2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. JIB-04

JIB-04 是 Jumonji 组蛋白去甲基酶 (Jumonji histone demethylase) 广谱抑制剂，能抑制 JARID1A，JMJD2E，JMJD3，JMJD2A，JMJD2B，JMJD2C 和 JMJD2D 的活性，其 IC50 值分别为 230，340，855，445，435，1100 和 290 nM。

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JIB-04 Chemical Structure

JIB-04 Chemical Structure

CAS No. : 199596-05-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥336
In-stock
1 mg ￥229
In-stock
5 mg ￥495
In-stock
10 mg ￥700
In-stock
25 mg ￥1204
In-stock
50 mg ￥1800
In-stock
100 mg ￥2880
In-stock
200 mg ￥4413
In-stock
500 mg 现货 询价
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of JIB-04:

JIB-04 相关抗体

Top Publications Citing Use of Products

    JIB-04 purchased from MCE. Usage Cited in: J Recept Signal Transduct Res. 2020 Aug;40(4):339-347.  [Abstract]

    JIB-04 blocks Ang II-induced cardiomyocyte fibrotic markers expression. H9c2 cells were pretreated with JIB-04 (0, 2.5, 5, and 10 lM) and then incubated with Ang II (1 lM) for 24 h. The fibrotic markers CTGF and TGF-β are detected by RT-qPCR.

    JIB-04 purchased from MCE. Usage Cited in: J Recept Signal Transduct Res. 2020 Aug;40(4):339-347.  [Abstract]

    JIB-04 blocks Ang II-induced cardiomyocyte hypertrophic markers expression. H9c2 cells are pretreated with JIB-04 (0, 2.5, 5, and 10 lM) and then incubated with Ang II (1 lM) for 24 h. The hypertrophic markers ANP and BNP are detected by RT-qPCR.

    JIB-04 purchased from MCE. Usage Cited in: J Recept Signal Transduct Res. 2020 Aug;40(4):339-347.  [Abstract]

    JIB-04 blocks Ang II-induced cardiomyocyte hypertrophic markers expression. H9c2 cells are pretreated with JIB-04 (0, 2.5, 5, and 10 lM) and then incubated with Ang II (1 lM) for 24 h. The hypertrophic markers a/b-MyHC and SKA are detected by RT-qPCR.

    JIB-04 purchased from MCE. Usage Cited in: J Recept Signal Transduct Res. 2020 Aug;40(4):339-347.  [Abstract]

    JIB-04 blocks Ang II-induced cardiomyocyte fibrotic markers expression. H9c2 cells were pretreated with JIB-04 (0, 2.5, 5, and 10 lM) and then incubated with Ang II (1 lM) for 24 h. The fibrotic markers Collagen I and Collagen IV are detected by RT-qPCR.

    查看 Histone Demethylase 亚型特异性产品:

    查看所有亚型
    KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.

    IC50 & Target

    KDM4

     

    KDM6

     

    KDM5

     

    体外研究
    (In Vitro)

    JIB-04 is consistently selective for cancer vs. normal cells, demonstrated by the higher sensitivity of lung and prostate cancer lines (with IC50?as low as 10 nM) compared to HBECs and PrSCs/PrECs. JIB-04 inhibits cellular Jumonji demethylase activity, and Jumonji levels affect JIB-04 action in cells[1]. JIB-04 significantly inhibits the proliferation of GB cell lines and stem-enriched cultures. JIB-04 exerts its maximal inhibitory activity against KDM5A, and modulates the expression of genes involved in the control of cancer cell growth and leads to hypermethylation of H3K4. Furthermore, JIB-04 (2500 nM) activates the autophagy and apoptotic pathways and inactivates PI3K. JIB-04 also cooperates with TMZ in killing GB cells[2].

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

    JIB-04 相关抗体:
    体内研究
    (In Vivo)

    JIB-04 results in a significant reduction in cancer-induced death rates in mice, prolonging survival[1]. JIB-04 (60, 40 and 20 mg/kg, i.p.) reaches bioactive concentration in the brain of the mice. The orthotopic GB xenograft model shows a trend toward longer survival in JIB-04-treated mice with an Hazard Ratio of 0.5[2].

