性能参数

产品名称

GSK J4 HCl

规格

10mM (in 1mL DMSO) 10mg 50mg

货号

GOY-Y3576

 含量

>98.00%

CAS

1797983-09-5

别名

N/A

化学名

ethyl 3-[[2-pyridin-2-yl-6-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidin-4-yl]amino]propanoate

分子式

C24H27N5O2.HCl

分子量

分子量 453.96

溶解度

≥ 13.9 mg/mL in DMSO, <2.53 mg/mL in EtOH, <2.4 mg/mL in H2O

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 J4 is a potent cell-permeable inhibitor of the histone H3 lysine 27 (H3K27) demethylase JMJD3, an essential component of regulatory transcriptional chromatin complexes, with the half maximal inhibition concentration IC50 value > 50 μM in vitro [1].

GSK J4 is an ethyl ester derivative of GSK J1, which is a potent JMJD3 inhibitor (IC50: 60 nM) with restricted cellular permeability due to the highly polar carboxylate group, and rapidly hydrolyzed by macrophage esterase upon administration leading to the generation of pharmacologically relevant intracellular concentration of GSK-J1 [1].

GSK J4 has also been found to dose-dependently inhibit the production of tumor-necrosis factor-α (TNF-α), a LPS-driven cytokine involved in various fnflammatory disorders, with IC50 value of 9μM [1].

鸟苷-5'-三磷酸三钠盐  36051-31-7  6-氨基烟酸甲酯  36052-24-1

5-溴-2,4-二氯嘧啶  36082-50-5  4-氨基-5-咪唑甲酰胺  360-97-4

N-苄基酮  3612-20-2  氯甲酰乙酸乙酯  36239-09-5

2-氯-3-吡啶甲醛  36404-88-3  3-氰基-1,2,4-三氮唑  636171

4-溴-1-氟-2-硝基苯  364-73-8  4-氟-3-硝基苯胺  364-76-1

3-吖丁啶羧酸  36476-78-5  N-(2-氯乙default-locale

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