MG-132

Key inhibitor for use in proteasome research.



BML-PI102-0005	5 mg	64.00 USD

BML-PI102-0025	25 mg	263.00 USD

Replaces Prod. #: ALX-260-092

Potent, cell permeable and selective proteasome inhibitor (K_i = 4nM).1 Inhibits NF-κB activation by preventing IκB degradation (IC₅₀ = 3μM). Blocks degradation of short-lived proteins, which in turn induces HSP and ER chaperone expression, leading to thermotolerance (1μM MG-132, 2 h.). Stimulates neurite outgrowth in PC12 cells (20nM optimal). IC₅₀’s for inhibition of Suc-LLVY-AMC and Z-LLL-AMC cleaving activities of proteasome were 0.85 and 0.1μM respectively.The ubiquitin-proteasome system (UPS) and autophagy serve as two complementary, reciprocally regulated protein degradation systems, thus blockade of UPS by MG-132 activates autophagy.

Product Specification

Alternative Name:	Z-Leu-Leu-Leu-CHO, Z-LLL-CHO

Formula:	C₂₆H₄₁N₃O₅

MW:	475.6

Purity:	≥98%

Appearance:	White solid.

Sequence:	Z-Leu-Leu-Leu-CHO

CAS:	133407-82-6

Solubility:	Soluble in DMSO (25mg/ml) or 100% ethanol (25mg/ml).

Long Term Storage:	-80°C

Use/Stability:	Solutions are stable for up to one week if stored at -20°C. Solutions are stable for up to two months if stored at -80°C.

Background / Technical Information:	Please click here for the comprehensive product datasheet. Replacement for ADI-HPK-116

Product Literature References

Induction of autophagy by proteasome inhibitor is associated with proliferative arrest in colon cancer cells: W.K. Wu, et al.; BBRC 374, 258 (2008), Abstract;

Role of proteasomal degradation in the cell cycle-dependent regulation of DNA topoisomerase IIalpha expression: L. Salmena, et al.; Biochem. Pharmacol. 61, 795 (2001), Abstract;

Proteasome inhibitors activate stress kinases and induce Hsp72. Diverse effects on apoptosis: A.B. Meriin, et al.; J. Biol. Chem. 273, 6373 (1998), Abstract;

Proteasome inhibition leads to a heat-shock response, induction of endoplasmic reticulum chaperones, and thermotolerance: K.T. Bush, et al.; J. Biol. Chem. 272, 9086 (1997), Abstract;

J. Adams & R. Stein; Ann. Rep. Med. Chem. 31, 279 (1996),

Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine: S. Tsubuki, et al.; J. Biochem. 119, 572 (1996), Abstract;

Selective inhibitors of the proteasome-dependent and vacuolar pathways of protein degradation in Saccharomyces cerevisiae: D.H. Lee & A.L. Goldberg; J. Biol. Chem. 271, 27280 (1996), Abstract;

The human cytomegalovirus US11 gene product dislocates MHC class I heavy chains from the endoplasmic reticulum to the cytosol: E.J. Wiertz, et al.; Cell 84, 769 (1996), Abstract;

Multiple proteolytic systems, including the proteasome, contribute to CFTR processing: T.J. Jensen, et al.; Cell 83, 129 (1995), Abstract;

The proteasome pathway is required for cytokine-induced endothelial-leukocyte adhesion molecule expression: M.A. Read, et al.; Immunity 2, 493 (1995), Abstract;

Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules: K.L. Rock, et al.; Cell 78, 761 (1994), Abstract;