GSK-J1 (cell impermeable)

Aliases: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
Catalog No: 14068 Format: 25 mg ¥4,490 Buy
Catalog No: 14069 Format: 5 mg ¥1,240 Buy

Application: Histone Methylation (HMT & HDM)

Chemical Properties

MW = 389.5
C22H23N5O2
CAS 1373422-53-7
>99% (TLC); NMR (Conforms)

Description

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 vitro assay. A cell permeable ethyl ester analog is also available (Catalog No. 14070).

Contents

Pale yellow powder. May be dissolved in DMSO (20 mg/ml, warm).

Storage Conditions

Store desiccated as supplied at room temperature for up to 2 years. Store solutions at -20°C for up to 3 months.

References

1. L Kruidenier et al. Nature 2012, 488:404

 

Chemical structure of GSK-J1.