性能参数

产品名称

GSK-J1 lithium salt

规格

10mg 50mg

货号

GOY-Y3501

 含量

>98.00%

CAS

N/A

别名

N/A

化学名

N/A

分子式

C22H22LiN5O2

分子量

分子量 395.38

溶解度

Soluble in DMSO

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. IC50: 60 nM (KDM6B)[2]

GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner[1]. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1 mM α-ketoglutarate, with IC50 of 11 μM and 94 μM, respectively[3].

[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]. Heinemann B, et al. Inhibition of demethylases by GSK-J1/J4. Nature. 2014 Oct 2;514(7520):E1-2. [3]. Horton JR, et al. Characterization of a Linked Jumonji Domain of the KDM5/JARID1 Family of Histone H3 Lysine 4 Demethylases. J Biol Chem. 2016 Feb 5;291(6):2631-46.

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