GSK J1 1373422-53-7

GSK J1
分子式：C22H23N5O2   分子量：389.45
 
產(chǎn)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.
靶點
           
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
穩(wěn)定性
2年 -20°C粉狀，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.