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

GSK-J1 lithium salt 

Cat. No.: HY-15648D
Handling Instructions

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

For research use only. We do not sell to patients.

GSK-J1 lithium salt Chemical Structure

GSK-J1 lithium salt Chemical Structure

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Other In-stock Forms of GSK-J1 lithium salt:

Other Forms of GSK-J1 lithium salt:

Top Publications Citing Use of Products

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

    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.
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    Description

    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

    IC50: 60 nM (KDM6B)[2]

    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].

    Molecular Weight

    395.38

    Formula

    C₂₂H₂₂LiN₅O₂

    SMILES

    [Li]OC(CCNC1=NC(C2=NC=CC=C2)=NC(N(CC3)CCC4=C3C=CC=C4)=C1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    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.

    References
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    Keywords:

    GSK-J1Histone DemethylaseInhibitorinhibitorinhibit

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