MG132 is a potent cell-permeable inhibitor of proteasome and calpain with IC50 of 100 nM and 1.2 μM respectively. MG132 inhibited the growth of HeLa cells via inducing the cell cycle arrest as well as triggering apoptosis. MG132 also inhibits NF-κB activation with an IC50 of 3 µM and prevents β-secretase cleavage. MG132 induces cell apoptosis through formation of reactive oxygen species or the upregulation and downregulation of these factors, which is ultimately dependent upon the activation of the caspase family of cysteine proteases.
In vitro, it induces neurite outgrowth in PC12 cells and has anticancer properties. Besides its apoptotic effect alone, MG132 also enhanced the antiglioma effect of the chemotherapeutics cisplatin, taxol and doxorubicin in C6 and U138MG cells, indicating an adjuvant/chemosensitizer potential.
Exp Ther Med. 2022 Sep 23;24(5):687.
MG132 protects against lung injury following brain death in rats
MG132 purchased from AbMole
J Cell Mol Med. 2022 May;26(9):2646-2657.
Venetoclax enhances DNA damage induced by XPO1 inhibitors: A novel mechanism underlying the synergistic antileukaemic effect in acute myeloid leukaemia
MG132 purchased from AbMole
Bioengineered. 2022 Apr;13(4):8000-8012.
UBE2B promotes ovarian cancer growth via promoting RAD18 mediated ZMYM2 monoubiquitination and stabilization
MG132 purchased from AbMole
Virol Sin. 2022 Aug 16;S1995-820X(22)00143-2.
CK1α upregulates the IFNAR1 expression to prompt the anti-HBV effect of type I IFN in hepatoma carcinoma cells
MG132 purchased from AbMole
Ecotoxicol Environ Saf. 2022 Jun 1;237:113564.
Environmental BPDE induced human trophoblast cell apoptosis by up-regulating lnc-HZ01/p53 positive feedback loop
MG132 purchased from AbMole
Cell Death Differ. 2022 Jul;29(7):1395-1408.
SARS-CoV-2 membrane protein causes the mitochondrial apoptosis and pulmonary edema via targeting BOK
MG132 purchased from AbMole
Cell Death Dis. 2021 Oct 16;12(11):955.
Essential role of zyxin in platelet biogenesis and glycoprotein Ib-IX surface expression
MG132 purchased from AbMole
Cell Death Dis. 2021 Aug 21;12(9):803.
USP14 maintains HIF1-α stabilization via its deubiquitination activity in hepatocellular carcinoma
MG132 purchased from AbMole
Int J Mol Sci. 2021 Aug 16;22(16):8779.
Autophagy Mediates the Degradation of Plant ESCRT Component FREE1 in Response to Iron Deficiency
MG132 purchased from AbMole
J Cancer. 2021 Oct 17;12(23):7041-7051.
N6-methyladenosine regulates ATM expression and downstream signaling
MG132 purchased from AbMole
Adv Sci (Weinh). 2021 Jan 6;8(4):2003205.
Inhibition Lysosomal Degradation of Clusterin by Protein Kinase D3 Promotes Triple-Negative Breast Cancer Tumor Growth
MG132 purchased from AbMole
PLoS Pathog. 2021 Feb;17(2):e100899.
CVB3 VP1 interacts with MAT1 to inhibit cell proliferation by interfering with Cdk-activating kinase complex activity in CVB3-induced acute
MG132 purchased from AbMole
Cell Biol Toxicol. 2022 Apr;38(2):291-310.
Lnc-HZ08 regulates BPDE-induced trophoblast cell dysfunctions by promoting PI3K ubiquitin degradation and is associated with miscarriage
MG132 purchased from AbMole
Mol Ther Nucleic Acids. 2020 Mar 6;19:1198-1208.
lncRNA RMST Suppressed GBM Cell Mitophagy through Enhancing FUS SUMOylation
MG132 purchased from AbMole
Aging (Albany NY). 2020 Jul 17;12(14):14699-14717.
