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MG-132

MG-132

产品编号 T2154   CAS 133407-82-6
别名: Z-Leu-Leu-Leu-CHO, Z-LLL-al

MG-132 是一种有效的细胞渗透性 26S 蛋白酶体抑制剂,IC50为 100 nM。它是一种肽醛,是自噬激活剂,可诱导凋亡

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MG-132, CAS 133407-82-6
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其他形式的 MG-132:
产品目录号及名称: MG-132 (T2154)
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纯度: 98%
纯度: 97%
纯度: 96.67%
纯度: 95.91%
纯度: 95%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 MG-132 is a potent cell-permeable 26S proteasome inhibitor (IC50: 100 nM). It also inhibits calpain (IC50: 1.2 μM).
靶点活性 Calpain:1.2 μM (cell free), 20S proteasome:100 nM (cell free)
体外活性 The IC50 of MG-132 for the alkali-denatured casein-degrading activity of m-calpain was around 1.2 μM. The IC50 for the ZLLL MCA-degrading activity of 20S proteasome by MG-132 was 100 nM [1]. It also inhibits proteasomal chymotrypsin-like peptidase activity (IC50: 24.2 nM) [2]. Dose-dependent inhibition of cell growth was observed in HeLa cells with an IC50 of approximately 5 μM MG132 for 24 h. The treatment with MG132 induced S, G2-M or non-specific phase arrests of the cell cycle dose-dependently. Treatment with MG132 induced apoptosis in a dose-dependent manner, as evidenced by sub-G1 cells and annexin V staining cells [3].
CellLine: MDBK cells
Concentration: 1μM
IncubationTime: 48h
Result: MG-132 induced a significant decrease in cytotoxicity of BoHV-1 infected cells.
CellLine: SEB-1 cells
Concentration: 20μM
IncubationTime: 24h
Result: MG-132 treatment markedly suppressed the proliferation of SEB-1 cells.
体内活性 MG132 (0.1 mg/kg/day) was intraperitoneally injected to rats with abdominal aortic banding (AAB) for 8 weeks. Results showed that treatment with MG132 significantly attenuated left ventricular (LV) myocyte area, LV weight/body weight, and lung weight/body weight ratios, decreased LV diastolic diameter and wall thickness and increased fractional shortening in AAB rats. AAB induced the phosphorylation of ERK1/2, JNK1, and p38 in cardiac myocytes. The elevated phosphorylation levels of ERK1/2 and JNK1 in AAB rats were significantly reversed by MG132 treatment [4]. MG132 significantly inhibited IκBα degradation thus preventing NFκB activation in vitro. MG132 preserved muscle and myofiber cross-sectional area by downregulating the muscle-specific ubiquitin ligases atrogin-1/MAFbx and MuRF-1 mRNA in vivo. This effect resulted in a diminished rehabilitation period [5].
Animal Model: Male BALB/c mice (specific pathogen-free (SPF) class, 4 weeks)
Dosage: 10μg/kg
Administration: Injected intraperitoneally; daily for 7 days
Result: MG-132 improved hemodynamics and inhibited the structural remodeling of the ventricle in mice with myocarditis.
Animal Model: Adult Sprague-Dawley rats (200–250 g)
Dosage: 10 mg/kg
Administration: Intraperitoneal injection, 10h
Result: MG-132 improved the lung tissue pathological changes and edema.
激酶实验 Inhibitory activities of ZLLa1 and ZLLLal against m-calpain and 20S proteasome were measured by previously described methods.For the m-calpain inhibitory assay,the 0.5 ml reaction mixture contained 0.24% alkali-denatured casein,28 mM 2-mercaptoethanol,0.94 unit of m-calpain,ZLLal or ZLLLal,6 mM CaCl2,and 0.1M Tris-HC1 (pH 7.5).The reaction was started by the addition of m-calpain solution and stopped by the addition of 0.5 ml of 10% trichloroacetic acid after incubation at 30℃ for 15 min.After centrifugation at 1,300×g for 10 min,the absorbance of the supernatant at 280 nm was