1. Epigenetics
  2. Histone Demethylase
  3. GSK-J1 lithium salt

GSK-J1 lithium salt 是一种有效的 H3K27me3/me2-demethylases JMJD3/KDM6BUTX/KDM6A 的抑制剂,对 KDM6B 的 IC50 值为 60 nM。

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GSK-J1 lithium salt Chemical Structure

GSK-J1 lithium salt Chemical Structure

CAS No. : 2309668-29-7

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GSK-J1 lithium salt 的其他形式现货产品:

Other Forms of GSK-J1 lithium salt:

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Top Publications Citing Use of Products

    GSK-J1 lithium salt purchased from MCE. Usage Cited in: Front Mol Neurosci. 2017 Mar 13;10:51.  [Abstract]

    GSK-J1 impaired zebrafish hair cell regeneration. 5 dpf larvae are treated with 400 μM Neomycin for 1 h followed by GSK-J1 exposure for 24 in the presence of BrdU. GSK-J1 significantly reduces the numbers of myosinVI-positive (green) hair cells and BrdU-positive (red) replicating cells.

    查看 Histone Demethylase 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    GSK-J1 lithium salt is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.

    IC50 & Target

    KDM6

     

    体外研究
    (In Vitro)

    GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner[1]. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1 mM α-ketoglutarate, with IC50 of 11 μM and 94 μM, respectively[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    分子量

    395.38

    Formula

    C22H22LiN5O2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    纯度 & 产品资料

    纯度: 98.26%

    参考文献
    Kinase Assay
    [1]

    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·H2O, 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    GSK-J1 lithium salt 相关分类

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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