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GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 hydrochloride is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM and inactive against a panel of demethylases of the JMJ family.
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Source | Mol Cells (2018). Figure 4. GSK J4 |
| Method | qRT- PCR | |
| Cell Lines | THP-1 cells | |
| Concentrations | 5 μM | |
| Incubation Time | 48 h | |
| Results | To further determine the mechanisms underlying transcriptional regulation of p21 via KDM6B, we conducted luciferase reporter assay using p21-luciferase reporter system in HEK 293T cells. Ectopic expression of KDM6B accelerated p21 transcription (Fig. 4B), whereas KDM6B inhibition by GSK-J4 showed reduction of p21 expression |
| Molecular Weight | 453.96 |
| Formula | C24H27N5O2.HCl |
| CAS Number | 1797983-09-5 |
| Solubility (25°C) | DMSO 50 mg/mL Water ~2.5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Histone demethylase Products |
|---|
| JIB-04
JIB-04 is a selective inhibitor of Jumonji histone demethylase with IC50 values of 230, 340, 435, 445, 855 and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C respectively. |
| GSK-J1
GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. GSK J1 is selective for the H3K27 demethylases JMJD3 and UTX. |
| OG-L002
OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively. |
| GSK-LSD1 dihydrochloride
GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). |
| GSK-J4
GSK-J4 is a cell permeable procompound rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. |
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