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Epigenetics & Chromatin

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 $335 Buy Now
Catalog No: 14069 Format: 5 mg $90 Buy Now
Application: Histone Methylation (HMT & HDM)

for GSK-J1 (cell impermeable)Chemical Properties

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

for GSK-J1 (cell impermeable)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).

for GSK-J1 (cell impermeable)Contents

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

for GSK-J1 (cell impermeable)Storage Conditions

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

for GSK-J1 (cell impermeable)References

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

 
Chemical structure of GSK-J1.

Chemical structure of GSK-J1.

 

Technical Data Sheet

GSK-J1 (cell impermeable)
 

Data Thumbnails

Chemical structure of GSK-J1.

Chemical structure of GSK-J1.
(Click image to enlarge.)