• 产品描述： GSK J4 HCl是一种细胞渗透性的GSK J1前体药物，是第一个选择性H3K27组蛋白去甲基化酶JMJD3和UTX抑制剂，无细胞试验中IC50为60 nM，抑制JMJ家族的去甲基化酶活性

• 靶点： JMJD3 (Cell-free assay):60 nM;HistoneDemethylase

• 体外研究：
  GSK-J4 Hydrochloride has cellular activity in Flag-JMJD3-transfected HeLa cells, in which GSK-J4 prevents the JMJD3-induced loss of nuclear H3K27me3 immunostaining. Administration of GSK-J4 increases total nuclear H3K27me3 levels in untransfected cells. GSK-J4 significantly reduces the expression of 16 of 34 LPS-driven cytokines, including tumour-necrosis factor-α (TNF-α).
  GSK-J4 Hydrochloride (5 μM; 48 hours) causes a more than 3-fold increase in mouse podocyte H3K27me3 content. H3K27me3 levels in cultured podocytes, GSK-J4 reduces Jagged-1 mRNA and Jagged-1 protein levels. Correspondingly, when exposed podocytes to the inducer of dedifferentiation TGF-β1, pretreatment with GSK-J4 preventes both the increase in intracellular N1-ICD levels and the increase in α-SMA and the decrease in podocin mRNA levels.
  GSK-J4 Hydrochloride (10, 25 nM) acts upon DCs promoting the differentiation of Treg cells, improving Treg stability and suppressive capacities, without affecting the differentiation of Th1 and Th17 cells.
  GSK-J4 Hydrochloride inhibits JMJD3 expression that is induced by TGF-β1.
  GSK-J4 Hydrochloride inhibits H3K4 demethylation at Xist, Nodal, and HoxC13 in female embryonic stem cells.

• 体内研究：
  GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A. It inhibits LPS-induced TNF-α production in human primary macrophages. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.

• 细胞实验： Cell lines: Mouse podocytes Concentrations: 5 μM Incubation Time: 48 h Method: Cells were serum starved for 4 hours, followed by treatment with EPZ-6438 (10 μM) or GSK-J4 (5 μM) for 48 hours.

• 动物实验： Animal Models: BALB/c mice Dosages: 10 mg/kg Administration: i.p.

• 参考文献：
  1. Kruidenier L, et al. Nature, 2012, 488(7411), 404-408. 2. Majumder S, et al. J Clin Invest. 2018 Jan 2;128(1):483-499.

• 溶解性： Soluble  in  DMSO、Ethanol、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.203 ml	11.014 ml	22.028 ml
  5 mM	0.441 ml	2.203 ml	4.406 ml
  10 mM	0.22 ml	1.101 ml	2.203 ml
  50 mM	0.044 ml	0.22 ml	0.441 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *