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文件

SML0701

GSK-J4

Name: GSK-J4
Brand: SIGMA

≥98% (HPLC)

别名:

3-((6-(4,5-二氢-1H-苯并[d]氮杂卓-3(2H)-基)-2-(吡啶-2-基)嘧啶-4-基)氨基)丙酸乙酯

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About This Item

经验公式（希尔记法）:

C₂₄H₂₇N₅O₂

CAS号:

1373423-53-0

分子量:

417.50

MDL编号:

MFCD22683852

UNSPSC代码:

51111800

PubChem化学物质编号:

329825585

NACRES:

NA.77

质量水平

100

检测方案

≥98% (HPLC)

形式

powder

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: 20 mg/mL, clear

储存温度

2-8°C

SMILES字符串

O=C(OCC)CCNC1=CC(N2CCC(C=CC=C3)=C3CC2)=NC(C4=CC=CC=N4)=N1

InChI

1S/C24H27N5O2/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)

InChI key

WBKCKEHGXNWYMO-UHFFFAOYSA-N

应用

GSK-J4已被用于研究KDM2B（Jumjji（JmjC）结构域组蛋白3赖氨酸36（H3K36）二脱甲基酶）抑制对胶质母细胞瘤细胞的存活和DNA修复潜力的影响。它还被用于磺酰罗丹明B（SRB）细胞生长检测和细胞活力检测。

生化/生理作用

GSK-J4一种细胞渗透性前药，可被巨噬细胞酯酶快速水解成GSK-J1。GSK-J1是一种有效的选择性jumonji H3K27去甲基化酶抑制剂。含有组蛋白去甲基化酶（JHDMs）的Jumonji C结构域是Fe（II）和α-酮戊二酸依赖性酶，它能够氧化甲基化组蛋白赖氨酸残基，从而导致它们的去甲基化。GSK-J1对KDM6亚家族成员JMJD3和UTX具有选择性，在JMJD3检测中的IC₅₀为60 nM，对JMJ家族的其他去甲基化酶以及超过100种测试激酶和组蛋白脱乙酰酶无活性。前药GSK-J4可抑制TNF-α的产生，在LPS刺激的人巨噬细胞中IC₅₀为9μM，并且可阻断类风湿性关节炎患者的巨噬细胞产生TNF-α。有关GSK-J4的特征描述和GSK-J1的完整特征描述，请访问结构基因组学联盟（SGC）网站上的GSK-J1探针摘要。

想要了解用于表观遗传靶标的其他SGC化学探针，请访问sigma.com/sgc

特点和优势

GSK-J4 是一种表观遗传化学探针，是通过与Structural Genomics Consortium (SGC)合作研发的。想要了解更多信息并查看其他SGC表观遗传探针，请访问sigma.com/SGC。

这种化合物是基因调控研究的特色产品。点击此处发现更多特色基因调控产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

其他说明

GSK-J4经过化学探针门户网（Chemical Probes Portal）的专业评审和推荐。有关更多信息，请访问化学探针门户网上的GSK-J4探针摘要。

WGK

WGK 3

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Not applicable

闪点(°C)

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Genome-wide association between Six4, MyoD, and the histone demethylase Utx during myogenesis.

Imane Chakroun et al.

FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 29(11), 4738-4755 (2015-08-01)

Adult skeletal muscles can regenerate after injury, due to the presence of satellite cells, a quiescent population of myogenic progenitor cells. Once activated, satellite cells repair the muscle damage by undergoing myogenic differentiation. The myogenic regulatory factors (MRFs) coordinate the

The H3K27me3-demethylase KDM6A is suppressed in breast cancer stem-like cells, and enables the resolution of bivalency during the mesenchymal-epithelial transition.

Joseph H Taube et al.

Oncotarget, 8(39), 65548-65565 (2017-10-17)

The deposition of the activating H3K4me3 and repressive H3K27me3 histone modifications within the same promoter, forming a so-called bivalent domain, maintains gene expression in a repressed but transcription-ready state. We recently reported a significantly increased incidence of bivalency following an

Targeting glioma stem?like cell survival and chemoresistance through inhibition of lysine?specific histone demethylase KDM2B.

Staberg M, et al.

Molecular Oncology, 12(3), 406-420 (2018)

EZH2, JMJD3, and UTX epigenetically regulate hepatic plasticity inducing retro-differentiation and proliferation of liver cells.

Natalia Pediconi et al.

Cell death & disease, 10(7), 518-518 (2019-07-10)

Modification of histones by lysine methylation plays a role in many biological processes, and it is dynamically regulated by several histone methyltransferases and demethylases. The polycomb repressive complex contains the H3K27 methyltransferase EZH2 and controls dimethylation and trimethylation of H3K27

Neuronal activity controls Bdnf expression via Polycomb de-repression and CREB/CBP/JMJD3 activation in mature neurons.

Ernest Palomer et al.

Nature communications, 7, 11081-11081 (2016-03-25)

It has been recently described that in embryonic stem cells, the expression of some important developmentally regulated genes is repressed, but poised for fast activation under the appropriate stimuli. In this work we show that Bdnf promoters are repressed by

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GSK-J4

≥98% (HPLC)

About This Item

属性

质量水平

检测方案

形式

储存条件

颜色

溶解性

储存温度

SMILES字符串

InChI

InChI key

相关类别

说明

应用

生化/生理作用

特点和优势

其他说明

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