AGK2

SKU: orb1222390

Description

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

Key Properties

• CAS Number: 304896-28-4
• MW: 434.27
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₃Cl₂N₃O₂
• SMILES: c1cc2c(cccn2)c(c1)NC(=O)/C(=C/c1ccc(o1)c1c(ccc(c1)Cl)Cl)/C#N
• Target: PDE
• Solubility: DMSO : 6 mg/mL 13.82 mM

Bioactivity

• 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) compared with 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).
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• 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AGK-2 | AGK-2 | AGK-2

Quick Database Links

Gene Symbol

PDE