133407-86-0

133407-86-0 structure

Name: MG-115
Chemical Name: Z-Leu-Leu-Norvalinal
CAS Number: 133407-86-0
Molecular Formula: C₂₅H₃₉N₃O₅
Molecular Weight: 461.59
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2018-02-10 08:00:00
Modify Date: 2024-01-06 22:58:21
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].

Name	Z-Leu-Leu-Norvalinal
Synonyms	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

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.

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