GSK-J4

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Chemical Structure| 1373423-53-0 同义名 : -
CAS号 : 1373423-53-0
货号 : A307207
分子式 : C24H27N5O2
纯度 : 99%+
分子量 : 417.5
MDL号 : MFCD22683852
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 GSK-J4, acting as a robust dual inhibitor of the demethylases JMJD3/KDM6B and UTX/KDM6A with IC50 values of 8.6 μM and 6.6 μM respectively, curbs LPS-induced TNF-α output in human primary macrophages with an IC50 of 9 μM. It effectively maintains H3K27me3 levels in the nucleus, notably reducing the expression of multiple LPS-driven cytokines, including TNF-α.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

11.98mL

2.40mL

1.20mL

23.95mL

4.79mL

2.40mL
参考文献

[1]Kruidenier L, et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8.

[2]Majumder S, et al. Shifts in podocyte histone H3K27me3 regulate mouse and human glomerular disease. J Clin Invest. 2018 Jan 2;128(1):483-499.

[3]Donas C, et al. The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs. J Autoimmun. 2016 Dec;75:105-117.