产品简介:
MG-132 蛋白酶体抑制剂
产品标签
MG-132（Z-Leu-Leu-Leu-CHO）；Proteasome Inhibitor蛋白酶体抑制剂；Calpain Inhibitor钙蛋白酶抑制剂；；NF-κB activation；CAS：133407-82-6；
产品信息
|
产品名称
|
产品编号
|
CAS NO.
|
规格
|
价格（元）
|
|
MG-132蛋白酶体抑制剂
|
MZ1701-0001MG
|
133407-82-6
|
1mg
|
215
|
产品描述
MG-132（MG132，MG 132），也称为Z-Leu-Leu-Leu-al，Z-Leu-Leu-Leu-CHO，是一种强效的，可逆且具细胞渗透性的蛋白酶体Proteasome抑制剂（IC50=100 nM），还是细胞周期和细胞周期蛋白降解所需的钙蛋白酶Calpain抑制剂（IC50=1.2 μM）[1]。A549细胞中MG-132（10μM）有效抑制TNFα诱导的NF-κB活化、IL-8基因转录和IL-8蛋白分泌，通过抑制蛋白酶体介导的IκBα降解来发挥作用[2]。MG-132（10μM）对NF-κB的抑制效应促使人胰腺癌细胞对依托泊甙Etoposide或阿霉素Doxorubicin的凋亡诱导更加敏感[3]。在PC3和DU145雄激素非依赖的前列腺癌（AIPCa）细胞系中MG-132能显著改善六磷酸肌醇（IP6）对细胞代谢的减低能力[4]。
本品以冻干粉形式提供，纯度≥98%，可溶于DMSO或无水乙醇配制成储存液，之后用培养基或生理缓冲液稀释到需要的工作浓度即可。
产品特性
1）CAS NO：133407-82-6
2）化学名：N-[(phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide
3）同义名：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）纯度：≥98%
7） 外观：白色至类白色固体
8）溶解性：溶于DMSO（30 mg/ml），无水乙醇（20mg/ml）
9）化学结构图：
保存与运输方法
保存：-20℃干燥保存，至少2年有效。
运输：常温运输。
产品使用
1） 使用前置于室温回温至少20min，并经短暂离心使得粉末/固体落在管底后再溶解。
2） 称取适量粉末溶于无水DMSO配制储存液（比如20 mg/ml，取500μl DMSO 加入10mg MG-132，涡旋混匀，直至完全溶解）。按照单次用量分装后-20ºC保存，避免反复冻存，至少1个月稳定，
也可置于-80℃延长保存周期。
3） 根据具体实验应用，选择合适的溶剂稀释到所需浓度。体外细胞实验，常用的工作浓度是5-50
µM，处理时间1-24h。本品的具体工作浓度和处理时间请参考相关文献，并根据自身实验条件（如实验目的，细胞种类，培养特性等）进行摸索和优化。
文献使用数据【仅作参考】
|
文献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
体外研究：
细胞类型（Cell type）：HeLa cells exposed to 10 or 100 J/m2 UV (254 nm) using a UV
crosslinker.
药物配制（Preparation）：MG132
dissolved in DMSO and diluted in DMEM.
实验方法（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.
|
|
文献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
体内研究：
动物模型（Animal Model）：Experimental murine colitis models: IL-10-deficient (IL-10−/−)
mice and dextran sulphate sodium (DSS)-induced colitis
药物配制（Preparation）：MG132 was dissolved in dimethyl sulphoxide (DMSO) and then
diluted in 500 µl sterile phosphate-buffered saline (PBS) for injection.
注射剂量（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.
给药途径（Administration）：Intraperitoneal (i.p.) injection
|
注意事项
1）本品仅用作科研用途，不得用作临床诊断或治疗，不得用于食品或药品，绝对禁止用在人身上。
2）为了您的安全和健康，请穿实验服并戴一次性手套操作。
参考文献
[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).
相关产品
|
货号
|
名称
|
规格
|
|
MZ0201-10MG
|
Rapamycin
(Sirolimus) 雷帕霉素（西罗莫司）
|
10mg
|
|
MZ0342-5MG
|
Dorsomorphin
Dihydrochloride
|
5mg
|
|
MX3270-1MG
|
Pan-caspase
Inhibitor Z-VAD(OMe)-FMK (Powder)
|
1mg
|
|
MZ3403-1G
|
Metformin
HCl 盐酸二甲双胍
|
1g
|
|
MZ1701-1MG
|
MG-132 蛋白酶体抑制剂
|
1mg
|
|
MZ1704-10MG
|
Bortezomib
(PS-341) 硼替佐米
|
10mg
|
— — Written/Edited by V.
Shallan【版权归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学和生物技术领域研究的试剂、仪器和实验室消耗品与实验服务工作，主要从事细胞生物学、植物学、分子生物学、免疫学、生物化学、蛋白组学。生物制药与诊断试剂研发生产等领域。 本公司秉承“以人为本，以诚为信、合同守信”的经营理念。坚持"品质保障"的原则为广大客户提供优质产品。
|