measured.The reaction mixture for the 20S proteasome inhibitory assay contained 0.1 M Tris-acetate,pH 7.0,20S proteasome,ZLLa1 or ZLLLal,and 25 μM substrate dissolved in dimethyl sulfoxide in a final volume of 1 ml.After incubation at 37℃ for 15 min,the reaction was stopped by the addition of 0.1 ml of 10% SDS and 0.9 ml of 0.1 M Tris-acetate,pH 9.0.The fluorescence of the reaction products was measured.To determine the IC50s against m-calpain and 20S proteasome,various concentrations of the synthetic peptide aldehydes were included in the assay mixture [1].
细胞实验 The effect of MG132 on HeLa cell growth was determined by trypan blue exclusion cell counting or measuring MTT dye absorbance of living cells as previously described. In brief, cells (5x10^5 cells per well) were seeded in 24-well plates for cell counting, and cells (5x10^4 cells per well) were seeded in 96-well microtiter plates for the MTT assay. After exposure to indicated amounts of MG132 for 24 h, cells in 24-well plates or 96-well plates were collected with trypsin digestion for trypan blue exclusion cell counting or were used for the MTT assay. Twenty microliters of MTT solution (2 mg/ml in PBS) was added to each well of 96-well plates. The plates were again incubated for 4 h at 37?C. MTT solution in the medium was aspirated off and 200 μl of DMSO was added to each well to solubilize the formazan crystals formed in viable cells. Optical density was measured at 570 nm using a microplate reader. Each plate contained multiple wells at a given experimental condition and multiple control wells. This procedure was replicated for 2-4 plates per condition [3].
动物实验 Male Sprague–Dawley rats (8 weeks old, 180 – 230 g) were used to establish a pressure-overload model as described previously. All animals were separated into four groups (10 rats per group): (i) vehicle-treated sham group; (ii) MG132-treated sham group; (iii) vehicle-treated abdominal aortic banding (AAB) group; and (iv) MG132-treated AAB group. Under intraperitoneal pentobarbital (50 mg/kg) anesthesia, AAB was created using a 5-0 suture tied twice around the abdominal aorta in which. a 21-gauge needle was inserted. The needle was then retracted yielding a 70 – 80% constriction with an outer aortic diameter of 0.8 mm. In the sham surgery rats, the same surgery was performed as described above except the aorta was constricted. At Day 3 after the surgery, MG132-treated rats were intraperitoneally injected with 0.1 mg/kg/day of MG132 for 8 weeks. All control animals were injected with a corresponding volume of vehicle only (0.1% DMSO) [4]. Sixteen-week-old male CD1 mice were used for all our experiments. Thirty minutes before the immobilization procedure, 0.1 mg/kg of buprenorphine was administrated IP. The mice were then anesthetized using isoflurane. The right hindlimb was immobilized as previously described. Briefly, the hindlimb was immobilized 7 days by stapling the foot exploiting normal dorso-tibial flexion using an Autosuture Royal 35W skin stapler. One tine was inserted close to the toe at the plantar portion of the foot while the other was inserted in the distal portion of the gastrocnemius. The other hindlimb was used as a control. During the immobilization period, the mice were injected subcutaneously with MG132 (7.5 mg/kg/dose) or vehicle (DMSO) twice daily. DMSO containing or not MG132 was diluted in sterile pure corn oil (1:100, injected volume 150 μL). After 7 days, the tibialis anterior (TA) muscles of immobilized and non-i
别名 Z-Leu-Leu-Leu-CHO, Z-LLL-al
化合物与蛋白结合的复合物

