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MS37452 Sale

目录号 : GC12630

An inhibitor of CBX7 chromodomain binding to H3K27me3

MS37452 Chemical Structure

Cas No.:423748-02-1

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1mg
¥442.00
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5mg
¥1,311.00
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10mg
¥2,179.00
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25mg
¥4,895.00
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Sample solution is provided at 25 µL, 10mM.

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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:
[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).

Chemical Properties

Cas No. 423748-02-1 SDF
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°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.5094 mL 12.5471 mL 25.0941 mL
5 mM 0.5019 mL 2.5094 mL 5.0188 mL
10 mM 0.2509 mL 1.2547 mL 2.5094 mL
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