JFD00244

- Overview
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    Background
    
    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.
- Properties
  - Alternative Name
    
    BML-266; 1,4-bis[[2-(4-hydroxyphenyl)ethyl]amino]-9,10-anthracenedione
    
    CAS Number
    
    96969-83-4
    
    Molecular Formula
    
    C30H26N2O4
    
    Molecular Weight
    
    478.5
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥ 95.00%
    
    Solubility
    
    ≤0.3mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

JFD00244

Background

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