GSK-<wbr/>J4 (hydro<wbr>chloride)

GSK-J4 (hydrochloride)

CAT N°: 12073
Price:

From 85.00 72.25

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 ?M in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNF? (IC50 = 9 µM).{21388}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-?-alanine, ethyl ester, monohydrochloride
  • Correlated keywords
    • 1373423-53-0 epigenetics demethylase histones JMJD3 cells differentiation developments inflammation cancers GSK-J1 pro-drug prodrugs H3 lysine 27 H3K27 H3K-27 GSKJ1 GSKs J1 GSKJ4 J4 inhibitors inhibits inhibitions macrophages reduce LPS induce induced proinflammatory inflammatory pro pro-inflammatory cytokines TNF.alpha. TNF-.alpha. TNF .alpha. TNF-alpha TNF-a TNF-? TNFalpha TNFa TNF? alpha ? HCl Structural Genomic Consortium SGC
  • Product Overview:
    The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.{19496,19494} GSK-J4 (hydrochloride) is an ethyl ester derivative of the JMJD3 selective histone demethylase inhibitor GSK-J1 (Item No. 12054) with an IC50 value greater than 50 ?M in vitro.{21388} Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNF? (IC50 = 9 µM).{21388}

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