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4'-bromo-Resveratrol
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。
4'-bromo-Resveratrol图片
CAS NO:1224713-90-9
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
4'-Bromo-resveratrol 是一种有效的双重抑制剂 Sirtuin-1 和 Sirtuin-3。 4'-Bromo-resveratrol 通过线粒体代谢重编程抑制黑色素瘤细胞的生长。 4'-Bromo-resveratrol 通过代谢重编程和影响细胞周期和细胞凋亡信号传导在黑色素瘤细胞中发挥抗增殖作用。
Cas No.1224713-90-9
别名5-[(E)-2-(4-溴苯基)乙烯基]间苯二酚,4′‐BR
化学名5-[(1E)-2-(4-bromophenyl)ethenyl]-1,3-benzenediol
Canonical SMILESOC1=CC(O)=CC(/C=C/C2=CC=C(Br)C=C2)=C1
分子式C14H11BrO2
分子量291.1
溶解度≤50mg/ml in ethanol;50mg/ml in DMSO;100mg/ml in dimethyl formamide
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

4'-bromo-Resveratrol is a Sirt1 and Sirt3 inhibitor.

Sirtuins are protein deacetylases regulating aging processes and many physiological functions. Resveratrol activates human Sirt1 and inhibits Sirt3, and can mimic calorie restriction effects including lifespan extension in lower organisms.

In vitro: Sirtuin modulation was studied by using 4’-bromo-resveratrol in a previous study. 4’-bromo-Resveratrol inhibited Sirt3 with much higher potency than resveratrol, and it also inhibited rather than activated Sirt1. Crystal structures of human Sirt3/peptide complexes of 4’ -bromo-resveratrol identified two binding sites. An internal site caused the potent inhibitory effect. 4’-bromo-Resveratrol interfered with NAD+ and substrate peptide binding, and it extended its bromo-phenyl group in a unrecognized site pocket. The second binding site for 4’-bromo-resveratrol was found to be located on the surface of Sirt3 and connected via two helices to peptide-binding active site loops. In Sirt1, this site appeared to comprise a residue that was essential for its activation by small molecules and 4’-bromo-resveratrol therefore constituted a candidate for the long-sought allosteric Sirt1 activator binding site [1].

In vivo: So far, there is no animal in vivo data for 4'-bromo-resveratrol.

Clinical trial: Up to now, 4'-bromo-resveratrol is still in the preclinical development stage.

Reference:
[1] Nguyen GT, Gertz M, Steegborn C.  Crystal structures of Sirt3 complexes with 4'-bromo-resveratrol reveal binding sites and inhibition mechanism. Chem Biol. 2013 Nov 21;20(11):1375-85.