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).
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
Chemicalprobes.org 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.
|Storage||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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 417.5. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.4 mL||11.98 mL||23.95 mL|
|5 mM||0.48 mL||2.4 mL||4.79 mL|
|10 mM||0.24 mL||1.2 mL||2.4 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Kruidenier et al (2012) A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 488 404 PMID: 22842901
Heinemann et al (2014) Inhibition of demethylases by GSK-J1/J4. Nature 514 E1 PMID: 25279926
If you know of a relevant reference for GSK J4, please let us know.
View Related Products by Product Action
Keywords: GSK J4, supplier, GSKJ4, histone, demethylases, inhibitors, inhibits, UTX, JMJD3, KDM6, H3K27, KDMs, proinflammatory, macrophages, tnf, alpha, tnfa, anti-inflammatory, epigenetics, Histone, Demethylases, Histone, Demethylases, Tocris Bioscience
6 Citations for GSK J4
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
Perrigue et al (2015) The histone demethylase jumonji coordinates cellular senescence including secretion of neural stem cell-attracting cytokines. Nature 13 636 PMID: 25652587
Carey et al (2015) Intracellular α-ketoglutarate maintains the pluripotency of embryonic stem cells. Cancer Metab 518 413 PMID: 25487152
Aspuria et al (2015) Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism. Nat Commun 2 21 PMID: 25671108
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
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
Do you know of a great paper that uses GSK J4 from Tocris? If so please let us know.
Literature in this Area
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases