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 shift, mass spectrometry...

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 H3K27-dependent manner.

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 1, the...

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 KDM5A (IC 50 values are 170, 550 and 6,800 nM respectively).

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 nM and 1.76 μM, respectively). No significant inhibitory activity against 100 protein kinases at a concentration of 30 μM. Anti-inflammatory effects.

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 oxygenate methylated histone lysine residues and thereby cause their demethylation.

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 vitro and in cells using an ester derivative (GSK-J4: 1 µM …

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 physiological functions including the inflammatory response, with the half maximal inhibition concentration IC50 value of 60 nM [1].