産品簡介:
MG-132 蛋白(bái)酶體抑制劑
産品标簽
MG-132（Z-Leu-Leu-Leu-CHO）；Proteasome Inhibitor蛋白(bái)酶體抑制劑；Calpain Inhibitor鈣蛋白(bái)酶抑制劑；；NF-κB activation；CAS：133407-82-6；
産品信息
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産品名稱
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産品編号
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CAS NO.
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規格
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價格（元）
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MG-132蛋白(bái)酶體抑制劑
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MZ1701-0001MG
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133407-82-6
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1mg
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215
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産品描述
MG-132（MG132，MG 132），也稱為(wèi)Z-Leu-Leu-Leu-al，Z-Leu-Leu-Leu-CHO，是一(yī)種強效的，可逆且具細胞滲透性的蛋白(bái)酶體Proteasome抑制劑（IC50=100 nM），還(hái)是細胞周期和細胞周期蛋白(bái)降解所需的鈣蛋白(bái)酶Calpain抑制劑（IC50=1.2 μM）[1]。A549細胞中MG-132（10μM）有效抑制TNFα誘導的NF-κB活化、IL-8基因轉錄和IL-8蛋白(bái)分泌，通(tōng)過抑制蛋白(bái)酶體介導的IκBα降解來發揮作用[2]。MG-132（10μM）對NF-κB的抑制效應促使人胰腺癌細胞對依托泊甙Etoposide或阿黴素Doxorubicin的凋亡誘導更加敏感[3]。在PC3和DU145雄激素非依賴的前列腺癌（AIPCa）細胞系中MG-132能(néng)顯著改善六磷酸肌醇（IP6）對細胞代謝的減低(dī)能(néng)力[4]。
本品以凍幹粉形式提供，純度≥98%，可溶于DMSO或無水(shuǐ)乙醇配制成儲存液，之後用培養基或生(shēng)理緩沖液稀釋到(dào)需要的工(gōng)作濃度即可。
産品特性
1）CAS NO：133407-82-6
2）化學名：N-[(phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide
3）同義名：MG132; MG 132; Z-Leu-Leu-Leu-CHO; Z-Leu-Leu-Leu-al;
Z-LLL-CHO;Carbobenzoxy-L-leucyl- L-leucyl-L-leucinal;
4）分子式：C26H41N3O5
5）分子量：475.6
6）純度：≥98%
7） 外觀：白(bái)色至類白(bái)色固體
8）溶解性：溶于DMSO（30 mg/ml），無水(shuǐ)乙醇（20mg/ml）
9）化學結構圖：
保存與運輸方法
保存：-20℃幹燥保存，至少2年(nián)有效。
運輸：常溫運輸。
産品使用
1） 使用前置于室溫回溫至少20min，并經短暫離心使得粉末/固體落在管底後再溶解。
2） 稱取适量粉末溶于無水(shuǐ)DMSO配制儲存液（比如20 mg/ml，取500μl DMSO 加入10mg MG-132，渦旋混勻，直至完全溶解）。按照(zhào)單次用量分裝後-20ºC保存，避免反複凍存，至少1個(gè)月(yuè)穩定，
也可置于-80℃延長(cháng)保存周期。
3） 根據具體實驗應用，選擇合适的溶劑稀釋到(dào)所需濃度。體外細胞實驗，常用的工(gōng)作濃度是5-50
µM，處理時間1-24h。本品的具體工(gōng)作濃度和處理時間請參考相(xiàng)關文獻，并根據自(zì)身實驗條件(jiàn)（如實驗目的，細胞種類，培養特性等）進行摸索和優化。
文獻使用數據【僅作參考】
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文獻1，MacLaren AP et al. p53-dependent apoptosis induced by
proteasome inhibition in mammary epithelial cells. Cell Death Differ. 2001
Mar;8(3):210-8. PMID: 11319603
體外研究：
細胞類型（Cell type）：HeLa cells exposed to 10 or 100 J/m2 UV (254 nm) using a UV
crosslinker.
藥物(wù)配制（Preparation）：MG132
dissolved in DMSO and diluted in DMEM.
