1. Metabolic Enzyme/Protease Autophagy Apoptosis
  2. Proteasome Autophagy Apoptosis
  3. MG-132

MG-132  (Synonyms: Z-Leu-Leu-Leu-al; MG132)

目录号: HY-13259 纯度: 99.97%
COA 产品使用指南

MG-132 (Z-Leu-Leu-Leu-al) 是一种有效的,可逆的蛋白酶体 (proteasome) 抑制剂,IC50 为 100 nM。MG-132 有效阻断 26S 蛋白酶体复合物的蛋白水解活性。MG-132 是一种肽醛,是自噬 (autophagy) 激活剂。MG-132 还诱导凋亡 (apoptosis)。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

MG-132 Chemical Structure

MG-132 Chemical Structure

CAS No. : 133407-82-6

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 858 篇科研文献

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    MG-132 purchased from MCE. Usage Cited in: Pharmacol Res. 2023 Feb 20;189:106704.  [Abstract]

    MG132 (10 µM) significantly reduces the degradation of YTHDC1 protein mediated by Dihydroartemisinin (DHA) in HSCs.

    MG-132 purchased from MCE. Usage Cited in: J Ethnopharmacol. 2023 Feb 13;307:116243.  [Abstract]

    Both MG-132 (10 μM) and Baf A1 (10 μM) markedly increase TGF-β1 protein expression in HG-stimulated SV40-MES-13 cells (Fig. C and D).

    MG-132 purchased from MCE. Usage Cited in: J Virol. 2023 Mar 6;e0198422.  [Abstract]

    MG-132 (200 nM; 24 h) significantly inhibits Newcastle disease virus (NDV) infection-caused degradation of β-catenin in DF-1 cells.

    MG-132 purchased from MCE. Usage Cited in: Cell Rep. 2020 Aug 4;32(5):107990.  [Abstract]

    PMs are treated with MG132 (10 μM). Endogenous YAP protein accumulated in the presence of MG132 starts from 2 h and further increases at 4 and 6 h after treatment in WT macrophages.

    MG-132 purchased from MCE. Usage Cited in: Brain Behav Immun. 2019 Jul;79:244-255.  [Abstract]

    Effect of autolysosome inhibitor (chloroquine, CQ, 50 μM) or proteasome inhibitor (MG132, 5 μM) on KA-induced NLRP3 degradation. Cells are treated with the inhibitors for 0.5 h before KA (10 μM, 2 h) treatment.

    MG-132 purchased from MCE. Usage Cited in: EMBO J. 2019 Mar 15;38(6):e100376.  [Abstract]

    Brcc3+/+ and Brcc3-/- (Abro1+/+ and Abro1-/-)BMDMs are treated with or without LPS for 1 h. Before LPS treatment, Brcc3-/- (Abro1-/-) BMDMs are pretreated with MG132 (10 μM) for 6 h to rescue the expression of ABRO1. Immunoblot analysis of NLRP3 and ABRO1 proteins in cell lysates immunoprecipitated with anti-ABRO1 antibody.

    MG-132 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 26;38(1):101.  [Abstract]

    HLF and Hep3B cells are treated with Mg132 (10 μg/ml) for 4 h, total protein is extracted and subjected to western blotting using anti-Flag, anti-p21, or anti-GAPDH antibodies.

    MG-132 purchased from MCE. Usage Cited in: J Exp Bot. 2019 Sep 24;70(18):4749-4762.  [Abstract]

    Cell-free degradation assay of recombinant His-PhCHS protein. Recombinant His- PhCHS is purified from Escherichia coli incubated with petal crude proteins at stages and treated with specific 26S proteasome inhibitor MG132 at various time intervals. Western blot analysis was conducted using an anti-His antibody and anti-β-actin protein concentration was used as a loading control.

    MG-132 purchased from MCE. Usage Cited in: Antioxid Redox Signal. 2019 May 20;30(15):1831-1848.  [Abstract]

    Tan-IIA increases the endogenous induction of Nrf2 induction and this effect is further enhanced by cotreatment with the proteasome inhibitor MG-132.

    MG-132 purchased from MCE. Usage Cited in: Molecules. 2019 Jan 22;24(3):393.  [Abstract]

    The HepG2 cells are pretreated for 5 h MG 132 which is a proteasome inhibitor. Then, the MARCH1 protein expressions in HepG2 cells treated with 0 μM, 5,0 μM SAF, and 2.5 μM MG 132 are measured by immunoblotting.

    MG-132 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 15;37(1):193.  [Abstract]

    Western blot is performed in HCC-LM3 cells transfected with HJURP knockdown lentivirus and treated with DMSO or MG132.

    MG-132 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 3;37(1):240.  [Abstract]

    Decrease of ERCC6 expression can be rescued with proteasome inhibitor MG132. Subconfluent SKOV3 cells are treated with FL118 and MG132 alone or in combination as shown for 8 h, followed by western blot analyses with ERCC6 antibody.

