2. Epigenetics Anti-infection
  3. Histone Methyltransferase Orthopoxvirus
  4. 3-Deazaneplanocin A

3-Deazaneplanocin A  (Synonyms: 3-去氮腺嘌呤A; DZNep; 3-Deazaneplanocin)

目录号: HY-10442 纯度: 99.80%
COA 产品使用指南 技术支持

3-Deazaneplanocin A (DZNep) 是一种有效的组蛋白甲基转移酶 (histone methyltransferase，EZH2) 抑制剂。3-Deazaneplanocin A 是一种有效的 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制剂。3-Deazaneplanocin A 具有抗正痘活性。

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3-Deazaneplanocin A Chemical Structure

3-Deazaneplanocin A Chemical Structure

CAS No. : 102052-95-9

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5 mg ￥4500
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Other Forms of 3-Deazaneplanocin A:

3-Deazaneplanocin A 相关抗体

Top Publications Citing Use of Products

    3-Deazaneplanocin A purchased from MCE. 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 MCE. 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 MCE. 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).

    查看 Histone Methyltransferase 亚型特异性产品:

    查看所有亚型
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    1.4 μM
    Compound: 4
    Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    		[PMID: 26010585]
    HCT-116 IC50
    0.26 μM
    Compound: 4
    Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    		[PMID: 26010585]
    MDA-MB-231 IC50
    0.3 μM
    Compound: 4
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    		[PMID: 26010585]
    PC-3 IC50
    9.39 μM
    Compound: 4
    Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    		[PMID: 26010585]
    SK-HEP1 IC50
    0.72 μM
    Compound: 4
    Cytotoxicity against human SKHEP1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human SKHEP1 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    		[PMID: 26010585]
    SNU-638 IC50
    0.91 μM
    Compound: 4
    Cytotoxicity against human SNU638 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human SNU638 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
    		[PMID: 26010585]
    Vero IC50
    > 500 μg/mL
    Compound: 2
    Cytotoxic effect on host cells during stationary phase of virus in vero cell cultures using MTT method
    Cytotoxic effect on host cells during stationary phase of virus in vero cell cultures using MTT method
    		10.1016/S0960-894X(01)80163-3
    Vero IC50
    0.55 μg/mL
    Compound: 2
    Cytotoxic effect on host cells during growth phase of virus in vero cell cultures using MTT method
    Cytotoxic effect on host cells during growth phase of virus in vero cell cultures using MTT method
    		10.1016/S0960-894X(01)80163-3
    体外研究
    (In Vitro)

    3-Deazaneplanocin A 是一种有效的组蛋白甲基转移酶 EZH2 抑制剂。处理 OCI-AML3 细胞 (1.0 μM) 显著增加 G0/G1 期细胞比例 (58.5%) ，伴随 S 期 (35.2%) 和 G2/M 期 (6.3%) 细胞数量减少 (P<0.05) ； (200 nM 至 2.0 μM, 48 小时) 浓度依赖性抑制 OCI-AML3 和 HL-60 细胞的集落生长；减少 EZH2 表达，尤其在 72 小时后显著降低 PANC-1、MIA-PaCa-2 和 LPc006 细胞的 EZH2 表达分别为 48%、32% 和 36%。对 PANC-1 细胞的增殖抑制作用较小，但对 MIA-PaCa-2 和 LPc006 细胞更敏感，IC0 值分别为 1±0.3 和 0.1±0.03 μM；在 NSCLC 细胞系中，IC0 值为 0.08 至 0.24 μM[1][2][3]。

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

    3-Deazaneplanocin A 相关抗体:
    体内研究
    (In Vivo)

    患有由 HL-60 细胞引起的急性髓系白血病 (AML) 的 NOD/SCID 小鼠，如果用 3-Deazaneplanocin A 和 Panobinostat (PS) 治疗，其存活率显著高于仅用 PS、3-Deazaneplanocin A 或载体治疗的小鼠 (P<0.05)。中位存活率如下：对照组，36 天；PS，42 天；3-Deazaneplanocin A，43 天；3-Deazaneplanocin A 加 PS，52 天[1]。用生理盐水治疗的大鼠体重随时间逐渐增加(平均增长率=每天 3.19%)。给予 20 mg/kg 3-Deazaneplanocin A 不仅在治疗后前三天显著降低大鼠的相对体重与初始体重相比(分别降低 2.0%、4.9% 和 1.2%)，而且从服药后第四天起将体重增长率抑制到每天 2.6%[4]。

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

    262.26

    Formula

    C12H14N4O3
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    3-去氮腺嘌呤A
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : 100 mg/mL (381.30 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

    • 方案 一

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

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.97%

    COA (292 KB) HNMR (257 KB) RP-HPLC (184 KB) MS (68 KB)

    产品使用指南 (1538 KB)
    参考文献
    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.
    参考文献

    3-Deazaneplanocin A 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 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

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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.

    Keywords:

    3-Deazaneplanocin A102052-95-9DZNep 3-Deazaneplanocin3-去氮腺嘌呤AHistone MethyltransferaseOrthopoxvirusInhibitorinhibitorinhibit

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