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 selectiveinhibitor of jumonji H3K27 histone demethylases JMJD3 and UTX (IC₅₀= 60 nM, human JMJD3). This is the first known inhibitor selective for theH3K27me3-specific JMJ subfamily which binds to the active catalytic site of theenzyme. The COOH group confers cell impermeability and as such is useful as astandard in in vitro assays. A cellpermeable ethyl ester analog (GSK-J4) is also available.

Physical Properties: Pale yellowpowder

MW=389.5 C₂₂H₂₃N₅O₂

Analysis: 99% (TLC); NMR (Conforms)

Solubilization: May be dissolved in DMSO (20 mg/ml, warm)

Storage: Store desiccated assupplied at ambient temperature for up to 2 years. Store solutions at -20°C forup to 3 months.

Amount: 5mg