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JFD00244
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。
JFD00244图片
CAS NO:96969-83-4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
JFD00244 是一种 sirtuin 2 (SIRT2) 抑制剂,具有抗肿瘤作用。 JFD00244 也是一种针对 SARS-CoV-2 的 Nsp-16 抑制剂。
Cas No.96969-83-4
别名BML-266
化学名1,4-bis[[2-(4-hydroxyphenyl)ethyl]amino]-9,10-anthracenedione
Canonical SMILESO=C(C1=C2C(NCCC3=CC=C(O)C=C3)=CC=C1NCCC4=CC=C(O)C=C4)C5=C(C=CC=C5)C2=O
分子式C30H26N2O4
分子量478.5
溶解度≤0.3mg/ml in ethanol;30mg/ml in DMSO;30mg/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

IC50: 56.7 μM

JFD00244 is an inhibitor of SIRT2.

Silent information regulator 2 (Sir2) protein, a nicotinamide adenine dinucleotide (NAD+) dependent class III histone deacetylase (HDAC), is present in prokaryotes and all eukaryotes. Sir2 can catalyze the cleavage of the glycosidic bond between nicotinamide and ADP-ribose of NAD+, followed by transfer of the acetyl group from an acetylated lysine residue to ADP-ribose, leading to free nicotinamide and 2’- and 3’-O-acetyl-ADP-ribose. Sir2 is needed for various cellular functions including cell cycle, metabolism, chromatin silencing, and life span.

In vitro: In a previou study, the molecular modeling and virtual screening were utilized to identify potential compounds, which were then subjected to experimental tests for their SIRT2 inhibitory activity. Five of the 15 tested compounds including JFD00244 displayed inhibitory activity toward SIRT2, resulting in a hit ratio of 33% in a micromolar level. JFD00244 and another analog of the five compounds yielded in vitro IC(50) values of 56.7 and 74.3 microM, respectively. On the basis of these results, a phenol moiety on the active compounds including JFD00244 was suggested to be critical for SIRT2 inhibitory activity. This phenol group, together with a hydrophobic moiety and hydrogen-bonding features, was thus recommended to form an active SIRT2 pharmacophore [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] Tervo AJ, Kyrylenko S, Niskanen P, Salminen A, Leppnen J, Nyrnen TH, Jrvinen T, Poso A.  An in silico approach to discovering novel inhibitors of human sirtuin type 2. J Med Chem. 2004 Dec 2;47(25):6292-8.