GSK J1 1373422-53-7
GSK J1
分子式:C22H23N5O2 分子量:389.45
产品描述
Potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50 = 60 nM for human JMJD3 in vitro). Exhibits no activity against a panel of JMJD family demethylases, and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30 μM. Ethyl ester derivative also available.
靶点
IC50
生物活性
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 IC50 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.
溶解性
DMSO 100 mM,乙醇 100 mM
稳定性
2年 -20°C粉状,6月-80°C溶于DMSO
特征
The first selective and potent histone demethylase JMJD3/UTX inhibitor; blocks demethylation of histone H3K27; showed no activity against a panel of JMJ family demethylases and 100 protein kinases.