Lactacystin is a kind of strong effect selective irreversible protease inhibitors body. Lactacystin is a kind of the earliest from Streptomyces (Streptomyces) from microbial metabolic, with differentiation function and inhibit tumor cell lines of the ability of cell cycle know-how for feature article. Lactacystin irreversible to alkylation 20 S protease body and the X.
In the accompanying protease body peptide inhibition of enzyme activity, led to a variety of the ubiquitin-proteasome the accumulation of the protein. Therefore, the influence of this kind of material is much effect and essentially depends on processed intracellular signaling protein expression mode. Be show that can restrain cell proliferation and induction of mice neuroblastoma cell lines such as neural 2 a nerve swelled the growth.
Lactacystin is a natural, irreversible, nonpeptide, cell permeable inhibitor that is more selective than peptide aldehydes but less selective than peptide boronates. Molecular Formula: C15H24N2O7S
Formula Weight: 376.43. Blocks proteasome activity by targeting the catalytic β-subunit. Has no effect on serine or cysteine proteases. Induces apoptosis inhuman monoblast U937 cells. Inhibits NF-κB activation by inhibiting IκB degradation (IC50=10 µM). Inhibits the ubiquitin proteasome pathway in cell culture. Inhibits cathepsin A. Upregulates HSP70 and HSP22, suggesting an initial neuroprotective pathway.
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