Home Epigenetics Histone Demethylase inhibitor - JMJD inhibitor GSK J1 For research use only.

GSK J1

GSK-J1 is a highly potent inhibitor of H3K27 histone demethylase JMJD3 (KDM6B) and UTX (KDM6A) with IC50 of 60 nM in cell-free assays for JMJD3 (KDM6B) , respectively, >10-fold selectivity over other tested demethylases, with IC50 of 0.95μM and 1.76μM towards JARID1B/C.

GSK J1 Chemical Structure

GSK J1 Chemical Structure

CAS No. 1373422-53-7

Purity & Quality Control

GSK J1 Related Products

Signaling Pathway

Histone Demethylase Signaling Pathways

Histone Demethylase Signaling Pathway

Biological Activity

Description GSK-J1 is a highly potent inhibitor of H3K27 histone demethylase JMJD3 (KDM6B) and UTX (KDM6A) with IC50 of 60 nM in cell-free assays for JMJD3 (KDM6B) , respectively, >10-fold selectivity over other tested demethylases, with IC50 of 0.95μM and 1.76μM towards JARID1B/C.
Targets
JMJD3 [1]
60 nM
In vitro
In vitro

In HEK-293 cells, GSK-J1 inhibits the activities of transiently transfected JMJD3 and UTX. GSK-J1 also inhibits TNF-α production by human primary macrophages by increasing total nuclear H3K27me3 levels. [1]

In MC3T3-E1 cells, GSK-J1 suppresses Runx2 and Osterix expressions and ALP activity, and increases the global levels of H3K27me3. [2]
Kinase Assay MALDI-TOF Analysis of JmjD3 and UTX Activity
Purified JmjD3 (1 μM) and UTX (3 μM) is incubated with 10 μM peptide [Biotin-KAPRKQLATKAARK(me3)SAPATGG] in 50 mM HEPES pH 7.5, 150 mM KCl, 50μM (NH4)2SO4·FeSO4·H2O, 1 mM 2-oxoglutarate, and 2 mM ascorbate (JmjD3, 3 minutes at 25°C; UTX, 20 minutes at 25°C) with various concentration of the inhibitor (0, 0.005, 0.01, 0.02, 0.05, 0.1 μM). 10mM EDTA is added to stop the reaction. The reaction is desalted by zip tip and spotted on a MALDI plate with α-cyano-4-hydroxycinnamic acid MALDI matrix. Samples are analysed on a MALDI-TOF R system.
In Vivo
In vivo

GSK-J1, a small molecule inhibitor of JMJD3, directly interfered with the transcription of inflammatory-related genes by H3K27me3 modification of their promoters.

Chemical Information & Solubility

Molecular Weight 389.45 Formula

C22H23N5O2
CAS No. 1373422-53-7 SDF Download GSK J1 SDF
Smiles C1CN(CCC2=CC=CC=C21)C3=NC(=NC(=C3)NCCC(=O)O)C4=CC=CC=N4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 77 mg/mL ( (197.71 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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