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CPI-637
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。
CPI-637图片
CAS NO:1884712-47-3
包装与价格：
包装价格(元)
10mg询价
50mg询价

CPI-637 是一种选择性且有效的 CBP/EP300 溴结构域抑制剂，对 CBP、EP300 和 BRD4 BD-1 的 IC50 值分别为 0.03 μM、0.051 μM 和 11.0 μM，对 CBP 的 EC50 值为 0.3 μM。
Cas No.1884712-47-3
化学名(S)-4-methyl-6-(1-methyl-3-(1-methyl-1H-pyrazol-4-yl)-1H-indazol-5-yl)-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one
Canonical SMILESO=C1NC2=CC=CC(C3=CC4=C(N(C)N=C4C5=CN(C)N=C5)C=C3)=C2N[C@@H](C)C1
分子式C22H22N6O
分子量386.45
溶解度≥ 19.3mg/mL in DMSO with gentle warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 0.03 and 11.0 μM for CBP/EP300 and BRD4, respectively.

CPI-637 is a CBP/EP300 bromodomain inhibitor.

It has been reported that among bromodomain-containing proteins implicated in various disease pathways, cyclic-AMP response element binding protein (CBP) and adenoviral E1A binding protein of 300 kDa (EP300), which is a highly homologous pair of bromodomain-containing transcriptional coactivators, are of great interest as potential drug targets due to their reported involvement in a variety of disease states.

In vitro: Previous study found that CPI-637 was potent against EP300, and its opposite enantiomer showed a over 200-fold loss in potency. Moreover, the biochemical potency of CPI-637 translated well into cells with CBP BRET EC50 of 0.3 μM, and CPI-637 demonstrated a more than 700-fold selectivity over the BET family of bromodomains. In addition, CPI-637 was also highly selective against other bromodomains, showing substantial biochemical activity only against BRD9. Furthermore, it was found that CPI-637 was able to inhibit the expression of MYC with an EC50 of 0.60 μM in a cellular assay,. [1].

In vivo: So far, there is no animal in vivo data reported.

Clinical trial: Up to now, CPI-637 is still in the preclinical development stage.

Reference:
[1] Taylor, A.  M. et al. Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637). ACS medicinal chemistry letters 7, 531-536, doi:10.1021/acsmedchemlett.6b00075 (2016).

 
 
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