Acetylation-mediated degradation of HSD17B4 regulates the progression of prostate cancer
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Oncogene. 2020 Apr;39(15):3163-3178.
The EGFR-ZNF263 Signaling Axis Silences SIX3 in Glioblastoma Epigenetically
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Front Cell Infect Microbiol. 2020 Apr 16;10:158.
Difluoromethylornithine, a Decarboxylase 1 Inhibitor, Suppresses Hepatitis B Virus Replication by Reducing HBc Protein Levels
MG132 purchased from AbMole
Mol Ther Nucleic Acids. 2020 Mar 6;19:1198-1208.
lncRNA RMST Suppressed GBM Cell Mitophagy through Enhancing FUS SUMOylation.
MG132 purchased from AbMole
New Phytol. 2020 Jan;225(1):250-267.
Phospho-mutant activity assays provide evidence for alternative phospho-regulation pathways of the transcription factor FER-LIKE IRON DEFICIENCY-INDUCED TRANSCRIPTION FACTOR.
MG132 purchased from AbMole
Cell Microbiol. 2020 Mar;22(3):e13148.
Hepatitis B virus X protein modulates upregulation of DHX9 to promote viral DNA replication.
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Oncology Letters. 2019 Feb 8.
Inhibition of the PI3K/AKT signaling pathway sensitizes diffuse large B‑cell lymphoma cells to treatment with proteasome inhibitors via suppression of BAG3.
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Curr Biol. 2018 Aug 20;28(16):2616-2623.e5.
Chloroplast Biogenesis Controlled by DELLA-TOC159 Interaction in Early Plant Development.
MG132 purchased from AbMole
Oncotarget. 2018 Feb;9(12):10470-10482.
The hypoxia-responsive lncRNA NDRG-OT1 promotes NDRG1 degradation via ubiquitin-mediated proteolysis in breast cancer cells.
MG132 purchased from AbMole
J Hematol Oncol. 2017 Jun 8;10(1):115.
SIX3, a tumor suppressor, inhibits astrocytoma tumorigenesis by transcriptional repression of AURKA/B
MG132 purchased from AbMole
Autophagy. 2017 Mar 4;13(3):538-553.
Acetylation targets HSD17B4 for degradation via the CMA pathway in response to estrone
MG132 purchased from AbMole
Eur Respir J. 2015 Jun;1590-602.
Deleterious impact of Pseudomonas aeruginosa on cystic fibrosis transmembrane conductance regulator function and rescue in airway epithelial cells.
MG132 purchased from AbMole
Cell Experiment | |
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Cell lines | Lung cancer cell lines A549 and H1299 |
Preparation method | Cell viability assay. Cell viability was determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells were seeded in 96-well plates at a density of 2.5x103/well 1 day prior to treatment. Then, cells were treated with MG132 or/and irradiation. After treatment, 20 µl of 5 mg/ml MTT solution was added into each well and incubated for 4 h. After the supernatant was removed, 100 µl of DMSO was added, and then placed in a microplate reader to measure OD value. Cell viability rate (vR) was calculated according to the following formula: vR = (OD in observed group/OD in 0 Gy group) x 100%. All assays were repeated 3 times in quintuplicate. |
Concentrations | 200 nM |
Incubation time | 6h |
Animal Experiment | |
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Animal models | Male mdx (C57BL/10ScSn DMD mdx) mice |
Formulation | Dissolved in DMSO, and diluted in PBS |
Dosages | ~10 μg/kg/day |
Administration | Injection |
Molecular Weight | 475.62 |
Formula | C26H41N3O5 |
CAS Number | 133407-82-6 |
Solubility (25°C) | DMSO 80 mg/mL Ethanol 20 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Ashley J Chui, et al. Science. N-terminal degradation activates the NLRP1B inflammasome
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