Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells[1].
Molekulargewicht:
572.74
Reinheit:
99.93
CAS Nummer:
[1403254-99-8]
Formel:
C34H44N4O4
Target-Kategorie:
Apoptosis,Histone Methyltransferase
Anwendungsbeschreibung:
MCE Product type: Reference compound
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