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

GSK-J4 

Cat. No.: HY-15648B Purity: >98.0%
Handling Instructions

GSK-J4 is a potent H3K27me3 histone lysine demethylase (KDM) inhibitor, with IC50s of 8.6 μM and 6.6 μM against KDM6B and KDM6A, respectively.

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

GSK-J4 Chemical Structure

GSK-J4 Chemical Structure

CAS No. : 1373423-53-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 158 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
50 mg USD 420 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 6 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).
    • Biological Activity

    • Protocol

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    • References

    • Customer Review

    Description

    GSK-J4 is a potent H3K27me3 histone lysine demethylase (KDM) inhibitor, with IC50s of 8.6 μM and 6.6 μM against KDM6B and KDM6A, respectively.

    IC50 & Target

    IC50: 8.6 µM (KDM6B), 6.6 µM (KDM6A)[5]

    In Vitro

    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 (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[2]. GSK-J4 inhibits the KDM6 family of H3K27me3 demethylases JMJD3 and UTX. GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1[3]. GSK-J4 inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells[4].

    In Vivo

    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[2].

    Molecular Weight

    417.50

    Formula

    C₂₄H₂₇N₅O₂

    CAS No.

    1373423-53-0

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    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.
    In Vivo:
    • 1.

      GSK-J4 is prepared in 0.1% DMSO in PBS[6].

    References
    Animal Administration
    [2]

    Six-to eight-week-old female C57BL/6 WT mice are injected by subcutaneous injection (s.c.) with 50 μg myelin oligodendrocyte glycoprotein 35-55 peptide (pMOG) emulsified in Complete Freund's Adjuvant (CFA) supplemented with heat-inactivated Mycobacterium tuberculosis H37 RA. In addition, mice receive intraperitoneal injection (i.p.) of 500 ng of pertussis toxin on days 0 and 2. Clinical signs are assessed daily according to the following scoring criteria: 0, no detectable signs; 1, flaccid tail; 2, hind limb weakness or abnormal gait; 3, complete hind limb paralysis; 4, paralysis of fore and hind limbs; and 5, moribund or death. A stock solution of GSK-J4 of 42 mg/mL (100 mM) is prepared in dimethyl sulfoxide (DMSO) to preserve stability. Before injection, the stock solution is diluted 1/10 with ethanol (DMSO: ethanol, 1:10 v/v) and brought to a final concentration of 140 μg/mL in PBS. In systemic drug evaluation experiments, each mouse receive daily i.p. injections (from days 0-5) of 100 μL of this solution containing 14.0 μg of the GSK-J4 (equivalent to 0.56 mg/kg of the drug). Control mice receive 100 μL of the vehicle during the same period. In other EAE experiments, 106 bone marrow-derived DCs from WT mice are treated with GSK-J4 or vehicle alone for 16 h, pulsed with 5 μg/mL of pMOG for 4 h and then transferred i.v. into WT C57BL/6 recipient mice 14 and 7 days before EAE induction. In other adoptive transfer EAE experiments, CD4+Foxp3+ Treg cells generated in the presence or absence of 25 nM GSK-J4 are purified by cell sorting and then 0.75×106 transferred i.v. into WT C57BL/6 recipient mice 1 day before EAE induction.

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

    References

    Purity: >98.0%

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