Background:

NCGC00247743 is a histone lysine demethylase KDM4 inhibitor.

Based on structure-activity relationship studies, a series of chemical compounds are derived from 8-hydroxyquinoline (8HQ) and shown to be active inhibitors of KDM4E and KDM4A. The effect of these compounds is tested on the growth of LNCaP cells and NCGC00247751 (A1), NCGC00244536 (B3), and NCGC00247743 (I9) are selected. These inhibitors inhibit LNCaP cell growth with IC50s in the μM range. These compounds also inhibit the enzymatic activity of other KDM4 isoforms although, interestingly, the potency and efficacy of B3 and A1 for KDM4A, 4C, and 4D are lower compared to that of NCGC00247743 (I9), suggesting a potential selectivity of the inhibitors for different isoforms of KDM4[1].

[1]. Duan L, et al. KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes. Chem Biol. 2015 Sep 17;22(9):1185-96.