| Description |
MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 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 (IC50 = 0.8 µM)[1].
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| Related Catalog |
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| Target |
IC50: 80 nM (PRDM9)[1]
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| In Vitro |
After 24 h of treatment, MRK-740 (3 µM) does not affect HEK293T cell growth at the IC90, 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[1].
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| References |
[1]. Abdellah Allali-Hassani, et al. Discovery of a Chemical Probe for PRDM9. Nat Commun. 2019 Dec 17;10(1):5759.
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