Biological Activity:
LDN-57444 is a novel potent and selective inhibitor of ubiquitin C-terminal hydrolase-L1 (UCH-L1) with IC50 ~0.88 μM. It has ~28-fold greater selectivity over UCH-L3 (ubiquitin C-terminal hydrolase L3). LDN-57444 can increase levels of highly ubiquitinated proteins and decreases ubiquitin proteasome activity. It causes cell death through the apoptosis pathway. LDN-57444’s activity leads to dramatic alterations in synaptic protein distribution and spine morphology in vivo.
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