| CAS NO: | 96969-83-4 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 478.5 |
| Cas No. | 96969-83-4 |
| Formula | C30H26N2O4 |
| Synonyms | BML-266 |
| Solubility | ≤0.3mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | 1,4-bis[[2-(4-hydroxyphenyl)ethyl]amino]-9,10-anthracenedione |
| Canonical SMILES | O=C(C1=C2C(NCCC3=CC=C(O)C=C3)=CC=C1NCCC4=CC=C(O)C=C4)C5=C(C=CC=C5)C2=O |
| 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。 |
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.
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