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Lactacystin

MCE China：Lactacystin

Brand：MedChemExpress (MCE)

Cat. No.HY-16594

CAS：133343-34-7

Purity：98.20%

Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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] .

In Vitro：Lactacystin (up to 25.6 µM, 1 h) has no cytotoxicity to HeLa or SH-SY5Y cells, and decreases RVP infection by 63.8% in HeLa and by 74.5% in SH-SY5Y cells[2]. Lactacystin (2.5 μM) in combination with Parthenolide (HY-N0141) (5 μM) causes a synergistic increase in the apoptotic fraction of the drug-resistant L1210 cells[3]. Lactacystin（2.5, 5 and 10 µM, 24 h）inhibits the proliferation (IC50 value of 10 μ M) and increases the apoptotic in C6 cells[4]. Lactacystin (10μM, 24 h) increases Cisplatin (HY-17394)-induced ER stress-associated apoptosis in Hela cells[5]. Lactacystin (7.5 μM, 4-48 h) increased reactive oxygen species and GSH levels in HT-29 cells[6]. Lactacystin (1, 2.5, 5 μM, 24 h) induces stellation in astrocytes from neonatal rat cortex[7]. Lactacystin (10μM, 8-24 h) induces apoptosis, G2/M cell cycle arrest in the PC12 cells[10].

In Vivo：Lactacystin (2 μg for ICV) induces a Parkinson’s disease-like motor phenotype 5-7 days after injection in young and adult mice[8]. Lactacystin (1.0 ug or 5.0 µg/20g for 7days) results in significantly smaller tumor and promotes apoptosis than control in C6 orthotopic xenograft tumor models[4]. Lactacystin (5 mg/kg/day, dissolved in drinking water, six weeks) induces model of hypertension in male adult Wistar rats[9].

IC50 & Target：IC50: 4.8 μM (proteasome)[1] Cellular Effect Cell Line Type Value Description References

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References：

[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.  [Content Brief]

[2]. Shaobo Wang, et al. The ubiquitin-proteasome system is essential for the productive entry of Japanese encephalitis virus. Virology. 2016 Nov;498:116-127.  [Content Brief]

[3]. 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.  [Content Brief]

[4]. 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.  [Content Brief]

[5]. 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.  [Content Brief]

[6]. 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/  [Content Brief]

[7]. Qing-Guo Ren, et al. Lactacystin stimulates stellation of cultured rat cortical astrocytes. Neurochem Res. 2009 May;34(5):859-66.  [Content Brief]

[8]. 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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]