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

GSK-J4 hydrochloride 

Cat. No.: HY-15648F
Handling Instructions

GSK-J4 hydrochloride 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 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.

For research use only. We do not sell to patients.

GSK-J4 hydrochloride Chemical Structure

GSK-J4 hydrochloride Chemical Structure

CAS No. : 1797983-09-5

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of GSK-J4 hydrochloride:

Top Publications Citing Use of Products

    GSK-J4 hydrochloride 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).
    • Biological Activity

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    • References

    • Customer Review

    Description

    GSK-J4 hydrochloride 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 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride 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]

    In Vitro

    GSK-J4 Hydrochloride 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 Hydrochloride (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 Hydrochloride (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 Hydrochloride inhibits JMJD3 expression that is induced by TGF-β1[4].
    GSK-J4 Hydrochloride inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells[5].

    In Vivo

    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 Hydrochloride (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 on a BKS background[2]
    Dosage: 10 mg/kg
    Administration: i.p.; thrice-weekly for 10 weeks
    Result: Attenuated the development of kidney disease in diabetic mice.
    Molecular Weight

    453.96

    Formula

    C₂₄H₂₈ClN₅O₂

    CAS No.

    1797983-09-5

    SMILES

    O=C(OCC)CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (275.35 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2028 mL 11.0142 mL 22.0284 mL
    5 mM 0.4406 mL 2.2028 mL 4.4057 mL
    10 mM 0.2203 mL 1.1014 mL 2.2028 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (4.58 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    Keywords:

    GSK-J4Histone DemethylaseH3K27me3/me2inflammationdendriticcellsTGF-βdiabeticmiceTh1Th17demethylaseInhibitorinhibitorinhibit

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    Product name:
    GSK-J4 hydrochloride
    Cat. No.:
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