产品
编 号:F122819
分子式:C15H24N2O7S
分子量:376.43
产品类型
结构图
CAS No: 133343-34-7
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生物活性:
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 .
体内研究:
Lactacystin (2 μg, ICV) 在注射后 5-7 天诱导年轻和成年小鼠帕金森病样运动表型。Lactacystin (1.0 ug或5.0μg/20g,连续7天) 导致 C6 原位异种移植肿瘤模型肿瘤明显缩小,并促进组织凋亡。Lactacystin (5 mg/kg/每天,溶解在水中,给药6周) 诱导成年雄性 Wistar 大鼠高血压模型。Animal Model:Male C57Bl/6RccHsd mice with 8-9 weeks (young) and 12-14 months (adult) old
Dosage:2 μg
Administration:Microinjection
Result:Induced a Parkinson’s disease-like motor phenotype 5-7 days after injection in young and adult mice.
Animal Model:Male C57Bl/6RccHsd mice
Dosage:2 μg, 7days
Administration:Intracerebroventricular injection (ICV)
Result:Induced spontaneous contralateral rotating behavior.
Animal Model:C6 orthotopic xenograft tumor models
Dosage:1.0 ug or 5.0? μg/20g for 7days
Administration:Intravenous injection (i.p.)
Result:Reduced the tumor volume. Showed polygonal condensed nuclei with brown Tunnel staining indicating apoptosis in tumor tissue. Increased the mRNA and protein level in the ratio of Bax to Bcl-2 in tumor tissue.
体外研究:
Lactacystin (高达 25.6 μM, 1 h) 对 HeLa 和 SH-SY5Y 细胞无细胞毒性,可使 HeLa 细胞和 SH-SY5Y 细胞的 RVP 感染率分别降低 63.8% 和 74.5%。Lactacystin (2.5 μM) 联合 Parthenolide (HY-N0141) (5 μM) 可协同增加耐药 L1210 细胞的凋亡比例。Lactacystin (2.5, 5 和 10 μM, 24 h) 抑制 C6 细胞的增殖 (IC50 值为 10 μM),增加凋亡。Lactacystin (10μM, 24 h) 增加 Hela 细胞内 Cisplatin (HY-17394) 诱导的内质网应激相关的凋亡。Lactacystin (7.5 μM, 4-48 h) 可提高 HT-29 细胞的活性氧和谷胱甘肽水平。Lactacystin (1, 2.5, 5 μM, 24 h) 诱导新生大鼠皮质星形胶质细胞星性化。Lactacystin (10 μM, 8-24 h) 诱导 PC12 细胞凋亡,G2/M 细胞周期阻滞。