| Name | GSK-J1 |
| 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. |
| 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. |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 38.9 mg/mL (99.88 mM), Sonication is recommended.
DMSO : 250 mg/mL (641.93 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.14 mM), Sonication is recommended.
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| Keywords | UTX (KDM6A) | JMJD3 (KDM6B) | Inhibitor | inhibit | HistoneDemethylase | Histone Demethylase | GSK-J-1 | GSK-J1 | GSKJ1 |
| Inhibitors Related | LSD1-IN-24 | Procaine | TFMB-(R)-2-HG | GSK-LSD1 dihydrochloride | GSK-J4 | FY-21 | Phenelzine sulfate | Pulrodemstat HCl | Daminozide | AS8351 | Procaine hydrochloride | Eicosapentaenoic Acid |
| Related Compound Libraries | Methylation Compound Library | Histone Modification Compound Library | Bioactive Compound Library | Epigenetics Compound Library | Chromatin Modification Compound Library | Multi-Target Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | NO PAINS Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
