Biological ActivitySAH-EZH2 is an EZH2/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)
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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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