2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide
2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide Basic information
- Product Name:
- 2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide
- Synonyms:
-
- 2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide
- SIRT2 Inhibitor, AGK2 - CAS 304896-28-4 - Calbiochem
- CS-2248
- AGK2;AGK-2;AGK 2
- AGK2
- SIRT2 Inhibitor, AGK2
- 2-Cyano-3-(5-(2,5-dichlorophenyl)furan-2-yl)-N-(quinolin-5-yl)acrylamide
- 2-Propenamide, 2-cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-
- CAS:
- 304896-28-4
- MF:
- C23H13Cl2N3O2
- MW:
- 434.27
- Product Categories:
-
- Inhibitors
- Mol File:
- 304896-28-4.mol
2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide Chemical Properties
- Boiling point:
- 675.1±55.0 °C(Predicted)
- Density
- 1.445±0.06 g/cm3(Predicted)
- storage temp.
- room temp
- solubility
- DMSO: soluble2mg/mL, clear (warmed)
- form
- Yellow solid
- pka
- 8.87±0.43(Predicted)
- color
- White to Yellow to Orange
2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide Usage And Synthesis
Uses
AGK2 is a SIRT2 inhibitor. AGK2 has been used in a study to determine that SIRT2 inhibition induces cell death and decreases the intracellular ATP level. AGK2 also rescues dopamine neurons from α-synuclein toxicity in Parkinson′s disease models.
Definition
ChEBI: 2-cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-(5-quinolinyl)-2-propenamide is a member of quinolines.
Biological Activity
Selective inhibitor of SIRT2 (IC 50 = 3.5 μ M). Displays no activity at SIRT1 and SIRT3 at concentrations up to 40 μ M. Reduces α -synuclein-mediated toxicity in in vitro and in vivo models of Parkinson's disease.
Biochem/physiol Actions
AGK2 is a SIRT2 inhibitor. AGK2 rescues dopamine neurons from α-synuclein toxicity in Parkinson′s disease models. IC50 for SIRT2 = 3.5 uM. AGK2 is >15-fold more selective for SIRT2 than SIRT1 and SIRT3. AGK2 may be the most selective SIRT2 inhibitor available.
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, 317(5837): 516-519.
[2]. scuderi c, stecca c, bronzuoli mr, et al. sirtuin modulators control reactive gliosis in an in vitro model of alzheimer's disease. front pharmacol, 2014, 5: 89.
[3]. rotili d, tarantino d, nebbioso a, et al. discovery of salermide-related sirtuin inhibitors: binding mode studies and antiproliferative effects in cancer cells including cancer stem cells. j med chem, 2012, 55(24): 10937-10947.
2-Cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamideSupplier
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