Chemical Name: N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine ethyl ester
Biological ActivityGSK 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.
External Portal InformationChemicalprobes.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.
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.
Inhibition of demethylases by GSK-J1/J4.
Heinemann et al.
A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
Kruidenier et al.
Citations for GSK J4
The citations listed below are publications that use Tocris products. Selected citations for GSK J4 include:
21 Citations: Showing 1 - 10
The Histone Demethylase Inhibitor GSK-J4 Is a Therapeutic Target for the Kidney Fibrosis of Diabetic Kidney Disease via DKK1 Modulation.
Authors: Yung-Chien Et al.
Int J Mol Sci 2022;23
Inhibitor of growth protein 3 epigenetically silences endogenous retroviral elements and prevents innate immune activation.
Authors: Jan E Et al.
Nucleic Acids Res 2021;49:12706-12715
Inhibition of macrophage histone demethylase JMJD3 protects against abdominal aortic aneurysms.
Authors: Alan Et al.
J Exp Med 2021;218
NFAT5 Amplifies Antipathogen Responses by Enhancing Chromatin Accessibility, H3K27 Demethylation, and Transcription Factor Recruitment.
Authors: Julia Et al.
J Immunol 2021;206:2652-2667
Suppression of canonical TGF-β signaling enables GATA4 to interact with H3K27me3 demethylase JMJD3 to promote cardiomyogenesis.
Authors: Peter M Et al.
J Mol Cell Cardiol 2021;153:44-59
Palmitate-TLR4 signaling regulates the histone demethylase, JMJD3, in macrophages and impairs diabetic wound healing.
Authors: Steven L Et al.
Eur J Immunol 2020;50:1929-1940
Bone Morphogenic Proteins Are Immunoregulatory Cytokines Controlling FOXP3+ Treg Cells.
Authors: Pawel Et al.
Cell Rep 2020;33:108219
Combined Targeting of Mutant p53 and Jumonji Family Histone Demethylase Augments Therapeutic Efficacy of Radiation in H3K27M DIPG.
Authors: Anatoly Et al.
Int J Mol Sci 2020;21
The Lysine Demethylase KDM5B Regulates Islet Function and Glucose Homeostasis.
Authors: Backe Et al.
J Diabetes Res 2019;2019:5451038
A KDM6A-KLF10 reinforcing feedback mechanism aggravates diabetic podocyte dysfunction.
Authors: Lin Et al.
EMBO Mol Med 2019;11
Jumonji Inhibitors Overcome Radioresistance in Cancer through Changes in H3K4 Methylation at Double-Strand Breaks.
Authors: Bayo Et al.
Cell Rep 2018;25:1040
RNA sequencing reveals resistance of TLR4 ligand-activated microglial cells to inflammation mediated by the selective jumonji H3K27 demethylase inhibitor.
Authors: Kyoung Hwa Et al.
Sci Rep 2017;7:6554
Structure of Nascent Chromatin Is Essential for Hematopoietic Lineage Specification.
Authors: Neal Et al.
Cell Rep 2017;19:295-306
Neuronal activity controls Bdnf expression via Polycomb de-repression and CREB/CBP/JMJD3 activation in mature neurons.
Authors: Palomer Et al.
Mol Cancer Res 2016;7:11081
Epigenomic Regulation of Schwann Cell Reprogramming in Peripheral Nerve Injury.
Authors: Ma Et al.
J Neurosci 2016;36:9135
Intracellular α-ketoglutarate maintains the pluripotency of embryonic stem cells.
Authors: Carey Et al.
Cancer Metab 2015;518:413
Jmjd3-Mediated H3K27me3 Dynamics Orchestrate Brown Fat Development and Regulate White Fat Plasticity.
Authors: Pan Et al.
Dev Cell 2015;35:568
Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism.
Authors: Aspuria Et al.
Nat Commun 2015;2:21
The histone demethylase jumonji coordinates cellular senescence including secretion of neural stem cell-attracting cytokines.
Authors: Perrigue Et al.
Transcriptomic Profiling and H3K27me3 Distribution Reveal Both Demethylase-Dependent and Independent Regulation of Developmental Gene Transcription in Cell Differentiation.
Authors: Kang Et al.
PLoS One 2015;10:e0135276
Stepwise histone modifications are mediated by multiple enzymes that rapidly associate with nascent DNA during replication.
Authors: Petruk Et al.
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Treated DIPG mice with GSKJ4. Compared survival rates for GSKJ4 alone, radiation alone, GSKJ4+RT treatments.
For animal treatments and in vitro assays.