IHMT-EZH2-426 [CAS 3018914-66-1]

IHMT-EZH2-426 (compound 38) is an effective covalent EZH2 degrader, with IC50 values of 1.3 nM, 1.2 nM, and 1.7-3.5 nM for EZH2 wild type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 reduces H3K27me3 and EZH2 levels and shows effective anti-proliferative effects in B-cell lymphoma and TNBC cell lines.

[3018914-66-1]

C31H35FN4O4S

578.7

O=C(C1=CC(C(C=CC(F)=C2)=C2NC(C=C)=O)=CC(N(C3CCOCC3)C)=C1C)NCC4=C(SC)C=C(C)NC4=O

Histone Methyltransferase

EZH2

10 mM in DMSO

Room temperature