Biological ActivityEZH2/EPP interaction inhibitor (Kd = 320 nM). Suppresses EZH2 expression and H3K27 trimethylation by PCR2 complex. Arrests proliferation and induces monocyte to macrophage differentiation of MLL-AF9 leukemia cell line.
(Modifications: Phe-1 = N-terminal Ac, X = (S)-2-(4-pentenyl)alanine, X-6 and X-10 stapled together with a double bond)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Targeted disruption of the EZH2-EED complex inhibits EZH2-dependent cancer.
Kim et al.
SWI/SNF-mutant cancers depend on catalytic and non-catalytic activity of EZH2.
Kim et al.
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