Lactacystin

Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM) . Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on[1][2] [3][4][5][6] [7][8][9][10].

Product Specifications

CAS Number

[133343-34-7]

UNSPSC

12352005

Target

Apoptosis; Cathepsin; Proteasome

Type

Natural Products

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Neuroscience-Neurodegeneration

Field of Research

Cancer; Infection; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/lactacystin.html

Purity

98.20

Solubility

DMSO : 20 mg/mL (ultrasonic; warming)

Smiles

O=C(O)[C@H](CSC([C@]([C@@H](O)[C@H]1C)([C@@H](O)C(C)C)NC1=O)=O)NC(C)=O

Molecular Formula

C15H24N2O7S

Molecular Weight

376.43

References & Citations

[1]Csizmadia V, et al. Effect of proteasome inhibitors with different chemical structures on the ubiquitin-proteasomesystem in vitro. Vet Pathol. 2010 Mar;47 (2) :358-67.|[2]Savolainen MH, et al. Nigral injection of a proteasomal inhibitor, lactacystin, induces widespread glial cell activationand shows various phenotypes of Parkinson's disease in young and adult mouse. Exp Brain Res. 2017 Jul;235 (7) :2189-2202.|[3] Shaobo Wang, et al. The ubiquitin-proteasome system is essential for the productive entry of Japanese encephalitis virus. Virology. 2016 Nov;498:116-127. |[4]Ann H Cory, et al. Lactacystin, a proteasome inhibitor, potentiates the apoptotic effect of parthenolide, an inhibitor of NFkappaB activation, on drug-resistant mouse leukemia L1210 cells. Anticancer Res 2002 Nov-Dec;22 (6C) :3805-9. |[5] Haifeng Wang, et al. The proteasome inhibitor lactacystin exerts its therapeutic effects on glioma via apoptosis: an in vitro and in vivo study. J Int Med Res. 2013 Feb;41 (1) :72-81. |[6]Ye Xu, et al. Proteasome inhibitor lactacystin enhances cisplatin cytotoxicity by increasing endoplasmic reticulum stress-associated apoptosis in HeLa cells. Mol Med Rep. 2015 Jan;11 (1) :189-95. |[7]Nils-Erik Huseby, et al. The proteasome inhibitor lactacystin enhances GSH synthesis capacity by increased expression of antioxidant components in an Nrf2-independent, but p38 MAPK-dependent manner in rat colorectal carcinoma cells. Free Radic Res. 2016;50 (1) :1-13. https://pubmed.ncbi.nlm.nih.gov/26530909/|[8]Qing-Guo Ren, et al. Lactacystin stimulates stellation of cultured rat cortical astrocytes. Neurochem Res. 2009 May;34 (5) :859-66.|[9]Fedor Simko, et al. Lactacystin-Induced Model of Hypertension in Rats: Effects of Melatonin and Captopril. Int J Mol Sci. 2017 Jul 25;18 (8) :1612.|[10]Zhentao Zhang, et al. Cell cycle events mediate lactacystin-induced apoptotic death of neuronal PC12 cells. Cell Biol Int. 2010 Dec;34 (12) :1181-7.