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]}. IC50 & Target:IC50: 4.8 μM (proteasome)^[1] 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 (10 μM, 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:Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

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].