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AGK7 (Synonyms: SIRT2 Inhibitor (Inactive Control))

Katalog-Nr.GC15931

AGK7 ist ein potenter Inhibitor von Sirtuin 2 (SIRT2).

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AGK7 Chemische Struktur

Cas No.: 304896-21-7

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

Chemical Properties

Cas No. 304896-21-7 SDF
Überlieferungen 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
Löslichkeit ≤0.5mg/ml in DMSO;0.2mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.3026 mL 11.5128 mL 23.0256 mL
5 mM 0.4605 mL 2.3026 mL 4.6051 mL
10 mM 0.2303 mL 1.1513 mL 2.3026 mL
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