EZH2-IN-14 is a selective EZH2 (Histone Metltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the metltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 metltransferase EZH1.
EZH2-IN-14 (C24) effectively reduces the H3K27me3 and H3K27me2 marks. EZH2-IN-14 has little effect on the level of EZH2 protein in MDA-MB-468 cells[1].
References:
[1]. Anqi Ma, et al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.