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Submit ReviewGSK J4
Description: Histone KDM inhibitor; cell permeable
Chemical Name: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine ethyl ester
Purity: ≥99% (HPLC)
Biological Activity for GSK J4
GSK J4 is a 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.
Negative Control also available.
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 for GSK J4
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.
Compound Libraries for GSK J4
GSK J4 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for GSK J4
| M. Wt | 417.5 |
| Formula | C24H27N5O2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1373423-53-0 |
| PubChem ID | 71729975 |
| InChI Key | WBKCKEHGXNWYMO-UHFFFAOYSA-N |
| Smiles | O=C(CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1)OCC |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for GSK J4
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.75 | 100 | |
| ethanol | 41.75 | 100 |
Preparing Stock Solutions for GSK J4
The following data is based on the product molecular weight 417.5. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for GSK J4
References for GSK J4
References are publications that support the biological activity of the product.
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.
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Keywords: GSK J4, GSK J4 supplier, GSKJ4, histone, demethylases, inhibitors, inhibits, UTX, JMJD3, KDM6, H3K27, KDMs, proinflammatory, macrophages, tnf, alpha, tnfa, anti-inflammatory, epigenetics, Histone, Demethylases, 4594, Tocris Bioscience
21 Citations for GSK J4
Citations are publications that use Tocris products. Selected citations for GSK J4 include:
Ma et al (2016) Epigenomic Regulation of Schwann Cell Reprogramming in Peripheral Nerve Injury. J Neurosci 36 9135 PMID: 27581455
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
Lin et al (2019) A KDM6A-KLF10 reinforcing feedback mechanism aggravates diabetic podocyte dysfunction. EMBO Mol Med 11 PMID: 30948420
Backe et al (2019) The Lysine Demethylase KDM5B Regulates Islet Function and Glucose Homeostasis. J Diabetes Res 2019 5451038 PMID: 31467927
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
Yung-Chien et al (2022) The Histone Demethylase Inhibitor GSK-J4 Is a Therapeutic Target for the Kidney Fibrosis of Diabetic Kidney Disease via DKK1 Modulation. Int J Mol Sci 23 PMID: 36012674
Steven L et al (2020) Palmitate-TLR4 signaling regulates the histone demethylase, JMJD3, in macrophages and impairs diabetic wound healing. Eur J Immunol 50 1929-1940 PMID: 32662520
Anatoly et al (2020) Combined Targeting of Mutant p53 and Jumonji Family Histone Demethylase Augments Therapeutic Efficacy of Radiation in H3K27M DIPG. Int J Mol Sci 21 PMID: 31940975
Pawel et al (2020) Bone Morphogenic Proteins Are Immunoregulatory Cytokines Controlling FOXP3+ Treg Cells. Cell Rep 33 108219 PMID: 33027660
Bayo et al (2018) Jumonji Inhibitors Overcome Radioresistance in Cancer through Changes in H3K4 Methylation at Double-Strand Breaks. Cell Rep 25 1040 PMID: 30355483
Neal et al (2017) Structure of Nascent Chromatin Is Essential for Hematopoietic Lineage Specification. Cell Rep 19 295-306 PMID: 28402853
Kyoung Hwa et al (2017) RNA sequencing reveals resistance of TLR4 ligand-activated microglial cells to inflammation mediated by the selective jumonji H3K27 demethylase inhibitor. Sci Rep 7 6554 PMID: 28747667
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
Pan et al (2015) Jmjd3-Mediated H3K27me3 Dynamics Orchestrate Brown Fat Development and Regulate White Fat Plasticity. Dev Cell 35 568 PMID: 26625958
Peter M et al (2021) Suppression of canonical TGF-β signaling enables GATA4 to interact with H3K27me3 demethylase JMJD3 to promote cardiomyogenesis. J Mol Cell Cardiol 153 44-59 PMID: 33359755
Julia et al (2021) NFAT5 Amplifies Antipathogen Responses by Enhancing Chromatin Accessibility, H3K27 Demethylation, and Transcription Factor Recruitment. J Immunol 206 2652-2667 PMID: 34031145
Alan et al (2021) Inhibition of macrophage histone demethylase JMJD3 protects against abdominal aortic aneurysms. J Exp Med 218 PMID: 33779682
Jan E et al (2021) Inhibitor of growth protein 3 epigenetically silences endogenous retroviral elements and prevents innate immune activation. Nucleic Acids Res 49 12706-12715 PMID: 34791430
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
Do you know of a great paper that uses GSK J4 from Tocris? Please let us know.
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Literature in this Area
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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.