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:
11 Citations: Showing 1 - 10
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
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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Reviews for GSK J4
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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.