Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, <10-fold selectivity over other tested demethylases.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 40.00 | |
10 mg | In stock | $ 63.00 | |
25 mg | In stock | $ 98.00 | |
50 mg | In stock | $ 187.00 | |
100 mg | In stock | $ 311.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 67.00 |
Description | GSK-J1 is a highly potent H3K27 histone demethylase inhibitor with IC50 of 28 nM and 53 nM in cell-free assays for JMJD3 (KDM6B) and UTX (KDM6A), respectively, >10-fold selectivity over other tested demethylases. |
Targets&IC50 | UTX (KDM6A):53 nM, JMJD3 (KDM6B):28 nM |
In vitro | In HEK-293 cells, GSK-J1 inhibits the activities of transiently transfected JMJD3 and UTX. GSK-J1 also inhibits TNF-α production by human primary macrophages by increasing total nuclear H3K27me3 levels. [1] In MC3T3-E1 cells, GSK-J1 suppresses Runx2 and Osterix expressions and ALP activity, and increases the global levels of H3K27me3. [2] |
Kinase Assay | 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·Water, 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. |
Synonyms | GSK J1 |
Molecular Weight | 389.45 |
Formula | C22H23N5O2 |
CAS No. | 1373422-53-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 38.9 mg/mL (100 mM)
DMSO: 38.9 mg/mL (100 mM)
You can also refer to dose conversion for different animals. More
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GSK-J1 1373422-53-7 Chromatin/Epigenetic Histone Demethylase inhibit GSK J1 Inhibitor GSKJ1 GSK-J-1 inhibitor