221 mL
    30 mM 0.1041 mL 0.5203 mL 1.0407 mL 2.6017 mL
    40 mM 0.0781 mL 0.3903 mL 0.7805 mL 1.9513 mL
    50 mM 0.0624 mL 0.3122 mL 0.6244 mL 1.5610 mL
    60 mM 0.0520 mL 0.2602 mL 0.5203 mL 1.3009 mL
    80 mM 0.0390 mL 0.1951 mL 0.3903 mL 0.9756 mL
    100 mM 0.0312 mL 0.1561 mL 0.3122 mL 0.7805 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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