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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
结构分类:抗生素 | 其他类 | 结构分类
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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