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MS37452

Names

[ CAS No. ]:
423748-02-1

[ Name ]:
MS37452

[Synonym ]:
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)-

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
628.8±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H26N2O5

[ Molecular Weight ]:
398.452

[ Flash Point ]:
334.1±31.5 °C

[ Exact Mass ]:
398.184174

[ LogP ]:
2.29

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.575

[ Storage condition ]:
20°C

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds