GSK J4

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GSK J4 | CAS No. 1373423-53-0 | Histone Demethylase Inhibitors
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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%

Product Details
Citations (21)
Supplemental Products
Reviews (2)

Biological Activity

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.

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.

Technical Data

M.Wt:
417.5
Formula:
C24H27N5O2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥99%
Storage:
Store at RT
CAS No:
1373423-53-0

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.

Additional Information

Licensing Caveats:
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.
Other Product-Specific Information:

Background References

  1. Inhibition of demethylases by GSK-J1/J4.
    Heinemann et al.
    Nature, 2014;514:E1
  2. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.
    Kruidenier et al.
    Nature, 2012;488:404

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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

  1. 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
  2. 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
  3. Inhibition of macrophage histone demethylase JMJD3 protects against abdominal aortic aneurysms.
    Authors: Alan Et al.
    J Exp Med  2021;218
  4. NFAT5 Amplifies Antipathogen Responses by Enhancing Chromatin Accessibility, H3K27 Demethylation, and Transcription Factor Recruitment.
    Authors: Julia Et al.
    J Immunol  2021;206:2652-2667
  5. 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
  6. 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
  7. Bone Morphogenic Proteins Are Immunoregulatory Cytokines Controlling FOXP3+ Treg Cells.
    Authors: Pawel Et al.
    Cell Rep  2020;33:108219
  8. 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
  9. The Lysine Demethylase KDM5B Regulates Islet Function and Glucose Homeostasis.
    Authors: Backe Et al.
    J Diabetes Res  2019;2019:5451038
  10. A KDM6A-KLF10 reinforcing feedback mechanism aggravates diabetic podocyte dysfunction.
    Authors: Lin Et al.
    EMBO Mol Med  2019;11
  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
  12. 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
  13. Structure of Nascent Chromatin Is Essential for Hematopoietic Lineage Specification.
    Authors: Neal Et al.
    Cell Rep  2017;19:295-306
  14. 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
  15. Epigenomic Regulation of Schwann Cell Reprogramming in Peripheral Nerve Injury.
    Authors: Ma Et al.
    J Neurosci  2016;36:9135
  16. Intracellular α-ketoglutarate maintains the pluripotency of embryonic stem cells.
    Authors: Carey Et al.
    Cancer Metab  2015;518:413
  17. Jmjd3-Mediated H3K27me3 Dynamics Orchestrate Brown Fat Development and Regulate White Fat Plasticity.
    Authors: Pan Et al.
    Dev Cell  2015;35:568
  18. Succinate dehydrogenase inhibition leads to epithelial-mesenchymal transition and reprogrammed carbon metabolism.
    Authors: Aspuria Et al.
    Nat Commun  2015;2:21
  19. The histone demethylase jumonji coordinates cellular senescence including secretion of neural stem cell-attracting cytokines.
    Authors: Perrigue Et al.
    Nature  2015;13:636
  20. 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
  21. Stepwise histone modifications are mediated by multiple enzymes that rapidly associate with nascent DNA during replication.
    Authors: Petruk Et al.
    Elife  2013;4:2841

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GSKJ4 in vivo use
By Xingyao He on 04/05/2019
Species: Mouse

Treated DIPG mice with GSKJ4. Compared survival rates for GSKJ4 alone, radiation alone, GSKJ4+RT treatments.


Worked very well
By Xingyao He on 11/30/2018

For animal treatments and in vitro assays.


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