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Merck
CN

SML0701

GSK-J4

≥98% (HPLC), jumonji H3K27 demethylase inhibitor, powder

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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关于此项目

经验公式（希尔记法）:
C24H27N5O2
化学文摘社编号:
1373423-53-0
分子量:
417.50
UNSPSC Code:
51111800
PubChem Substance ID:
329825585
NACRES:
NA.77
MDL number:
MFCD22683852

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产品名称

GSK-J4, ≥98% (HPLC)

SMILES string

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

InChI key

WBKCKEHGXNWYMO-UHFFFAOYSA-N

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)

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

相关类别

Application

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。

Biochem/physiol Actions

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
GSK-J4是一种有效的选择性jumonji H3K27去甲基化酶抑制剂。

Features and Benefits

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。

Other Notes

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。

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000215864
0000215863
0000215864
0000215863
0000193051

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访问文档库

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
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)
Inhibitor of H3K27 demethylase JMJD3/UTX GSK-J4 is a potential therapeutic option for castration resistant prostate cancer.
Morozov V M, et al.
Oncotarget, 8(37), 62131-62131 (2017)
Cristian Doñas et al.
Journal of autoimmunity, 75, 105-117 (2016-08-17)
As it has been established that demethylation of lysine 27 of histone H3 by the lysine-specific demethylase JMJD3 increases immune responses and thus elicits inflammation, we hypothesize that inhibition of JMJD3 may attenuate autoimmune disorders. We found that in vivo administration
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
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