化合物GSK J1 T6847

Product Introduction
Bioactivity


英文名: GSK-J1

描述: GSK-J1 是一种高效的 H3K27 组蛋白去甲基化酶抑制剂，在无细胞试验中对 JMJD3 (KDM6B) 和 UTX (KDM6A) 的 IC50 分别为 28 nM 和 53 nM，比其他测试的去甲基化酶选择性高 10 倍以上。

激酶实验: Purified JmjD3 (1 μM) and UTX (3 μM) is incubated with 10 μM peptide [BiotinKAPRKQLATKAARK(me3 )SAPATGG] in 50 mM HEPES pH 7.5, 150 mM KCl, 50 μM (NH4)2SO4·FeSO4·Water, 1 mM 2-oxoglutarate, and 2 mM ascorbate (JmjD3, 3 minutes at 25°C; UTX, 20 minutes at 25°C) with various concentration of the inhibitor (0, 0.005, 0.01, 0.02, 0.05, 0.1 μM). 10 mM EDTA is added to stop the reaction. The reaction is desalted by zip tip and spotted on a MALDI plate with α-cyano-4-hydroxycinnamic acid MALDI matrix. Samples are analysed on a MALDI-TOF R system.

体外活性: In HEK-293 cells, GSK-J1 inhibits the activities of transiently transfected JMJD3 and UTX. GSK-J1 also inhibits TNF-α production by human primary macrophages by increasing total nuclear H3K27me3 levels. [1] In MC3T3-E1 cells, GSK-J1 suppresses Runx2 and Osterix expressions and ALP activity, and increases the global levels of H3K27me3. [2]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 38.9 mg/mL (100 mM)
DMSO : 38.9 mg/mL (100 mM)


关键字: inhibit | Inhibitor | GSK-J1 | Histone Demethylase | GSKJ1 | GSK-J-1

相关产品: Eicosapentaenoic Acid | KDM5-C49 HCl | Seclidemstat | GSK-LSD1 | GSK-LSD1 dihydrochloride | LSD1-IN-20 | Procaine | NCD38 TFA | Ryuvidine | IOX1

相关库: Anti-Aging Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Epigenetics Compound Library | Methylation Compound Library | Stem Cell Differentiation Compound Library | Histone Modification Compound Library | NO PAINS Compound Library | Bioactive Compound Library | Chromatin Modification Compound Library

化合物GSK J1 T6847信息由TargetMol中国为您提供，如您想了解更多关于化合物GSK J1 T6847报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途