Lactacystin蛋白酶体抑制剂,133343-34-7

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Lactacystin

CAS No. : 133343-34-7

MCE 国际站：Lactacystin

产品活性：Lactacystin 是一种有效的、口服活性、不可逆的、细胞渗透性的，选择性的 20S 蛋白酶体 (proteasome) 抑制剂 (IC₅₀ = 4.8 μM)。Lactacystin 还能抑制溶酶体酶组织蛋白酶 A (cathepsin A)。Lactacystin 抑制细胞生长，诱导细胞凋亡 (apoptosis) 和周期阻滞，并具有抗病毒和抗氧化活性。Lactacystin 诱导神经突生长，诱发高血压。Lactacystin 在癌症、神经系统疾病、高血压和疟疾等方面具有研究潜力。

研究领域：Metabolic Enzyme/Protease  |  Apoptosis  |  Protein Tyrosine Kinase/RTK

作用靶点：Proteasome  |  Apoptosis  |  ROS Kinase

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.
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.
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.
Lactacystin (10μM, 24 h) increases Cisplatin (HY-17394)-induced ER stress-associated apoptosis in Hela cells.
Lactacystin (7.5 μM, 4-48 h) increased reactive oxygen species and GSH levels in HT-29 cells.
Lactacystin (1, 2.5, 5 μM, 24 h) induces stellation in astrocytes from neonatal rat cortex.
Lactacystin (10μM, 8-24 h) induces apoptosis, G2/M cell cycle arrest in the PC12 cells.

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.
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.
Lactacystin (5 mg/kg/day, dissolved in drinking water, six weeks) induces model of hypertension in male adult Wistar rats.

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