N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-b-alanine
GSK-J1 is a potent and selective
inhibitor of jumonji H3K27 histone demethylases JMJD3 and UTX (IC50
= 60 nM, human JMJD3). This is the first known inhibitor selective for the
H3K27me3-specific JMJ subfamily which binds to the active catalytic site of the
enzyme. The COOH group confers cell impermeability and as such is useful as a
standard in in vitro assays. A cell
permeable ethyl ester analog (GSK-J4) is also available.
Physical Properties: Pale yellow
powder
MW=389.5 C22H23N5O2
Analysis: 99% (TLC); NMR (Conforms)
Solubilization: May be dissolved in DMSO (20 mg/ml, warm)
Storage: Store desiccated as
supplied at ambient temperature for up to 2 years. Store solutions at -20°C for
up to 3 months.
Amount: 5mg 
