GSK J4 HCl


CAS No. : 1797983-09-5

GSK J4 HCl,1797983-09-5
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000389
Synonyms:N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine, ethyl ester, monohydrochloride
Molecular Formula:C24H27N5O2 • HCl
Molecular Weight:454.0
Target:JMJD3
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Assay:≥95%
Appearance:A crystalline solid
Cat No:I000389
Cas No:1797983-09-5
Product-Name:GSK J4 HCl
InChIKey:TYXWLTBYINKVNT-UHFFFAOYSA-N
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.
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.
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