Other grades of this product :
| MS37452 Basic information |
| Product Name: | MS37452 | | Synonyms: | MS37452;1-(2,3-dimethoxybenzoyl)-4-[(3-methylphenoxy)acetyl]piperazine;Ethanone, 1-[4-(2,3-dimethoxybenzoyl)-1-piperazinyl]-2-(3-methylphenoxy)-;1-(4-(2,3-Dimethoxybenzoyl)piperazin-1-yl)-2-(m-tolyloxy)ethanone | | CAS: | 423748-02-1 | | MF: | C22H26N2O5 | | MW: | 398.45224 | | EINECS: | | Product Categories: | | Mol File: | 423748-02-1.mol |
| MS37452 Chemical Properties |
| 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 |
| MS37452 Usage And Synthesis |
| 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 |
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