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JFD00244 Sale

(Synonyms: BML-266) 目录号 : GC14686

An inhibitor of SIRT2

JFD00244 Chemical Structure

Cas No.:96969-83-4

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1mg
¥444.00
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5mg
¥967.00
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10mg
¥1,522.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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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.

Chemical Properties

Cas No. 96969-83-4 SDF
别名 BML-266
化学名 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
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°C
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1 mg 5 mg 10 mg
1 mM 2.0899 mL 10.4493 mL 20.8986 mL
5 mM 0.418 mL 2.0899 mL 4.1797 mL
10 mM 0.209 mL 1.0449 mL 2.0899 mL
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