EZH2-IN-14

Names

[ CAS No. ]:
1979157-17-9

[ Name ]:
EZH2-IN-14

Biological Activity

[Description]:

EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Histone Methyltransferase

[In Vitro]

EZH2-IN-14 (C24) 有效减少H3K27me3 和 H3K27me2 蛋白水平，但对 MDA-MB-468 细胞中 EZH2 蛋白水平影响不大[1]。 Cell Viability Assay[1] Cell Line: MDA-MB-468 cells Concentration: 4 μM Incubation Time: 6 hours, 12 hours, 24 hours, 48 hours Result: Reduced the H3K27me3 and H3K27me2 marks.

[References]

[1]. Anqi Ma, et al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.  

Chemical & Physical Properties

[ Molecular Formula ]:
C31H39N7O2

[ Molecular Weight ]:
541.69

Related Compounds