MRK-740, a chemical probe, 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).
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