EPZ-6438

• Background:

  EPZ-6438 competitively binds to the S-adenosylmethionine (SAM) binding site of EZH2 and also non-competitively binds to the binding sites of peptide or nucleosome substrate. EPZ-6438 selectively inhibits EZH2 with selectivity 35-fold greater than EZH1. Study results have suggested that EPZ-6438 exhibits dramatic and permanent anti-tumor activity in MRT models through synergistic effects of EPZ-6438-mediated EZH2 inhibition on several cancer pathways.

• Description:

  EPZ-6438 is a potent and bio-available inhibitor of EZH2, the catalytic subunit of polycomb repressive complex 2 (PRC2) catalyzing the methylation of lysine 27 of histone H3 (H3K27), that inhibits the activity of human PRC2-containing wild-type EZH2 (Ki = 2.5 nM) .

• Purity:

  ≥ 99% by HPLC

• Solubility:

  Soluble in EtOH

• Molecular Formula:

  C34H44N4O4

• Shipping Conditions:

  Room Temperature (continental US) or Gel Packs

• Storage Conditions:

  Store desiccated at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

• Calculated Molecular Weight:

  572.7 Da

• CAS Number:

  1403254-99-8