1. Epigenetics Apoptosis Cell Cycle/DNA Damage
  2. DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog
  3. Decitabine

Decitabine  (Synonyms: 5-Aza-2'-deoxycytidine; 5-AZA-CdR; NSC 127716)

Cat. No.: HY-A0004 Purity: 99.87%
COA Handling Instructions

Décitabine (NSC 127716) est un antimétabolite analogue de désoxycytidine et un ADN méthyltransférase. Décitabine incorporée dans l'ADN à la place de la cytosine peut piéger par covalence la ADN méthyltransférase dans l'ADN, provoquant une inhibition irréversible de l'enzyme. Décitabine induit un arrêt cellulaire G2/M et l'apoptose cellulaire. Décitabine a une activité puissante anticancéreuse.

Decitabin (5-Aza-2'-Desoxycytidin) ist ein deoxycytidine analogue antimetabolite und DNA methyltransferase-Inhibitor. Decitabin wird anstelle von Cytosin in die DNA eingebaut und kann die DNA methyltransferase kovalent an die DNA binden, was zu einer irreversiblen Hemmung des Enzyms führt. Decitabin induziert den G2/M-Anhalt der Zelle und die apoptosis. Decitabin hat eine starke krebsbekämpfende Wirkung.

Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.

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Decitabine Chemical Structure

Decitabine Chemical Structure

CAS No. : 2353-33-5

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Solid + Solvent
10 mM * 1 mL in DMSO
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Customer Review

Based on 93 publication(s) in Google Scholar

Top Publications Citing Use of Products

79 Publications Citing Use of MCE Decitabine

RT-PCR
WB
Proliferation Assay
IF

    Decitabine purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2022 Mar 29;2022:2371807.  [Abstract]

    The mRNA expression of GSDME is detected using RT-PCR after treatment with different concentrations of Decitabine for 3 days (the cells were centrifuged, and decitabine is replaced every day).

    Decitabine purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2022 Mar 29;2022:2371807.  [Abstract]

    The protein level of GSDME in cells is quantitatively analysed by western blot in Y79 and WERI-RB-1 cells after Decitabine (2 nM; 3 days) treatment.

    Decitabine purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2022 Mar 29;2022:2371807.  [Abstract]

    The protein level of GSDME in cells is detected using immunofluorescence in Y79 and WERI-RB-1 cells after Decitabine (2 nM; 3 days) treatment.

    Decitabine purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2022 Mar 29;2022:2371807.  [Abstract]

    The toxicity of decitabine to Y79 and WERI-RB-1 cells is detected by CCK-8 assay at different concentrations of Decitabine.

    Decitabine purchased from MedChemExpress. Usage Cited in: Theranostics. 2021 Mar 20;11(11):5605-5619.  [Abstract]

    The mRNA levels of PCK2 in RCC cell lines after 5-AZA treatment. PCK2 protein expression in RCC cell lines after 5-AZA treatment.

    Decitabine purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 May 24;e13072.  [Abstract]

    The indicated HSCs are subjected to DNMTs inhibitor (5‐azadC, 2 μM), G9a inhibitor (UNC0642, 2 μM) and pan‐HDAC inhibitor (ITF‐2357, 100 nM) for 48 h, or EZH2 inhibitor (EPZ‐6438, 10 μM) for 72h. KLF14 expression is measured by Western blotting analyses.

    Decitabine purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 May 24;e13072.  [Abstract]

    The indicated HSCs are subjected to DNMTs inhibitor (5‐azadC, 2 μM), G9a inhibitor (UNC0642, 2 μM) and pan‐HDAC inhibitor (ITF‐2357, 100 nM) for 48 h, or EZH2 inhibitor (EPZ‐6438, 10 μM) for 72h. KLF14 expression is measured by RT‐qPCR.

    Decitabine purchased from MedChemExpress. Usage Cited in: Prog Neurobiol. 2021 Feb 23;102028.  [Abstract]

    The TF changes induced by DNMT3L in these cells are not affected with Decitabine (10 µM; for 24 hours) treatment in most genes tested, except NEUROD2 and NEUROG2 as shown by qRTPCR.

    Decitabine purchased from MedChemExpress. Usage Cited in: Oncogene. 2020 Aug;39(33):5507-5519.  [Abstract]

    Quantitative real-time PCR analysis of CDH13 expression after 5 μM Decitabine treatment.

    Decitabine purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2020 Dec;140(12):2442-2454.e5.  [Abstract]

    In EZH2 mutant cells, after six days of drug treatment with both GSK126 and 0.5 μM Decitabine, Significant upregulation of RASSF5, EPAS1, ITGB2, and NDRG1 target gene expression is seen in EZH2 mutant cell lines.

    Decitabine purchased from MedChemExpress. Usage Cited in: J Invest Dermatol. 2020 Dec;140(12):2442-2454.e5.  [Abstract]

    In EZH2 mutant cells, after six days of drug treatment with both GSK126 and 0.5 μM Decitabine, Western blots shows complete elimination of H3K37me3 with reductions in DNMT1A, DNMT3A, and DNMT3B.

