GSK J1

Name: GSK J1
Brand: Tocris Bioscience
SKU: 4593

Tocris Bioscience, part of Bio-Techne | Catalog # 4593

Citations (8)

COA / SDS

Potent JMJD3/UTX inhibitor

Key Product Details

Description:	Potent JMJD3/UTX inhibitor
Chemical Name:	N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine
Purity:	≥99% (HPLC)
Molecular Weight:	389.45

View Full Technical Details for GSK J1

Technical Data
Citations

Biological Activity for GSK J1

GSK J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 (KDM6B) and UTX (KDM6A) (IC₅₀ values are 28 and 53 nM respectively). Also inhibits KDM5B, KDM5C and KDM5A (IC₅₀ values are 170, 550 and 6,800 nM respectively). Exhibits no activity against a panel of other histone demethylases (IC₅₀ >20 μM), and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30 μM.

Ethyl ester derivative and Negative Control also available.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the GSK J1 probe summary on the SGC website.

Compound Libraries for GSK J1

GSK J1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GSK J1

M. Wt	389.45
Formula	C₂₂H₂₃N₅O₂
Storage	Desiccate at RT
Purity	≥99% (HPLC)
CAS Number	1373422-53-7
PubChem ID	56963315
InChi Key	AVZCPICCWKMZDT-UHFFFAOYSA-N
Smiles	O=C(CCNC1=NC(C2=CC=CC=N2)=NC(N3CCC(C=CC=C4)=C4CC3)=C1)O

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 J1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	38.94	100
	ethanol	38.94	100

Preparing Stock Solutions for GSK J1

The following data is based on the product molecular weight 389.45.

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	2.57 mL	12.84 mL	25.68 mL
5 mM	0.51 mL	2.57 mL	5.14 mL
10 mM	0.26 mL	1.28 mL	2.57 mL
50 mM	0.05 mL	0.26 mL	0.51 mL

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Reconstitution Calculator

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References for GSK J1

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