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Histone Demethylases

Histone demethylase inhibitors block the enzymes that remove methyl groups from lysine residues on histones. Lysine-specific demethylase 1 (LSD1) is a flavin-dependent amine oxidase that demethylates mono- and dimethylated lysine 4 of histone H3 (H3K4). The larger Jumonji C (JmjC) domain family uses iron and 2-oxoglutarate as cofactors, and some members also remove trimethyl marks. SP2509 and GSK2879552 are inhibitors of LSD1 used in chromatin and differentiation studies. GSK J1 targets two demethylases of lysine 27 on histone H3 (H3K27), Jumonji domain-containing protein 3 (JMJD3) and ubiquitously transcribed X-chromosome tetratricopeptide repeat protein (UTX). GSK-J4 is its cell-permeable ester, used for studies in intact cells. JIB-04 acts on several JmjC demethylases, and YUKA1 inhibits lysine-specific demethylase 5A (KDM5A).

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  • PROTAC KDM4 degrader-1
    Cat. No.
    A32503
    CAS No.
    3102423-10-6

    PROTAC KDM4 degrader-1

    PROTAC KDM4 Degrader-1 is a potent proteolysis targeting chimera (PROTAC) designed to selectively degrade KDM4A-C while sparing KDM4D. This compound demonstrates significant antiproliferative effects in esophageal cancer cells, inducing apoptosis and cell cycle arrest. Additionally, PROTAC KDM4 Degrader-1 effectively inhibits histone H3 lysine demethylation, making it a valuable tool for research into cancer biology and epigenetic regulation.

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