MG-115

- Overview
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    Background
    
    MG-115 (Z-Leu-Leu-Nva-H) is a potent, reversible peptide aldehyde inhibitor of proteasome chymotrypsin-like and caspase-like activities. It induces p53 dependent apoptosis. Blockade of proteasomal degradation by MG115 can activate autophagy.
    Treatment with proteasome inhibitors Z-Leu-Leu-Nva-H (MG-115) or Z-Leu-Leu-Leu-H (MG-132) prevented the accelerated degradation of these mutant receptors, resulting in increased amounts of the mutant receptors in the COS-7 cells [1].
    A potent, reversible proteasome inhibitor with Ki of 21 nM for 20S proteasome and 35 nM for 26S proteasome. The inhibition of proteasome was through specific inhibition of chymotrypsin-like activity of the proteasome. Also shown to induce apoptosis in Rat-1 and PC12 cells via a p3-independent pathway.
    
    1. Involvement of heat shock protein 90 in the degradation of mutant insulin receptors by the proteasome. Imamura, T., Haruta, T., Takata, Y., Usui, I., Iwata, M., Ishihara, H., Ishiki, M., Ishibashi, O., Ueno, E., Sasaoka, T., Kobayashi, M. J. Biol. Chem. (1998)
- Properties
  - Alternative Name
    
    Carbobenzoxy-L-leucyl-L-leucyl-L-norvalinal, Z-LL-Nva-CHO, Proteasome Inhibitor XII,MG115; benzyl N-[(2S)-4-methyl-1-[[(2S)-4-methyl-1-oxo-1-[[(2S)-1-oxopentan-2-yl]amino]pentan-2-yl]amino]-1-oxopentan-2-yl]carbamate
    
    CAS Number
    
    133407-86-0
    
    Molecular Formula
    
    C25H39N3O5
    
    Molecular Weight
    
    461.59
    
    Appearance
    
    A solid
    
    Purity
    
    99.02%
    
    Solubility
    
    ≥23.08 mg/mL in DMSO; insoluble in H2O; ≥26.5 mg/mL in EtOH
    
    Storage
    
    Store at -20°C. The product is not stable in solution, please dissolve it immediately before use.
    
    * For Research Use Only
- Reference
  - 1. Wang Y, Lu S, et al. "Sonic hedgehog induces GLT-1 degradation via PKC delta to suppress its transporter activities." Neuroscience. 2017 Oct 6;365:217-225. PMID:28993237

MG-115

Background

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