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

    308.76

    Formula

    C17H13ClN4
    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    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： 

    DMSO 中的溶解度 : 50 mg/mL (161.94 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    Ethanol 中的溶解度 : 2 mg/mL (6.48 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 3.2387 mL 16.1935 mL 32.3871 mL
    5 mM 0.6477 mL 3.2387 mL 6.4774 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。

    • 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：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.74 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% Corn Oil

      Solubility: ≥ 1.25 mg/mL (4.05 mM); 澄清溶液

      此方案可获得 ≥ 1.25 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

      以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    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： 0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (32.39 mM); 悬浊液; 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
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 98.29%

    COA (287 KB) LCMS (94 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    For cell viability assays, cells are plated at 1500-3000 cells/well in 96 well plates and treated the next day with increasing doses of compound over 4 days and their viability assessed by standard MTS assays using Promega’s Cell Titer or Cell Titer-Glo reagents. Absorbance at 490 nm and 650 nm or luminescence is measured by a Spectra Max or a FlouroStar Omega plate reader. Data are normalized to the untreated controls (100% viability). Each cell line is tested in 2-5 independent assays, each containing 4-8 replicates. IC50 values are calculated using DIVISA, a high-throughput software, developed in house, for storing and analyzing drug sensitivity assays. Dose-response curves are plotted using a non-linear regression model and IC50s are determined from the fitted curves. The average IC50 derived from 2-5 independent assays, each containing 4-8 replicates is reported.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    For xenografts, 4-6 week old female nude mice are housed under standard conditions in a clean facility at UTSW. Two million H358 cells or five million A549 cells are injected subcutaneously and allowed to grow for 2-3 weeks with monitoring. When tumors reach appr 200 mm3, therapy is started in weight and tumor volume matched pairs (n=7 for each treatment group for each cell line). Drug or vehicle is administered by inter-peritoneal injection in 10% DMSO 90% sesame oil 2 to 3 times weekly for 5 weeks at 110 mg/kg to all mice harboring H358 xenografts or 3 times per week by gavage in 12.5% Cremophor EL, 12.5% DMSO as an aqueous suspension at 55 mg/kg to mice harboring A549 xenografts. Tumor volumes are monitored twice weekly by caliper measurements. Animals are weighed and observed during the five weeks of treatment. At the end point, mice are euthanized by CO2 asphyxiation and cervical dislocation, and blood, tumors and major organs collected and weighed. Paired, unequal variance, one-tailed t-tests are performed across treatment groups using Excel software.

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

    JIB-04 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
    Ethanol / DMSO 1 mM 3.2387 mL 16.1935 mL 32.3871 mL 80.9677 mL
    5 mM 0.6477 mL 3.2387 mL 6.4774 mL 16.1935 mL
    DMSO 10 mM 0.3239 mL 1.6194 mL 3.2387 mL 8.0968 mL
    15 mM 0.2159 mL 1.0796 mL 2.1591 mL 5.3978 mL
    20 mM 0.1619 mL 0.8097 mL 1.6194 mL 4.0484 mL
    25 mM 0.1295 mL 0.6477 mL 1.2955 mL 3.2387 mL
    30 mM 0.1080 mL 0.5398 mL 1.0796 mL 2.6989 mL
    40 mM 0.0810 mL 0.4048 mL 0.8097 mL 2.0242 mL
    50 mM 0.0648 mL 0.3239 mL 0.6477 mL 1.6194 mL
    60 mM 0.0540 mL 0.2699 mL 0.5398 mL 1.3495 mL
    80 mM 0.0405 mL 0.2024 mL 0.4048 mL 1.0121 mL
    100 mM 0.0324 mL 0.1619 mL 0.3239 mL 0.8097 mL
    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:

    JIB-04199596-05-9JIB04JIB 04Histone DemethylaseApoptosisInhibitorinhibitorinhibit

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