實驗方法（Assay）：HeLa cells were grown to about 60% confluence in DMEM at 37°C
in the presence of 5% CO2. MG132 dissolved in DMSO was added (5 µM final
concentration). For mock treatment, DMSO alone was added. Cells were
incubated for 1 h before UV irradiation. For UV treatment, medium in the
Petri dishes was removed, and cells were exposed to 10 or 100 J/m2 UV (254
nm) using a UV crosslinker. Medium containing MG132 or DMSO alone was added
back to the respective Petri dishes, and cells were transferred back to the
incubator for the time course experiment.
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文獻2，Inoue S et al.The effect of proteasome inhibitor MG132 on experimental
inflammatory bowel disease. Clin Exp Immunol. 2009 Apr;156(1):172-82. PMID: 19220323
體内研究：
動物(wù)模型（Animal Model）：Experimental murine colitis models: IL-10-deficient (IL-10−/−)
mice and dextran sulphate sodium (DSS)-induced colitis
藥物(wù)配制（Preparation）：MG132 was dissolved in dimethyl sulphoxide (DMSO) and then
diluted in 500 µl sterile phosphate-buffered saline (PBS) for injection.
注射劑量（Dosages）：Female IL-10−/− mice at 4 weeks of age were divided into four
groups and treated with intraperitoneal injection three times a week as
follows: group A, 0·01% DMSO as the control; group B, 0·6 µmol/kg MG132;
group C, 3·0 µmol/kg MG132; and group D, 15·0 µmol/kg MG132. All mice were
killed after 4 weeks of treatment by cervical dislocation under ether
anaesthesia.
Female C57BL/6 mice were given 3% DSS (molecular weight 36–50
kDa) in their drinking water for 5 days, and then switched to regular
drinking water. Mice were injected intraperitoneally with 15·0 µmol/kg MG132
(prepared in the same way as for IL-10−/− mice) or 0·01% DMSO as the control
three times a week from day 0 to the end of the experiment. On day 10, the
mice were killed.
給藥途徑（Administration）：Intraperitoneal (i.p.) injection
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注意事(shì)項
1）本品僅用作科研用途，不得用作臨床診斷或治療，不得用于食品或藥品，絕對禁止用在人身上(shàng)。
2）為(wèi)了您的安全和健康，請穿實驗服并戴一(yī)次性手套操作。
參考文獻
[1] Tsubuki
S, et al. Differential inhibition of calpain and proteasome activities by
peptidyl aldehydes of di-leucine and tri-leucine. J Biochem,119(3), 572-576 (1996).
[2] Fiedler MA, et al. Inhibition of TNF-alpha-induced
NF-kappaB activation and IL-8 release in A549 cells with the proteasome
inhibitor MG-132. Am J Respir Cell Mol Biol, 19(2), 259-268 (1998).
[3] A. Arlt, J. Vorndamm, M. Breitenbroich, et al. Inhibition
of NF- k B sensitizes human pancreatic carcinoma cells to apoptosis induced by
etoposide (VP16) or doxorubicin. Oncogene 20, 859-868 (2001).
[4] Diallo JS, et al. Enhanced killing of
androgen-independent prostate cancer cells using inositol hexakisphosphate in
combination with proteasome inhibitors. Br J Cancer, 99(10), 1613-1622 (2008).
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— — Written/Edited by V.
Shallan【版權歸MKBio懋康所有】
上海夢澤生物科技有限公司是一(yī)家涉足于生(shēng)命科學和生(shēng)物(wù)技(jì)術(shù)領域研究的試劑、儀器(qì)和實驗室消耗品與實驗服務工(gōng)作，主要從(cóng)事(shì)細胞生(shēng)物(wù)學、植物(wù)學、分子生(shēng)物(wù)學、免疫學、生(shēng)物(wù)化學、蛋白(bái)組學。生(shēng)物(wù)制藥與診斷試劑研發生(shēng)産等領域。 本公司秉承“以人為(wèi)本，以誠為(wèi)信、合同守信”的經營理念。堅持"品質保障"的原則為(wèi)廣大客戶提供優質産品。
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