MG132

生物活性

MG-132是一种蛋白酶体抑制剂，IC50为100 nM，也抑制钙蛋白酶，IC50为1.2 μM。MG132通过诱导细胞周期停滞以及引发细胞凋亡来抑制HeLa细胞的生长。MG-132 (10 μM) 通过抑制蛋白酶体介导的IκBα降解，有效抑制A549细胞中TNF-α诱导的NF-κB活化。

体内研究中，MG-132（ip，0.1 mg/kg/day）通过调节ERK1/2和JNK1信号通路，减轻压力超负荷引起的心脏肥大。MG-132治疗通过下调肌肉特异性泛素连接酶atrogin-1/MAFbx 和MuRF-1 mRNA，显著减少小鼠体内固定化诱导的骨骼肌萎缩。

实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）

细胞实验
细胞系	Lung cancer cell lines A549 and H1299
方法	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.
浓度	200 nM
处理时间	6h

动物实验
动物模型	Male mdx (C57BL/10ScSn DMD mdx) mice
配制	Dissolved in DMSO, and diluted in PBS
剂量	~10 μg/kg/day
给药处理	Injection

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的Km系数
	动物 A的Km系数

例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。

化学数据

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass	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	4.205 mL
10 mM	0.2103 mL	1.0513 mL	2.1025 mL

使用AbMole产品发表的文献

• 

  Aging (Albany NY). 2020 Jul 17;12(14):14699-14717.

  Acetylation-mediated degradation of HSD17B4 regulates the progression of prostate cancer
  MG132购买自AbMole

• 

  Oncogene. 2020 Apr;39(15):3163-3178.

  The EGFR-ZNF263 Signaling Axis Silences SIX3 in Glioblastoma Epigenetically
  MG132购买自AbMole

• 

  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购买自AbMole

• 

  Mol Ther Nucleic Acids. 2020 Mar 6;19:1198-1208.

  lncRNA RMST Suppressed GBM Cell Mitophagy through Enhancing FUS SUMOylation.
  MG132购买自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购买自AbMole

• 

  Cell Microbiol. 2020 Mar;22(3):e13148.

  Hepatitis B virus X protein modulates upregulation of DHX9 to promote viral DNA replication.
  MG132购买自AbMole

• 

  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.
  MG132购买自AbMole

• 

  Curr Biol. 2018 Aug 20;28(16):2616-2623.e5.

  Chloroplast Biogenesis Controlled by DELLA-TOC159 Interaction in Early Plant Development.
  MG132购买自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购买自AbMole

• 

  J Hematol Oncol. 2017 Jun 8;10(1):115.

  SIX3, a tumor suppressor, inhibits astrocytoma tumorigenesis by transcriptional repression of AURKA/B
  MG132购买自AbMole

• 

  Autophagy. 2017 Mar 4;13(3):538-553.

  Acetylation targets HSD17B4 for degradation via the CMA pathway in response to estrone
  MG132购买自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购买自AbMole

客户产品验证及相关生物数据

	数据来源	New Phytol (2020 Jan). Figure 7. MG132 (Abmole Bioscience, Houston, TX, USA)
	方法	Quantitative cell-free degradation assay
	细胞系	tobacco leaf epidermis cells
	浓度	100 μM
	处理时间	0, 60, 120 and 240 min
	实验结果	Proteasomal inhibitor MG132 antagonized this degradation and confirmed proteasomal involvement in FIT protein turnover.

	数据来源	Current Biology (2018). Figure 3. MG132 (Abmole Bioscience)
	方法	In vivo CoIP
	细胞系	Total protein
	浓度	20 mM
	处理时间	12 h
	实验结果	PAC-treated WT seedlings incubated with MG132 (a proteasome inhibitor) had increased TOC159 levels, implicating degradation by the UPS.

	数据来源	Oncotarget (2018 Feb). Figure5. MG132 (Abmole Bioscience, Houston, USA)
	方法	Co-immunoprecipitation
	细胞系	MCF-7 cells
	浓度	20 μM
	处理时间	4 h
	实验结果	When MCF-7 & SKBR3 cells were treated with both cycloheximide and MG132, a proteasome inhibitor, NDRG1-OT1_v4 no longer promoted NDRG1 degradation

	数据来源	Journal of Hematology & Oncology (2017). Figure 5. MG132 (Abmole Bioscience)
	方法	Immunofluorescence analysis
	细胞系	U251, U87 and U118 cell lines
	浓度	20 μM
	处理时间	2 h
	实验结果	Astrocytoma patients with a low expression of SIX3 and mutant p53 are more sensitive to treatment with aurora kinase inhibitors.

