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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 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.

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. This compound also inhibits calpain with IC50 of 1.2 μM. This chemical induces neurite outgrowth in PC12 cells at an optimal concentration of 20 nM, displaying 500 times more potency than ZLLal. [1] This compound (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] This chemical treatment potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition. [3] Unlike BzLLLCOCHO or PS-341, this compound 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 this chemical than BzLLLCOCHO. [4] This compound (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] This chemical 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] Treatment with this compound 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 incubation 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 this compound 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

参考

  • https://pubmed.ncbi.nlm.nih.gov/8830056/
  • https://pubmed.ncbi.nlm.nih.gov/9698598/
  • https://pubmed.ncbi.nlm.nih.gov/11319603/
  • https://pubmed.ncbi.nlm.nih.gov/16778216/
  • https://pubmed.ncbi.nlm.nih.gov/17332355/
  • https://pubmed.ncbi.nlm.nih.gov/18941459/
  • https://pubmed.ncbi.nlm.nih.gov/14507673/
  • https://pubmed.ncbi.nlm.nih.gov/21843349/
  • https://pubmed.ncbi.nlm.nih.gov/20112914/

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Anisomelic acid promotes proteasomal degradation of HPV16 E6 via E3 ligase recruitment: A mass spectrometry-based interactome study [ J Proteomics, 2026, 322:105536] PubMed: 40967472
Lymph node environment drives FSP1 targetability in metastasizing melanoma [ Nature, 2025, 10.1038/s41586-025-09709-1] PubMed: 41193799
VCP downstream metabolite glycerol-3-phosphate (G3P) inhibits CD8+T cells function in the HCC microenvironment [ Signal Transduct Target Ther, 2025, 10(1):26] PubMed: 39848960
NAP1L1 degradation by FBXW7 reduces the deubiquitination of HDGF-p62 signaling to stimulate autophagy and induce primary cisplatin chemosensitivity in nasopharyngeal carcinoma [ Mol Cancer, 2025, 24(1):152] PubMed: 40414865
NAP1L1 degradation by FBXW7 reduces the deubiquitination of HDGF-p62 signaling to stimulate autophagy and induce primary cisplatin chemosensitivity in nasopharyngeal carcinoma [ Mol Cancer, 2025, 24(1):152] PubMed: 40414865
MAPK13 phosphorylates PHGDH and promotes its degradation via chaperone-mediated autophagy during liver injury [ Cell Discov, 2025, 11(1):15] PubMed: 39962071
Alterations in PD-L1 succinylation shape anti-tumor immune responses in melanoma [ Nat Genet, 2025, 57(3):680-693] PubMed: 40069506
Transcriptional repressor Capicua is a gatekeeper of cell-intrinsic interferon responses [ Cell Host Microbe, 2025, 33(4):512-528.e7] PubMed: 40132591
A heterotrimeric protein complex assembles the metazoan V-ATPase upon dissipation of proton gradients [ Nat Struct Mol Biol, 2025, 10.1038/s41594-025-01610-9] PubMed: 40646309
Harnessing the FGFR2/NF2/YAP signaling-dependent necroptosis to develop an FGFR2/IL-8 dual blockade therapeutic strategy [ Nat Commun, 2025, 16(1):4128] PubMed: 40319089

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。