您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > MS37452
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
MS37452
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MS37452图片
CAS NO:423748-02-1
规格:98%
分子量:398.5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
competitive inhibitor of CBX7 chromodomain binding to H3K27me3
CAS:423748-02-1
分子式:C22H26N2O5
分子量:398.5
纯度:98%
存储:Store at -20°C

Background:

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).