1. Metabolic Enzyme/Protease
  2. Adenosine Deaminase
  3. 8-Azaadenosine

8-Azaadenosine is a potent ADAR1 inhibitor and an A-to-I editing inhibitor. 8-Azaadenosine blocks RNA editing and inhibits proliferation, 3D growth, invasion, and migration in thyroid cancer cells.

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

CAS No. : 10299-44-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    8-Azaadenosine purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Dec;13(12):4840-4855.

    Schematic illustration showing the drug treatment protocol. 8-Azaadenosine (2 mg/kg) was injected intraperitoneally every four days for 28 days for hypoxia or 35 days for SuHx (hypoxia combined with Su5416) PH models.

    8-Azaadenosine purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Dec;13(12):4840-4855.

    Hemodynamic analysis showing the therapeutic effects of 8-Azaadenosine (2 mg/kg, every four days for 28 days, ip) on Right ventricular systolic pressure (RVSP), and right ventricle (RV)/left ventricle (LV)+S weight ratio, n = 6.

    8-Azaadenosine purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Dec;13(12):4840-4855.

    Hematoxylin-eosin staining (HE) staining showing that 8-Azaadenosine significantly attenuated the increased median wall thickness of pulmonary vascular vessels caused by either hypoxia alone or SuHx, n = 6. NOR, normoxia; HYP, hypoxia, ns, no significance; Statistical analysis was performed with two-way ANOVA followed by Dunnett's test.

    8-Azaadenosine purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Dec;13(12):4840-4855.

    CCK8 analysis showing the concentration-dependent effect of 8-Azaadenosine (0.01-0.1 μmol/L) on hypoxia-stimulated cell viability, n = 6.

    8-Azaadenosine purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Dec;13(12):4840-4855.

    EdU staining assay showing that 8Aza abolished hypoxia-induced cell proliferation, n = 6. NOR, normoxia; HYP, hypoxia; NC, negative control; SI, siRNA of ADAR1; OE, ADAR1 overexpression plasmid.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    8-Azaadenosine is a potent ADAR1 inhibitor and an A-to-I editing inhibitor. 8-Azaadenosine blocks RNA editing and inhibits proliferation, 3D growth, invasion, and migration in thyroid cancer cells[1][2].

    Cellular Effect
    Cell Line Type Value Description References
    HEp-2 ED50
    0.8 μM
    Compound: 4, 8-azaadenosine
    Cytotoxicity against human Hep2 cells assessed as growth inhibition
    Cytotoxicity against human Hep2 cells assessed as growth inhibition
    [PMID: 556773]
    HEp-2 IC50
    0.7 μM
    Compound: 1
    Cytotoxicity against H.Ep cells
    Cytotoxicity against H.Ep cells
    [PMID: 6620307]
    HEp-2 IC50
    < 0.02 μM
    Compound: 1
    Cytotoxicity against H.Ep cells in the presence of 0.1 ug/mL pentostatin.
    Cytotoxicity against H.Ep cells in the presence of 0.1 ug/mL pentostatin.
    [PMID: 6620307]
    In Vitro

    8-Azaadenosine targets ADAR (adenosine deaminases acting on double-stranded RNA) activity only and does not affect ADAR1 mRNA levels[1][2].
    8-Azaadenosine (10-25 nM) restores let-7 miRNA biogenesis commensurate with a reduction in ADAR1 expression, RNA editing activity and LIN28B expression in JAK2/BCR-ABL1 transduced progenitors after two weeks in stromal co-culture[1].
    8-Azaadenosine (10, 100 nM) shows no effect on BCR-ABL and JAK2 signaling, as demonstrated by qRT-PCR analysis and p-CRKL and p-STAT5a Western blot analysis[1].
    8-Azaadenosine (0.1, 0.5, 1, 2 μM; 5 days) decreases cell viability/proliferation in a dose-dependent manner in TPC1 and Cal62 cells[2].
    8-Azaadenosine (1, 2 μM; 16 hours) impedes invasion and migration of TPC1 and Cal62 cells[2].
    8-Azaadenosine (1, 2 μM) inhibits the editing activity in TPC1 and Cal62 cells. By contrast, ADAR1 mRNA levels remains stable in both cells lines[2].

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

    Molecular Weight

    268.23

    Formula

    C9H12N6O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC1=NC=NC2=C1N=NN2[C@@H]3O[C@@H]([C@H]([C@H]3O)O)CO

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (932.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 3.33 mg/mL (12.41 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.7281 mL 18.6407 mL 37.2814 mL
    5 mM 0.7456 mL 3.7281 mL 7.4563 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.08 mg/mL (7.75 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.75 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    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: 99.94%

    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 (stored under nitrogen). 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
    H2O / DMSO 1 mM 3.7281 mL 18.6407 mL 37.2814 mL 93.2036 mL
    5 mM 0.7456 mL 3.7281 mL 7.4563 mL 18.6407 mL
    10 mM 0.3728 mL 1.8641 mL 3.7281 mL 9.3204 mL
    DMSO 15 mM 0.2485 mL 1.2427 mL 2.4854 mL 6.2136 mL
    20 mM 0.1864 mL 0.9320 mL 1.8641 mL 4.6602 mL
    25 mM 0.1491 mL 0.7456 mL 1.4913 mL 3.7281 mL
    30 mM 0.1243 mL 0.6214 mL 1.2427 mL 3.1068 mL
    40 mM 0.0932 mL 0.4660 mL 0.9320 mL 2.3301 mL
    50 mM 0.0746 mL 0.3728 mL 0.7456 mL 1.8641 mL
    60 mM 0.0621 mL 0.3107 mL 0.6214 mL 1.5534 mL
    80 mM 0.0466 mL 0.2330 mL 0.4660 mL 1.1650 mL
    100 mM 0.0373 mL 0.1864 mL 0.3728 mL 0.9320 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    • 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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    Product Name:
    8-Azaadenosine
    Cat. No.:
    HY-115686
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