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SML0701

GSK-J4

Name: GSK-J4
Brand: SIGMA

≥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

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

desiccated

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属性

产品名称

GSK-J4, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 20 mg/mL, clear

storage temp.

2-8°C

SMILES string

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

说明

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。

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存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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