GSK J4 hydrochloride

CAS No. 1373423-53-0

GSK J4 hydrochloride( —— )

Catalog No. M11540 CAS No. 1373423-53-0

GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 46 In Stock
5MG 75 In Stock
10MG 118 In Stock
25MG 215 In Stock
50MG 346 In Stock
100MG 524 In Stock
200MG 663 In Stock
500MG Get Quote In Stock
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Biological Information

  • Product Name
    GSK J4 hydrochloride
  • Note
    Research use only, not for human use.
  • Brief Description
    GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM.
  • Description
    GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.(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).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.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.GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1.GSK-J4 inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells.(In Vivo):GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice.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.
  • 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).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. 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.GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1.GSK-J4 inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells.
  • In Vivo
    GSK-J4 Hydrochloride (10 mg/kg; i.p.; thrice-weekly for 10 weeks) attenuates the development of kidney disease in diabetic mice.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. Animal Model:Eight-week-old male db/m and db/db mice Dosage:10 mg/kg Administration:i.p.; thrice-weekly for 10 weeks Result:Attenuated the development of kidney disease in diabetic mice.
  • Synonyms
    ——
  • Pathway
    Chromatin/Epigenetic
  • Target
    Histone Demethylase
  • Recptor
    JMJD3
  • Research Area
    Inflammation/Immunology
  • Indication
    ——

Chemical Information

  • CAS Number
    1373423-53-0
  • Formula Weight
    453.96
  • Molecular Formula
    C24H27N5O2·HCl
  • Purity
    >98% (HPLC)
  • Solubility
    Ethanol: 90 mg/mL warmed (198.25 mM); DMSO: 90 mg/mL warmed (198.25 mM)
  • SMILES
    CCOC(=O)CCNC1=NC(=NC(=C1)N1CCC2=CC=CC=C2CC1)C1=CC=CC=N1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Kruidenier L, et al. Nature, 2012, 488(7411), 404-408.
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