423748-02-1

423748-02-1 structure

Name: MS37452
Chemical Name: 1-[4-(2,3-Dimethoxy-benzoyl)-piperazin-1-yl]-2-m-tolyloxy-ethanone
CAS Number: 423748-02-1
Molecular Formula: C₂₂H₂₆N₂O₅
Molecular Weight: 398.452
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2018-07-09 17:15:17
Modify Date: 2024-01-10 19:26:47
MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].

Name	1-[4-(2,3-Dimethoxy-benzoyl)-piperazin-1-yl]-2-m-tolyloxy-ethanone
Synonyms	1-[4-(2,3-Dimethoxybenzoyl)-1-piperazinyl]-2-(3-methylphenoxy)ethanone 1-[4-(2,3-dimethoxybenzoyl)piperazin-1-yl]-2-(3-methylphenoxy)ethanone 1-[4-(2,3-Dimethoxy-benzoyl)-piperazin-1-yl]-2-m-tolyloxy-ethanone Ethanone, 1-[4-(2,3-dimethoxybenzoyl)-1-piperazinyl]-2-(3-methylphenoxy)-

Description	MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Epigenetics >> Histone Methyltransferase
Target	CBX7[1]
In Vitro	MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control[1]. MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1]. RT-PCR[1] Cell Line: PC3 cells Concentration: 125-500 μM Incubation Time: 12 hours Result: Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively.
References	[1]. Ren C, et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chem Biol. 2015;22(2):161-168.

RIDADR	NONH for all modes of transport