<Suppliers Price>

MRK-740

Names

[ CAS No. ]:
2387510-80-5

[ Name ]:
MRK-740

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Histone Methyltransferase

[Target]

IC50: 80 nM (PRDM9)[1]


[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].

[References]

[1]. Abdellah Allali-Hassani, et al. Discovery of a Chemical Probe for PRDM9. Nat Commun. 2019 Dec 17;10(1):5759.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H32N6O3

[ Molecular Weight ]:
464.56

Related Compounds