1. Epigenetics Anti-infection
  2. Histone Methyltransferase Orthopoxvirus
  3. 3-Deazaneplanocin A

3-Deazaneplanocin A  (Synonyms: DZNep; 3-Deazaneplanocin)

Cat. No.: HY-10442 Purity: 99.97%
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3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity.

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

3-Deazaneplanocin A Chemical Structure

3-Deazaneplanocin A Chemical Structure

CAS No. : 102052-95-9

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Customer Review

Based on 25 publication(s) in Google Scholar

Other Forms of 3-Deazaneplanocin A:

Top Publications Citing Use of Products

    3-Deazaneplanocin A purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Oct 23;11(10):906.  [Abstract]

    Western blot analysis of EZH2, ZIC4, H3K27me3, and β-actin in HepG2 without or with DZNep (10 μM) treatment for 72 h.

    3-Deazaneplanocin A purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):2061-2067.  [Abstract]

    Western blot analysis of H3K27me3, bcatenin and RUNX2 protein accumulation in hDFSCs transfected by EZH2-siRNA and treated with DMSO or DZNep after 3 days of osteogenic induction.

    3-Deazaneplanocin A purchased from MedChemExpress. Usage Cited in: J Am Soc Nephrol. 2016 Jul;27(7):2021-34.  [Abstract]

    Immunoblotting mouse podocytes for (A) EZH2 and (B) H3K27me3 under control conditions or after DZNep treatment for 48 hours. Initial immunoblotting experiments confirm the presence of EZH2 protein in cultured mouse podocytes and its depletion with DZNep (A) together with a concurrent reduction in H3K27me3 levels (B).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor[1][2]. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity[6][7].

    IC50 & Target

    EZH2[1]

    In Vitro

    3-Deazaneplanocin A is a potent histone methyltransferase EZH2 inhibitor. Treatment of OCI-AML3 cells with 3-Deazaneplanocin A (1.0 μM) results in a significant increase in accumulation of cells in the G0/G1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G2/M phases (6.3%) of the cell cycle (P<0.05). Treatment with 3-Deazaneplanocin A (200 nM to 2.0 μM) for 48 hours, dose dependently, inhibits colony growth of OCI-AML3 and HL-60 cells[1]. 3-Deazaneplanocin A reduces the expression of EZH2, especially after 72 hours (e.g. 48%, 32% and 36% reduction of EZH2 in PANC-1, MIA-PaCa-2 and LPc006 cells, respectively)[2]. 3-Deazaneplanocin A shows minimal growth inhibition in PANC-1 cells. More than 50% of these cells are still growing after exposure at the highest concentration (20 μM). MIA-PaCa-2 and LPc006 cells are much more sensitive, with IC0 values of 1±0.3 and 0.1±0.03 μM, respectively[2]. 3-Deazaneplanocin A causes dose-dependent inhibition of cell proliferation of NSCLC cell lines, and the IC0 values range from 0.08 to 0.24 μM[3].

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

    In Vivo

    The survival of NOD/SCID mice with acute myeloid leukemia (AML) due to HL-60 cells is significantly higher, if treated with 3-Deazaneplanocin A and Panobinostat (PS) compare to treatment with PS, 3-Deazaneplanocin A, or vehicle alone (P<0.05). Median survival is as follows: control, 36 days; PS, 42 days; 3-Deazaneplanocin A, 43 days; and 3-Deazaneplanocin A plus PS, 52 days[1]. There is a progressive increase in weight of rats treated with physiological saline in a time-dependent manner (the mean growth rate=3.19% per day). Administration of 20 mg/kg 3-Deazaneplanocin A not only markedly reduces the relative weight of the rats compare to the initial weight (−2.0%, −4.9% and −1.2%) in the first three days post-treatment, but also suppresses the weight growth rate to 2.6% per day from the fourth day onwards post-dose[4].

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

    Molecular Weight

    262.26

    Formula

    C12H14N4O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O[C@@H]1[C@H](O)C(CO)=C[C@H]1N2C=NC3=C2C=CN=C3N

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    H2O : 125 mg/mL (476.63 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.8130 mL 19.0650 mL 38.1301 mL
    5 mM 0.7626 mL 3.8130 mL 7.6260 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

    • Protocol 1

      3-Deazaneplanocin A (DZNep) is prepared in PBS[5].

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    (per animal)

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    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
    References
    Cell Assay
    [1]

    AML HL-60 cells are obtained and maintained. OCI-AML-3 cells are cultured in α minimum essential medium with 10% fetal bovine serum, 1% penicillin/streptomycin, and 1% nonessential amino acids. To analyze synergism between 3-Deazaneplanocin A and PS in inducing apoptosis, cells are treated with 3-Deazaneplanocin A (100-750 nM) and PS (5-20 nM) at a constant ratio for 48 hours. The percentage of apoptotic cells is determined by flow cytometry. The combination index (CI) for each drug combination is obtained by median dose effect of Chou and Talalay, using the CI equation within the commercially available software Calcusyn[1].

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

    Animal Administration
    [1][4]

    Mice[1]
    HL-60 cells (5 million) are injected into the tail vein of female nonobese diabetic/severe combined immunodeficiency (NOD/SCID) mice, and the mice are monitored for 7 days. The following treatments are administered in cohorts of 7 mice for each treatment: vehicle alone, 1 mg/kg 3-Deazaneplanocin A, 10 mg/kg PS, and 3-Deazaneplanocin A plus PS. Treatments are initiated on day 7. 3-Deazaneplanocin A is administered twice per week (Tuesday-Thursday) intraperitoneally for 2 weeks, and then discontinued. PS is administered 3 days per week (Monday, Wednesday, and Friday) for 4 weeks. The survival of mice from the tail vein model is represented with a Kaplan-Meier survival plot.
    Rats[4]
    Male wistar rats are used. The acute toxicity study is carried out to determine the NOAEL of 3-Deazaneplanocin A in rats. In total, 20 rats are divided into 4 groups of five each. Three groups are intravenously administered 20, 15, 10 mg/kg body weight (BW) 3-Deazaneplanocin A solution by the tail vein. The remaining group is given physiological saline (0.9% NaCl saline) as the control group. Then, the NOAEL of free 3-Deazaneplanocin A is determined, depending on the following endpoint parameters obtained.

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 3.8130 mL 19.0650 mL 38.1301 mL 95.3252 mL
    5 mM 0.7626 mL 3.8130 mL 7.6260 mL 19.0650 mL
    10 mM 0.3813 mL 1.9065 mL 3.8130 mL 9.5325 mL
    15 mM 0.2542 mL 1.2710 mL 2.5420 mL 6.3550 mL
    20 mM 0.1907 mL 0.9533 mL 1.9065 mL 4.7663 mL
    25 mM 0.1525 mL 0.7626 mL 1.5252 mL 3.8130 mL
    30 mM 0.1271 mL 0.6355 mL 1.2710 mL 3.1775 mL
    40 mM 0.0953 mL 0.4766 mL 0.9533 mL 2.3831 mL
    50 mM 0.0763 mL 0.3813 mL 0.7626 mL 1.9065 mL
    60 mM 0.0636 mL 0.3178 mL 0.6355 mL 1.5888 mL
    80 mM 0.0477 mL 0.2383 mL 0.4766 mL 1.1916 mL
    100 mM 0.0381 mL 0.1907 mL 0.3813 mL 0.9533 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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