2387510-80-5

2387510-80-5 structure

Name: MRK-740
Chemical Name: MRK-740
CAS Number: 2387510-80-5
Molecular Formula: C₂₅H₃₂N₆O₃
Molecular Weight: 464.56
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2020-08-09 23:19:36
Modify Date: 2024-04-03 08:38:06
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].

Name	MRK-740

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.

Molecular Formula	C₂₅H₃₂N₆O₃
Molecular Weight	464.56