    MG-132 purchased from MCE. Usage Cited in: Cancer Res. 2019 Feb 1;79(3):534-545.  [Abstract]

    Cells are transfected with GYS2 siRNA and pre-incubated with MG-132 (20 μM) for 12 h. Cell lysate are immunoprecipitated by anti-Ub and immunoblotted by anti-p53.

    MG-132 purchased from MCE. Usage Cited in: EBioMedicine. 2018 Aug;34:243-255.  [Abstract]

    MPC1 protein expression in primary mouse hepatocytes incubated with pyruvate for 8 h in the presence of MG-132.

    MG-132 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.  [Abstract]

    Different concentrations of two classical proteasome inhibitors PS-341 and MG132 are added. AGS cells are either untreated or treated with PS-341 (25 nM) or MG132 (0.1 μM) for 24 h in the absence or presence of baf A1 (100 nM).

    MG-132 purchased from MCE. Usage Cited in: Cell Prolif. 2018 Aug;51(4):e12451.  [Abstract]

    Immunoblot analysis of CDK4 in cells treated with 4 μM of CGN for 24 hours in the presence and absence of MG132.

    MG-132 purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Feb 1;146:251-259.  [Abstract]

    In the absence of MG132, the protein degradation pathways are intact, the Tau protein level is significantly decreased in peptide 1-treated group.

    MG-132 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523.  [Abstract]

    The accumulated poly-ubiquitinated protein is detected by Western blotting after J-Lat 10.6 cells are treated with DMSO, PR-957 (100 nM), PR-957 (150 nM) or MG132 (500 nM) for 48 h.

    MG-132 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Apr 19;9:377.  [Abstract]

    Immunoblot levels of highly molecular weight (HMW)-ubiquitinated proteins and pSer129-α-syn after inhibiting the ubiquitin-proteasome system (UPS) by various concentrations of MG132 (0.25, 0.5, and 1 μM) in SH-SY5Y cells.

    MG-132 purchased from MCE. Usage Cited in: Mol Plant Pathol. 2018 Dec;19(12):2623-2634.  [Abstract]

    Destabilization of BRC1 mediated by SWP1 is inhibited by proteasome inhibitors Epoxomicin and MG132.

    MG-132 purchased from MCE. Usage Cited in: Cell Cycle. 2018;17(13):1591-1601.  [Abstract]

    The protein level of CCNB1 in different groups is analyzed by Western blot; MG132 significantly increases the protein level of CCNB1 in oocytes from CRS group mice. Western blotting showing the reduced expression of securin is rescued by MG132 in CRS group mouse oocytes.

    MG-132 purchased from MCE. Usage Cited in: Mol Immunol. 2018 Nov 13;104:69-78.  [Abstract]

    Western analysis of proteins expression with treatment of IKK-16 or MG-132.

    MG-132 purchased from MCE. Usage Cited in: Oncol Lett. 2018 Nov;16(5):5900-5906.  [Abstract]

    Treatment with the 26S proteasome inhibitor, MG 132 (10 µM), rescues the downregulation of NEK 8 in the pVHL overexpressing SGC 7901 cells.

    MG-132 purchased from MCE. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Oct;1864(10):3322-3338.  [Abstract]

    The neonatal rat cardiomyocytes (NRCMs) are treated with MG132 (10 μM). The protein expression level of PPARα in the indicated group.

    MG-132 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Dec 1;410:112-123.  [Abstract]

    Immunoprecipitation of ubiquitin from lysates of U-2 OS cells expressing CHOP after treatment with different concentrations of MG7 for 48 h. Cells are incubated with MG132 (20 mM) for 4 h before harvest. Cell lysates are immunoblotted with the indicated antibodies.

    MG-132 purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 7;7(1):2929.  [Abstract]

    p53 and Cell apoptosis. MCF7 and MDA-MB-231 cells are treated with 80 μM ω-3 FFAs, 20 μM ATRA alone or in combination for 48 h. The expression of PARP and p53 protein. β-Actin is used as an internal control.

    MG-132 purchased from MCE. Usage Cited in: J Inorg Biochem. 2017 Oct;175:92-100.  [Abstract]

    TPEN-triggered PML-RARα degradation in NB4 cells is reversed by MG-132 treatment. NB4 cells are treated with 5 μM TPEN with or without the presence of 1 μM MG-132 for the indicated durations (0–12 h) and then lysed. The lysates are analyzed for PML-RARα and RARα protein levels by western blotting.

    MG-132 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2017 Sep 2;490(4):1168-1175.  [Abstract]

    Treatment of CHO-K1 cells with proteasome inhibitor, MG-132 results in elevated SR-B1 protein levels. The cells with MG-132, a potent proteasome inhibitor that inhibit ubiquitin/proteasome-dependent protein degradation, and MG-132 treatment significantly enhances cellular SR-B1 protein level.

    MG-132 purchased from MCE. Usage Cited in: Université de Montréal. Octobre 2017.

