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    InvivoChem Cat #: V2660
    CAS #: 1373423-53-0 Purity ≥98%

    Description: GSK J4 is a novel, cell permeable, and potent prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase (KDM) JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and is inactive against a panel of demethylases of the JMJ family. GSK-J4 is used to probe the consequences of demethylation of H3K27me3. GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF). 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.

    References: Nature. 2012 Aug 16;488(7411):404-8;  2016 Dec;75:105-117.

    Related CAS#:1797983-09-5 (HCl)

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    Molecular Weight (MW)417.5
    CAS No.1373423-53-0 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: ≥ 36 mg/mL
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Synonyms GSK-J-4; GSK-J 4; GSK-J4

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    In Vitro

    In vitro activity: GSK J4 HCl is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 with an IC50 value greater than 50 μM in vitro. GSK J4 HCl is used to probe the consequences of demethylation of H3K27me3. In human primary macrophages, GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines, including pro-inflammatory tumour necrosis factor (TNF). In addition, GSK-J4 prevents the lipopolysaccharide-induced loss of H3K27me3 associated with the TNF transcription start sites and blocked the recruitment of RNA polymerase II.

    Kinase Assay: Jumonji C domain-containing histone demethylases (JHDMs) are Fe(II) and α-ketoglutarate dependent enzymes that oxygenate methylated histone lysine residues and thereby cause their demethylation. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. The prodrug GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. GSK J4 is an inhibitor of JMJD3 and UTX.

    Cell Assay: GSK J4 inhibited TNF-α protein production in a dose-dependent manner, with an IC50 value of 9 μM. Cells used: Human primary macrophages

    In VivoGSK J4 showed significant growth-inhibitory activity against SF8628 subcutaneous tumors.
    Animal modelMice harboring subcutaneous SF8628 K27M xenografts
    Formulation & Dosage100 mg/kg/day; i.p.; for 10 days

    Nature. 2012 Aug 16;488(7411):404-8; Nat Med. 2014 Dec;20(12):1394-6.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


    GSKJ4 treatment shows K27M antitumor activity in vivo.  2014 Dec;20(12):1394-6.


    GSKJ4 increases K27 methylation, inhibits K27M glioma cell growth and prevents K27M colony formation.  2014 Dec;20(12):1394-6.


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