AEG 3482

Names

[ Name ]:
AEG 3482

[Synonym ]:
hms1538b12
6-Phenylimidazo[2,1-b][1,3,4]thiadiazole-2-sulfonamide
Imidazo[2,1-b]-1,3,4-thiadiazole-2-sulfonamide, 6-phenyl-
unii-7ezf1a283n

Biological Activity

[Description]:

AEG3482 is a potent antiapoptotic compound that inhibits Jun kinase (JNK) activity through induced expression of heat shock protein 70 (HSP70). AEG3482 directly binds HSP90, thereby facilitating HSF1-dependent expression of HSP70 and HSP25[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Neurological Disease

Signaling Pathways >> MAPK/ERK Pathway >> JNK

[Target]

JNK[1]

[In Vitro]

AEG3482 (0.3-30 μM; 2 d) inhibits nerve growth factor (NGF) withdrawal-induced death in SCG neurons, with an EC50 of ∼20 μM[1]. AEG3482 (1-80 μM; 40 h) inhibits p75NTR- and NRAGE- mediated apoptosis of PC12 cells in a dose-dependent manner[1]. AEG3482 (10-40 μM; 30 h) inhibits p75NTR- and NRAGE-mediated JNK activation in PC12 cells[1]. Apoptosis Analysis[1] Cell Line: PC12 cells Concentration: 1, 2.5, 5, 10, 20, 40, 80 μM Incubation Time: 40 hours Result: Reduced p75NTR- or NRAGE-induced cell death by greater than 90% at the concentration of 40 μM. Exerted a slight toxic effect in cells infected with the LacZ control at the concentration of 80 μM. Western Blot Analysis[1] Cell Line: PC12 cells Concentration: 10, 20, 40 μM Incubation Time: 30 hours Result: Attenuated p75NTR- and NRAGE-induced c-Jun phosphorylation and caspase-3 cleavage, and the levels of c-Jun protein.

[References]

[1]. Salehi AH, et, al. AEG3482 is an antiapoptotic compound that inhibits Jun kinase activity and cell death through induced expression of heat shock protein 70. Chem Biol. 2006 Feb;13(2):213-23.

Chemical & Physical Properties

[ Density]:
1.8±0.1 g/cm3

[ Molecular Formula ]:
C₁₀H₈N₄O₂S₂

[ Molecular Weight ]:
280.326

[ Exact Mass ]:
280.008881

[ PSA ]:
126.97000

[ LogP ]:
1.32

[ Index of Refraction ]:
1.835

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

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