2. Epigenetics
    Apoptosis
  3. Histone Demethylase
    Apoptosis
  4. GSK-J4

GSK-J4 

製品番号: HY-15648B 純度: 99.64%
COA 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. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

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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
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solution
10 mM * 1 mL in DMSO USD 174 在庫あり
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 174 在庫あり
Estimated Time of Arrival: December 31
Solid
10 mg USD 158 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 462 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 700 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 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 27 publication(s) in Google Scholar

Other Forms of GSK-J4:

Top Publications Citing Use of Products

    GSK-J4 purchased from MCE. Usage Cited in: Cancer Cell Int. 2020 Jun 3;20:209.  [Abstract]

    The mRNA expression level of PKC-α is detected using qRT-PCR. GAPDH is used as an internal control.

    GSK-J4 purchased from MCE. Usage Cited in: Cancer Cell Int. 2020 Jun 3;20:209.  [Abstract]

    After treatment with GSK-J4, the expression levels of PKC-α and p-Bcl2 in KG-1a cells are detected by Western blotting.

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

    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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    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]. GSK-J4 induces endoplasmic reticulum stress-related apoptosis[4].

    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].

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

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

    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

    Appearance

    Solid

    分子式

    C24H27N5O2
    CAS 番号
    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: ≥ 2.08 mg/mL (4.98 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

    *All of the co-solvents are available by MCE.
    純度とドキュメンテーション

    純度: 99.64%

    COA (254 KB) HNMR (208 KB) LCMS (111 KB)

    取扱説明書 (2659 KB)
    参考文献
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    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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    Keywords:

    GSK-J41373423-53-0Histone DemethylaseApoptosisH3K27me3/me2inflammationdendriticcellsTGF-βdiabeticmiceTh1Th17demethylaseInhibitorinhibitorinhibit

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