MG-132
Synonym(s):Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal, Z-LLL-CHO, Proteasome Inhibitor XI;MG-132;Proteasome Inhibitor XI, Z-Leu-Leu-Leu-CHO, Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal;Z-Leu-Leu-Leu-al
- CAS NO.:133407-82-6
- Empirical Formula: C26H41N3O5
- Molecular Weight: 475.62
- MDL number: MFCD00674886
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
![MG-132 Structural](https://img.chemicalbook.in/CAS/GIF/133407-82-6.gif)
What is MG-132?
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.
The Uses of MG-132
MG 132 is a potent, membrane-permeable proteasome inhibitor. It induces neurite outgrowth in PC12 cells. Neuroprotective product.
The Uses of MG-132
A proteasome and NF-κB inhibitor.
What are the applications of Application
MG-132 [Z-Leu- Leu-Leu-CHO] is a proteasome and NF-κB inhibitor which is used as a tool for perturbing the proteasome-regulated degradation of intracellular proteins
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)
References
1) Tsubuki et al. (1996), Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine; J. Biochem.,? 119 572 2) Wu? et al. (2010), Macroautophagy and ERK phosphorylation counteract the antiproliferative effect of proteasome inhibitor in gastric cancer cells; Autophagy, 6 228 3) Meriin? et al. (1998), Proteasome inhibitors activate stress kinases and induce Hsp72. Diverse effects on apoptosis; J. Biol. Chem., 273 6373 4) Fiedler et al. (1998), Inhibition of TNF-alpha-induced NF-kappaB activation and IL-8 release in A549 cells with the proteasome inhibitor MG-132; Am. J. Respir. Cell Mol. Biol., 19 259
Properties of MG-132
Melting point: | 80-84℃ (DEC.) |
Boiling point: | 682.0±55.0 °C(Predicted) |
alpha | -61~-67° |
Density | 1.073 |
Flash point: | 366℃ |
storage temp. | -20°C |
solubility | methanol: 1 mg/mL |
form | solid film |
pka | 11.14±0.46(Predicted) |
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. |
Safety information for MG-132
Signal word | Warning |
Pictogram(s) |
![]() Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. |
Computed Descriptors for MG-132
InChIKey | TZYWCYJVHRLUCT-VABKMULXSA-N |
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