MG132

製品コードS2619 バッチS261920

印刷

化学情報

Chemical Structure Synonyms (S,R,S)-(-)-MG-132, Z-Leu-D-Leu-Leu-al Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26H41N3O5
分子量 475.62 CAS No. 1211877-36-9
Solubility (25°C)* 体外 DMSO 95 mg/mL (199.73 mM)
Ethanol 95 mg/mL (199.73 mM)
Water Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MG132 ((S,R,S)-(-)-MG132, Z-Leu-D-Leu-Leu-al) は、強力なプロテアソーム（ChTL、TL、PGPH） 阻害剤です。 MG132 はカルパイン (calpain) も阻害します (IC50 = 1.2 μM)。
in vitro

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

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]

プロトコル(参考用のみ)

キナーゼアッセイ 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 細胞株 KIM-2, HC11, and ES
濃度 Dissolved in DMSO, final concentrations ~25 μM
反応時間 24 and 48 hours
実験の流れ

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 動物モデル Male mdx (C57BL/10ScSn DMD mdx) mice
投薬量 ~10 μg/kg/day
投与方法 Injection

カスタマーフィードバック

Data from [Data independently produced by Nat Cell Biol, 2015, 17(1), 95-103]

Data from [Data independently produced by Cell Rep, 2015, 11(9), 1458-73]

Data from [Data independently produced by Toxicol Appl Pharmacol, 2015, 286(2), 135-41]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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