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GSK-J4 is a cell permeable prodrug rapidly hydrolyzed by macrophage esterases to GSK-J1, a potent selective jumonji H3K27 demethylase inhibitor. GSK-J4 inhibited TNF-α production with an IC50 of 9 μM in LPS-stimulated human macrophages and blocked the production of TNF-α by macrophages derived from patients with rheumatoid arthritis. GSK-J1 is selective for the KDM6 subfamily members JMJD3 and UTX with an IC50 of 60 nM in a JMJD3 assay, and is inactive against other demethylases of the JMJ family and over 100 tested kinases and histone deacetylases.
Sci China Life Sci. 2025 Feb 17; .
Inhibition of KDM6B prevents osteoarthritis by blocking growth plate-like H3K27me3 loss in bivalent genes
GSK-J4 purchased from AbMole
Mol Cancer Ther. 2021 Oct;20(10):1868-1879.
Pharmaceutical Interference of the EWS-FLI1–driven Transcriptome By Cotargeting H3K27ac and RNA Polymerase Activity in Ewing Sarcoma
GSK-J4 purchased from AbMole
Sci Transl Med. 2018 May 16.
Targeted inhibition of histone H3K27 demethylation is effective in high-risk neuroblastoma
GSK-J4 purchased from AbMole
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Source | Oncotarget (2018). Figure 4. GSK-J4 |
| Method | XTT assay | |
| Cell Lines | LNCaP and DU 145 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24 h, 48 h and 72 h | |
| Results | JMJD3 expression with GSK-J4 treatment was reduced by 61% for LNCaP and by around 20% for DU 145 and PC-3 |
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Source | Sci Transl Med (2018). Figure 4. GSK-J4 (Abmole Bioscience) |
| Method | Seventy-two–hour Cell Titer-Glo assay | |
| Cell Lines | neuroblastoma cell lines | |
| Concentrations | 1 μM | |
| Incubation Time | 72 hours | |
| Results | The venetoclax/GSK-J4 combination suppressed the growth of several MYCN-amplified neuroblastoma cell lines, which was due to an increase in the induction of apoptosis by the combination compared to GSK-J4 or venetoclax single-agent therapy |
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Source | Sci Transl Med (2018). Figure 3. GSK-J4 (Abmole Bioscience) |
| Method | Cell viability assays | |
| Cell Lines | SH-SY5Y cells | |
| Concentrations | 1 μM | |
| Incubation Time | 6 days | |
| Results | Furthermore, the combination of RA and GSK-J4 induced both the differentiation marker CHD5 and several ER stress markers, including PUMA, after 6 days of treatment |
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Source | Sci Transl Med (2018). Figure 2. GSK-J4 (Abmole Bioscience) |
| Method | Western blot | |
| Cell Lines | neuroblastoma cell lines | |
| Concentrations | 1 μM | |
| Incubation Time | 72 hours | |
| Results | Consistent with a role for PUMA in GSK-J4–mediated efficacy, RNA-seq and Western blot analyses indicated induction of BBC3/PUMA, whereas knockdown of BBC3 by short hairpin–mediated RNA (shRNA) silencing protected cells from GSK-J4–induced apoptosis/necrosis |
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Source | Sci Transl Med (2018). Figure 1. GSK-J4 (Abmole Bioscience) |
| Method | cell viability assay | |
| Cell Lines | Neuroblastoma cell lines | |
| Concentrations | 1 μM | |
| Incubation Time | 72 hours | |
| Results | GSK-J4 delivered daily was sufficient to induce tumor regressions in the IMR32 model, completely block growth in the COG-N-561 PDX, and inhibit tumor growth in the FELIX PDX and CHLA20 models |
| Molecular Weight | 417.5 |
| Formula | C24H27N5O2 |
| CAS Number | 1373423-53-0 |
| Solubility (25°C) | DMSO 28 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 |
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| 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. |
| GSK-J4 hydrochloride
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 procompound 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. |
| 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). |
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Products are for research use only. Not for human use. We do not sell to patients.
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