MG-132 Inhibitor CAS No. 133407-82-6

Cat. No.	Name	Size	Price
KI0523	MG-132	5 mg	$80
	MG-132	25 mg	$272
	MG-132	100 mg	$752

Chemical Characteristic

Product Name	MG-132
Synonyms	ZLLLal
CAS No.	133407-82-6
Molecular Weight	475.62
Formula	C₂₆H₄₁N₃O₅
Chemical Name	N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-L-leucinamide
Smiles	C(=O)(C(NC(=O)C(NC(=O)OCc1ccccc1)CC(C)C)CC(C)C)N[C@@H](CC(C)C)C=O
Chemical Structure
Documents	HPLC MS COA

Biological activities

MG-132 is a proteasome inhibitor. The IC50 for the benzyloxycarbonyl-leucyl-leucyl- leucine-4-methylcoumaryl-7-amide (MG-132-MCA)-degrading activity of 20S proteasome by MG-132 is 100 nM. MG-132 strongly inhibits calpain and proteasome activities in vitro.^[1] MG-132 inhibits hepatitis C virus RNA replication with an IC50 of 0.21 nM. ^[2] MG-132 upregulates heat-shock gene transcription without heat shock. MG-132 induces hyperphosphorylation and DNA-binding activity of HSF1 in the absence of heat shock (at 37 ?C). ^[3] MG-132 induces cell cycle arrest in tobacco BY2 cells during metaphase and inhibition of the proteolysis of chimeric cyclin-CAT fusion proteins. ^[4] MG-132 upregulates Apo2L/TRAIL death receptor 5 expression in both Bax-proficient and -deficient HCT116 cells. MG-132 effectively cooperates with Apo2L/TRAIL to induce apoptosis in both Bax-proficient and ??eficient cells. ^[5] Long-term treatment with MG-132 attenuates pressure-overload-induced cardiac hypertrophy and improves cardiac function in AAB rats through regulation of ERK1/2 and JNK1 signaling pathways. ^[6]

Protocols

MG-132 is dissolved in DMSO in a final volume of 1 mL. ^[1]

References

[1] Tsubuki S, et al. Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine. J Biochem. 1996, 119(3): 572-576. [2] Ujino S, et al. Combination therapy for hepatitis C virus with heat-shock protein 90 inhibitor 17-AAG and proteasome inhibitor MG-132. Antivir Chem Chemother. 2010, 20(4): 161-167. [3] Kim D, et al. Proteasome inhibitors MG-132 and lactacystin hyperphosphorylate HSF1 and induce hsp70 and hsp27 expression. Biochem Biophys Res Commun. 1999, 254(1): 264- 268. [4] Genschik P, et al. Cell cycle -dependent proteolysis in plants. Identification Of the destruction box pathway and metaphase arrest produced by the proteasome inhibitor mg132. Plant Cell. 1998, 10(12): 2063-2076. [5] He Q, et al. Proteasome inhibitor MG-132 upregulates death receptor 5 and cooperates with Apo2L/TRAIL to induce apoptosis in Bax-proficient and -deficient cells. Oncogene. 2004, 23(14): 2554-2558. [6] Chen B, et al. MG132, a proteasome inhibitor, attenuates pressure- overload-induced cardiac hypertrophy in rats by modulation of mitogen-activated protein kinase signals. Acta Biochim Biophys Sin (Shanghai). 2010, 42(4): 253-258.

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