MG-115

Names

[ Name ]:
MG-115

[Synonym ]:
L-Leucinamide, N-[(phenylmethoxy)carbonyl]-L-leucyl-N-[(1S)-1-formylbutyl]-
N-[(Benzyloxy)carbonyl]-L-leucyl-N-[(2S)-1-oxo-2-pentanyl]-L-leucinamide
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
MG115 Z-LLnV

Biological Activity

[Description]:

MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis[1][2][3].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome

[Target]

Ki: 21 nM (20S proteasome); 35 nM (26 Sproteasome)[1]

[In Vitro]

MG-115 (0.1-10 μM; 24 h) dose-dependently decreases the viability of HepG2 cells[3]. MG-115 (0.1-10 μM; 24 h) amplifies the reporter gene expression mediated by CWK18 DNA condensates[3]. Cell Viability Assay[3] Cell Line: HepG2 cells Concentration: 0.1, 1, 2, 5, 10 μM Incubation Time: 24 hours Result: Dose-dependently decreased cell viability. Inhibited the proteasomal activity, with an IC50 of 2 μM.

[References]

[1]. Rock KL, et, al. Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules. Cell. 1994 Sep 9;78(5):761-71.

[2]. Lopes UG, et, al. p53-dependent induction of apoptosis by proteasome inhibitors. J Biol Chem. 1997 May 16;272(20):12893-6.

[3]. Kim J, et, al. The proteasome metabolizes peptide-mediated nonviral gene delivery systems. Gene Ther. 2005 Nov;12(21):1581-90.

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Boiling Point ]:
678.8±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₅H₃₉N₃O₅

[ Molecular Weight ]:
461.59

[ Flash Point ]:
364.3±31.5 °C

[ Exact Mass ]:
461.288971

[ PSA ]:
113.60000

[ LogP ]:
5.41

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.508

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Development of two novel high-throughput assays to quantify ubiquitylated proteins in cell lysates: application to screening of new anti-malarials.

Malaria Journal 14 , 200, (2015)

The ubiquitin proteasome system (UPS) is one of the main proteolytical pathways in eukaryotic cells and plays an essential role in key cellular processes such as cell cycle, stress response, signal tr...

3,4,5-tricaffeoylquinic acid attenuates proteasome inhibition-mediated programmed cell death in differentiated PC12 cells.

Neurochem. Res. 39(8) , 1416-25, (2014)

The dysfunction of the proteasome system is suggested to be implicated in neuronal degeneration. Caffeoylquinic acid derivatives have demonstrated anti-oxidant and anti-inflammatory effects. However, ...

HEMERA Couples the Proteolysis and Transcriptional Activity of PHYTOCHROME INTERACTING FACTORs in Arabidopsis Photomorphogenesis.

Plant Cell 27 , 1409-27, (2015)

Phytochromes (phys) are red and far-red photoreceptors that control plant development and growth by promoting the proteolysis of a family of antagonistically acting basic helix-loop-helix transcriptio...