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CAS No.: 1797983-09-5

GSK-J4 HCl Catalog No. CSN19181

Synonyms: GSK-J4 (hydrochloride);1373423-53-0(Free Base);GSK-J4 HCl

GSK-J4 HCl is selective inhibitor of jumonji H3K27 demethylase. It can attenuate lipopolysaccharide (LPS)-induced proinflammatory cytokine production.

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技术信息

生物活性

描述The jumonji histone demethylases are essential components of transcriptional chromatin complexes. GSK-J4 HCl is a cell-permeable prodrug of GSK-J1, which selectively inhibits H3K27 demethylases JMJD3 and UTX with an IC50 value of 60nM. GSK-J4 at 25μM prevented JMJD3-induced loss of nuclear H3K27me3 immunostaining in Flag-JMJD3-transfected HeLa cells. GSK-J4 treatment also increased the total nuclear H3K27me3 level in non-transfected cells. GSK-J4 at 30μM inhibited LPS-induced inflammation in human primary macrophages derived from healthy volunteers. The IC50 value of GSK-J4 for inhibiting TNF-α protein production was 9μM. GSK-J4 at a concentration of 30μM prevented LPS-induced loss of H3K27me3 associated with the TNFA TSS^[2]. In dextran sodium sulphate-treated mice, treatment with 1mg/kg GSK-J4 for 5 days reduced bodyweight loss and morbidity rate compared to the control group^[3].
作用机制GSK-J4 HCl is the ethyl ester derivative of GSK-J1, a selective inhibitor of H3K27 histone demethylase JMJD3 and UTX. GSK-J1 binds in the catalytic pocket of JMJD3. The bidentate interaction between the pyridyl-pyrimidine biaryl of GSK-J1 and the catalytic metal is critical for enzyme inhibition^[1].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CUTLL1	2 μM	Growth inhibitory assay	-	affects cell growth	25132549
CUTLL1	2 μM	Apoptosis assay	-	induces apoptosis	25132549
CUTLL1	2 μM	Function assay	-	induces cell cycle arrest	25132549

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参考文献

[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
[2] 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
[3] Doñas C, Neira J, Osorio-Barrios F, Carrasco M, Fernández D, Prado C, Loyola A, Pacheco R, Rosemblatt M. The demethylase inhibitor GSK-J4 limits inflammatory colitis by promoting de novo synthesis of retinoic acid in dendritic cells. Sci Rep. 2021 Jan 14;11(1):1342

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2028 mL
- 11.0142 mL
- 22.0284 mL
- 5 mM
- 0.4406 mL
- 2.2028 mL
- 4.4057 mL
- 10 mM
- 0.2203 mL
- 1.1014 mL
- 2.2028 mL

技术信息

CAS号

1797983-09-5

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H28ClN5O2

运输

蓝冰

分子量

453.96

别名

GSK-J4 (hydrochloride);1373423-53-0(Free Base);GSK-J4 HCl

溶解度

DMSO	88.0 mg/mL (193.8 mM) warming
Ethanol	90.0 mg/mL (198.3 mM) warming

动物实验配方

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CUTLL1	2 μM	Growth inhibitory assay	-	affects cell growth	25132549
CUTLL1	2 μM	Apoptosis assay	-	induces apoptosis	25132549
CUTLL1	2 μM	Function assay	-	induces cell cycle arrest	25132549
CUTLL1	6 μM	Kinase assay	-	leads to increased H3K27me3	25132549
ESCs	1.8 µM	Function assay	-	induces DNA damage along with activation of the DNA damage response	26759175
H3.3	6 μM	Kinase assay	-	increases K29 methylation	25401693
H3.3	6 μM	Growth inhibitory assay	-	inhibits K29M glioma cell growth	25401693
human astrocytes	6 μM	Kinase assay	-	increases K33 methylation	25401693
human astrocytes	6 μM	Growth inhibitory assay	-	inhibits K33M glioma cell growth	25401693
Raw 264.7	0.8192 µM	Function assay	-	inhibits TNF-α production	26776360
SF7761	6 μM	Kinase assay	-	increases K27 methylation	25401693
SF7761	6 μM	Growth inhibitory assay	-	inhibits K27M glioma cell growth	25401693
SF8628	6 μM	Kinase assay	-	increases K28 methylation	25401693
SF8628	6 μM	Growth inhibitory assay	-	inhibits K28M glioma cell growth	25401693
SF9012	6 μM	Kinase assay	-	increases K30 methylation	25401693
SF9012	6 μM	Growth inhibitory assay	-	inhibits K30M glioma cell growth	25401693
SF9402	6 μM	Kinase assay	-	increases K31 methylation	25401693
SF9402	6 μM	Growth inhibitory assay	-	inhibits K31M glioma cell growth	25401693
SF9427	6 μM	Kinase assay	-	increases K32 methylation	25401693
SF9427	6 μM	Growth inhibitory assay	-	inhibits K32M glioma cell growth	25401693
TG neurons	50 μM	Function assay	-	inhibits HSV-1 reactivation from sensory neurons	25552720
Th17	80 nM	Function assay	-	inhibits cell differentiation	25840993
β-cells	20 μM	Function assay	-	blunts IFNγ, Il-1β, and TNFα-induced chemokine gene expression	26505193
β-cells	20 μM	Function assay	-	induces β-cell dysfunction	26505193

GSK-J4 HCl Catalog No. CSN19181

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