1394854-51-3

Basic information

• Product Name: GSK J5
• Synonyms: GSK J5;GSK-J5;N-[2-(3-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine ethyl ester
• CAS NO: 1394854-51-3
• Molecular Formula: C24H27N5O2
• Molecular Weight: 417.50348
• Mol File: 1394854-51-3.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Solubility: insoluble in H2O; ≥17.3 mg/mL in EtOH with ultrasonic; ≥19.5 mg/mL in DMSO
• CAS DataBase Reference: GSK J5(CAS DataBase Reference)
• NIST Chemistry Reference: GSK J5(1394854-51-3)
• EPA Substance Registry System: GSK J5(1394854-51-3)

Safety Data

• Hazardous Substances Data: 1394854-51-3(Hazardous Substances Data)

Usage

Description

GSK J5 is an inactive isomer of GSK J4 (G797555), a cell permeable inhibitor of the histone demethylase JMJD3/UTX. It is a compound that has been synthesized and studied for its potential applications in various fields, particularly in the context of its interaction with histone demethylases.

Uses

Used in Pharmaceutical Research:
GSK J5 is used as a research compound for studying the role of histone demethylases, specifically JMJD3/UTX, in various biological processes. The compound helps researchers understand the function and regulation of these enzymes, which can be crucial for developing targeted therapies for certain diseases.
Used in Drug Development:
GSK J5 is used as a starting point for the development of new drugs that target histone demethylases. By understanding the structure and activity of GSK J5, researchers can design more potent and selective inhibitors that can be used as therapeutic agents.
Used in Epigenetic Studies:
GSK J5 is used as a tool in epigenetic research to investigate the role of histone demethylation in gene regulation, cellular processes, and disease development. Understanding the epigenetic mechanisms can provide insights into the development of novel therapeutic strategies for various conditions.
Used in Chemical Biology:
GSK J5 is used as a probe in chemical biology to explore the interactions between small molecules and their target proteins, such as histone demethylases. This can help in the discovery of new biological pathways and potential drug targets.

Biological Activity

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.