GSK J4
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GSK J4 is a chemical compound that functions as a potent and selective inhibitor of the histone demethylase KDM6B (JMJD3). It acts by binding to the active site of KDM6B, preventing the demethylation of histone H3 lysine 27 (H3K27). This inhibition leads to an accumulation of H3K27me3, resulting in the repression of genes involved in various cellular processes. By modulating the epigenetic landscape, GSK J4 may influence gene expression patterns and cellular differentiation. Its mechanism of action involves disrupting the balance of histone methylation, thereby impacting the transcriptional regulation of specific genes. In development setting, GSK J4 is utilized to investigate the role of KDM6B in epigenetic regulation and to the downstream effects of histone methylation changes on cellular function.
GSK J4 References
- The histone demethylase inhibitor GSK-J4 limits inflammation through the induction of a tolerogenic phenotype on DCs. | Doñas, C., et al. 2016. J Autoimmun. 75: 105-117. PMID: 27528513
- The pharmacological role of histone demethylase JMJD3 inhibitor GSK-J4 on glioma cells. | Sui, A., et al. 2017. Oncotarget. 8: 68591-68598. PMID: 28978140
- GSK-J4-Mediated Transcriptomic Alterations in Differentiating Embryoid Bodies. | Mandal, C., et al. 2017. Mol Cells. 40: 737-751. PMID: 29047260
- Therapeutic potential of GSK-J4, a histone demethylase KDM6B/JMJD3 inhibitor, for acute myeloid leukemia. | Li, Y., et al. 2018. J Cancer Res Clin Oncol. 144: 1065-1077. PMID: 29594337
- Antiproliferative effect of the histone demethylase inhibitor GSK-J4 in chondrosarcomas. | Lhuissier, E., et al. 2019. IUBMB Life. 71: 1711-1719. PMID: 31241814
- Oncogenic KRAS Sensitizes Lung Adenocarcinoma to GSK-J4-Induced Metabolic and Oxidative Stress. | Hong, BJ., et al. 2019. Cancer Res. 79: 5849-5859. PMID: 31506334
- The antischistosomal potential of GSK-J4, an H3K27 demethylase inhibitor: insights from molecular modeling, transcriptomics and in vitro assays. | Lobo-Silva, J., et al. 2020. Parasit Vectors. 13: 140. PMID: 32178714
- Synergy of GSK-J4 With Doxorubicin in KRAS-Mutant Anaplastic Thyroid Cancer. | Lin, B., et al. 2020. Front Pharmacol. 11: 632. PMID: 32477122
- GSK-J4 induces cell cycle arrest and apoptosis via ER stress and the synergism between GSK-J4 and decitabine in acute myeloid leukemia KG-1a cells. | Chu, X., et al. 2020. Cancer Cell Int. 20: 209. PMID: 32514253
- Histone H3K27 methyltransferase EZH2 and demethylase JMJD3 regulate hepatic stellate cells activation and liver fibrosis. | Jiang, Y., et al. 2021. Theranostics. 11: 361-378. PMID: 33391480
- The demethylase inhibitor GSK-J4 limits inflammatory colitis by promoting de novo synthesis of retinoic acid in dendritic cells. | Doñas, C., et al. 2021. Sci Rep. 11: 1342. PMID: 33446666
- Effects of GSK-J4 on JMJD3 Histone Demethylase in Mouse Prostate Cancer Xenografts. | Sanchez, A., et al. 2022. Cancer Genomics Proteomics. 19: 339-349. PMID: 35430567
- GSK-J4, a Specific Histone Lysine Demethylase 6A Inhibitor, Ameliorates Lipotoxicity to Cardiomyocytes via Preserving H3K27 Methylation and Reducing Ferroptosis. | Xu, K., et al. 2022. Front Cardiovasc Med. 9: 907747. PMID: 35722096
- The Histone Demethylase Inhibitor GSK-J4 Is a Therapeutic Target for the Kidney Fibrosis of Diabetic Kidney Disease via DKK1 Modulation. | Hung, PH., et al. 2022. Int J Mol Sci. 23: PMID: 36012674
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GSK J4, 10 mg | sc-391114 | 10 mg | $215.00 | |||
GSK J4, 50 mg | sc-391114A | 50 mg | $860.00 |