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GSK-J4 Hydrochloride

Catalog No. T4383 CAS 1797983-09-5

Synonyms: GSK J4 HCl, GSK J4 HCl (1373423-53-0 free base)

GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.

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GSK-J4 Hydrochloride, CAS 1797983-09-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 81.00
10 mg	In stock	$ 129.00
25 mg	In stock	$ 229.00
50 mg	In stock	$ 382.00
100 mg	In stock	$ 562.00
200 mg	In stock	$ 785.00
1 mL * 10 mM (in DMSO)	In stock	$ 142.00

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Purity: 98.36%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.
Targets&IC50	JMJD3:50 μM, JMJD3 (cell-free assay):60 nM
In vitro	When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 μM).
In vivo	Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.

Synonyms	GSK J4 HCl, GSK J4 HCl (1373423-53-0 free base)
Molecular Weight	453.97
Formula	C24H28ClN5O2
CAS No.	1797983-09-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 20 mg/mL

DMSO: 50 mg/mL (110.14 mM)

References and Literature

1. Yan N,etal.GSKJ4, an H3K27me3 demethylase inhibitor, effectively suppresses the breast cancer stem cells.Exp Cell Res. 2017 Oct 15;359(2):405-414. 2. Kruidenier L,etal.A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.Nature. 2012 Aug 16;488(7411):404-8. 3. Li Y,etal.Therapeutic potential of GSK-J4, a histone demethylase KDM6B/JMJD3 inhibitor, for acute myeloid leukemia.J Cancer Res Clin Oncol. 2018 Jun;144(6):1065-1077. 4. Mandal C,etal.GSK-J4-Mediated Transcriptomic Alterations in Differentiating Embryoid Bodies.Mol Cells. 2017 Oct;40(10):737-751. 5. Sui A,etal.The pharmacological role of histone demethylase JMJD3 inhibitor GSK-J4 on glioma cells.Oncotarget. 2017 Aug 2;8(40):68591-68598.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Bioactive Compound Library Methylation Compound Library Stem Cell Differentiation Compound Library Chromatin Modification Compound Library Histone Modification Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Epigenetics Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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