GSK J4

Pricing Availability   Qty
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)
Datasheet
Citations (11)
Reviews
Literature (3)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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.

View Related Products by Target

View Related Products by Product Action

View all Histone Demethylase Inhibitors

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

11 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

Ma et al (2016) Epigenomic Regulation of Schwann Cell Reprogramming in Peripheral Nerve Injury. J Neurosci 36 9135 PMID: 27581455

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


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Reviews for GSK J4

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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