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GSK-J4 Hydrochloride

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

diabetic|demethylase|dendritic|GSK-J4|GSKJ4 Hydrochloride|GSK-J4 Hydrochloride|GSK-J-4 Hydrochloride|GSK J4 HCl|GSK J4 HCl (1373423-53-0 free base)|GSK J4 Hydrochloride|inhibit|inflammation|H3K27me3/me2|HistoneDemethylase|Histone Demethylase|1373423-53-0|1373423-53-0 free base|cells|TGF-β|Th1|Th17|Inhibitor|JMJD3|mice

验证数据展示

  • CAS No.: 1797983-09-5

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

产品信息

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%， 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 store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 diabetic|demethylase|dendritic|GSK-J4|GSKJ4 Hydrochloride|GSK-J4 Hydrochloride|GSK-J-4 Hydrochloride|GSK J4 HCl|GSK J4 HCl (1373423-53-0 free base)|GSK J4 Hydrochloride|inhibit|inflammation|H3K27me3/me2|HistoneDemethylase|Histone Demethylase|1373423-53-0|1373423-53-0 free base|cells|TGF-β|Th1|Th17|Inhibitor|JMJD3|mice

靶点活性

JMJD3:50 μM|JMJD3 (cell-free assay):60 nM

体内活性

作为一种前药，GSK-J4 在细胞内迅速水解成否则无法进入细胞的 GSK-J1，后者对纯净酶展示出 60 nM 的 IC50 值。组蛋白 H3 赖氨酸 27 (H3K27) 的去甲基化酶 JMJD3 在细胞分化、发育、炎症反应及癌症的转录调控中扮演重要角色。

体外活性

当GSK-J4被施用于人类原代巨噬细胞时，可以减少LPS诱导的促炎细胞因子产量，尤其是显著降低TNFα的产量（IC50 = 9 μM）。

溶解度

Ethanol:20 mg/mL (44.06 mM);DMSO:50 mg/mL (110.14 mM)

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.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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C1   V1   C2   V2