LDN-91946 is a potent, selective and uncompetitive UCH-L1 inhibitor that targets the enzyme-substrate complex, but not the free enzyme.
LDN-91946 is a potent, selective and uncompetitive UCH-L1 inhibitor that targets the enzyme-substrate complex, but not the free enzyme. Ubiquitin C-terminal hydrolase L1 (UCH-L1) is a deubiquitinating enzyme. It is one of the most abundant proteins in the brain. UCKL1 plays a key role in processing polyubiquitin and ubiquitylated proteolytic peptides. The enzyme has been linked to Parkinson disease and lung cancer. LDN-91946 inhibits UCH-L1-catalyzed substrate hydrolysis in an uncompetitive manner by targeting the enzyme-substrate complex, but not the free enzyme. The compound is quite specific and is exhibiting little activity against UCH-L3, TGase 2, Papain, or Caspase-3 even at concentrations as high as 20 μM. Compound was recently launched by Calbiochem. LDN-57444 is acts as competitive inhibitor.