EPZ-719 (EPZ 719) is a potent, selective SETD2 histone methyltransferase inhibitor with IC50 of 8 nM.
EPZ-719 displayed a >8000-fold selectivity in a panel of 14 other histone methyltransferases, showing a remarkable level of selectivity over these closely related and potentially confounding targets.
EPZ-719 demonstrated the activity in a cellular context using an in-cell Western (ICW) cell biochemical assay in A549 cells by monitoring the H3K36 trimethyl mark with IC50 of 23 nM.
EPZ-719 potent antiproliferative activity against multiple myeloma cell lines, KMS34 and KMS1, with LTP day 14 IC50 of 25 nM and 211 nM.
EPZ-719 is an attractive tool compound for the interrogation of SETD2 biology that enables in vivo target validation studies.