    Decitabine purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2019 Oct;78(10):1420-1429.  [Abstract]

    Western blot of PPARγ, MMP13, Aamts5, Aggrecan and Collagen2 from Sham, DMM and 5Aza-treated mouse joint tissues ( (0.35 mg/kg; intraperitoneal injection daily; 10 weeks).

    Decitabine purchased from MedChemExpress. Usage Cited in: Ann Rheum Dis. 2019 Oct;78(10):1420-1429.  [Abstract]

    Western blot of PPARγ from mouse chondrocytes treated with IL-1β (10 ng/mL) for 24 hours in absence or presence 5Aza of various doses (0, 1, 5 and 10 µM).

    Decitabine purchased from MedChemExpress. Usage Cited in: J Allergy Clin Immunol. 2019 Jun;143(6):2038-2051.e12.  [Abstract]

    Naive CD41 T cells are stimulated with anti-CD3/CD28 in the presence of mock stimulant or Decitabine (5-aza-29-deoxycytidine; 1 µM). Real-time PCR analysis of Il4 and Il13 mRNA after 24 hours of stimulation and IL-4 and IL-13 concentrations in culture supernatants after 72 hours of stimulation are measured.

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    Description

    Decitabine (NSC 127716) is an orally active deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity[1][2].

    IC50 & Target[5]

    DNMT1

     

    DNMT3A

     

    DNMT3B

     

    In Vitro

    Decitabine treatment significantly inhibits cell growth of SNU719, NCC24 and KATOIII 96 hours after exposure to decitabine. Decitabine induces G2/M arrest and apoptosis in EBVaGC, inhibits invasion ability, and up-regulates E-cadherin expression for EBVaGC[1].
    ? Only high concentrations (10 μM) Decitabine (0.1-1 μM; 24-72 hours) results in a G2 phase arrest, which is accompanied by a reduction of cells in G1 phase[3].
    ? Decitabine up-regulates DCTPP1 and dUTPase expression in HeLa cells[4].

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

    Cell Cycle Analysis[1]

    Cell Line: HCT116 cells
    Concentration: 0.1, 1, 10 µM
    Incubation Time: 24, 48, 72 hours
    Result: Only high drug concentrations (10 µM) resulted in a G2 phase arrest, which was accompanied by a reduction of cells in G1 phase.
    In Vivo

    Decitabine (1.0 mg/kg, p.o.) in combination with tetrahydrouridine (THU) causes severe toxicity occurs in female CD-1 mice, and results in an increased sensitivity to decitabine toxicity correlating with decitabine plasma levels[5].
    ? Decitabine (1.0 mg/kg; i.p.; once daily for 5 consecutive days) leads to regression of EL4 tumors established in C57BL/6 Mice[7].

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

    Animal Model: C57BL/6 mice (bearing EL4 cells)[6]
    Dosage: 1.0 mg/kg
    Administration: Intraperitoneal injection; once daily for 5 consecutive days
    Result: Caused continuous tumor regression even after Decitabine treatment was stopped.
    Clinical Trial
    Molecular Weight

    228.21

    Formula

    C8H12N4O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O[C@H]1C[C@H](N2C(N=C(N)N=C2)=O)O[C@@H]1CO

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, protect from light

    *In solvent : -80°C, 1 years; -20°C, 6 months (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (219.10 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 20 mg/mL (87.64 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.3819 mL 21.9096 mL 43.8193 mL
    5 mM 0.8764 mL 4.3819 mL 8.7639 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, 1 years; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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 (10.95 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 (10.95 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 10 mg/mL (43.82 mM); Clear solution; Need ultrasonic

    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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.97%

    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, 1 years; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 4.3819 mL 21.9096 mL 43.8193 mL 109.5482 mL
    5 mM 0.8764 mL 4.3819 mL 8.7639 mL 21.9096 mL
    10 mM 0.4382 mL 2.1910 mL 4.3819 mL 10.9548 mL
    15 mM 0.2921 mL 1.4606 mL 2.9213 mL 7.3032 mL
    20 mM 0.2191 mL 1.0955 mL 2.1910 mL 5.4774 mL
    25 mM 0.1753 mL 0.8764 mL 1.7528 mL 4.3819 mL
    30 mM 0.1461 mL 0.7303 mL 1.4606 mL 3.6516 mL
    40 mM 0.1095 mL 0.5477 mL 1.0955 mL 2.7387 mL
    50 mM 0.0876 mL 0.4382 mL 0.8764 mL 2.1910 mL
    60 mM 0.0730 mL 0.3652 mL 0.7303 mL 1.8258 mL
    80 mM 0.0548 mL 0.2739 mL 0.5477 mL 1.3694 mL
    DMSO 100 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0955 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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      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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