compound introduction
MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC 50 of 80 nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9 -dependent trimethylation of H3K4 ( IC 50 = 0.8 µM) In Vitro After 24?h of treatment, MRK-740 (3?μM) does not affect HEK293T cell growth at the IC 90 , but some toxicity is observed at 10?μM. MRK-740 is an equipotent inhibitor of H3K4 methylation in MCF7 cells. In cells, MRK-740 specifically and directly inhibits H3K4 methylation at endogenous PRDM9 target loci. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 80 nM (PRDM9)
