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GSK-J4

Catalog No. T3100 CAS 1373423-53-0

Synonyms: GSK J4 HCl

GSK-J4 (GSK J4 HCl) is a potent H3K27me3 demethylase inhibitor, with IC50s of 8.6 μM and 6.6 μM towards KDM6B and KDM6A respectively. It is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.

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GSK-J4, CAS 1373423-53-0

Pack Size	Availability	Price/USD
2 mg	In stock	$ 51.00
5 mg	In stock	$ 83.00
10 mg	In stock	$ 131.00
25 mg	In stock	$ 239.00
50 mg	In stock	$ 384.00
100 mg	In stock	$ 582.00
200 mg	In stock	$ 737.00
1 mL * 10 mM (in DMSO)	In stock	$ 144.00

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Purity: 99.98%

Purity: 98.24%

Purity: 97.07%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK-J4 (GSK J4 HCl) is a potent H3K27me3 demethylase inhibitor, with IC50s of 8.6 μM and 6.6 μM towards KDM6B and KDM6A respectively. It is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.
Targets&IC50	JMJD3:
In vivo	GSK-J4 (0.5 mg/kg, i.p.) significantly reduces the severity and delays the onset of the disease of the mouse model of experimental autoimmune encephalomyelitis[2].
Animal Research	GSK-J4 is prepared in DMSO and diluted 1/10 with ethanol.Six-to eight-week-old female C57BL/6 WT mice are injected by subcutaneous injection (s.c.) with 50 μg myelin oligodendrocyte glycoprotein 35-55 peptide (pMOG) emulsified in Complete Freund's Adjuvant (CFA) supplemented with heat-inactivated Mycobacterium tuberculosis H37 RA. In addition, mice receive intraperitoneal injection (i.p.) of 500 ng of pertussis toxin on days 0 and 2. Clinical signs are assessed daily according to the following scoring criteria: 0, no detectable signs; 1, flaccid tail; 2, hind limb weakness or abnormal gait; 3, complete hind limb paralysis; 4, paralysis of fore and hind limbs; and 5, moribund or death. A stock solution of GSK-J4 of 42 mg/mL (100 mM) is prepared in dimethyl sulfoxide (DMSO) to preserve stability. Before injection, the stock solution is diluted 1/10 with ethanol (DMSO: ethanol, 1:10 v/v) and brought to a final concentration of 140 μg/mL in PBS. In systemic drug evaluation experiments, each mouse receive daily i.p. injections (from days 0-5) of 100 μL of this solution containing 14.0 μg of the GSK-J4 (equivalent to 0.56 mg/kg of the drug). Control mice receive 100 μL of the vehicle during the same period. In other EAE experiments, 106 bone marrow-derived DCs from WT mice are treated with GSK-J4 or vehicle alone for 16 h, pulsed with 5 μg/mL of pMOG for 4 h and then transferred i.v. into WT C57BL/6 recipient mice 14 and 7 days before EAE induction. In other adoptive transfer EAE experiments, CD4+Foxp3+ Treg cells generated in the presence or absence of 25 nM GSK-J4 are purified by cell sorting and then 0.75×106 transferred i.v. into WT C57BL/6 recipient mice 1 day before EAE induction.

Synonyms	GSK J4 HCl
Molecular Weight	417.5
Formula	C24H27N5O2
CAS No.	1373423-53-0

Storage

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

Solubility Information

Ethanol: 41.75 mg/ml(100 mM)

DMSO: 41.75 mg/ml(100 mM)

References and Literature

1. Kruidenier L, et al. Nature, 2012, 488(7411), 404-408. 2. Donas C, et al. The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs. J Autoimmun. 2016 Dec;75:105-117. 3. Lin B, Lu B, Hsieh I, et al. Synergy of GSK-J4 With Doxorubicin in KRAS-Mutant Anaplastic Thyroid Cancer[J]. Frontiers in Pharmacology. 2020, 11. 4. Chen, Hong, et al. . Histone demethylase UTX is a therapeutic target for diabetic kidney disease [J]. J Physiol. 2019 Mar;597(6):1643-1660.

Citations

1. Zheng B, Liu J, Gao A, et al. Epigenetic reprogramming of H3K27me3 and DNA methylation during leaf-to-callus transition in peach. Horticulture Research. 2022 2. Lin B, Lu B, Hsieh I, et al. Synergy of GSK-J4 With Doxorubicin in KRAS-Mutant Anaplastic Thyroid Cancer. Frontiers in Pharmacology. 2020, 11

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Chromatin Modification Compound Library Bioactive Compound Library Epigenetics Compound Library Methylation Compound Library Histone Modification Compound Library Bioactive Compounds Library Max Endoplasmic Reticulum Stress Compound Library NO PAINS Compound Library Apoptosis Compound Library

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Keywords

GSK-J4 1373423-53-0 Apoptosis Chromatin/Epigenetic Histone Demethylase GSKJ4 Inhibitor H3K27me3/me2 demethylase diabetic inflammation Th17 TGF-β mice cells dendritic GSK-J-4 inhibit Th1 GSK J4 HCl GSK J4 inhibitor

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