Enzymes

LDN-57444 is a cell permeable ubiquitin C-terminal hydrolase (UCH-L1) inhibitor (Ki=0.4 µM). Decreases proteasome activity and increases levels of ubiquitinated proteins. Induces apoptosis and causes dramatic alterations in synaptic protein distribution and spine morphology in vivo. LDN-57444 is a useful tool to study UCH-L1 in different pathological conditions such as cancer and neurodegeneration.

LDN-57444 is a cell permeable ubiquitin C-terminal hydrolase (UCH-L1) inhibitor (Ki=0.4 µM). Decreases proteasome activity and increases levels of ubiquitinated proteins. Induces apoptosis and causes dramatic alterations in synaptic protein distribution and spine morphology in vivo. LDN-57444 is a useful tool to study UCH-L1 in different pathological conditions such as cancer and neurodegeneration.

NSC 632839 hydrochloride is an inhibitor of USP (ubiquitin isopeptidase) activity that displays no effect on the proteolytic activity of the proteasome. Induces apoptosis via a Bcl-2-dependent and apoptosome-independent pathway of caspase activation.

NSC 632839 hydrochloride is an inhibitor of USP (ubiquitin isopeptidase) activity that displays no effect on the proteolytic activity of the proteasome. Induces apoptosis via a Bcl-2-dependent and apoptosome-independent pathway of caspase activation.

P22077 is a cell permeable inhibitor of the ubiquitin-specific protease USP7 (IC50=8.6 µM), and the closely related deubiquitinase (DUB) USP47. P22077 showed weak or no inhibition (EC50 >50µM) towards a panel of 14 isopeptidases and other proteases. Treatment of cells with P22077 (20-40 µM) causes an accumulation of K48-linked ubiquitinated species, and down regulation of the USP7 targets HDM2 and claspin.

PR-619 is a non-selective, reversible inhibitor of deubiquitinases/deubiquitylases (DUBs) and ubiquitin-like isopeptidases. PR-619 inhibits many deubiquitinating enzymes in the 5-20 µM range. Additionally, PR-619 is cell permeable and treatment of cells results in the accumulation of both ubiquitin and sumo-conjugated proteins.

PR-619 is a non-selective, reversible inhibitor of deubiquitinases/deubiquitylases (DUBs) and ubiquitin-like isopeptidases. PR-619 inhibits many deubiquitinating enzymes in the 5-20 µM range. Additionally, PR-619 is cell permeable and treatment of cells results in the accumulation of both ubiquitin and sumo-conjugated proteins.

PS-341 (Pyz-Phe-boroLeu) is the active ingredient in Bortezomib. PS-341 is a reversible, cell permeable, potent, and selective proteasome inhibitor (Ki=0.6 nM). It binds the catalytic site of the 26S proteasome with high affinity and specificity. Inhibits proliferation of a number of tumor cell lines (IC50=7 nM). Inhibits TNF synthesis and FGF-induced angiogenesis.

PS-341 (Pyz-Phe-boroLeu) is the active ingredient in Bortezomib. PS-341 is a reversible, cell permeable, potent, and selective proteasome inhibitor (Ki=0.6 nM). It binds the catalytic site of the 26S proteasome with high affinity and specificity. Inhibits proliferation of a number of tumor cell lines (IC50=7 nM). Inhibits TNF synthesis and FGF-induced angiogenesis.