Lactacystin is a microbial metabolite isolated from Streptomyces that is now widely used as a selective inhibitor of the 20S proteasome. Clasto-lactacystin β-lactone was later identified as the active metabolite of lactacystin, resulting from the elimination of cysteine and the formation of a reactive β-lactone. Both lactacystin and its β-lactone metabolite induce differentiation and inhibit cell cycle progression in several tumor cell lines. Clasto-lactacystin β-lactone irreversibly alkylates subunit X of the 20S proteasome. It is at least 10 times more active than the parent compound; this increased activity may be a function of increased cell permeability. Inhibition of proteasome peptidase activity results in the accumulation of a variety of ubiquitinated proteins which would normally undergo rapid degradation. Thus, the effects of clasto-lactacystin β-lactone are pleiotropic and depend substantially on the expression pattern of signaling proteins within the treated cell.
Clasto-Lactacystin β-lactone, a natural active metabolite of lactacystin, which is a metabolite of Streptomyces, acts as an irreversible 20S proteasome inhibitor.
IC50&Target
20S proteasome
体外研究
Clasto-Lactacystin β-lactone is a natural active metabolite of lactacystin, which is a metabolite of Streptomyces. Clasto-Lactacystin β-lactone is the cell cycle progression in an osteosarcoma cell line. Clasto-Lactacystin β-lactone is an irreversible 20S proteasome inhibitor, and also acts as a partial inhibitor of branched amino acid preferring peptidase (BrAAP). β-Lactone inactivates approximately 60% of the BrAAP activity rapidly, and the remaining 40% of the BrAAP activity is inactivated by β-lactone at a 50-fold slower rate.
分子式
C10H15NO4
分子量
213.23
CAS号
154226-60-5
中文名称
Clasto-乳胞素 β-内酯
运输条件
Room temperature in continental US; may vary elsewhere.