GSK J4

Name: GSK J4
Brand: Tocris Bioscience
SKU: 4594
Rating: 5 (2 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 4594

Citations (54)

COA / SDS

Histone KDM inhibitor; cell permeable

Key Product Details

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)
Molecular Weight:	417.5

View Full Technical Details for GSK J4

Technical Data
Citations

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.

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.

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 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 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	2.40 mL	11.98 mL	23.95 mL
5 mM	0.48 mL	2.40 mL	4.79 mL
10 mM	0.24 mL	1.20 mL	2.40 mL
50 mM	0.05 mL	0.24 mL	0.48 mL

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Reconstitution Calculator

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References for GSK J4

References are publications that support the biological activity of the product.

Heinemann Inhibition of demethylases by GSK-J1/J4. Nature 2014 PMID: 25279926
Kruidenier A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 2012 PMID: 22842901