2. Epigenetics
  3. Histone Demethylase
  4. GSK-J1

GSK-J1 

Cat. No.: HY-15648 Purity: 99.76%
COA 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
Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 85 In-stock
Solid
5 mg USD 49 In-stock
10 mg USD 77 In-stock
25 mg USD 127 In-stock
50 mg USD 226 In-stock
100 mg USD 374 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of GSK-J1:

GSK-J1 Related Antibodies

Top Publications Citing Use of Products

    GSK-J1 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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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

    KDM6

     

    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.

    GSK-J1 Related Antibodies
    Molecular Weight

    389.45

    Appearance

    Solid

    Formula

    C22H23N5O2
    CAS No.
    SMILES

    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
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (128.39 mM; Need ultrasonic)

    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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.76%

    COA (250 KB) LCMS (110 KB)

    Handling Instructions (2659 KB)
    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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    GSK-J1 Related Classifications

    Help & FAQs
    • 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.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    GSK-J11373422-53-7Histone DemethylaseInhibitorinhibitorinhibit

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