MG132

Item no.	S2619-25
Manufacturer	Selleckchem
CASRN	1211877-36-9
Amount	25 mg
Quantity options	100 mg 1 g 10 g 10 mM/1 mL 25 mg 5 mg 5 g
Category	Oncology Neuroscience Neural Lineage Markers Neuroinflammation Metabolism Diabetes Glucose Homeostasis Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer Breast Cancer Testicular & Prostate Cancer Lymphatic System Cancer Neuronal Cell Markers
Type	Inhibitors
Specific against	other
Smiles	CC(C)CC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	(S,R,S)-(-)-MG-132,Z-Leu-D-Leu-Leu-al
Similar products	MG-132, 133407-82-6
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	475, 62
Administration	Injection
Animal Models	Male mdx (C57BL/10ScSn DMD mdx) mice
Cell lines	KIM-2, HC11, and ES
Concentrations	Dissolved in DMSO, final concentrations ca.25 uM
Dosages	ca.10 ug/kg/day
Formulation	Dissolved in DMSO, and diluted in PBS
IC50	100 nM [1], 100 nM [1], 100 nM [1], 100 nM [1], 100 nM [1], 100 nM [1]
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 uM. MG-132 also inhibits calpain with IC50 of 1.2 uM. 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 uM) potently inhibits TNF-alpha-induced NF-kappaB activation, interleukin-8 (IL-8) gene transcription, and IL-8 protein release in A549 cells by inhibition of proteasome-mediated IkappaBalpha 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 uM) 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, beta-dystroglycan, alpha-bdystroglycan, and alpha-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]
Incubation Time	24, and 48 hours
Kinase Assay	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 uM 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.
Method	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.
Solubility (25C)	DMSO 95 mg/mL, Water <1 mg/mL, Ethanol 95 mg/mL
Information	MG132 ((S, R, S)-(-)-MG132, Z-Leu-D-Leu-Leu-al) is a potent proteasome (ChTL, TL, and PGPH) inhibitor. MG132 also inhibits calpain (IC50=1.2 μM). MG132 can be used to induce animal models of Parkinson’s disease.
Chemical Name	benzyl (S)-4-methyl-1-((S)-4-methyl-1-((S)-4-methyl-1-oxopentan-2-ylamino)-1-oxopentan-2-ylamino)-1-oxopentan-2-ylcarbamate

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