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AB144395

GSK-J4, histone demethylase JMJD3/UTX inhibitor

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(6 Publications)

MW 454 Da, Purity >98%. Cell permeable histone demethylase JMJD3/UTX inhibitor. Attenuates LPS-induced proinflammatory cytokine production in macrophages (IC50 = 9 μM, TNF-α release). Prodrug of GSK-J1. Rapidly hydrolyzes to GSK-J1 intracellularly.
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Chemical Structure - GSK-J4, histone demethylase JMJD3/UTX inhibitor (AB144395)
  • Chemical Structure

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Chemical Structure - GSK-J4, histone demethylase JMJD3/UTX inhibitor (AB144395)

2D chemical structure image of ab144395, GSK-J4, histone demethylase JMJD3/UTX inhibitor

Key facts

CAS number

1797983-09-5

Purity

>98%

Form

Solid

form

Molecular weight

454 Da

Molecular formula

C<sub>2</sub><sub>4</sub>H<sub>2</sub><sub>8</sub>ClN<sub>5</sub>O<sub>2</sub>

PubChem

71729974

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 100mM

Biochemical name

GSK-J4 hydrochloride

Biological description

Cell permeable histone demethylase JMJD3/UTX inhibitor. Attenuates LPS-induced proinflammatory cytokine production in macrophages (IC50 = 9 μM, TNF-α release). Prodrug of GSK-J1. Rapidly hydrolyzes to GSK-J1 intracellularly.

Canonical smiles

CCOC(=O)CCNC1=CC(=NC(=N1)C2=CC=CC=N2)N3CCC4=CC=CC=C4CC3.Cl

InChi

InChI=1S/C24H27N5O2.ClH/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);1H

InChiKey

TYXWLTBYINKVNT-UHFFFAOYSA-N

IUPAC Name

ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate;hydrochloride

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months

Product protocols

Publications (6)

Recent publications for all applications. Explore the full list and refine your search

Environmental toxicology 38:754-769 PubMed36537648

2022

JMJD3 downregulates IL4i1 aggravating lipopolysaccharide-induced acute lung injury via H3K27 and H3K4 demethylation.

Applications

Unspecified application

Species

Unspecified reactive species

Yizhuo Gao,Na Wang,Dong Jia

Cell death discovery 8:475 PubMed36456564

2022

H3K27 tri-demethylase JMJD3 inhibits macrophage apoptosis by promoting ADORA2A in lipopolysaccharide-induced acute lung injury.

Applications

Unspecified application

Species

Unspecified reactive species

Yizhuo Gao,Na Wang,Dong Jia

Stem cell research & therapy 12:14 PubMed33413595

2021

microRNA-27b shuttled by mesenchymal stem cell-derived exosomes prevents sepsis by targeting JMJD3 and downregulating NF-κB signaling pathway.

Applications

Unspecified application

Species

Unspecified reactive species

Jia Sun,Xuan Sun,Junhui Chen,Xin Liao,Yixuan He,Jinsong Wang,Rui Chen,Sean Hu,Chen Qiu

Journal of immunology (Baltimore, Md. : 1950) 202:1088-1098 PubMed30626691

2019

Histone H3K27 Demethylase Negatively Controls the Memory Formation of Antigen-Stimulated CD8 T Cells.

Applications

Unspecified application

Species

Unspecified reactive species

Takeshi Yamada,Shogo Nabe,Koji Toriyama,Junpei Suzuki,Kazuki Inoue,Yuuki Imai,Atsushi Shiraishi,Katsuto Takenaka,Masaki Yasukawa,Masakatsu Yamashita

Neuropharmacology 141:113-125 PubMed30165076

2018

The histone demethylase KDM6B in the medial prefrontal cortex epigenetically regulates cocaine reward memory.

Applications

Unspecified application

Species

Unspecified reactive species

Yu-Xiang Zhang,Rita C Akumuo,Rodrigo A España,Chun-Xia Yan,Wen-Jun Gao,Yan-Chun Li

Anticancer research 36:6083-6092 PubMed27793936

2016

Impact of H3K27 Demethylase Inhibitor GSKJ4 on NSCLC Cells Alone and in Combination with Metformin.

Applications

Unspecified application

Species

Unspecified reactive species

Hikaru Watarai,Masashi Okada,Kenta Kuramoto,Hiroyuki Takeda,Hirotsugu Sakaki,Shuhei Suzuki,Shizuka Seino,Hiroyuki Oizumi,Mitsuaki Sadahiro,Chifumi Kitanaka
View all publications

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