MS37452
- Product Name
- MS37452
- CAS No.
- 423748-02-1
- Chemical Name
- MS37452
- Synonyms
- MS37452;1-(2,3-dimethoxybenzoyl)-4-[(3-methylphenoxy)acetyl]piperazine;1-(4-(2,3-Dimethoxybenzoyl)piperazin-1-yl)-2-(m-tolyloxy)ethanone;1-[4-(2,3-Dimethoxybenzoyl)-1-piperazinyl]-2-(3-methylphenoxy)-ethanone;Ethanone, 1-[4-(2,3-dimethoxybenzoyl)-1-piperazinyl]-2-(3-methylphenoxy)-;1-[4-(2,3-dimethoxybenzoyl)piperazin-1-yl]-2-(3-methylphenoxy)ethan-1-one;MS 37452,Histone Methyltransferase,transcription,Inhibitor,MS37452,p16/CDKN2A,anticancer,H3K27me3,derepress,CBX7 chromodomain,inhibit,INK4A/ARF,MS-37452
- CBNumber
- CB43060612
- Molecular Formula
- C22H26N2O5
- Formula Weight
- 398.45224
- MOL File
- 423748-02-1.mol
MS37452 Property
- Boiling point:
- 628.8±55.0 °C(Predicted)
- Density
- 1.209±0.06 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
- form
- powder
- pka
- -1.31±0.70(Predicted)
- color
- white to beige
N-Bromosuccinimide Price
- Product number
- SML1405
- Product name
- MS37452
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $142
- Updated
- 2023/06/20
- Product number
- SML1405
- Product name
- MS37452
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $451
- Updated
- 2023/06/20
- Product number
- 17533
- Product name
- MS37452
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $38
- Updated
- 2024/03/01
- Product number
- 17533
- Product name
- MS37452
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $111
- Updated
- 2024/03/01
- Product number
- 17533
- Product name
- MS37452
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $184
- Updated
- 2024/03/01
MS37452 Chemical Properties,Usage,Production
Description
Chromobox homolog 7 (CBX7) functions through its N-terminal chromodomain, which recognizes histone 3 trimethyl lysine 27 (H3K27me3), to repress gene transcription. It plays a key role in gene transcription in cellular processes related to stem cell self-renewal and differentiation, as well as tumor progression. MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 μM). At 250 μM, it has been shown to derepress transcription of the polycomb repressive complex target gene p16/CDKN2A in prostate cancer cells.
Uses
MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3 and has been shown to derepress transcription of the polycomb repressive complex target gene.
Biochem/physiol Actions
MS37452 is a selective Chromobox homolog 7 (CBX7) modulator that disrupts CBX7ChD binding to H3K27me3. MS37452 inhibits CBX7 binding to INK4/ARF gene locus, and induces decline of p14/ARF and p16/INK4a in human PC3 cells.
in vitro
in a previous study, the crystal structures revealed the binding modes of ms37452 and its close analogs that competed against h3k27me3 binding via interactions with key residues in the methyl-lysine binding pocket of cbx7chd. it was further found that ms37452 as the lead compound was able to derepress the transcription of polycomb repressive complex target gene p16/cdkn2a through displacing cbx7 binding to the ink4a/arf locus in prostate cancer cells. these findings showed that ms37452 and its close analogs had the potential to be developed into high-potency chemical modulators targeting cbx7 functions in gene transcription in various disease pathways [1].
References
[1] ren, c. ,morohashi, k.,plotnikov, a.n., et al. small-molecule modulators of methyl-lysine binding for the cbx7 chromodomain. chemistry & biology 22, 161-168 (2015).
MS37452 Preparation Products And Raw materials
Raw materials
Preparation Products
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