Product Description

JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2).1,2 It inhibits colony formation of primary human CD34+ chronic myelogenous leukemia (CML) stem/progenitor cells but not non-cancerous human CD34+ hematopoietic stem/progenitor cells when used at concentrations ranging from 0.5 to 5 µM.2 It also reduces global levels of trimethylated histone 3 lysine 27 (H3K27Me3), a mark that is regulated by PRC2, in K562 cells. JQEZ5 (75 mg/kg per day) induces regression of tumors in an EZH2-driven transgenic mouse model of lung adenocarcinoma.1WARNING This product is not for human or veterinary use.