	数据来源	Journal of Hematology & Oncology (2017). Figure 3. MG132 (Abmole Bioscience)
	方法	Western blotting
	细胞系	U251, U87 and U118 cell lines
	浓度	20 μM
	处理时间	2 h
	实验结果	When we knocked down AURKA, MG132 resulted in increased AURKB expression and had less effect on AURKA (Fig. 3e).

	数据来源	Institut für Biochemie der Universität Stuttgart (2014). Figure 21. MG132 (Abmole Bioscience)
	方法	MG-132 was dissolved in DMSO. To verify that the activity was sufficiently inhibited, peptide cleavage assays were performed.
	细胞系
	浓度	200 μM
	处理时间	2 h
	实验结果	As shown above, GST-Nup53 was immobilized on glutathione sepharose beads (Figure 21A, load, bottom lane; Coomassie blue stained gel) and incubated with equal amounts of CP or Blm10-CP. To confirm that equal amounts of proteasome were used, the loads were separated by SDS-PAGE, and the gel was subsequently stained with Coomassie blue and immunoblotted against the HA-tag of 4 (Figure 21A, load).

	数据来源	Faculté de Médecine (2015). Figure 5. MG132 (Abmole Bioscience)
	方法
	细胞系	CFBE-wt cells
	浓度	5 μM
	处理时间	18h
	实验结果	In fact, our data obtained in the presence of MG132 and/or cycloheximide (Fig. 4 and 5) indicated that CFTR synthesis may also be affected by PsaDM. Our study, as well as data from the literature, thus indicated that P. aeruginosa exoproducts may impact CFTR protein synthesis, degradation and trafficking/recycling to the cell membrane.

	数据来源	Faculté de Médecine (2015). Figure 4. MG132 (Abmole Bioscience)
	方法
	细胞系	CFBE-wt cells
	浓度	5 μM
	处理时间	18h
	实验结果	In fact, our data obtained in the presence of MG132 and/or cycloheximide (Fig. 4 and 5) indicated that CFTR synthesis may also be affected by PsaDM. Our study, as well as data from the literature, thus indicated that P. aeruginosa exoproducts may impact CFTR protein synthesis, degradation and trafficking/recycling to the cell membrane.

	数据来源	ERJ Express.(2015). Figure 5. MG132 (Abmole Bioscience, Kowloon, Honk Hong)
	方法	Immunoblotting
	细胞系	CFBE-ΔF508 and CFBE-wt cell lines
	浓度
	处理时间	18 h
	实验结果	To confirm that the huge accumulation of CFTR protein observed after proteasomal inhibition with MG132 (MG132+LB at 18 h) (fig. 5a and b) was secondary to newly synthesised CFTR proteins, we verified that a co treatment with CHX (MG132+CHX+LB) totally prevented CFTR accumulation.

	数据来源	ERJ Express.(2015). Figure 4. MG132 (Abmole Bioscience, Kowloon, Honk Hong)
	方法	Immunoblotting
	细胞系	CFBE-ΔF508 and CFBE-wt cell lines
	浓度
	处理时间	2 h, 8 h, 18 h
	实验结果	In fact, our data obtained in the presence of MG132 and/or CHX (figs 4 and 5) indicated that CFTR synthesis may also be affected by PsaDM.

	数据来源	Autophage (2016) . Figure 2. MG132 (Abmole BioScience, M1902)
	方法	Western blot
	细胞系	HEK293T, MCF7 or MDA-MB-231 cells
	浓度	10 μM
	处理时间	6 h
	实验结果	Results showed that NH4Cl, but not MG132, 3-MA or wortmannin, induced the accumulation of HSD17B4 protein (Fig. 2A ), indicating that the degradation of HSD17B4 is independent of the proteasome and macroautophagy pathways.

参考文献

MG132, a proteasome inhibitor, induces apoptosis in tumor cells.
Guo N, et al. Asia Pac J Clin Oncol. 2012 May 15. PMID: 22897979.

Proteasome inhibitor MG132 induces selective apoptosis in glioblastoma cells through inhibition of PI3K/Akt and NFkappaB pathways, mitochondrial dysfunction, and activation of p38-JNK1/2 signaling.
Zanotto-Filho A, et al. Invest New Drugs. 2012 Feb 28. PMID: 22367315.

The effect of MG132, a proteasome inhibitor on HeLa cells in relation to cell growth, reactive oxygen species and GSH.
Han YH, et al. Oncol Rep. 2009 Jul;22(1):215-21. PMID: 19513526.