| Bioactivity | 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] . | |||||||||
| Target | IC50: 4.8 μM (proteasome) | |||||||||
| Invitro | 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%[2]。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[3]。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[4]。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[5]。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[6]。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[7]。Lactacystin (10 μM, 8-24 h) 诱导 PC12 细胞凋亡，G2/M 细胞周期阻滞[10]。 Cell Viability Assay[4] Cell Line: | |||||||||
| In Vivo | 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[8]。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[4]。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[9]。 Animal Model: | |||||||||
| Name | Lactacystin | |||||||||
| CAS | 133343-34-7 | |||||||||
| Formula | C15H24N2O7S | |||||||||
| Molar Mass | 376.43 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
|
|||||||||
| Reference | [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. [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. [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. [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. [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. [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/ [7]. Qing-Guo Ren, et al. Lactacystin stimulates stellation of cultured rat cortical astrocytes. Neurochem Res. 2009 May;34(5):859-66. [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. [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. [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. |
Lactacystin
CAS: 133343-34-7 F: C15H24N2O7S W: 376.43
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.