GSK-J4
JMJ H3K27 Demethylase inhibitor (Cell Permeable) / Histone demethylase JMJD3/UTX inhibitor. Inhibits demethylation of histone H3K27. Reduces LPS-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release). Cell permeable, ethyl ester of GSK J11. Rescues newborn pups from embryonic lethality in BRAF knockin mice which recapitulate major features of RASopathies2.
Biochemicals & reagents
1373423-53-0
1) Kruidenier et al. (2012), Selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response; Nature, 488 404 2) Inoue et al. (2014) New Braf knockin mice provide a pathogenic mechanism of developmental defects and therapeutic approach in cardio-facio-cutaneous syndrome; Hum. Mol. Genet., July 17, Epub ahead of print
-20°C
TARGET: Protein demethylase -- PATHWAY: Chromatin; Cytokine; Posttranslational modification -- RESEARCH AREA: Epigenetics; Immunology -- DISEASE AREA: Inflammation