Irreversible caspase-3 inhibitors as active site probes

Details Irreversible caspase-3 inhibitors as active site probes Irreversible caspase-3 inhibitors as active site probes

C - Chemistry, Metallurgy

07

B

C07B 59/00 (2006.01) C07C 237/22 (2006.01) C07K 5/00 (2006.01) C12Q 1/00 (2006.01) G01N 33/534 (2006.01)

Patent

CA 2514441

The present invention encompasses a compound of Formula (I) useful as caspase active site probes. These probes can be used to determine whether a caspase has been activated, in cells or in tissues of animal models of various pathologies. Furthermore, through competition based assays, these caspase active site probes can be used to calculate the percentage of occupancy of active caspases by other, unlabeled inhibitors.

L'invention concerne un composé de formule (I) utile en tant que sondes de sites actifs de caspase. Ces sondes peuvent être utilisées pour déterminer si une caspase a été activée, dans des cellules ou dans des tissus de modèles animaux de pathologies variées. En outre, grâce à des dosages par compétition, ces sondes de sites actifs de caspase peuvent être utilisées pour calculer le pourcentage d'occupation de caspases actives par d'autres inhibiteurs non marqués.

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