MG-132
| Code | Size | Price |
|---|
| AG-CP3-0011-M001 | 1 mg | £25.00 |
Quantity:
| AG-CP3-0011-M005 | 5 mg | £60.00 |
Quantity:
| AG-CP3-0011-M025 | 25 mg | £160.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
Ambient
Storage:
-20°C
Further Information
Alternate Names/Synonyms:
Z-LLL-CHO; Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal; MG132
Appearance:
White solid.
CAS:
133407-82-6
EClass:
32160000
Form (Short):
liquid
Handling Advice:
Keep cool and dry.
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
InChiKey:
TZYWCYJVHRLUCT-VABKMULXSA-N
Long Description:
Chemical. CAS: 133407-82-6. Formula: C26H41N3O5. MW: 475.6. Potent, cell permeable and selective, reversible proteasome inhibitor. Blocks degradation of short-lived proteins and induces a heat shock response. NF-kappaB activation inhibitor through IkappaB degradation. Cell permeable, reversible peptide aldehyde inhibitor. Calpain and cathepsin inhibitor. Has anticancer properties by inducing cell cycle arrest and activating apoptosis in various cancer cell lines. Has adjuvant/chemosensitizer potential. Neurite outgrowth stimulator in PC12 cells. Prevents beta-secretase cleavage. Autophagy activator.
MDL:
MFCD00674886
Molecular Formula:
C26H41N3O5
Molecular Weight:
475.6
Package Type:
Vial
Product Description:
Potent, cell permeable and selective, reversible proteasome inhibitor [2, 7]. Blocks degradation of short-lived proteins and induces a heat shock response [2, 6, 7]. NF-kappaB activation inhibitor through IkappaB degradation [3, 8]. Cell permeable, reversible peptide aldehyde inhibitor. Calpain and cathepsin inhibitor [4, 11]. Has anticancer properties by inducing cell cycle arrest and activating apoptosis in various cancer cell lines [8, 9, 12,13,15]. Has adjuvant/chemosensitizer potential [8]. Neurite outgrowth stimulator in PC12 cells [1]. Prevents beta-secretase cleavage [5, 10]. Autophagy activator [12, 14].
Purity:
>97% (HPLC)
Sequence:
Z-Leu-Leu-Leu-aldeyhde
SMILES:
[H]C(=O)[C@]([H])(CC(C)C)NC(=O)[C@]([H])(CC(C)C)NC(=O)[C@]([H])(CC(C)C)NC(=O)OCC1=CC=CC=C1
Solubility Chemicals:
Soluble in DMSO or ethanol.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
Isolation and characterization of possible target proteins responsible for neurite outgrowth induced by a tripeptide aldehyde in PC12H cells: Y. Saito, et al.; BBRC 184, 419 (1992) | Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules: K.L. Rock, et al.; Cell 78, 761 (1994) | The ubiquitin-proteasome pathway is required for processing the NF-kappa B1 precursor protein and the activation of NF-kappa B: V.J. Palombella, et al.; Cell 78, 773 (1994) | Differential inhibition of calpain and proteasome activities by peptidyl aldehydes of di-leucine and tri-leucine: S. Tsubuki, et al.; J. Biochem. 119, 572 (1996) | The carboxyl termini of beta-amyloid peptides 1-40 and 1-42 are generated by distinct gamma-secretase activities: H. Klafki, et al.; J. Biol. Chem. 271, 28655 (1996) | Proteasome inhibition leads to a heat-shock response, induction of endoplasmic reticulum chaperones, and thermotolerance: K.T. Bush, et al.; J. Biol. Chem. 272, 9086 (1997) | Proteasome inhibitors: valuable new tools for cell biologists: D.H. Lee & A.L. Goldberg; Trends Cell Biol. 8, 397 (1998) | Inhibition of NF-kappaB sensitizes human pancreatic carcinoma cells to apoptosis induced by etoposide (VP16) or doxorubicin: A. Arlt, et al.; Oncogene 20, 859 (2001) | Potential of the proteasomal inhibitor MG-132 as an anticancer agent, alone and in combination: D. Banerjee & A. Liefshitz; Anticancer Res. 21, 3941 (2001) | The protease inhibitor, MG132, blocks maturation of the amyloid precursor protein Swedish mutant preventing cleavage by beta-Secretase: M.L. Steinhilb, et al.; J. Biol. Chem. 276, 4476 (2001) | The proteasome inhibitor MG132 protects against acute pancreatitis: T. Letoha, et al.; Free Radic. Biol. Med. 39, 1142 (2005) | Induction of autophagy by proteasome inhibitor is associated with proliferative arrest in colon cancer cells: W.K. Wu, et al.; BBRC 374, 258 (2008) | Synthesis, radiosynthesis, and biological evaluation of new proteasome inhibitors in a tumor targeting approach: M. Vivier, et al.; J. Med. Chem. 51, 1043 (2008) | Mechanisms of cross-talk between the ubiquitin-proteasome and autophagy-lysosome systems: V.I. Korolchuk, et al.; FEBS Lett. 584, 1393 (2010) | MG132, a proteasome inhibitor, induces apoptosis in tumor cells: N. Guo & Z. Peng; Asia Pac. J. Clin. Oncol. 9, 6 (2013) | AQP2 Abundance is Regulated by the E3-Ligase CHIP Via HSP70: M. Centrone, et al.; Cell Physiol. Biochem. 44, 515 (2017) | Sal-like 4 protein levels in breast cancer cells are post-translationally down-regulated by tripartite motif containing 21: J. Itou, et al.; J. Biol. Chem. ahead of print (2018)