CAS |
133407-82-6 |
English Name |
MG-132 |
Synonym |
Z-Leu-Leu-Leu-al;L-FMAU;Z-LEU-LEU-LEU-AL;蛋白酶体抑制剂; |
Purity |
≥98% |
Unit |
Bottle |
Molecular Formula |
C26H41N3O5 |
Molecular Weight |
475.62 |
Appearance |
White to yellow solid |
Storage |
Powder : -20℃, 2 years;In solvent(mother liquid): -20℃, 1 month; -80℃, 6 months |
Solubility |
Soluble in DMSO≥5mg/ml |
MDL |
MFCD00674886 |
InChIKey |
TZYWCYJVHRLUCT-VABKMULXSA-N |
InChI |
InChI=1S/C26H41N3O5/c1-17(2)12-21(15-30)27-24(31)22(13-18(3)4)28-25(32)23(14-19(5)6)29-26(33)34-16-20-10-8-7-9-11-20/h7-11,15,17-19,21-23H,12-14,16H2,1-6H3,(H,27,31)(H,28,32)(H,29,33)/t21-,22-,23-/m0/s1 |
PubChem CID |
462382 |
SMILES |
O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@@H](CC(C)C)C(N[C@H](C([H])=O)CC(C)C)=O)=O)CC(C)C |
Description |
MG-132 is a novel, specific, potent, reversible and cell-permeable proteasome inhibitor, and also inhibits calpain. It is also a polypeptide aldehyde, a potent autophagy activator. |
Target Point |
Proteasome;Autophagy |
Passage |
Autophagy;Metabolic Enzyme&Protease |
IC50 |
IC50: 24.2 nM (chymotrypsin-like activity) [1] |
Data Literature Source |
[1]. Braun HA, et al. Tripeptide mimetics inhibit the 20 S proteasome by covalent bonding to the active threonines. J Biol Chem. 2005 Aug 5; 280 (31) :28394-401.[2]. Han YH, et al. The effect of MG132, a proteasome inhibitor on HeLa cells in relation to cell growth, reactive oxygen species and GSH. Oncol Rep. 2009 Jul; 22 (1) :215-21.[3]. Fan WH, et al. Proteasome inhibitor MG-132 induces C6 glioma cell apoptosis via oxidative stress. Acta Pharmacol Sin. 2011 May; 32 (5) :619-25.[4]. Matsumoto Y, et al. Enhanced efficacy against cervical carcinomas through polymeric micelles physically incorporating theproteasome inhibitor MG132. Cancer Sci. 2016 Jun; 107 (6) :773-81.[5]. Chen B, et al. MG132, a proteasome inhibitor, attenuates pressure-overload-induced cardiac hypertrophy in rats by modulation of mitogen-activated protein kinase signals. Acta Biochim Biophys Sin (Shanghai) . 2010 Apr; 42 (4) :253-8. |
Specification |
5mg 10mM*1mL (in DMSO) 10mg 25mg |