1. Epigenetics
  2. Histone Demethylase
  3. GSK-J4

GSK-J4 

製品番号: HY-15648B 純度: 99.17%
取扱説明書

GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1.

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GSK-J4 構造式

GSK-J4 構造式

CAS 番号 : 1373423-53-0

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 158 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 144 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 420 在庫あり
Estimated Time of Arrival: December 31
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200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of GSK-J4:

Top Publications Citing Use of Products

    GSK-J4 purchased from MCE. Usage Cited in: J Clin Invest. 2018 Jan 2;128(1):483-499.

    Immunoblotting for H3K27me3 in cultured mouse podocytes treated with the Jmjd3 and UTX inhibitor GSK-J4 (5 μM for 48 hours) (n=3).
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    • 参考文献

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    製品説明

    GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1[1][2][3].

    IC50 & Target

    IC50: 8.6 µM (JMJD3/KDM6B), 6.6 µM (UTX/KDM6A)[6]

    体外実験

    GSK-J4 has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α)[1].
    GSK-J4 (5 μM; 48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels[2].
    GSK-J4 (10, 25 nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells[3].
    GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1[4].
    GSK-J4 inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells[5].

    体内実験

    GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice[2].
    GSK-J4 (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis[3].

    Animal Model: Eight-week-old male db/m and db/db mice[2]
    Dosage: 10 mg/kg
    Administration: i.p.; thrice-weekly for 10 weeks
    Result: Attenuated the development of kidney disease in diabetic mice.
    分子量

    417.50

    分子式

    C₂₄H₂₇N₅O₂

    CAS 番号

    1373423-53-0

    SMILES

    O=C(OCC)CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=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 : ≥ 36 mg/mL (86.23 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3952 mL 11.9760 mL 23.9521 mL
    5 mM 0.4790 mL 2.3952 mL 4.7904 mL
    10 mM 0.2395 mL 1.1976 mL 2.3952 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.99 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    参考文献

    純度: 99.17%

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    Keywords:

    GSK-J4Histone DemethylaseH3K27me3/me2inflammationdendriticcellsTGF-βdiabeticmiceTh1Th17demethylaseInhibitorinhibitorinhibit

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    製品名:
    GSK-J4
    製品番号:
    HY-15648B
    数量:
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