2. Epigenetics Metabolic Enzyme/Protease Anti-infection
  3. Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus
  4. 3-Deazaneplanocin A hydrochloride

3-Deazaneplanocin A (hydrochloride)  (Synonyms: DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride; 3-デアザネプラノシンA塩酸塩)

製品番号: HY-12186 純度: 99.90%
COA 取扱説明書 Technical Support

3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities.

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CAS 番号 : 120964-45-6

容量 価格（税別） 在庫状況 数量
1 mg $108 在庫あり
5 mg $350 在庫あり
10 mg $550 在庫あり
25 mg $980 在庫あり
50 mg $1500 在庫あり
100 mg $2400 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 35 publication(s) in Google Scholar

Other Forms of 3-Deazaneplanocin A hydrochloride:

3-Deazaneplanocin A (hydrochloride) 関連抗体

Top Publications Citing Use of Products

顧客検証

RT-PCR
Cell Proliferation/Viability Assay
In Vivo Efficacy Study
IHC
WB
IP

    3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Med. 2026 Jan 5;223(1):e20250603.  [Abstract]

    The levels of p-RIPK1(S166), CC8, CC3, and ADK were detected by Western blotting using DZNep (3-Deazaneplanocin A: 10 μM; 12 h).

    3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12.  [Abstract]

    Immunoblot of MYCN in the presence of various EZH2 inhibitors. Kelly cells were respectively treated with 5 μM of 3-Deazaneplanocin A hydrochloride, GSK126 or EPZ6438 for 48 h before subjected to immunoblotting.

    3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12.  [Abstract]

    Proliferation of Kelly cells was measured upon administration of 5 μM of 3-Deazaneplanocin A hydrochloride (5 days), GSK126 or EPZ6438.

    3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12.  [Abstract]

    Proliferation of Kelly cells was measured upon 3-Deazaneplanocin A hydrochloride treatment (5 μM, 5 days) with or without ectopic expression of the MYCN T50A.

    3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12.  [Abstract]

    Kelly xenografts were subjected to 3-Deazaneplanocin A hydrochloride (0.75-6 mg/kg) or GSK126 treatments at the indicated doses. Images of subcutaneous tumors (n = 3 per group) under various treatments are shown.

    3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12.  [Abstract]

    Kaplan-Meier survival plot of tumor-bearing TH-MYCN+/+ mice treated with 3-Deazaneplanocin A hydrochloride (3 mg/kg) or GSK126 (50 mg/kg). Significant difference between the 3-Deazaneplanocin A hydrochloride-treated group versus control was determined by log-rank test.

    3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Jan 10;13(1):12.  [Abstract]

    Immunohistochemistry detection of Ezh2, MYCN, and H3K27me3 upon 3-Deazaneplanocin A hydrochloride (3 mg/kg) or GSK126 treatment.

    3-Deazaneplanocin A hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 23;12(1):1237.  [Abstract]

    BT-R cells were treated with the specified compound 3-Deazaneplanocin A (DZNEP: 5 μM) for 48 hours. Then, the expression level of JAK2 mRNA was determined by RT-PCR and normalized to the expression level in the vector-treated cells.

    3-Deazaneplanocin A hydrochloride 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 hydrochloride 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 hydrochloride 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).

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

    MEF cells transfected or untransfected with siAdk were stimulated with Flag-TNFα (10 ng/ml) for 15 min, followed by pretreatment with DZNep (3-Deazaneplanocin A: 10 μM), 5-ITu (20 μM), or adenosine (1 mM) for 1 h. Anti-Flag antibody was used to immunoprecipitate complex I, and the levels of RIPK1 R606me2s in complex I or whole-cell lysates were determined by Western blotting.

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

    HEK293T cells were co-transfected with HA-tagged RIPK1-DD and Flag-tagged RIPK1-DD expression plasmids for 24 hours. Cells were then treated with DZNep (3-Deazaneplanocin A: 10 μM), siADK, or adenosine (1 mM). The interaction between Flag-tagged and HA-tagged proteins was detected by immunoprecipitation and Western blotting.

    Histone Methyltransferase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor[1][2]. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor[6]. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities[7].

    IC50 & Target[1]

    EZH2

     

    体外実験

    3-Deazaneplanocin A (DZNep) hydrochloride 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 (DZNep) hydrochloride 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 (DZNep) hydrochloride 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±0.3 and 0.10±0.03 μM, respectively[2]. 3-Deazaneplanocin A (DZNep) hydrochloride 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.

    3-Deazaneplanocin A (hydrochloride) 関連抗体
    体内実験

    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 (DZNep) and LBH589 (PS) compare to treatment with PS, 3-Deazaneplanocin A[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 (DZNep) 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.
    分子量

    298.73

    分子式

    C12H15ClN4O3
    CAS 番号
    Appearance

    Solid

    Color

    White to light brown

    SMILES

    O[C@@H]1[C@H](O)C(CO)=C[C@H]1N2C=NC3=C2C=CN=C3N.[H]Cl
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    H2O : 50 mg/mL (167.38 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3475 mL 16.7375 mL 33.4750 mL
    5 mM 0.6695 mL 3.3475 mL 6.6950 mL
    10 mM 0.3348 mL 1.6738 mL 3.3475 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 (sealed storage, away from moisture). 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.

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    一般には略語で表示されます：C1V1 = C2V2

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    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: 50 mg/mL (167.38 mM); Clear solution; Need ultrasonic

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    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).
    純度とドキュメンテーション

    純度: 99.98%

    COA (255 KB) RP-HPLC (194 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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, 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].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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) DZNep 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 DZNep is determined, depending on the following endpoint parameters obtained.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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 (sealed storage, away from moisture). 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 3.3475 mL 16.7375 mL 33.4750 mL 83.6876 mL
    5 mM 0.6695 mL 3.3475 mL 6.6950 mL 16.7375 mL
    10 mM 0.3348 mL 1.6738 mL 3.3475 mL 8.3688 mL
    15 mM 0.2232 mL 1.1158 mL 2.2317 mL 5.5792 mL
    20 mM 0.1674 mL 0.8369 mL 1.6738 mL 4.1844 mL
    25 mM 0.1339 mL 0.6695 mL 1.3390 mL 3.3475 mL
    30 mM 0.1116 mL 0.5579 mL 1.1158 mL 2.7896 mL
    40 mM 0.0837 mL 0.4184 mL 0.8369 mL 2.0922 mL
    50 mM 0.0670 mL 0.3348 mL 0.6695 mL 1.6738 mL
    60 mM 0.0558 mL 0.2790 mL 0.5579 mL 1.3948 mL
    80 mM 0.0418 mL 0.2092 mL 0.4184 mL 1.0461 mL
    100 mM 0.0335 mL 0.1674 mL 0.3348 mL 0.8369 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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    3-Deazaneplanocin A hydrochloride Related Classifications

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    Keywords:

    3-Deazaneplanocin A120964-45-6DZNepNSC 6179893-DeazaneplanocinNSC617989NSC-617989Histone MethyltransferaseS-adenosylhomocysteine hydrolase (SAHH)OrthopoxvirusSAHHInhibitorinhibitorinhibit

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    製品名:
    3-Deazaneplanocin A hydrochloride
    製品番号:
    HY-12186
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