GSK-J4 HCl

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Chemical Structure| 1797983-09-5 同义名 : GSK-J4 (hydrochloride);GSK-J4 hydrochloride
CAS号 : 1797983-09-5
货号 : A608057
分子式 : C24H28ClN5O2
纯度 : 98%
分子量 : 453.964
MDL号 : MFCD26142638
存储条件:

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 60 mg/mL(132.17 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 3 mg/mL(6.61 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方:
生物活性
靶点
  • KDM6

    JMJD3, IC50:60 nM

描述 The jumonji histone demethylases are essential components of transcriptional chromatin complexes. GSK-J4 HCl is a cell-permeable prodrug of GSK-J1, which selectively inhibits H3K27 demethylases JMJD3 and UTX with an IC50 value of 60nM. GSK-J4 at 25μM prevented JMJD3-induced loss of nuclear H3K27me3 immunostaining in Flag-JMJD3-transfected HeLa cells. GSK-J4 treatment also increased the total nuclear H3K27me3 level in non-transfected cells. GSK-J4 at 30μM inhibited LPS-induced inflammation in human primary macrophages derived from healthy volunteers. The IC50 value of GSK-J4 for inhibiting TNF-α protein production was 9μM. GSK-J4 at a concentration of 30μM prevented LPS-induced loss of H3K27me3 associated with the TNFA TSS[2]. In dextran sodium sulphate-treated mice, treatment with 1mg/kg GSK-J4 for 5 days reduced bodyweight loss and morbidity rate compared to the control group[3].
作用机制 GSK-J4 HCl is the ethyl ester derivative of GSK-J1, a selective inhibitor of H3K27 histone demethylase JMJD3 and UTX. GSK-J1 binds in the catalytic pocket of JMJD3. The bidentate interaction between the pyridyl-pyrimidine biaryl of GSK-J1 and the catalytic metal is critical for enzyme inhibition[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CUTLL1 2 μM Growth inhibitory assay affects cell growth 25132549
CUTLL1 2 μM Apoptosis assay induces apoptosis 25132549
CUTLL1 2 μM Function assay induces cell cycle arrest 25132549
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.01mL

2.20mL

1.10mL

22.03mL

4.41mL

2.20mL

参考文献

[1]Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8

[2]Kruidenier L, Chung CW, Cheng Z, Liddle J, Che K, Joberty G, Bantscheff M, Bountra C, Bridges A, Diallo H, Eberhard D, Hutchinson S, Jones E, Katso R, Leveridge M, Mander PK, Mosley J, Ramirez-Molina C, Rowland P, Schofield CJ, Sheppard RJ, Smith JE, Swales C, Tanner R, Thomas P, Tumber A, Drewes G, Oppermann U, Patel DJ, Lee K, Wilson DM. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature. 2012 Aug 16;488(7411):404-8

[3]Doñas C, Neira J, Osorio-Barrios F, Carrasco M, Fernández D, Prado C, Loyola A, Pacheco R, Rosemblatt M. The demethylase inhibitor GSK-J4 limits inflammatory colitis by promoting de novo synthesis of retinoic acid in dendritic cells. Sci Rep. 2021 Jan 14;11(1):1342