histone h3k27me3

GSK-J4 (GSK J4 HCl) is a cell permeable prodrug of GSK-J1, a dual inhibitor of the H3K27me3 me2 demethylases JMJD3 KDM6B and UTX KDM6A (IC50=8.6 6.6 μM). GSK-J4 induces endoplasmic reticulum stress-related apoptosis.

PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 (Kis: 0.7 and 3.0 nM, respectively).

HDM-IN-1 (Compound A4) is an inhibitor of fungal histone demethylase (HDM) that inhibits H3K27me3 in Cryptococcus neoformans and Candida auris, with IC50 values of 134 nM and 12 nM, respectively. It demonstrates inhibitory activity against these fungi by preventing biofilm and capsule formation, with an MIC80 of 0.5-2 μg mL. Additionally, HDM-IN-1 exhibits antifungal activity in ICR mouse models.

MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM).

GSK-J4 Hydrochloride (GSK J4 HCl) is a cell permeable, potent and selective histone demethylase(JMJD3 )inhibitor. is an ethyl ester derivative of the GSK-J1 with an IC50 value greater than 50 μM in vitro.

JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).

EZH2-IN-14 is a selective inhibitor of EZH2 (Histone Methyltransferase) with an IC50 value of 12 nM, targeting the methyltransferase activity of EZH2 PRC2 and reducing H3K27me3 levels. It exhibits more than 200-fold selectivity for EZH2 over the closely related H3K27 methyltransferase, EZH1.