Proteasome and calpain are the main nonlysosomal proteases responsible for intracellular proteolysis. MG-132 is a potent cell-permeable inhibitor of both proteasome and calpain with respective IC50 values of 0.1µM and 1.25µM. MG-132 induced neurite outgrowth in PC12 cells at a concentration of 20nM. In rabbit erythrocytes, MG-132 penetrated cell membrane and inhibited the autolysis at the dose of 100µM[3]. MG-132 also showed inhibitory activity on cell growth in both human ocular melanoma IPC227F cells and murine melanoma B16 cells with IC50 values of 42 and 77nM, respectively[4]. In airway epithelial cells, pretreatment with 10μM MG-132 for 1h inhibited TNF-α-stimulated IL-8 protein production and release. Moreover, preincubation of cells with 10μM MG-132 reversed the effects of TNF-α on the transcriptional activity of IL-8 gene, IκB degradation, and NF-κB activation[5]. In mice with hindlimb immobilization, twice-daily subcutaneous injections of MG-132 (7.5 mg/kg/dose) significantly increased the running time on treadmill as compared to DMSO-treated group. However, no significant difference in the running time of MG132- and DMSO-treated mice was observed after 11 days of remobilization[6].
作用机制
MG-132 inhibits proteasome primarily via acting on the chymotrypsin-like site in the subunit. It also inhibits the caspase-like site at high concentrations[7].
MG-132 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MNs
1 µM
48 hours
To explore the role of GSDME in motor neuron injury
Neuron. 2023 Apr 19;111(8):1222-1240.e9.
PDCCs
4 µM
6 days
MG-132 was used as a positive control for cell survival.
Adv Sci (Weinh). 2022 Aug;9(22):e2201539.
A172
10 µM
6 hours
To suppress proteasome-mediated protein degradation
Redox Biol. 2022 Oct;56:102451.
HepG2
20 µM
6 hours
To examine the ubiquitination of exogenous p53 protein.
Sci Adv. 2021 Aug 25;7(35):eabf4304.
293T cells
20 µM
7 hours
To detect ubiquitination of proteins
Nat Commun. 2021 Feb 2;12(1):734.
GIST cells
20 µM
8 hours
To analyze the protein levels of USP5 and TRIM21.
Adv Sci (Weinh). 2024 Sep;11(34):e2401171.
Primary schwannoma cells
10 µM
3 hours
Monitor proteasoma-dependent degradation.
Brain. 2023 Apr 19;146(4):1697-1713.
HEK293 cells
20, 40, 80 µM
4 hours
Induction of proteasome stress
Cell Metab. 2021 Jun 1;33(6):1137-1154.e9.
MEFs
10 µM
1 hour
MG132 was used to inhibit the proteasome activity, leading to analysis of STING pathway activation.
Nat Commun. 2022 Nov 15;13(1):6977.
HEK293-EBNA
10 µM
24 hours
The treatment was used to assess the effects on ubiquitination assays.
Nat Commun. 2022 Sep 2;13(1):5173.
HCT116, HT29
1 µM
24 hours
To evaluate the effect of TKD on KRAS degradation in cancer cells.
Cell Discov. 2024 Jun 28;10(1):70.
IPSC derived cardiomyocytes
10 µM
3 hours
Assess the effects of MG132 on hypoxia treatment in cardiomyocytes.
Redox Biol. 2022 Jun;52:102295.
293T cells
10 µM
48 hours
MG132 is used to inhibit proteasome degradation and help determine the degradation pathway of mHTT.
Adv Sci (Weinh). 2023 Nov;10(31):e2301120.
HCT116, RKO
20 µM
6 hours
To analyze the ubiquitination of proteins involved in NF-κB signaling.
Cell Death Differ. 2024 Feb;31(2):203-216.
MDA-MB-231
10 µM
6 hours
MG132 was used to assess its effect on Vimentin expression and ubiquitination.
Mol Cancer. 2021 Feb 2;20(1):25.
HEK293T cells
10 µM
6 hours
Knockdown of USP14 significantly reduced the TAZ protein level, which was restored in the cells treated with the proteasome inhibitor MG132.
Cell Death Differ. 2023 Jan;30(1):1-15.
HeLa cells
10 µM
6hours
Explore the impact of MG132 on MARVELD1 and PARP1 interactions
Cell Death Differ. 2023 Apr;30(4):922-937.
TuBo mammospheres
10 µM
8 hours
To analyze the effect of MG132 on protein extraction from mammospheres.
Nat Commun. 2023 May 11;14(1):2350.
CS cells
10 µM
8 hours
To analyze the expression of proteins; results showed significant differences based on statistical analysis.
Cell Death Differ. 2021 Jul;28(7):2221-2237.
293T cells and NP cells
10 µM
8 hours
The goal was to analyze GPX4 ubiquitination. This experimentation is implied but not explicitly detailed in the effects.
Adv Sci (Weinh). 2023 May;10(13):e2207216.
Jurkat cells
50 µM
8 hours
To assess the degradation efficiency of PROTAC toolbox on targeted proteins.
Adv Sci (Weinh). 2024 Jul;11(25):e2308186.
HeLa cells
10 µM
16 hours
To evaluate the effect of Delanzomib on the plasma membrane expression of pathogenic pendrin variants. Results showed that Delanzomib significantly increased the plasma membrane expression levels of pathogenic pendrin variants.
Int J Mol Med. 2025 May;55(5):69.
293 Phoenix cells
1-10 µM
16 hours
To evaluate the rescue effect of Delanzomib on the protein expression and ion transport function of pathogenic pendrin variants. Results showed that Delanzomib significantly increased the total protein levels and ion transport function of pathogenic pendrin variants.
Int J Mol Med. 2025 May;55(5):69.
HEK293T cells
10 µM
6 hours
Proteasome inhibition MG132 stabilized PD-L1 during gallic acid treatment
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