1. Epigenetics
  2. Histone Demethylase

GSK-J1 

Cat. No.: HY-15648 Purity: 99.92%
Handling Instructions

GSK-J1 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 Chemical Structure

GSK-J1 Chemical Structure

CAS No. : 1373422-53-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 121 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 340 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Other Forms of GSK-J1:

Top Publications Citing Use of Products

    GSK-J1 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    GSK-J1 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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (84.73 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5677 mL 12.8386 mL 25.6772 mL
    5 mM 0.5135 mL 2.5677 mL 5.1354 mL
    10 mM 0.2568 mL 1.2839 mL 2.5677 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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
    Molecular Weight

    389.45

    Formula

    C₂₂H₂₃N₅O₂

    CAS No.

    1373422-53-7

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
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    Product Name:
    GSK-J1
    Cat. No.:
    HY-15648
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    GSK-J1

    Cat. No.: HY-15648