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Histone Lysine Demethylase Inhibitor VIII, GSK-J4-CAS 1373423-53-0-Calbiochem

品牌
Sigma-Aldrich
CAS
1373423-53-0
货号
420205
规格纯度
Histone Lysine Demethylase Inhibitor VIII, GSK-J4, CAS 1373423-53-0, is converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (~ 25 to 50 μM in HeLa cultures).
参考价格
3056.54 *本价格含增值税费
促销
服务
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  • 增值税票
数量
-+
产品名称:
1373423-53-0
Histone Lysine Demethylase Inhibitor VIII, GSK-J4-CAS 1373423-53-0-Calbiochem
GSK-J1 Pro-Drug, JHDM Inhibitor II Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate
产品介绍:

产品说明

一般描述

The H3K27me3 demethylase inhibitor GSK-J1 (Cat. No. 420204) against JMJD3 and UTX is made cell-permeable by ethyl ester derivatization to facilitate cellular delivery ([medium GSK-J4]t=0 = 30 µM; [cellular GSK-J1]t=1h = 1.6 µM). The pro-drug GSK-J4, being ineffective in cell-free assays, is effectively converted to GSK-J1 intracellularly and inhibits nuclear H3K27me3 levels in both untransfected and JMJD3-transfected HeLa cells (25 to 50 µM). Simultaneous inhibition of cellular JMJD3 and UTX by GSK-J4 treatment is shown to block LPS-induced production of several proinflammatory cytokines, including TNF-α (IC50 = 9 µM by ELISA), in primary human macrophage cultures.
A cell-permeable GSK-J1 (Cat. No. 420204) prodrug that is ineffective in cell-free assays, but is effectively converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (effective conc. 25 to 50 µM in HeLa cultures). GSK-J4 treatment is shown to block LPS-induced TNF-α production in primary human macrophage cultures (IC50 = 9 µM by ELISA).


This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the SGC website (http://www.thesgc.org/scientists/chemical_probes/GSKJ1).

包装

10 mg in Glass bottle
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Reversible: yes

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months for -20°C.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C24H27N5O2
分子量417.50
MDL编号MFCD22683852

产品性质

质量水平100
测定≥98% (HPLC)
形式semisolid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 tan
溶解性DMSO: 100 mg/mL
运输ambient
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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