EPZ5676 | 27625-1

EPZ5676 | 27625-1 | Gentaur US, UK & Europe Disrtribition

Category: Methyltransferase/Inhibitors / Activators

Application: N/A

Background: EPZ5676 is a potent inhibitor of DOT1L histone methyltransferase that, according to X-ray crystallographic analysis, occupies the S-adenosyl methionine (SAM) binding pocket of DOT1L and induces conformational changes in DOT1L resulting in the opening of a hydrophobic pocket beyond the amino acid portion of SAM. EPZ5676 has been investigated for the treatment of MLL-rearranged leukemia in multiple studies where results have shown that EPZ5676 inhibits H3K79 methylation and the expression of MLL-fusion target gene and potently kills acute leukemia cell lines bearing MLL translocation.

Description: EPZ-5676 is an S-adenosyl methionine (SAM) competitive inhibitor of protein methyltransferase DOT1L with Ki of 80 pM.

Product Type: Inhibitor

Shippement Condition: Room temp. (continental US) or gel packs