Catalog No.: PC-21618Not For Human Use, Lab Use Only.
Pinometostat (EPZ-5676) is a potent and selective inhibitor of DOT1L histone methyltransferase activity with Ki of 0.08 nM, 37000-fold selectivity over other methyltransferases.
Pinometostat (EPZ-5676) is a potent and selective inhibitor of DOT1L histone methyltransferase activity with Ki of 0.08 nM, 37000-fold selectivity over other methyltransferases. EPZ-5676 occupies the S-adenosyl methionine (SAM) binding pocket and induces conformational changes in DOT1L. Pinometostat (EPZ-5676) potently inhibits cellular H3K79 methylation with IC50 of 3 nM and 5 nM in MV4-11 and HL60 (non–MLL-rearranged) cells, respectively, inhibits MLL-fusion target gene expression. Pinometostat (EPZ-5676) selectively inhibits proliferation of MLL-rearranged leukemia cells with IC50 of 3.5 nM (MV4-11 proliferation), demonstrates nanomolar antiproliferative activity against most of the MLL-rearranged cell lines, but not non-MLL-rearranged cell lines. EPZ-5676 (70 mg/kg) causes complete and sustained regression in rodent subcutaneous (SC) MV4-11 xenograft models.
