AGK2


Catalog No. size PriceQuantity
M6535-2 2mg solid $121
M6535-10 10mg solid $494

Description

Cas:304896-28-4

Product Information:

AGK2 is a potent and selective inhibitor of sirtuin 2 (SIRT2).

 

Chemical Formula: C23H13Cl2N3O2

 

Exact Mass: 433.0385

 

Molecular Weight: 434.276

 

Elemental Analysis: C, 63.61; H, 3.02; Cl, 16.33; N, 9.68; O, 7.37

 

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

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

AGK2 significantly inhibits cell proliferation in a dose-dependent manner. AGK2 also significantly inhibits cell growth in a dose-dependent manner without inducing cytotoxicity at low doses. Twelve days after AGK2 (5 μM) treatment, cells show a significantly reducing colony forming ability in soft agar to 46% of the control cells. Western blot analysis shows that the levels of CDK4 or CDK6 and cyclin D1 are decreased after AGK2 treatment in a dose-dependent manner. In addition, AGK2 inhibits the expression of p53 protein. Treatment of microglial BV2 cells with 10 μM AGK2 leads to a significant increase in PAR signals. Treatment of microglial BV2 cells with 10 μM AGK2 also leads to a significant decrease in the intracellular ATP and significant increases in both late-stage apoptosis and necrosis of the cells.

 

In Vivo:

AGK2 significantly reduces mortality and decreases levels of cytokines in blood (TNF-α: 298.3±24.6 vs 26.8±2.8 pg/mL, p=0.0034; IL-6: 633.4±82.8 vs 232.6±133.0 pg/mL, p=0.0344) and peritoneal fluid (IL-6: 704.8±67.7 vs 391.4±98.5 pg/mL, p=0.033) compare to vehicle control. AGK2 also suppresses the TNF-α and IL-6 production in the culturing splenocytes (TNF-α: 68.1±6.4 vs 23.9±2.8 pg/mL, p=0.0009; IL-6: 73.1±4.2 vs 49.6±3.0 pg/mL; p=0.0051).

 

 

References:

 

  1. Biella G, Fusco F, Nardo E, Bernocchi O, Colombo A, Lichtenthaler SF, Forloni G, Albani D. Sirtuin 2 Inhibition Improves Cognitive Performance and Acts on Amyloid-β Protein Precursor Processing in Two Alzheimer's Disease Mouse Models. J Alzheimers Dis. 2016 Jun 30;53(3):1193-207. doi: 10.3233/JAD-151135. PubMed PMID: 27372638.

 

  1. Shimizu K, Quillinan N, Orfila JE, Herson PS. Sirtuin-2 mediates male specific neuronal injury following experimental cardiac arrest through activation of TRPM2 ion channels. Exp Neurol. 2016 Jan;275 Pt 1:78-83. doi: 10.1016/j.expneurol.2015.10.014. Epub 2015 Oct 30. PubMed PMID: 26522013; PubMed Central PMCID: PMC5193101.

 

  1. Scuderi C, Stecca C, Bronzuoli MR, Rotili D, Valente S, Mai A, Steardo L. Sirtuin modulators control reactive gliosis in an in vitro model of Alzheimer's disease. Front Pharmacol. 2014 May 13;5:89. doi: 10.3389/fphar.2014.00089. eCollection 2014. PubMed PMID: 24860504; PubMed Central PMCID: PMC4027795.

 

  1. Rotili D, Tarantino D, Nebbioso A, Paolini C, Huidobro C, Lara E, Mellini P, Lenoci A, Pezzi R, Botta G, Lahtela-Kakkonen M, Poso A, Steinkühler C, Gallinari P, De Maria R, Fraga M, Esteller M, Altucci L, Mai A. Discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. J Med Chem. 2012 Dec 27;55(24):10937-47. doi: 10.1021/jm3011614. Epub 2012 Dec 12. PubMed PMID: 23189967.

 

  1. Mai A. Small-molecule chromatin-modifying agents: therapeutic applications. Epigenomics. 2010 Apr;2(2):307-24. doi: 10.2217/epi.10.7. Review. PubMed PMID: 22121876.

 

Products are for research use only. Not for human use.

 

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