Jul 29, 2012 · GSK-J1 is selective for the H3K27 demethylases JMJD3 and UTX and is inactive against a panel of demethylases of the JMJ family, as measured by a combination of thermal …

Potent and selective H3K27 histone demethylase inhibitor (IC 50 = 60 nM, JMJD3). Inhibits UTX. Some activity for the H3K4me3/2/1 demethylases Jarid1b and Jarid1c (IC 50 values are 950 …

Oct 1, 2014 · In agreement with the published data 1, our results show that GSK-J1 is a highly potent inhibitor of KDM6B and KDM6A. Moreover, and also in agreement with Kruidenier et al …

GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an …

GSK J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 (KDM6B) and UTX (KDM6A) (IC 50 values are 28 and 53 nM respectively). Also inhibits KDM5B, KDM5C and …

GSK-J1 is a potent selective jumonji H3K27 demethylase inhibitor. Jumonji C domain-containing histone demethylases (JHDMs) are Fe (II) and α-ketoglutarate dependent enzymes that …

Here we present in collaboration with GlaxoSmithKline the first selective and potent histone demethylase inhibitor (GSK-J1) that has significant activity (IC 50 60 nM for human JmjD3) in …

GSK J1 is a potent and selective inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3, a Fe2+- and α-ketoglutarate-dependent oxygenase involved in a variety of …

Here, we aimed to investigate the role of JMJD3 in the lipopolysaccharide (LPS)-induced mastitis model. GSK-J1, a small molecule inhibitor of JMJD3, was applied to treat LPS-induced …