- MG-132
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- $81.00 / 25mg
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2026-02-03
- CAS:133407-82-6
- Min. Order:
- Purity: 97.66%
- Supply Ability: 10g
- MG-132
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- $1.00 / 1g
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2019-12-20
- CAS:133407-82-6
- Min. Order: 1g
- Purity: 99.99%
- Supply Ability: 2tons
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| | MG-132 Chemical Properties |
| Melting point | 80-84℃ (DEC.) | | alpha | -61～-67° | | Boiling point | 682.0±55.0 °C(Predicted) | | density | 1.073 | | Fp | 366℃ | | storage temp. | -20°C | | solubility | methanol: 1 mg/mL | | pka | 11.14±0.46(Predicted) | | form | solid film | | color | White | | Water Solubility | Soluble in ethanol, chloroform, methanol, water. | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO, DMF or ethanol may be stored at -20° for up to 1 week. | | InChIKey | TZYWCYJVHRLUCT-VABKMULXSA-N | | SMILES | C(N)(=O)[C@H](CC(C)C)N(C(=O)[C@H](CC(C)C)NC(OCC1=CC=CC=C1)=O)[C@H](C=O)CC(C)C |
| Risk Statements | 36/37/38 | | Safety Statements | 24/25 | | WGK Germany | 3 | | HS Code | 29242990 | | Storage Class | 11 - Combustible Solids |
| | MG-132 Usage And Synthesis |
| Description | MG-132 (133407-82-6) is a specific inhibitor of the chymotrypsin-like activity of the 20S proteasome (IC50=100 nM with Z-LLL-AMC as substrate).1 Also inhibits calpain (IC50=1.25 μM).1 Suppresses gastric cancer cell proliferation and induces macro-autophagy.2 Activates stress kinases and induces Hsp72.3 Induces neurite outgrowth.1 MG-132 blocks NFκB activation by blocking IκB proteolysis (IC50=3 μM).4 Cell permeable. | | Uses | A proteasome and NF-κB inhibitor. | | Uses | MG 132 is a potent, membrane-permeable proteasome inhibitor. It induces neurite outgrowth in PC12 cells. Neuroprotective product. | | Definition | ChEBI: A tripeptide that is L-leucyl-L-leucyl-L-leucine in which the C-terminal carboxy group has been reduced to the corresponding aldehyde and the N-terminal amino group is
protected as its benzyloxycarbonyl derivative. | | General Description | Potent, reversible, and cell-permeable proteasome inhibitor (Ki = 4 nM). Reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable stains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. Activates c-Jun N-terminal kinase (JNK1) and inhibits NF-κB activation (IC50 = 3 μM). | | Biological Activity | Potent cell-permeable inhibitor of proteasome (IC 50 = 100 nM) and calpain (IC 50 = 1.2 μ M). Inhibits TNF- α -induced NF- κ B activation and I κ B α degradation. Induces neurite outgrowth in PC12 cells and has anticancer properties in vitro . | | Biochem/physiol Actions | Cell permeable: yes | | storage | -20°C (desiccate) | | Background | MG-132 is a potent proteasome and calpain inhibitor. Research studies have shown that MG-132 prevents degradation of the proteasome substrates SucLLVY-MCA and ZLLL-MCA with an IC50 of 850 nM and 100 nM, respectively, as well as inhibits casein-degrading activity of m-calpain with an IC50 of 1.25 µM. Investigators have demonstrated that MG-132 inhibits TNF-α-induced NF-κB activation and IL-8 release in A549 cells. Proteasome inhibition with MG-132 prevents degradation of short-lived proteins, which correlates with increased expression of HSP and ER chaperone proteins. MG-132 induces apoptosis in Hep G2 cells in a time- and dose-dependent manner. Proteasome inhibitors like MG-132 are important research tools for studying cellular degradation of the ubiquitin-proteasome pathway. | | References | [1] S TSUBUKI. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine.[J]. Journal of biochemistry, 1996, 119 3: 572-576. DOI:10.1093/oxfordjournals.jbchem.a021280
[2] WILLIAM KA KEI WU. Macroautophagy and ERK phosphorylation counteract the antiproliferative effect of proteasome inhibitor in gastric cancer cells.[J]. Autophagy, 2010, 6 2: 228-238. DOI:10.4161/auto.6.2.11042
[3] A B MERIIN. Proteasome inhibitors activate stress kinases and induce Hsp72. Diverse effects on apoptosis.[J]. The Journal of Biological Chemistry, 1998, 273 11: 6373-6379. DOI:10.1074/jbc.273.11.6373
[4] M A FIEDLER J M S K Wernke Dollries. Inhibition of TNF-alpha-induced NF-kappaB activation and IL-8 release in A549 cells with the proteasome inhibitor MG-132.[J]. American Journal of Respiratory Cell and Molecular Biology, 1998, 19 2: 259-268. DOI:10.1165/ajrcmb.19.2.3149 |
| | MG-132 Preparation Products And Raw materials |
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