MG-132 化学構造
分子量: 475.62

品質と確認

カスタマーレビュー(4)

製品情報

  • Combination Therapy
    併用療法
  • Compare Proteasome Inhibitors
    Proteasome阻害剤を比較
  • 研究分野

製品の説明

生物活性

情報 MG-132は、100nMのIC50によるプロテアソームの強力な阻害剤です。
目標

Proteasome

IC50

100 nM [1]

In vitro試験 MG-132 displays >1000 times more activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of 20S proteasome with IC50 of 100 nM versus 110 μM. MG-132 also inhibits calpain with IC50 of 1.2 μM. MG-132 induces neurite outgrowth in PC12 cells at an optimal concentration of 20 nM, displaying 500 times more potency than ZLLal. [1] MG-132 (10 μM) potently inhibits TNF-α-induced NF-κB activation, interleukin-8 (IL-8) gene transcription, and IL-8 protein release in A549 cells by inhibition of proteasome-mediated IκBα degradation. [2] MG-132 treatment potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition. [3] Unlike BzLLLCOCHO or PS-341, MG-132 treatment results in weak inhibition of the chymotrypsinlike (CT-L) and peptidylglutamyl peptide hydrolysing (PGPH) activities of the 26S proteasome, whereas multiple myeloma cells (U266 and OPM-2) are more sensitive to induction of apoptosis by MG-132 than BzLLLCOCHO. [4] MG-132 (1 μM) sensitizes TRAIL-resistant prostate cancer cells by activating the AP-1 family members c-Fos and c-Jun, which, in turn, repress the antiapoptotic molecule c-FLIP(L). [5] MG-132 significantly enhances the ability of inositol hexakisphosphate (IP6) to reduce cellular metabolic activity in both PC3 and DU145 androgen-independent prostate cancer (AIPCa) cell lines. [6]
In vivo試験 Administration of MG-132 effectively rescues the expression levels and plasma membrane localization of dystrophin, β-dystroglycan, α-bdystroglycan, and α-sarcoglycan in skeletal muscle fibers from mdx mice, reduces muscle membrane damage, and ameliorates the histopathological signs of muscular dystrophy. [7] MG-132 treatment significantly reduces immobilization-induced skeletal muscle atrophy in mice, by downregulating the muscle-specific ubiquitin ligases atrogin-1/MAFbx and MuRF-1 mRNA. [8]
臨床試験
特集

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ:

[1]

Measurement of inhibitory activities of MG-132 against 20S proteasome The reaction mixture for the 20S proteasome inhibitory assay contains 0.1 M Tris-acetate, pH 7.0, 20S proteasome, MG-132, and 25 μM substrate dissolved in dimethyl sulfoxide in a final volume of 1 mL. After incuba tion at 37 °C for 15 minutes, the reaction is stopped by the addition of 0.1 mL of 10% SDS and 0.9 mL of 0.1M Tris acetate, pH 9.0. The fluorescence of the reaction products is measured. To determine the IC50 against 20S proteasome, various concentrations of MG-132 are included in the assay mixture.

細胞アッセイ:

[3]

細胞系 KIM-2, HC11, and ES
濃度 Dissolved in DMSO, final concentrations ~25 μM
処理時間 24, and 48 hours
方法

Cells are exposed to various concentrations of MG-132 for 24, and 48 hours. Supernatant and monolayer cells are harvested by centrifugation and fixed in 70% ethanol in PBS for staining with acridine orange. Equal volumes of cells and acridine orange (5 mg/mL in PBS) are mixed on a microscope slide and examined by fluorescence microscopy. For annexin V analysis, cells are harvested by centrifugation and stained with annexin V and propidium iodide. For cell cycle analysis, cells are rehydrated in PBS at room temperature for 10 minutes, followed by staining with propidium iodide (5 mg/mL). All samples are analyzed using a Coulter Epics XL flow cytometer.

動物実験:

[7]

動物モデル Male mdx (C57BL/10ScSn DMD mdx) mice
製剤 Dissolved in DMSO, and diluted in PBS
投薬量 ~10 μg/kg/day
管理 Injection
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, pH 4 6 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
1

参考

化学情報

Download MG-132 SDF
分子量 475.62
化学式

C26H41N3O5

CAS No. 133407-82-6
保管 2年-20℃
6月-80℃in DMSO
別名
溶解度 (25°C) * In vitro DMSO 95 mg/mL (199 mM)
<1 mg/mL (<1 mM)
エタノール 95 mg/mL (199 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80, pH 4 6 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 benzyl (S)-4-methyl-1-((S)-4-methyl-1-((S)-4-methyl-1-oxopentan-2-ylamino)-1-oxopentan-2-ylamino)-1-oxopentan-2-ylcarbamate

研究分野

カスタマーレビュー (4)


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Rating
Source EMBO Mol Med, 2013, 5, 397–412. MG-132 purchased from Selleck
Method Western Blot
Cell Lines MEF cells
Concentrations 30 uM
Incubation Time 6 h
Results Treatment of MEF with proteasome inhibitor MG132 resulted in similar increase of steady state levels of intracellular ATZ in both GFP- and TFEB- transfected Cells.

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Rating
Source FEBS Letters 586 (2012) 3787–3792. MG-132 purchased from Selleck
Method Western Blot
Cell Lines Hela cells
Concentrations
Incubation Time 12 h
Results When GSK-3 (Ser9) degradation was blocked by proteasome inhibitor (MG132), the increased amount of phosphorylated GSK-3 (Ser9) in responding to NOK was more clearly observed in the HeLa-NOK-HA cells (Fig. C).

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Rating
Source Dr. Edison DUKE-NUS Graduate Medical School Singapore.. MG-132 purchased from Selleck
Method Western blot
Cell Lines NIH3T3 cells
Concentrations 25 μM
Incubation Time 1-4 h
Results By adding MG132, a proteasome inhibitor, the degradation of Per2 was dramatically decreased within 4 hours treatment.

Click to enlarge
Rating
Source EMBO Mol Med, 2013, 5(3), 397-412. MG-132 purchased from Selleck
Method Western blot
Cell Lines MEF
Concentrations 30 μM
Incubation Time
Results Treatment of MEF with proteasome inhibitor MG132 resulted in similar increase of steady state levels of intracellular ATZ in both GFP- and TFEB-transfected cells.

製品表彰状 (17)

技術サポート&よくある質問(FAQ)

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