MG-132 [Z-Leu- Leu-Leu-CHO] CAS: 133407-82-6
MF: C26H41N3O5
MW: 475.62

MG-132 [Z-Leu- Leu-Leu-CHO] (CAS 133407-82-6)

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MG-132 [Z-Leu- Leu-Leu-CHO] is rated 5.0 out of 5 by 2.
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Noms alternatifs: MG-132 [Z-Leu- Leu-Leu-CHO] also known as (S)-MG132; Z-LLL-al; Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal; N-CBZ-leucine-leucine-leucinal; Z-Leu-Leu-Leu-CHO; Z-Leu-Leu-Leu-al; MG132; MG-132; S)-MG132
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 intr
Numéro CAS: 133407-82-6
Pureté: >98%
Masse Moléculaire: 475.62
Formule Moléculaire: C26H41N3O5
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
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MG-132 [Z-Leu-Leu-Leu-CHO] is a potent, reversible, and cell-permeable proteasome inhibitor. MG-132 [Z-Leu- Leu-Leu-CHO] is used as a tool for perturbing the proteasome-regulated degradation of intracellular proteins. These proteins processed by the proteasome are involved in inflammatory processes and cell cycle regulation, presenting broad relevance for aldehydic proteasome inhibitors of this type. For instance, MG-132 suppresses NF-κB activation (at 10 μM) by preventing IκB degradation (IC50=3 μM), which blocks the transcription factor from providing chemoresistance to cancer cells. Also, MG-132 has been shown to prevent beta-secretase cleavage of amyloid precursor protein (APP). Additionally, MG-132 is an inhibitor of 26S Proteasome and calpain, as well as, an activator of JNK1, c-Jun and c-Fos.

Related products include sc-351846 (sc-351846).


Références

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. Steinhilb, M. L., et al. 2001. J Biol Chem. 276(6):4476-4484. PMID: 11084038

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

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

6. Ye, X. et al. 2014. PLoS Pathog. 10(4): e1004070. PMID: 24722419

État Physique :
Solid
Séquence :
Z-Leu-Leu-Leu-CHO
Solubilité :
Soluble in ethanol (100 mM), and DMSO (100 mM).
STOCKAGE :
Store at -20° C
Activité Optique :
α20D -65.5, c = 1 in chloroform
IC50 :
NF-κB activation: IC50 = 3 µM; Suc-LLVY-AMC cleaving activity of proteasome: IC50 = 0.85 µM; Z-LLL-AMC cleaving activity of proteasome: IC50 = 0.1 µM; calpain: IC50 = 1.2 µM; IκBα degradation: IC50 = 3 µM
Ki Data :
proteasome: Ki= 4 nM
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
WGK Allemagne :
3
RTECS :
OH2824610
PubChem CID :
Numéro MDL :
MFCD00674886
SMILES :
CC(C)C[[email protected]@H](C=O)NC(=O)[[email protected]](CC(C)C)NC(=O)[[email protected]](CC(C)C)NC(=O)OCC1=CC=CC=C1

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CERTIFICAT D'ANALYSE

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MG-132 [Z-Leu- Leu-Leu-CHO] (CAS 133407-82-6)  Références bibliographiques

Consultez les publications faisant référence à l' utilisation de MG-132 [Z-Leu- Leu-Leu-CHO] (CAS 133407-82-6). Cliquez sur le lien pour afficher lentrée PubMed .

Citations 1 à 10 sur un total de 122

PMID: # 34271072  Vankadara, S.|Xuan Wong, Y.|Liu, B.|Yang See, Y.|Hong Tan, L.|Wen Tan, Q.|Wang, G.|Karuna, R.|Guo, X.|Ting Tan, S.|Yi Fong, J.|Joy, J.|Brian Chia, CS.| et al. 2021. Bioorg Med Chem Lett. 128263.

PMID: # 33474722  Yang, Y.|Ma, Q.|Li, Z.|Wang, H.|Zhang, C.|Liu, Y.|Li, B.|Wang, Y.|Cui, Q.|Xue, F.|Ai, D.|Zhu, Y.|He, J.| et al. 2021. Br J Pharmacol. 178: 1524-1540.

PMID: # 34004371  Scholtès, GK.|Sawyer, AM.|Vaca, CC.|Clerc, I.|Roh, M.|Song, C.|D'Aquila, RT.| et al. 2021. Transl Res.

PMID: # 33637846  Chandrasekaran, S.|Schneps, CM.|Dunleavy, R.|Lin, C.|DeOliveira, CC.|Ganguly, A.|Crane, BR.| et al. 2021. Commun Biol. 4: 249.

PMID: # 34188037  Hang, Q.|Zeng, L.|Wang, L.|Nie, L.|Yao, F.|Teng, H.|Deng, Y.|Yap, S.|Sun, Y.|Frank, SJ.|Chen, J.|Ma, L.| et al. 2021. Nat Commun. 12: 4033.

PMID: # 34029592  Gaborit, B.|Govers, R.|Altié, A.|Brunel, JM.|Morange, P.|Peiretti, F.| et al. 2021. J Biol Chem. 100818.

PMID: # 33922657  Tseng, WC.|Chen, CY.|Chern, CY.|Wang, CA.|Lee, WC.|Chi, YC.|Cheng, SF.|Kuo, YT.|Chiu, YC.|Tseng, ST.|Lin, PY.|Liou, SJ.|Li, YC.|Chen, CC.| et al. 2021. Int J Mol Sci. 22:

PMID: # 31676796  García-Pastor, C.|Benito-Martínez, S.|Moreno-Manzano, V.|Fernández-Martínez, AB.|Lucio-Cazaña, FJ.| et al. 2019. Sci Rep. 9: 15868.

PMID: # 31078367  Joa, H. et al. 2019. Phytomedicine. 152938.

PMID: # 30821592  Peng, M.|Wang, J.|Tian, Z.|Zhang, D.|Jin, H.|Liu, C.|Xu, J.|Li, J.|Hua, X.|Xu, J.|Huang, C.|Huang, C.| et al. 2019. Autophagy.

Citations 1 à 10 sur un total de 122
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