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  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鹽酸鹽; DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride)

目錄號(hào): HY-12186 純度: 99.88%
COA 產(chǎn)品使用指南

3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) 是一種有效的組蛋白甲基轉(zhuǎn)移酶 (EZH2) 抑制劑。3-Deazaneplanocin A hydrochloride 是一種有效的 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制劑。3-Deazaneplanocin A hydrochloride 還具有抗正痘病毒 (orthopoxvirus) 和抗天花病毒活性。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

3-Deazaneplanocin A hydrochloride Chemical Structure

3-Deazaneplanocin A hydrochloride Chemical Structure

CAS No. : 120964-45-6

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規(guī)格 價(jià)格 是否有貨 數(shù)量
1 mg ￥900
In-stock
5 mg ￥3100
In-stock
10 mg ￥4900
In-stock
25 mg 現(xiàn)貨 詢(xún)價(jià)
50 mg 現(xiàn)貨 詢(xún)價(jià)
100 mg 現(xiàn)貨 詢(xún)價(jià)
200 mg   詢(xún)價(jià)  
500 mg   詢(xún)價(jià)  

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Customer Review

Other Forms of 3-Deazaneplanocin A hydrochloride:

    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).

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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

     

    體外研究
    (In Vitro)

    3-Deazaneplanocin A hydrochloride (DZNep) hydrochloride 是一種有效的組蛋白甲基轉(zhuǎn)移酶 EZH2 抑制劑。用 3-Deazaneplanocin A hydrochloride (1.0 μM) 處理 OCI-AML3 細(xì)胞導(dǎo)致細(xì)胞在 G0/G1 期的積累顯著增加 (58.5%) 伴隨細(xì)胞周期S期 (35.2%) 和G2/M期 (6.3%) 細(xì)胞數(shù)減少 (P<0.05)。用 3-Deazaneplanocin A hydrochloride (200 nM 至 2.0 μM) 處理 48 小時(shí)，劑量依賴(lài)性抑制 OCI-AML3 和 HL-60 細(xì)胞的集落生長(zhǎng)[1]。
    3-Deazaneplanocin A hydrochloride (DZNep) 鹽酸鹽可降低 EZH2 的表達(dá)，尤其是在 72 小時(shí)后 (例如 PANC-1、MIA-PaCa-2 和 LPc006 細(xì)胞中的 EZH2 分別降低 48%、32% 和 36%)[2]。
    3-Deazaneplanocin A hydrochloride (DZNep) hydrochloride 在 PANC-1 細(xì)胞中表現(xiàn)出最小的生長(zhǎng)抑制。超過(guò) 50% 的這些細(xì)胞在最高濃度 (20 μM) 暴露后仍在生長(zhǎng)。MIA-PaCa-2 和 LPc006 細(xì)胞更為敏感，IC0 值分別為 1.0±0.3 和 0.10±0.03 μM[2]。3-Deazaneplanocin A hydrochloride (DZNep) hydrochloride 劑量依賴(lài)性地抑制 NSCLC 細(xì)胞系的細(xì)胞增殖，IC0 值范圍為 0.08 至 0.24 μM[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    如果用 3-Deazaneplanocin A hydrochloride (DZNep) 和 LBH589 (PS) 處理，與用 PS、3-Deazaneplanocin A hydrochloride 處理相比，由于 HL-60 細(xì)胞而患有急性髓性白血病 (AML) 的 NOD/SCID 小鼠的存活率明顯更高[1]。用生理鹽水處理的大鼠的體重以時(shí)間依賴(lài)性方式逐漸增加 (平均增長(zhǎng)率=每天3.19%)。給藥 20 mg/kg 3-Deazaneplanocin A hydrochloride (DZNep) 不僅在處理后的前三天顯著降低大鼠的相對(duì)體重 (-2.0%、-4.9% 和-1.2%)，而且從給藥后第 4 天開(kāi)始，每天的體重增長(zhǎng)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 號(hào)
    性狀

    固體

    顏色

    White to light brown

    中文名稱(chēng)

    3-去氮腺嘌呤A鹽酸鹽
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)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)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    H2O 中的溶解度 : 50 mg/mL (167.38 mM; 超聲助溶)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： PBS

      Solubility: 50 mg/mL (167.38 mM); 澄清溶液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.98%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    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.

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    產(chǎn)品名稱(chēng)：
    3-Deazaneplanocin A hydrochloride
    目錄號(hào)：
    HY-12186
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