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Lactacystin

MCE 國際站：Lactacystin

品牌：MedChemExpress (MCE)

貨號：HY-16594

CAS：133343-34-7

中文名稱：蛋白酶體抑制劑

Synonyms：蛋白酶體抑制劑

純度：98.20%

存儲條件：粉末 -20°C 3 年 溶劑中 -80°C 6 個(gè)月 -20°C 1 個(gè)月

運(yùn)輸條件：美國大陸的室溫；其他地方可能有所不同。

產(chǎn)品活性：Lactacystin 是一種有效的、口服活性、不可逆的、細(xì)胞滲透性的，選擇性的 20S 蛋白酶體 (proteasome) 抑制劑 (IC50 = 4.8 μM)。Lactacystin 還能抑制溶酶體酶組織蛋白酶 A (cathepsin A)。Lactacystin 抑制細(xì)胞生長，誘導(dǎo)細(xì)胞凋亡 (apoptosis) 和周期阻滯，并具有抗病毒和抗氧化活性。Lactacystin 誘導(dǎo)神經(jīng)突生長，誘發(fā)高血壓。Lactacystin 在癌癥、神經(jīng)系統(tǒng)疾病、高血壓和瘧疾等方面具有研究潛力。

生物活性：Lactacystin 是一種強(qiáng)效、口服、不可逆、細(xì)胞通透性、選擇性 20S 蛋白酶體抑制劑（IC50 = 4.8 μM）。Lactacystin 還抑制溶酶體酶蛋白酶 A。Lactacystin 抑制細(xì)胞生長并誘導(dǎo)細(xì)胞凋亡和細(xì)胞周期停滯，并具有抗病毒和抗氧化活性。Lactacystin 誘導(dǎo)神經(jīng)突生長和高血壓。Lactacystin 具有研究癌癥、神經(jīng)系統(tǒng)疾病、高血壓和瘧疾等的潛力[1] [2] [3] [4] [5] [6] [7] [8] [9] [10] 。

體外：Lactacystin (高達(dá) 25.6 µM, 1 h) 對 HeLa 和 SH-SY5Y 細(xì)胞無細(xì)胞毒性，可使 HeLa 細(xì)胞和 SH-SY5Y 細(xì)胞的 RVP 感染率分別降低 63.8% 和 74.5%[2]。 Lactacystin (2.5 μM) 聯(lián)合 Parthenolide (HY-N0141) (5 μM) 可協(xié)同增加耐藥 L1210 細(xì)胞的凋亡比例[3]。 Lactacystin (2.5, 5 和 10 µM, 24 h) 抑制 C6 細(xì)胞的增殖 (IC50 值為 10 μM)，增加凋亡[4]。 Lactacystin (10μM, 24 h) 增加 Hela 細(xì)胞內(nèi) Cisplatin (HY-17394) 誘導(dǎo)的內(nèi)質(zhì)網(wǎng)應(yīng)激相關(guān)的凋亡[5]。 Lactacystin (7.5 μM, 4-48 h) 可提高 HT-29 細(xì)胞的活性氧和谷胱甘肽水平[6]。 Lactacystin (1, 2.5, 5 μM, 24 h) 誘導(dǎo)新生大鼠皮質(zhì)星形膠質(zhì)細(xì)胞星性化[7]。 Lactacystin (10 μM, 8-24 h) 誘導(dǎo) PC12 細(xì)胞凋亡，G2/M 細(xì)胞周期阻滯[10]。 MCE尚未獨(dú)立證實(shí)這些方法的準(zhǔn)確性。僅供參考。

體內(nèi)：Lactacystin (2 μg, ICV) 在注射后 5-7 天誘導(dǎo)年輕和成年小鼠帕金森病樣運(yùn)動(dòng)表型[8]。 Lactacystin (1.0 ug或5.0µg/20g，連續(xù)7天) 導(dǎo)致 C6 原位異種移植腫瘤模型腫瘤明顯縮小，并促進(jìn)組織凋亡[4]。 Lactacystin (5 mg/kg/每天，溶解在水中，給藥6周) 誘導(dǎo)成年雄性 Wistar 大鼠高血壓模型[9]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50 & Target：4.8 μM (proteasome)[1]

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參考文獻(xiàn)：

[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]. 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.
[3].  Shaobo Wang, et al. The ubiquitin-proteasome system is essential for the productive entry of Japanese encephalitis virus. Virology. 2016 Nov;498:116-127.
[4]. 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.
[5].  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.
[6]. 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.
[7]. 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.
[8]. Qing-Guo Ren, et al. Lactacystin stimulates stellation of cultured rat cortical astrocytes. Neurochem Res. 2009 May;34(5):859-66.
[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.