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. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC
50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases. For full characterization details, please visit the
GSK-J1 probe summary on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for epigenetic targets, visit
sigma.com/sgcGSK-J1 is also termed as 3-((6-(4,5-Dihydro-1
H-benzo[
d]azepin-3(2
H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate.
[2] It may disturb the differentiation of specific neuronal subtypes in growing rat retina.
[3]