IHMT-EZH2-426 (compound 38) is a potent covalent degrader of EZH2, demonstrating IC50 values of 1.3 nM for EZH2 wild-type, 1.2 nM for EZH2-A687V, and 1.7-3.5 nM for EZH2-Y641F/Y641N/Y641S mutants. The compound effectively inhibits proliferation in B-cell lymphoma and triple-negative breast cancer (TNBC) cell lines due to its capacity to diminish H3K27me3 and EZH2 levels [1].
Molecular Weight:
578.7
Formula:
C31H35FN4O4S
Target:
Histone Methyltransferase
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