Drug intelligence / Profile preview

JIB-04

Development stage
Preclinical
Lead developer
Baylor College of Medicine
Modality
Small Molecules
01

Overview

JIB-04 is a small molecule, pan-selective inhibitor of the Jumonji family of histone demethylases (JumonjiC-domain histone demethylases). It inhibits multiple members of the KDM4, KDM5, and KDM6 families with nanomolar potency. The compound has demonstrated anticancer activity in vitro and in vivo by reducing tumor burden and prolonging survival in mouse models. Mechanistically, it suppresses translation initiation and enhances sensitivity to mTOR inhibitors. JIB-04 also exhibits broad-spectrum antiviral activity against several DNA and RNA viruses, including SARS-CoV-2, both in vitro (primary human bronchial epithelial cells) and in vivo (porcine coronavirus model), as well as antifungal activity targeting fungal histone demethylases. It crosses the blood-brain barrier and has shown efficacy against temozolomide-resistant glioblastoma cells[1][2][3][4][5].

Other names
(E)-5-chloro-2-(2-(phenyl(pyridin-2-yl)methylene)hydrazinyl)pyridine
02

Targets

JmjC-KDM (Jumonji C-domain-containing histone demethylase)

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