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Medchemexpress LLC Tazemetostat | 1403254-99-8 | 572.74 | 5 MG
Supplier: Medchemexpress LLC 5MGHY13803
Tazemetostat is a potent, selective, and orally available EZH2 inhibitor. It inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. It also inhibits EZH2 with IC50s of 11 nM in peptide assay and 16 nM in nucleosome assay. Additionally, it inhibits rat EZH2 with an IC50 of 4 nM and EZH1 with an IC50 of 392 nM. It induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells.
- Targets histone methyltransferase and apoptosis
- Inhibits wild-type EZH2 activity with a Ki value of 2.5 nM
- IC50 values for EZH2: 11 nM (peptide assay) and 16 nM (nucleosome assay)
- IC50 for rat EZH2: 4 nM
- IC50 for EZH1: 392 nM
- Induces apoptosis and differentiation in SMARCB1-deleted MRT cells
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