GSK-J4 HCl

• CAT Number: I007039
• CAS Number: 1797983-09-5 (HCl)
• Molecular Formula: C24H28ClN5O2
• Molecular Weight: 453.97
• Purity: ≥95%
• Synonyms: GSK-J4 HCl; GSK J4 HCl; GSK-J4 hydrochloride.;ethyl 3-((2-(pyridin-2-yl)-6-(1,2,4,5-tetrahydro-3H-benzo[d]azepin-3-yl)pyrimidin-4-yl)amino)propanoate hydrochloride
• Target: Histone demethylase Inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°C for short term or -20 °C for long term
• SMILES: O=C(OCC)CCNC1=NC(C2=NC=CC=C2)=NC(N3CCC4=CC=CC=C4CC3)=C1

GSK-J4 is a cell permeable, potent and selective histone demethylase. GSK-J4 is a 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 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).

Reference

1:Mathur R, Sehgal L, Havranek O, Köhrer S, Khashab T, Jain N, Burger JA, Neelapu SS, Davis RE, Samaniego F. Inhibition of demethylase KDM6B sensitizes diffuse large B-cell lymphoma to chemotherapeutic drugs. Haematologica. 2016 Oct 14. pii: haematol.2016.144964. [Epub ahead of print] PubMed PMID: 27742770.