Promotional price valid on web orders only. Your contract pricing may differ. Interested in signing up for a dedicated account number?
Learn More
Learn More
AdipoGen EPZ-6438 (5 mg)
Supplier: AdipoGen AGCR13743M005
Chemical. CAS: 1403254-99-8. Formula: C34H44N4O4. MW: 572.7. EPZ-6438 is a potent orally bioavailable, selective inhibitor of the lysine methyltransferase EZH2 (Ki = 2.5nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27). EPZ-6438 competitively binds to the S-adenosylmethionine (SAM) binding site of EZH2 and non-competitively to the binding sites of peptide or nucleosome substrate. It shows also in vitro potency for EZH2 mutations (Y641F, C, H, N, S and A677G). PRC2 is the only protein methyltransferase that can methylate H3K27 and H3K27 is the only significant substrate for PRC2. Aberrant trimethylation of H3K27 is oncogenic in a broad spectrum of human cancers such as B cell NHL.EPZ-6438 blocks histone H3 lysine 27 trimethylation in both wild-type and mutant lymphoma cells (IC50 range from 2-90nM). EPZ-6438 has potent anticancer properties.
Product Content Correction
The Fisher Scientific Encompass Program offers items which are not part of our distribution portfolio. These products typically do not have pictures or detailed descriptions. However, we are committed to improving your shopping experience. Please use the form below to provide feedback related to the content on this product.
Product Title
Spot an opportunity for improvement?Share a Content Correction