T2154_2

Crystal structure of MG-132 covalently bound to the main protease (3CLpro/Mpro) of SARS-CoV-2.

分子量 475.62
分子式 C26H41N3O5
CAS No. 133407-82-6

存储

 | Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

H2O: Insoluble

Ethanol: 47.5 mg/mL (100 mM)

DMSO: 90 mg/mL (189.23 mM)

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. 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. 2. Harhouri K, et al. MG132-induced progerin clearance is mediated by autophagy activation and splicing regulation. EMBO Mol Med. 2017 Sep;9(9):1294-1313. 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. Luo Q, Wu X, Zhao P, et al. OTUD1 Activates Caspase‐Independent and Caspase‐Dependent Apoptosis by Promoting AIF Nuclear Translocation and MCL1 Degradation. Advanced Science. 2021: 2002874. 5. 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. 6. Caron AZ, et al. The proteasome inhibitor MG132 reduces immobilization-induced skeletal muscle atrophy in mice. BMC Musculoskelet Disord. 2011 Aug 15;12:185. 7. 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. 8. Matsumoto Y, et al. Enhanced efficacy against cervical carcinomas through polymeric micelles physically incorporating theproteasome inhibitor MG132. Cancer Sci. 2016 Jun;107(6):773-81. 9. Guzmán-Téllez P, Martínez-Valencia D, Silva-Olivares A, et al. Naegleria fowleri and Naegleria gruberi 20S proteasome: identification and characterization[J]. European Journal of Cell Biology. 2020: 151085

文献引用

1. Ding L, Chen X, Zhang W, et al.Canagliflozin primes antitumor immunity by triggering PD-L1 degradation in endocytic recycling.The Journal of Clinical Investigation.2023, 133(1). 2. Zhang W, Pan X, Xu Y, et al.Mevalonate improves anti-PD-1/PD-L1 efficacy by stabilizing CD274 mRNA.Acta Pharmaceutica Sinica B.2023 3. Liu X, Fang Y, Lv X, et al.Deubiquitinase OTUD6A in macrophages promotes intestinal inflammation and colitis via deubiquitination of NLRP3.Cell Death & Differentiation.2023: 1-15. 4. Yin L, Ye Y, Zou L, et al.AR antagonists develop drug resistance through TOMM20 autophagic degradation-promoted transformation to neuroendocrine prostate cancer.Journal of Experimental & Clinical Cancer Research.2023, 42(1): 1-19. 5. Zhuge R, Wang C, Wang J, et al.hCINAP regulates the differentiation of embryonic stem cells by regulating NEDD4 liquid-liquid phase-separation-mediated YAP1 activation.Cell Reports.2023, 42(1): 111935. 6. Zhao X, Ma Y, Li J, et al.The AEG-1-USP10-PARP1 axis confers radioresistance in esophageal squamous cell carcinoma via facilitating homologous recombination-dependent DNA damage repair.Cancer Letters.2023: 216440. 7. Cao D, Duan L, Huang B, et al.The SARS-CoV-2 papain-like protease suppresses type I interferon responses by deubiquitinating STING.Science Signaling.2023, 16(783): eadd0082. 8. Li Y M, Mei Y C, Liu A H, et al.Gcn5-and Bre1-mediated Set2 degradation promotes chronological aging of Saccharomyces cerevisiae.Cell Reports.2023, 42(10). 9. Lin X, Lin T, Wang X, et al.Sesamol serves as a p53 stabilizer to relieve rheumatoid arthritis progression and inhibits the growth of synovial organoids.Phytomedicine.2023: 155109. 10. Zhu X, Huang N, Ji Y, et al.Brusatol induces ferroptosis in oesophageal squamous cell carcinoma by repressing GSH synthesis and increasing the labile iron pool via inhibition of the NRF2 pathway.Biomedicine & Pharmacotherapy.2023, 167: 115567.
NM-3 ZNL 02-096 JHU395 PI3K/Akt/mTOR-IN-2 CP 461 AK301 SFI003 (-)-Anonaine

相关化合物库

该产品包含在如下化合物库中:
染色质修饰分子库 泛素化化合物库 HIF-1化合物库 自噬库 已知活性化合物库 抗癌活性化合物库 细胞凋亡化合物库 共价抑制剂库 抗衰老化合物库 抗癌化合物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

MG-132 133407-82-6 Apoptosis Autophagy Proteases/Proteasome Ubiquitination Proteasome Inhibitor MG132 MG 132 complex peptide calpain Z-Leu-Leu-Leu-CHO proteolytic aldehyde inhibit Z-LLL-al 26S inhibitor

 

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