GSK-J4 (cell permeable)

Aliases: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine ethyl ester
Catalog No: 14070 Format: 25 mg $345 Buy
Catalog No: 14071 Format: 5 mg $95 Buy
Application: Histone Methylation (HMT & HDM)

Chemical Properties

MW = 417.5
C24H27N5O2
CAS 1373423-53-0
>99% (TLC); NMR (Conforms)

Description

Histone demethylase JMJD3/UTX inhibitor. Inhibits demethylation of histone H3K27. Reduces LPS-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 µM for the inhibition of TNFα release). Cell permeable, ethyl ester of GSK J1 (Catalog No. 14068)(ref 1). Rescues newborn pups from embryonic lethality in BRAF knock-in mice which recapitulate major features of RASopathies (ref 2).

Contents

Yellow wax. May be dissolved in DMSO (40 mg/ml); Ethanol (40 mg/ml).

Storage Conditions

Store desiccated as supplied at -20°C 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
2. SI Inoue et al. Hum. Mol. Genet. 2014 July 17, Epub.

 
Chemical structure of GSK-J4.

Chemical structure of GSK-J4.