GSK J4 HCl

Inhibitor of H3K27 demethylase JMJD3,potent and cell-permeable CAS# 1373423-53-0

GSK J4 HCl

Catalog No. BCC2230----Order now to get a substantial discount!

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GSK J4 HCl: 5mg $58 In Stock
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Chemical structure

GSK J4 HCl

3D structure

Chemical Properties of GSK J4 HCl

Cas No. 1373423-53-0 SDF Download SDF
PubChem ID 71729975 Appearance Powder
Formula C24H27N5O2 M.Wt 417.5
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 100 mM in ethanol
Chemical Name ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate
SMILES CCOC(=O)CCNC1=NC(=NC(=C1)N2CCC3=CC=CC=C3CC2)C4=CC=CC=N4
Standard InChIKey WBKCKEHGXNWYMO-UHFFFAOYSA-N
Standard InChI InChI=1S/C24H27N5O2/c1-2-31-23(30)10-14-26-21-17-22(28-24(27-21)20-9-5-6-13-25-20)29-15-11-18-7-3-4-8-19(18)12-16-29/h3-9,13,17H,2,10-12,14-16H2,1H3,(H,26,27,28)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GSK J4 HCl

DescriptionHistone 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.

GSK J4 HCl Dilution Calculator

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GSK J4 HCl Molarity Calculator

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Preparing Stock Solutions of GSK J4 HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.3952 mL 11.976 mL 23.9521 mL 47.9042 mL 59.8802 mL
5 mM 0.479 mL 2.3952 mL 4.7904 mL 9.5808 mL 11.976 mL
10 mM 0.2395 mL 1.1976 mL 2.3952 mL 4.7904 mL 5.988 mL
50 mM 0.0479 mL 0.2395 mL 0.479 mL 0.9581 mL 1.1976 mL
100 mM 0.024 mL 0.1198 mL 0.2395 mL 0.479 mL 0.5988 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GSK J4 HCl

GSK J4 is a potent cell-permeable inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3, an essential component of regulatory transcriptional chromatin complexes, with the half maximal inhibition concentration IC50 value > 50 μM in vitro [1].

GSK J4 is an ethyl ester derivative of GSK J1, which is a potent JMJD3 inhibitor (IC50: 60 nM) with restricted cellular permeability due to the highly polar carboxylate group, and rapidly hydrolyzed by macrophage esterase upon administration leading to the generation of pharmacologically relevant intracellular concentration of GSK-J1 [1].

GSK J4 has also been found to dose-dependently inhibit the production of tumor-necrosis factor-α (TNF-α), a LPS-driven cytokine involved in various fnflammatory disorders, with IC50 value of 9μM [1].

Reference

References:
[1] Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8. doi: 10.1038/nature11262.

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References on GSK J4 HCl

A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.[Pubmed:22842901]

Nature. 2012 Aug 16;488(7411):404-8.

The jumonji (JMJ) family of histone demethylases are Fe2+- and alpha-ketoglutarate-dependent oxygenases that are essential components of regulatory transcriptional chromatin complexes. These enzymes demethylate lysine residues in histones in a methylation-state and sequence-specific context. Considerable effort has been devoted to gaining a mechanistic understanding of the roles of histone lysine demethylases in eukaryotic transcription, genome integrity and epigenetic inheritance, as well as in development, physiology and disease. However, because of the absence of any selective inhibitors, the relevance of the demethylase activity of JMJ enzymes in regulating cellular responses remains poorly understood. Here we present a structure-guided small-molecule and chemoproteomics approach to elucidating the functional role of the H3K27me3-specific demethylase subfamily (KDM6 subfamily members JMJD3 and UTX). The liganded structures of human and mouse JMJD3 provide novel insight into the specificity determinants for cofactor, substrate and inhibitor recognition by the KDM6 subfamily of demethylases. We exploited these structural features to generate the first small-molecule catalytic site inhibitor that is selective for the H3K27me3-specific JMJ subfamily. We demonstrate that this inhibitor binds in a novel manner and reduces lipopolysaccharide-induced proinflammatory cytokine production by human primary macrophages, a process that depends on both JMJD3 and UTX. Our results resolve the ambiguity associated with the catalytic function of H3K27-specific JMJs in regulating disease-relevant inflammatory responses and provide encouragement for designing small-molecule inhibitors to allow selective pharmacological intervention across the JMJ family.

Description

Histone KDM inhibitor; cell permeable,GSK-J4 is a potent H3K27me3 demethylase inhibitor, with IC50s of 8.6 µM and 6.6 µM towards KDM6B and KDM6A respectively.

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