An orally bioavailable

EPZ6438 – 5 mg

Brand:
Cayman
CAS:
1403254-99-8
Storage:
-20
UN-No:
Non-Hazardous - /

EPZ6438 is an orally bioavailable, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 2.5 nM), the enzymatic subunit of polycomb repressive complex 2.{28475} It displays a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other histone methyltransferases.{28475} EPZ6438 blocks histone H3 lysine 27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM).{28476} EPZ6438 has been shown to induce apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and to promote their regression in xenograft-bearing mice.{28475}  

 

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Description

An orally bioavailable, selective inhibitor of EZH2 (Ki = 2.5 nM); blocks H3K27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM); induces apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and promotes their regression in xenograft-bearing mice

Formal name: N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4′-(4-morpholinylmethyl)-[1,1′-biphenyl]-3-carboxamide

Synonyms:  Tazemetostat

Molecular weight: 572.7

CAS: 1403254-99-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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