    Unsynchronized control and ARF6 cells are treated with DMSO or MG132 (10 μM) for 1h or 4h, lysed and total ubiquitinated proteins are determined using western blot (n=3).
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis[1][2][3].

    IC50 & Target

    IC50: 100 nM (Proteasome), 1.2 μM (Calpain)[1][3]

    体外研究
    (In Vitro)

    MG-132 (Z-Leu-Leu-Leu-al) 在低浓度 (30 nM) 下启动 PC12 细胞的神经突生长,是一种非常强的 20S 蛋白酶体抑制剂[3]
    MG-132 (10 μM;1 小时) 可逆转 A549 细胞中 TNF-α 对 IκB 降解和 NF-κ B 活化的影响[4]
    MG- 132 (0.75-5 μM;24 小时) 通过 26S 蛋白酶体抑制作用在 KIM-2 细胞中有效诱导 p53 依赖性细胞凋亡[5]
    MG-132 (10-40 μM;24小时) 以时间依赖性和浓度依赖性方式显著降低 C6 神经胶质瘤细胞的活力,并显示 IC50 在 24 小时时为 18.5 μM[6]
    MG-132 (18.5 μM;24 小时) 诱导抗凋亡蛋白 Bcl-2XIAP 的下调,并上调促凋亡蛋白 Baxcaspase-3 的表达[6]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[3]

    Cell Line: C6 glioma cells
    Concentration: 10, 20, 30, 40 μM
    Incubation Time: 24 hours
    Result: Significantly reduced the viability of C6 glioma cells beginning at 6 h in both time- and concentration-dependent manners and showed the IC50 of 18.5 μM at 24 hours.

    Western Blot Analysis[3]

    Cell Line: A549 cells
    Concentration: 10 μM
    Incubation Time: 1 hour
    Result: Reversed the effects of TNF-α on IκB degradation and resulted in a reversal of TNF-α-induced NF-κB activation.
    体内研究
    (In Vivo)

    MG-132 (10 mg/kg;腹腔注射;从注射 EC9706 细胞后 5 天开始每天施用 25 天) 显著抑制 EC9706 异种移植物的肿瘤生长,而不会对小鼠造成毒性[7]
    MG-132 (1 mg/kg;静脉注射;每周两次,持续 4 周) 对携带 HeLa 肿瘤的小鼠显示出有效的肿瘤抑制作用[8]
    MG-132 (1-10 μg/kg/day;皮下植入渗透泵;持续 8 天) 显著增加小鼠骨骼肌裂解液中 β-肌营养不良聚糖、α-肌营养不良聚糖、α-肌肌聚糖和抗肌萎缩蛋白的表达水平 (6 月龄雄性 C57BL/10ScSn DMD mdx 小鼠)[9]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: 5- to 6-weeks old female athymic nude mice (EC9706 xenograft)
    Dosage: 10 mg/kg
    Administration: I.p.; daily for 25 days starting 5 days after EC9706 cells injection
    Result: Significantly inhibited tumor growth of the EC9706 xenograft without causing toxicity to the mice.
    Animal Model: Five-week-old female C.B-17/lcr-scid/scidJcl mice (bearing HeLa cells)[8]
    Dosage: 1 mg/kg
    Administration: Intravenous injection; twice a week for 4 weeks
    Result: The growth inhibition rates in HeLa tumors was 49% compared to the control.
    分子量

    475.62

    Formula

    C26H41N3O5

    CAS 号
    性状

    固体

    颜色

    White to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (210.25 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1025 mL 10.5126 mL 21.0252 mL
    5 mM 0.4205 mL 2.1025 mL 4.2050 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (3.51 mM); 澄清溶液

      此方案可获得 ≥ 1.67 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1.67 mg/mL (3.51 mM); 悬浊液; 超声助溶

      此方案可获得 1.67 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.97%

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1025 mL 10.5126 mL 21.0252 mL 52.5630 mL
    5 mM 0.4205 mL 2.1025 mL 4.2050 mL 10.5126 mL
    10 mM 0.2103 mL 1.0513 mL 2.1025 mL 5.2563 mL
    15 mM 0.1402 mL 0.7008 mL 1.4017 mL 3.5042 mL
    20 mM 0.1051 mL 0.5256 mL 1.0513 mL 2.6281 mL
    25 mM 0.0841 mL 0.4205 mL 0.8410 mL 2.1025 mL
    30 mM 0.0701 mL 0.3504 mL 0.7008 mL 1.7521 mL
    40 mM 0.0526 mL 0.2628 mL 0.5256 mL 1.3141 mL
    50 mM 0.0421 mL 0.2103 mL 0.4205 mL 1.0513 mL
    60 mM 0.0350 mL 0.1752 mL 0.3504 mL 0.8760 mL
    80 mM 0.0263 mL 0.1314 mL 0.2628 mL 0.6570 mL
    100 mM 0.0210 mL 0.1051 mL 0.2103 mL 0.5256 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    MG-132
    目录号:
    HY-13259
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