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

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.

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CAS 番号 : 199596-05-9

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 60 在庫あり
Solution
10 mM * 1 mL in DMSO USD 60 在庫あり
Solid
5 mg $55 在庫あり
10 mg $88 在庫あり
50 mg $220 在庫あり
100 mg $385 在庫あり
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カスタマーレビュー

Based on 20 publication(s) in Google Scholar

Other Forms of JIB-04:

JIB-04 関連抗体

Top Publications Citing Use of Products

    JIB-04 purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

    Histone Demethylase 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
    KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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

     

    Cellular Effect
    Cell Line Type Value Description References
    A549 EC50
    <0.01 μM
    Compound: 47
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability
    		[PMID: 34555614]
    MCF7 GI50
    0.022 μM
    Compound: 48; JIB-04
    Cytotoxicity against human MCF7 cells assessed as cell growth inhibition
    Cytotoxicity against human MCF7 cells assessed as cell growth inhibition
    		[PMID: 32883639]
    MCF7 GI50
    22 nM
    Compound: 9
    Antiproliferative activity against human MCF7 cells assessed as growth inhibition
    Antiproliferative activity against human MCF7 cells assessed as growth inhibition
    		[PMID: 30343192]
    MDA-MB-231 GI50
    0.3 μM
    Compound: 48; JIB-04
    Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition
    Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition
    		[PMID: 32883639]
    MDA-MB-231 GI50
    300 nM
    Compound: 9
    Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition
    Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition
    		[PMID: 30343192]
    U2OS CC50
    ~ 10 μM
    Compound: 14; JIB-04
    Cytotoxicity against human U2OS cells expressing tetracyclin/Dox-inducible N-terminal 3xFLAG/C-terminal GFP tagged human TET1 catalytic domain (1481 to 2136 residues) assessed as effect on nuclear count by DAPI staining based analysis
    Cytotoxicity against human U2OS cells expressing tetracyclin/Dox-inducible N-terminal 3xFLAG/C-terminal GFP tagged human TET1 catalytic domain (1481 to 2136 residues) assessed as effect on nuclear count by DAPI staining based analysis
    		[PMID: 38294854]
    体外実験

    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].

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

    JIB-04 関連抗体
    体内実験

    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].

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

    308.76

    分子式

    C17H13ClN4
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    ClC1=CN=C(N/N=C(C2=CC=CC=C2)/C3=NC=CC=C3)C=C1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (161.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 2 mg/mL (6.48 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.3239 mL 1.6194 mL 3.2387 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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

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    Volume
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    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.74 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 1.25 mg/mL (4.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (32.39 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 98.63%

    COA (249 KB) HNMR (231 KB) RP-HPLC (260 KB) MS (71 KB)

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

    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]

    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.

    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. 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
    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
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    JIB-04 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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

    質量   濃度   体積   分子量 *
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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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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    製品名:
    JIB-04
    製品番号:
    HY-13953
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