(R)-MG-132 CAS: 1211877-36-9
MF: C26H41N3O5
MW: 475.62

(R)-MG-132 (CAS 1211877-36-9)

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別名: (R)-MG-132 is also known as Z-LLL-CHO.
アプリケーション: (R)-MG-132 is a potent, cell-permeable, reversible and selective inhibitor, key in proteasome research.
CAS 番号: 1211877-36-9
Purity: ≥98%
Molecular Weight: 475.62
Molecular Formula: C26H41N3O5
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* Refer to Certificate of Analysis for lot specific data (including water content).
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(R)-MG-132 is a potent, reversible and cell permeable proteasome inhibitor. The ubiquitin-proteasome pathway plays an integral role in the selective degradation of intracellular proteins. While important for clearing damaged or misfolded proteins, this proteolytic pathway also regulates the availability of key proteins involved in the control of inflammatory processes, cell cycle regulation, and gene expression. After treatment for one hour at 100 nM, (R)-MG-132 inhibits 50% and 31% of proteasome activity in lysates of J558L multiple myeloma cells and EMT6 breast cancer cells, respectively. The (R)-MG-132 stereoisomer is a more effective inhibitor of chymotrypsin-like (ChTL), trypsin-like (TL), and peptidylglutamyl peptide hydrolyzing proteasome (PGPH) activities compared to (S)-MG-132 (IC50 = 0.22 µM versus 0.89 µM (ChTL); 34.4 µM versus 104.43 µM (TL); 2.95 µM versus 5.70 µM (PGPH), respectively).

Related products include the S conformer, MG-132 [Z-Leu- Leu-Leu-CHO] (sc-201270). (R)-MG-132 is also known as Z-LLL-CHO, (R)-MG132, MG-132, (R)-MG 132, and N-[(Phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formyl-3-methylbutyl]-D-leucinamide; carbobenzoxy-Leu-Leu-leucinal.


参考文献

1. Lee, D.H. and Goldberg, A.L. 1998. Trends Cell Biol. 8: 397-403. PMID: 9789328

2. Arlt, A., et al. 2001. Oncogene. 20: 859-868. PMID: 11314019

3. Elliott, P.J., et al. 2003. J. Mol. Med. 81: 235-245. PMID: 12700891

4. Vivier, M., et al. 2008. J. Med. Chem. 51: 1043-1047. PMID: 18237109

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (20 mM).
保存方法 :
Store at -20° C
IC50 :
20S proteasome: IC50 = 0.22 nM; Chymotrypsin trypsin-like activity of 20S proteasome : IC50 = 220 nM (human); Peptidylglutamyl peptide hydrolyzing-like activity of 20S proteasome : IC50 = 2950 nM (human); Trypsin-like activity of 20S proteasome : IC50 = 34.4 µM (human)
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
PubChem CID :
SMILES :
CC(C)C[[email protected]@H](CC=O)NC(=O)[[email protected]@H](CC(C)C)NC(=O)[[email protected]](CC(C)C)NC(=O)OCC1=CC=CC=C1

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(R)-MG-132 (CAS 1211877-36-9)  参考文献

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PMID: # 28086019  Haidar, M. et al. 2017. ACS Infect Dis. 3: 216-224.

PMID: # 26250624  Jewett, K. et al. 2015. J Neurochem.

PMID: # 25927990  Amaya, M. et al. 2015. PLoS ONE. 10: e0124792.

PMID: # 24608790  Peuget, S. et al. 2014. Cell Death Differ. 21: 1107-18.

PMID: # 23319609  Yang, F. et al. 2013. Proc. Natl. Acad. Sci. U.S.A. 110: 1863-8.

PMID: # 22461906  Lazar, C. et al. 2012. PloS one. 7: e34169.

PMID: # 32446175  Redox Biol. 34: 101571.

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