| CAS NO: | 423748-02-1 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 423748-02-1 |
| 化学名 | 1-[4-(2,3-dimethoxybenzoyl)-1-piperazinyl]-2-(3-methylphenoxy)-ethanone |
| Canonical SMILES | COC1=CC=CC(C(N2CCN(C(COC3=CC(C)=CC=C3)=O)CC2)=O)=C1OC |
| 分子式 | C22H26N2O5 |
| 分子量 | 398.5 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Ki = 43 μM MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3. Chromobox homolog 7 (CBX7) functions via its N-terminal chromodomain, which recognizes histone 3 trimethyl lysine 27 (H3K27me3), to repress gene transcription. Chromobox homolog 7 plays a critical role in gene transcription in cellular processes associated with stem cell differentiation and self-renewal, as well as tumor progression. 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]. In vivo: Up to now, there is no animal in vivo data reported. Clinical trial: So far, no clinical study has been conducted. Reference: |
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