| AGK7cell-permeable, selective inhibitor of SIRT2 |
Sample solution is provided at 25 µL, 10mM.
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| Cas No. | 304896-21-7 | SDF | Download SDF |
| Synonyms | SIRT2 Inhibitor (Inactive Control) | ||
| Chemical Name | 2-cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-8-quinolinyl-2-propenamide | ||
| Canonical SMILES | O=C(/C(C#N)=C/C1=CC=C(C2=CC(Cl)=CC=C2Cl)O1)NC3=CC=CC4=C3N=CC=C4 | ||
| Formula | C23H13Cl2N3O2 | M.Wt | 434.3 |
| Solubility | ≤0.5mg/ml in DMSO;0.2mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
AGK7 is an inactive control of AGK2, a cell-permeable and selective SIRT2 inhibitor [1][2].
The sirtuins are members of the histone deacetylase family of proteins that participate in many cellular functions and play an important role in aging. Silent information regulator 2 (Sir2) is a nicotinamide adenine dinucleotide-dependent histone deacetylase (HDAC) in yeast that participates in cell protection and cell cycle regulation. Human SIRT2 is involved in cell cycle regulation through the deacetylation ofα-tubulin [1].
AGK7 is an inactive control of AGK2 to be used in experiments with AGK2. AGK2 is a cell-permeable, potent and selective SIRT2 inhibitor with IC50 value of 3.5 μM. AGK2 slightly inhibited SIRT1 and 3 only at concentrations over 40 μM. Relative to an inactive control AGK7, AGK2 increased acetylated tubulin. In H4 cells transfected with α-Syn, AGK2 reduced α-Syn-mediated toxicity in a dose-dependent way. By contrast, the inactive AGK7 had no effect. In H4 cells cotransfected withα-Syn and synphilin-1, the inactive AGK7 failed to affect a-Syn aggregation, whereas AGK2 promoted the formation of enlarged inclusions [1].
References:[1]. Outeiro TF, Kontopoulos E, Altmann SM, et al. Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson"s disease. Science. 2007 Jul 27;317(5837):516-9.[2]. Cole PA. Chemical probes for histone-modifying enzymes. Nat Chem Biol. 2008 Oct;4(10):590-7.
