Home>>Signaling Pathways>> Chromatin/Epigenetics>> Sirtuin>>JFD00244
JFD00244 Catalog No.GC14686

inhibitor of SIRT2

Size Price Stock Qty
1mg
$31.00
In stock
5mg
$69.00
In stock
10mg
$109.00
In stock

Customer Review

Based on customer reviews.

Tel: (626) 353-8530 Email: sales@glpbio.com

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

View current batch:

Chemical Properties

Cas No. 96969-83-4 SDF
Synonyms BML-266
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
Formula C30H26N2O4 M.Wt 478.5
Solubility ≤0.3mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

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.

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.