CAS NO: | 1224713-90-9 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 291.1 |
Cas No. | 1224713-90-9 |
Formula | C14H11BrO2 |
Solubility | ≤50mg/ml in ethanol;50mg/ml in DMSO;100mg/ml in dimethyl formamide |
Chemical Name | 5-[(1E)-2-(4-bromophenyl)ethenyl]-1,3-benzenediol |
Canonical SMILES | OC1=CC(O)=CC(/C=C/C2=CC=C(Br)C=C2)=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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.