Cat. No. 4594

GSK J4 C24H27N5O2 [1373423-53-0]

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Chemical Name: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine ethyl ester

Biological Activity

Histone lysine demethylase (KDM) inhibitor; blocks demethylation of histone H3K27. Attenuates lipopolysaccharide (LPS)-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release). Cell permeable. Ethyl ester derivative of GSK J1 (Cat. No. 4593).

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details of GSK J4, a cell permeable derivative of GSK J1, please visit the GSK J1 probe summary on the SGC website.

External Portal Information is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK J4 is reviewed on the chemical probes website.

Technical Data

Soluble to 100 mM in DMSO and to 100 mM in ethanol
>99 %
Store at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Heinemann et al (2014) Inhibition of demethylases by GSK-J1/J4. Nature 514 E1. PMID: 25279926.

Kruidenier et al (2012) A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 488 404. PMID: 22842901.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for GSK J4 include:

Palomer et al (2016) Neuronal activity controls Bdnf expression via Polycomb de-repression and CREB/CBP/JMJD3 activation in mature neurons. Mol Cancer Res 7 11081. PMID: 27010597.

Aspuria et al (2015) Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism. Nat Commun 2 21. PMID: 25671108.

Carey et al (2015) Intracellular α-ketoglutarate maintains the pluripotency of embryonic stem cells. Cancer Metab 518 413. PMID: 25487152.

Kang et al (2015) Transcriptomic Profiling and H3K27me3 Distribution Reveal Both Demethylase-Dependent and Independent Regulation of Developmental Gene Transcription in Cell Differentiation. PLoS One 10 e0135276. PMID: 26263556.

Perrigue et al (2015) The histone demethylase jumonji coordinates cellular senescence including secretion of neural stem cell-attracting cytokines. Nature 13 636. PMID: 25652587.

Petruk et al (2013) Stepwise histone modifications are mediated by multiple enzymes that rapidly associate with nascent DNA during replication. Elife 4 2841. PMID: 24276476.

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Keywords: GSK J4, supplier, GSKJ4, histone, demethylases, inhibitors, inhibits, UTX, JMJD3, KDM6, H3K27, KDMs, proinflammatory, macrophages, tnf, alpha, tnfa, anti-inflammatory, epigenetics, Tocris Bioscience, Histone Demethylase Inhibitor products

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