Stemcell, 100-1642, GSK-J4 (Hydrochloride)

Inhibit cell proliferation and induce apoptosis in cancer cells with GSK-J4 (Hydrochloride), an epigenetic modifier and selective inhibitor of the Jumonji domain-containing protein D3 (JMJD3) histone demethylase (IC50 = 9 µM). JMJD3 demethylates the tri-methylated lysine 27 on histone H3 (H3K27me3) to activate transcription (Kruidenier et al. Nature, 2012). Dysregulation of H3K27me3 marks have been associated with different cancers. Through the inhibition of JMJD3, GSK-J4 can impact key pathways such as cell proliferation, cell cycle, and apoptosis that are often targeted by anti-cancer agents (Dalpatraj et al. Int J Cancer, 2023).

GSK-J4 (Hydrochloride) has been used for:

CANCER RESEARCH

· Inhibit cell proliferation and migration and induce apoptosis in human glioma cell lines (Sui et al. Oncotarget, 2017).

· Induce apoptosis and cell cycle arrest in human acute myeloid leukemia cells and slow disease progression in a leukemia mouse model (Chu et al. Cancer Cell Int, 2020; Li et al. J Cancer Res Clin Oncol, 2018).

· Reduce cell proliferation of castration-resistant human prostate cancer cells (Morozov et al. Oncotarget, 2017).

· Induce cell cycle arrest and inhibit cell proliferation of human and mouse medulloblastoma cell lines (Deng et al. Front Oncol, 2022).

· Increase differentiation, endoplasmic reticulum stress, and apoptosis in human neuroblastoma cell lines and reduce tumor growth in a mouse xenograft model (Lochmann et al. Sci Transl Med, 2018).