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Description: AGK2 is a novel, potent, and selective inhibitor of SIRT2 (sirtuin 2, histone deacetylase) with potential anti-inflammatory activity. As a cell-permeable epigenetic modifier, AGK2 inhibits SIRT2 with an IC50 value of 3.5 μM and showed little effects on SIRT1 and 3 at concentrations of over 40 μM. AGK 2 increased the level of acetylated tubulin heterodimers in bovine brain. In primary rat astrocytes, AGK-2 (35 μM) significantly inhibited astrocyte viability and proliferation and also inhibited astrocyte activation induced by beta amyloid 1-42 (Aβ 1-42).
References: Science. 2007 Jul 27;317(5837):516-9; Biochem Biophys Res Commun. 2012 Jan 6;417(1):468-72; Oncotarget. 2013 Dec;4(12):2354-65.
Product Catalog 2022
Guide to Product Handling
Synonym: AGK-2; AGK-2; AGK-2.
Chemical Name: 2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide
InChi Key: SVENPFFEMUOOGK-SDNWHVSQSA-N
InChi Code: InChI=1S/C23H13Cl2N3O2/c24-15-6-8-19(25)18(12-15)22-9-7-16(30-22)11-14(13-26)23(29)28-21-5-1-4-20-17(21)3-2-10-27-20/h1-12H,(H,28,29)/b14-11+
SMILES Code: O=C(NC1=C2C=CC=NC2=CC=C1)/C(C#N)=C/C3=CC=C(C4=CC(Cl)=CC=C4Cl)O3
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: In SIRT2-myc-expressing HeLa cells, AGK2 effectively inhibits the activity of SIRT2, and increases acetylated tubulin. AGK2 protects dopaminergic neurons from α-Syn–induced toxicity in primary midbrain cultures. AGK2 induces both necrosis and caspase-3-dependent apoptosis in C6 glioma cells. SIRT2 also decreases merlin-mutant viability of mouse schwann cells (MSCs) without substantially reducing wild-type MSC viability.
Cell Assay: Cells are exposed to different concentrations of AGK2 in 1 mL of 0.3% basal medium agar containing 10% FBS. The cultures are maintained at 37°C in a 5% CO2 incubator for 10-15 days, and the cell colonies are scored using an inverted microscope
Science. 2007 Jul 27;317(5837):516-9; Oncotarget. 2013 Dec;4(12):2354-65.; Curr Mol Med. 2015;15(7):634-41.
Purity ≥98%
COA
MSDS
NMR