MG-132

Bezeichnung:MG-132

CAS-Nr133407-82-6

Englisch Name:MG-132

CBNumberCB3298042

SummenformelC26H41N3O5

Molgewicht475.62

MOL-Datei133407-82-6.mol

MG-132 physikalisch-chemischer Eigenschaften

Schmelzpunkt	80-84℃ (DEC.)
alpha	-61～-67°
Siedepunkt	682.0±55.0 °C(Predicted)
Dichte	1.073
Flammpunkt	366℃
storage temp.	-20°C
Löslichkeit	methanol: 1 mg/mL
Aggregatzustand	solid film
pka	11.14±0.46(Predicted)
Farbe	White
Wasserlöslichkeit	Soluble in ethanol, chloroform, methanol, water.
Stabilität	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

Sicherheit

R-Sätze:	36/37/38
S-Sätze:	24/25
WGK Germany	3
HS Code	29242990

Gefahreninformationscode (GHS)

MG-132 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Verwenden
MG 132 is a potent, membrane-permeable proteasome inhibitor. It induces neurite outgrowth in PC12 cells. Neuroprotective product.
Verwenden
A proteasome and NF-κB inhibitor.
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.
Allgemeine Beschreibung
Potent, reversible, and cell-permeable proteasome inhibitor (K_i = 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).
Biologische Aktivität
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
Lager
-20°C (desiccate)
Einzelnachweise
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

MG-132 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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