2. Epigenetics
  3. Histone Demethylase
  4. GSK-J1

GSK-J1, a chemical probe, is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.

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CAS 番号 : 1373422-53-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 53 在庫あり
Solution
10 mM * 1 mL in DMSO USD 53 在庫あり
Solid
5 mg $49 在庫あり
10 mg $77 在庫あり
25 mg $127 在庫あり
50 mg $226 在庫あり
100 mg $374 在庫あり
200 mg   お問い合わせ  
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カスタマーレビュー

Based on 17 publication(s) in Google Scholar

Other Forms of GSK-J1:

GSK-J1 関連抗体

Top Publications Citing Use of Products

    GSK-J1 purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2017 Mar 13;10:51.  [Abstract]

    GSK-J1 impaired zebrafish hair cell regeneration. 5 dpf larvae are treated with 400 μM Neomycin for 1 h followed by GSK-J1 exposure for 24 in the presence of BrdU. GSK-J1 significantly reduces the numbers of myosinVI-positive (green) hair cells and BrdU-positive (red) replicating cells.

    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

    GSK-J1, a chemical probe, is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.

    IC50 & Target

    KDM6

     

    Cellular Effect
    Cell Line Type Value Description References
    HepG2 IC50
    39.75 μM
    Compound: GSK-J1
    Antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 36931124]
    MCF7 IC50
    33.67 μM
    Compound: GSK-J1
    Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 36931124]
    MGC-803 IC50
    29.31 μM
    Compound: GSK-J1
    Antitumor activity against human MGC-803 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antitumor activity against human MGC-803 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 36931124]
    PC-3 IC50
    20.33 μM
    Compound: GSK-J1
    Antitumor activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antitumor activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    		[PMID: 36931124]
    Sf9 IC50
    16 nM
    Compound: 4; GSK-J1
    Inhibition of C-terminal FLAG-tagged human KDM6B expressed in expressed in Sf9 cells pre-incubated for 4 hrs before substrate addition and measured after 1 hr by AlphaScreen assay
    Inhibition of C-terminal FLAG-tagged human KDM6B expressed in expressed in Sf9 cells pre-incubated for 4 hrs before substrate addition and measured after 1 hr by AlphaScreen assay
    		[PMID: 30928196]
    体外実験

    GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner[1]. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1 mM α-ketoglutarate, with IC50 of 11 μM and 94 μM, respectively[3].

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

    GSK-J1 関連抗体
    分子量

    389.45

    分子式

    C22H23N5O2
    CAS 番号
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    OC(CCNC1=NC(C2=NC=CC=C2)=NC(N(CC3)CCC4=C3C=CC=C4)=C1)=O
    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 (128.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5677 mL 12.8386 mL 25.6772 mL
    5 mM 0.5135 mL 2.5677 mL 5.1354 mL
    10 mM 0.2568 mL 1.2839 mL 2.5677 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)

    Mass
    =
    Concentration
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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: ≥ 2.5 mg/mL (6.42 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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: 99.94%

    COA (250 KB) LCMS (93 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [1]

    Purified JmjD3 (1 μM) and UTX (3 μM) is incubated with 10 μM peptide [BiotinKAPRKQLATKAARK(me3 )SAPATGG] in 50 mM HEPES pH 7.5, 150 mM KCl, 50 μM (NH4)2SO4·FeSO4·H2O, 1 mM 2-oxoglutarate, and 2 mM ascorbate (JmjD3, 3 minutes at 25°C; UTX, 20 minutes at 25°C) with various concentration of the inhibitor (0, 0.005, 0.01, 0.02, 0.05, 0.1 μM). 10 mM EDTA is added to stop the reaction. The reaction is desalted by zip tip and spotted on a MALDI plate with α-cyano-4-hydroxycinnamic acid MALDI matrix. Samples are analysed on a MALDI-TOF R system.

    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
    DMSO 1 mM 2.5677 mL 12.8386 mL 25.6772 mL 64.1931 mL
    5 mM 0.5135 mL 2.5677 mL 5.1354 mL 12.8386 mL
    10 mM 0.2568 mL 1.2839 mL 2.5677 mL 6.4193 mL
    15 mM 0.1712 mL 0.8559 mL 1.7118 mL 4.2795 mL
    20 mM 0.1284 mL 0.6419 mL 1.2839 mL 3.2097 mL
    25 mM 0.1027 mL 0.5135 mL 1.0271 mL 2.5677 mL
    30 mM 0.0856 mL 0.4280 mL 0.8559 mL 2.1398 mL
    40 mM 0.0642 mL 0.3210 mL 0.6419 mL 1.6048 mL
    50 mM 0.0514 mL 0.2568 mL 0.5135 mL 1.2839 mL
    60 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0699 mL
    80 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8024 mL
    100 mM 0.0257 mL 0.1284 mL 0.2568 mL 0.6419 mL
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    GSK-J1 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    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:

    GSK-J11373422-53-7Histone DemethylaseInhibitorinhibitorinhibit

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    製品名:
    GSK-J1
    製品番号:
    HY-15648
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