產(chǎn)品信息

產(chǎn)品簡介：

MG-132是一種蛋白酶體抑制劑，IC50為100 nM，也抑制鈣蛋白酶，IC50為1.2 μM。MG132通過誘導(dǎo)細(xì)胞周期停滯以及引發(fā)細(xì)胞凋亡來抑制HeLa細(xì)胞的生長。MG-132 (10 μM) 通過抑制蛋白酶體介導(dǎo)的IκBα降解，有效抑制A549細(xì)胞中TNF-α誘導(dǎo)的NF-κB活化。體內(nèi)研究中，MG-132（ip，0.1 mg/kg/day）通過調(diào)節(jié)ERK1/2和JNK1信號通路，減輕壓力超負(fù)荷引起的心臟肥大。MG-132治療通過下調(diào)肌肉特異性泛素連接酶atrogin-1/MAFbx 和MuRF-1 mRNA，顯著減少小鼠體內(nèi)固定化誘導(dǎo)的骨骼肌萎縮。

本品以凍干粉形式提供，純度≥98%，可溶于DMSO或無水乙醇配制成儲(chǔ)存液，之后用培養(yǎng)基或生理緩沖液稀釋到需要的工作濃度即可。

產(chǎn)品性質(zhì)

英文別名（English Synonym）： MG132; MG 132; Z-Leu-Leu-Leu-CHO; Z-Leu-Leu-Leu-al; Z-LLL-CHO;Carbobenzoxy-L-leucyl- L-leucyl-L-leucinal

化學(xué)名（Chemical Name）：N-[(phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide

靶點(diǎn)（Target）：ChTL(20S Proteasomes)/ 0.22 μM, PGPH(20S Proteasomes)/2.95 μM，TL(20S Proteasomes)/34.4 μM

CAS 號（CAS NO.）：133407-82-6

分子式（Molecular Formula）：C26H41N3O5

分子量（Molecular Weight）：475.6

外觀（Appearance）：白色至類白色固體

純度（Purity）：＞98%

溶解性（Solubility）：溶于DMSO（30 mg/ml），無水乙醇（20mg/ml）

運(yùn)輸與保存方法

冰袋運(yùn)輸。粉末直接保存于-20 oC，有效期2年。溶于DMSO、乙醇。建議分裝后-20oC避光保存，避免反復(fù)凍存，至少可存放6個(gè)月。

相關(guān)產(chǎn)品：

使用濃度

【具體使用濃度請參考相關(guān)文獻(xiàn)，并根據(jù)自身實(shí)驗(yàn)條件（如實(shí)驗(yàn)?zāi)康?，?xì)胞種類，培養(yǎng)特性等）進(jìn)行摸索和優(yōu)化。】

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） 稱取適量粉末溶于無水DMSO配制儲(chǔ)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(fù)凍存，至少1個(gè)月穩(wěn)定， 也可置于-80℃延長保存周期。

3） 根據(jù)具體實(shí)驗(yàn)應(yīng)用，選擇合適的溶劑稀釋到所需濃度。體外細(xì)胞實(shí)驗(yàn)，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(xiàn)，并根據(jù)自身實(shí)驗(yàn)條件（如實(shí)驗(yàn)?zāi)康?，?xì)胞種類，培養(yǎng)特性等）進(jìn)行摸索和優(yōu)化。

相關(guān)實(shí)驗(yàn)（數(shù)據(jù)來自于公開發(fā)表的文獻(xiàn)，僅供參考）

使用方法【源自文獻(xiàn)，僅作參考】

文獻(xiàn)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(xì)胞類型（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(yàn)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(xiàn)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(nèi)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

參考文獻(xiàn)

1. Tsubuki S, et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem. 1996 Mar;119(3):572-6.

2. Braun HA, et al. Tripeptide mimetics inhibit the 20 S proteasome by covalent bonding to the active threonines. J Biol Chem. 2005 Aug 5;280(31):28394-401.

3. Han YH, et al. The effect of MG132, a proteasome inhibitor on HeLa cells in relation to cell growth, reactive oxygen species and GSH. Oncol Rep. 2009 Jul;22(1):215-21.

4. Chen B, et al. MG132, a proteasome inhibitor, attenuates pressure-overload-induced cardiac hypertrophy in rats by modulation of mitogen-activated protein kinase signals. Acta Biochim Biophys Sin (Shanghai). 2010 Apr;42(4):253-8.

5. Caron AZ, et al. The proteasome inhibitor MG132 reduces immobilization-induced skeletal muscle atrophy in mice. BMC Musculoskelet Disord. 2011 Aug 15;12:185.