產(chǎn)品簡(jiǎn)介:
MG-132 蛋白酶體抑制劑
產(chǎn)品標簽
MG-132（Z-Leu-Leu-Leu-CHO）；Proteasome Inhibitor蛋白酶體抑制劑；Calpain Inhibitor鈣蛋白酶抑制劑；；NF-κB activation；CAS：133407-82-6；
產(chǎn)品信息
|
產(chǎn)品名稱(chēng)
|
產(chǎn)品編號
|
CAS NO.
|
規格
|
價(jià)格（元）
|
|
MG-132蛋白酶體抑制劑
|
MZ1701-0001MG
|
133407-82-6
|
1mg
|
215
|
產(chǎn)品描述
MG-132（MG132，MG 132），也稱(chēng)為Z-Leu-Leu-Leu-al，Z-Leu-Leu-Leu-CHO，是一種強效的，可逆且具細胞滲透性的蛋白酶體Proteasome抑制劑（IC50=100 nM），還是細胞周期和細胞周期蛋白降解所需的鈣蛋白酶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蛋白分泌，通過(guò)抑制蛋白酶體介導的IκBα降解來(lái)發(fā)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或阿霉素Doxorubicin的凋亡誘導更加敏感[3]。在PC3和DU145雄激素非依賴(lài)的前列腺癌（AIPCa）細胞系中MG-132能顯著(zhù)改善六磷酸肌醇（IP6）對細胞代謝的減低能力[4]。
本品以?xún)龈煞坌问教峁?，純度?8%，可溶于DMSO或無(wú)水乙醇配制成儲存液，之后用培養基或生理緩沖液稀釋到需要的工作濃度即可。
產(chǎn)品特性
1）CAS NO：133407-82-6
2）化學(xué)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(guān)：白色至類(lèi)白色固體
8）溶解性：溶于DMSO（30 mg/ml），無(wú)水乙醇（20mg/ml）
9）化學(xué)結構圖：
保存與運輸方法
保存：-20℃干燥保存，至少2年有效。
運輸：常溫運輸。
產(chǎn)品使用
1） 使用前置于室溫回溫至少20min，并經(jīng)短暫離心使得粉末/固體落在管底后再溶解。
2） 稱(chēng)取適量粉末溶于無(wú)水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）。按照單次用量分裝后-20oC保存，避免反復凍存，至少1個(gè)月穩定，
也可置于-80℃延長(cháng)保存周期。
3） 根據具體實(shí)驗應用，選擇合適的溶劑稀釋到所需濃度。體外細胞實(shí)驗，常用的工作濃度是5-50
μM，處理時(shí)間1-24h。本品的具體工作濃度和處理時(shí)間請參考相關(guān)文獻，并根據自身實(shí)驗條件（如實(shí)驗目的，細胞種類(lèi)，培養特性等）進(jìn)行摸索和優(yōu)化。
文獻使用數據【僅作參考】
|
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(lèi)型（Cell type）：HeLa cells exposed to 10 or 100 J/m2 UV (254 nm) using a UV
crosslinker.
藥物配制（Preparation）：MG132
dissolved in DMSO and diluted in DMEM.
實(shí)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.
|
|
文獻2，Inoue S et al.The effect of proteasome inhibitor MG132 on experimental
in?ammatory bowel disease. Clin Exp Immunol. 2009 Apr;156(1):172-82. PMID: 19220323
體內研究：
動(dòng)物模型（Animal Model）：Experimental murine colitis models: IL-10-deficient (IL-10?/?)
mice and dextran sulphate sodium (DSS)-induced colitis
藥物配制（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
|
注意事項
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。
2）為了您的安全和健康，請穿實(shí)驗服并戴一次性手套操作。
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).
相關(guān)產(chǎn)品
|
貨號
|
名稱(chēng)
|
規格
|
|
MZ0201-10MG
|
Rapamycin
(Sirolimus) 雷帕霉素（西羅莫司）
|
10mg
|
|
MZ0342-5MG
|
Dorsomorphin
Dihydrochloride
|
5mg
|
|
MX3270-1MG
|
Pan-caspase
Inhibitor Z-VAD(OMe)-FMK (Powder)
|
1mg
|
|
MZ3403-1G
|
Metformin
HCl 鹽酸二甲雙胍
|
1g
|
|
MZ1701-1MG
|
MG-132 蛋白酶體抑制劑
|
1mg
|
|
MZ1704-10MG
|
Bortezomib
(PS-341) 硼替佐米
|
10mg
|
— — Written/Edited by V.
Shallan【版權歸MKBio懋康所有】
上海懋康生物科技有限公司是一家涉足于生命科學(xué)和生物技術(shù)領(lǐng)域研究的試劑、儀器和實(shí)驗室消耗品與實(shí)驗服務(wù)工作，主要從事細胞生物學(xué)、植物學(xué)、分子生物學(xué)、免疫學(xué)、生物化學(xué)、蛋白組學(xué)。生物制藥與診斷試劑研發(fā)生產(chǎn)等領(lǐng)域。 本公司秉承“以人為本，以誠為信、合同守信”的經(jīng)營(yíng)理念。堅持"品質(zhì)保障"的原則為廣大客戶(hù)提供優(yōu)質(zhì)產(chǎn)品。
|
