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

3-Deazaneplanocin A hydrochloride  (Synonyms: 3-去氮腺嘌呤A盐酸盐; DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride)

目录号: HY-12186 纯度: 99.88%
COA 产品使用指南

摩尔计算器

3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) 是一种有效的组蛋白甲基转移酶 (EZH2) 抑制剂。3-Deazaneplanocin A hydrochloride 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 hydrochloride 还具有抗正痘病毒 (orthopoxvirus) 和抗天花病毒活性。

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3-Deazaneplanocin A hydrochloride Chemical Structure

3-Deazaneplanocin A hydrochloride Chemical Structure

CAS No. : 120964-45-6

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1 mg ￥900
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5 mg ￥3100
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10 mg ￥4900
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Customer Review

Other Forms of 3-Deazaneplanocin A hydrochloride:

3-Deazaneplanocin A hydrochloride 相关抗体

Top Publications Citing Use of Products

    3-Deazaneplanocin A hydrochloride 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 hydrochloride 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 hydrochloride 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 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

     

    体外研究
    (In Vitro)

    3-Deazaneplanocin A hydrochloride (DZNep) hydrochloride 是一种有效的组蛋白甲基转移酶 EZH2 抑制剂。用 3-Deazaneplanocin A hydrochloride (1.0 μM) 处理 OCI-AML3 细胞导致细胞在 G0/G1 期的积累显著增加 (58.5%) 伴随细胞周期S期 (35.2%) 和G2/M期 (6.3%) 细胞数减少 (P<0.05)。用 3-Deazaneplanocin A hydrochloride (200 nM 至 2.0 μM) 处理 48 小时，剂量依赖性抑制 OCI-AML3 和 HL-60 细胞的集落生长[1]。
    3-Deazaneplanocin A hydrochloride (DZNep) 盐酸盐可降低 EZH2 的表达，尤其是在 72 小时后 (例如 PANC-1、MIA-PaCa-2 和 LPc006 细胞中的 EZH2 分别降低 48%、32% 和 36%)[2]。
    3-Deazaneplanocin A hydrochloride (DZNep) hydrochloride 在 PANC-1 细胞中表现出最小的生长抑制。超过 50% 的这些细胞在最高浓度 (20 μM) 暴露后仍在生长。MIA-PaCa-2 和 LPc006 细胞更为敏感，IC0 值分别为 1.0±0.3 和 0.10±0.03 μM[2]。3-Deazaneplanocin A hydrochloride (DZNep) hydrochloride 剂量依赖性地抑制 NSCLC 细胞系的细胞增殖，IC0 值范围为 0.08 至 0.24 μM[3]。

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

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

    如果用 3-Deazaneplanocin A hydrochloride (DZNep) 和 LBH589 (PS) 处理，与用 PS、3-Deazaneplanocin A hydrochloride 处理相比，由于 HL-60 细胞而患有急性髓性白血病 (AML) 的 NOD/SCID 小鼠的存活率明显更高[1]。用生理盐水处理的大鼠的体重以时间依赖性方式逐渐增加 (平均增长率=每天3.19%)。给药 20 mg/kg 3-Deazaneplanocin A hydrochloride (DZNep) 不仅在处理后的前三天显著降低大鼠的相对体重 (-2.0%、-4.9% 和-1.2%)，而且从给药后第 4 天开始，每天的体重增长率也被抑制到 2.6%[4]。

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

    298.73

    Formula

    C12H15ClN4O3
    CAS 号
    性状

    固体

    颜色

    White to light brown

    中文名称

    3-去氮腺嘌呤A盐酸盐
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

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

    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : 50 mg/mL (167.38 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 3.3475 mL 16.7375 mL 33.4750 mL
    5 mM 0.6695 mL 3.3475 mL 6.6950 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    * 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，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： PBS

      Solubility: 50 mg/mL (167.38 mM); 澄清溶液; 超声助溶

    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: 99.98%

    COA (298 KB) RP-HPLC (194 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, 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) 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.

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

    3-Deazaneplanocin A hydrochloride 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 3.3475 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

    * 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 A120964-45-6DZNepNSC 6179893-Deazaneplanocin3-去氮腺嘌呤A盐酸盐NSC617989NSC-617989Histone MethyltransferaseOrthopoxvirusInhibitorinhibitorinhibit

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