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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-GSK-J4
GSK-J4

Chemical Structure : GSK-J4

CAS No.: 1373423-53-0

GSK-J4 (GSK-J4 hydrochloride)

货号: PC-21211Not For Human Use, Lab Use Only.

GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively, GSK-J4 s a cell permeable prodrug of GSK-J1.

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10 mg ¥880 In stock
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50 mg ¥2280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively, GSK-J4 s a cell permeable prodrug of GSK-J1.
GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with IC50 of 9 uM.
GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining in Flag-JMJD3-transfected HeLa cells.
GSK-J4 inhibits JMJD3 expression that is induced by TGF-β1, inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells.
GSK-J4 attenuates the development of kidney disease in diabetic mice.

物理化学性质&存储条件

分子量 453.97
分子式 C24H28ClN5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate hydrochloride

参考文献

1. Kruidenier L, et al. Nature. 2012 Aug 16;488(7411):404-8.

2. Majumder S, et al. J Clin Invest. 2018 Jan 2;128(1):483-499.

3. Donas C, et al. J Autoimmun. 2016 Dec;75:105-117.

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