GSK J5 HCl

Please contact us at for specific academic pricing.

Background

GSK J5 HCl is the hydrochloride form of GSK J5. GSK J5 is an inactive isomer of GSK J4 and a cell-permeable ester derivative of inactive control GSK J2. Lysine-specific demethylase 6B (KDM6B), also known as Jumonji domain-containing protein D3 (JMJD3), was overexpressed in patients with AML and these patients have a poor prognosis. KDM6B-specific pharmacological inhibitor GSK-J4 had a significant anti-proliferative effect in AML cell lines and freshly isolated BM monocytes (MNCs) from AML patients, while H3K27me3 levels were also increasing. GSK-J4 also caused apoptosis and cell cycle arrest in vitro, and reduced tumor burden in vivo in AML xenograft mouse models. It is worth noting that injection of GSK-J4 attenuated disease progression in a human AML xenograft mouse model. Treatment with GSK-J4 mainly resulted in downregulation of DNA replication and cell cycle-related pathways, and prevents the expression of HOX, a key cancer gene. ChIP-qPCR verified the increased H3K27me3 enrichment in the HOX gene transcription initiation site [1].
[1]. Li Y, Zhang M, Sheng M, Zhang P, Chen Z, Xing W, Bai J, Cheng T, Yang FC, Zhou Y. Therapeutic potential of GSK-J4, a histone demethylase KDM6B/JMJD3 inhibitor, for acute myeloid leukemia. J Cancer Res Clin Oncol. 2018 Jun;144(6):1065-1077. doi: 10.1007/s00432-018-2631-7. Epub 2018 Mar 28. PubMed PMID: 29594337; PubMed Central PMCID: PMC5948279.