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GSK-J4 Hydrochloride

GSK-J4 Hydrochloride (GSK J4 HCl) 是 H3K27me3/me2 去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 双抑制剂，IC50分别为 8.6 和 6.6 μM。它是 GSK-J1 的乙酯衍生物，体外 IC50 值大于 50 μM。它抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α，IC50值为 9 μM。

CAS号

1797983-09-5

分子式

C24H28ClN5O2

主要靶点

Histone Demethylase

仅限科研使用

Cat No : CM04531

Print datasheet

Synonyms

GSK J4 HCl (1373423-53-0 free base)|GSK J4 HCl

验证数据展示

  • CAS No.: 1797983-09-5

    GSK-J4 Hydrochloride
    CAS#: 1797983-09-5

产品信息

GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.

CAS号 1797983-09-5
分子式 C24H28ClN5O2
主要靶点 Histone Demethylase
主要通路 表观遗传
分子量 453.97
纯度 98.36%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 GSK J4 HCl (1373423-53-0 free base)|GSK J4 HCl

靶点活性

JMJD3(in vitro):50 μM|JMJD3(cell free):60 nM

体内活性

Acting as a prodrug, GSK-J4 is rapidly hydrolyzed in cells to the otherwise cell impermeable GSK-J1, which exhibits an IC50 value of 60 nM for the purified enzyme. The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.

体外活性

When administered to human primary macrophages, GSK-J4 can reduce LPS-induced proinflammatory cytokine production, most notably including that of TNFα (IC50 = 9 μM).

溶解度

Ethanol:20 mg/mL,DMSO:30 mg/mL

参考文献

1.Yan N,etal.GSKJ4, an H3K27me3 demethylase inhibitor, effectively suppresses the breast cancer stem cells.Exp Cell Res. 2017 Oct 15;359(2):405-414.
2.Kruidenier L,etal.A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response.Nature. 2012 Aug 16;488(7411):404-8.
3.Li Y,etal.Therapeutic potential of GSK-J4, a histone demethylase KDM6B/JMJD3 inhibitor, for acute myeloid leukemia.J Cancer Res Clin Oncol. 2018 Jun;144(6):1065-1077.
4.Mandal C,etal.GSK-J4-Mediated Transcriptomic Alterations in Differentiating Embryoid Bodies.Mol Cells. 2017 Oct;40(10):737-751.
5.Sui A,etal.The pharmacological role of histone demethylase JMJD3 inhibitor GSK-J4 on glioma cells.Oncotarget. 2017 Aug 2;8(40):68591-68598.

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