AGK2


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

Description

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

Product information

CAS Number: 304896-28-4

Molecular Weight: 434.27

Formula: C23H13Cl2N3O2

Synonym:

AGK-2

AGK 2

Chemical Name: 2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide

Smiles: N#CC(=CC1=CC=C(O1)C1=CC(Cl)=CC=C1Cl)C(=O)NC1=CC=CC2=NC=CC=C21

InChiKey: SVENPFFEMUOOGK-SDNWHVSQSA-N

InChi: 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+

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO: 10 mg/mLwarmed(23.02 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.
  2. 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.
  3. 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.

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

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