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AA74-1 is an extremely potent and selective inhibitor of the serine hydrolase acyl-peptide hydrolase (APEH) with an IC50 of 5 nM in mouse T-cell proteomes. AA74-1 potently blocked the activity of its target serine hydrolase, APEH, in mice in vivo without significantly affecting other enzymes. The APEH inhibition caused accumulation of N-acetylated proteins and stimulated cellular proliferation in T cells.
The APEH gene is deleted in some cancers, in which it has been proposed to serve as a potential tumor suppressor, and is involved in the degradation of oligomeric amyloid-beta which could make it a new target for therapy aimed at reducing neurodegeneration in Alzheimer′s disease. AA74-1 is the first selective tool for studying APEH activity.
| Molecular Weight | 308.42 |
| Formula | C16H28N4O2 |
| CAS Number | 1361532-00-4 |
| Solubility (25°C) | DMSO: ≥15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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