Cayman Chemical | Lactacystin | Description (CAS 133343-34-7)

70980 Lactacystin

(CAS 133343-34-7)

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Lactacystin is a microbial metabolite isolated from Streptomyces that is now widely used as a selective inhibitor of the 20 S proteasome.^1,2,3 Lactacystin was first characterized by its ability to induce differentiation and inhibit cell cycle progression in several tumor cell lines. At concentrations from 2 to 10 µM, lactacystin induces the outgrowth of neurites in the neuroblastoma cell line Neuro 2A.⁴ Lactacystin irreversibly alkylates subunit X of the 20 S proteasome.³ The concomitant 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 lactacystin are pleiotropic and depend substantially on the expression pattern of signalling proteins within the treated cell.

1 Omura, S., Fujimoto, T.T., Otoguro, K., et al. Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells. J Antibiotics 44 113-116 (1991 Jan 1).

2 Corey, E.J., Reichard, G.A. Total synthesis of lactacystin. J Am Chem Soc 114 10677-10678 (1992).

3 Fenteany, G., Schreiber, S.L. Lactacystin, proteasome function, and cell fate. J Biol Chem 273(15) 8545-8548 (1998).

4 Fenteany, G., Standaert, R.F., Reichard, G.A., et al. A β-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line. Proc Natl Acad Sci USA 91 3358-3362 (1994).

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Pricing updated 2010-03-19.
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