Chemical Name: 1-[1-(4-Chlorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-piperidinyl)ethanone
Biological ActivityPotent USP14 inhibitor (IC50 = 60 nM). Demonstrates >30-fold selectivity for USP14 over USP5 (IsoT). Enhances degradation of proteasome substrates in vitro. Increases degradation of wild type and pathological tau in MEFs, primary neuronal cultures and human iPSC derived neurons.
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An inhibitor of the proteasomal deubiquitinating enzyme USP14 induces tau elimination in cultured neurons.
Boselli M, Lee BH, Robert J et al.
J. Biol. Chem.
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