MG-132 [Z-Leu-Leu-Leu-CHO] A proteasome and NF-κB inhibitor

MG-132 [Z-Leu-Leu-Leu-CHO]  (CAS 133407-82-6)

MG-132 [Z-Leu-Leu-Leu-CHO] | CAS 133407-82-6 is rated 5.0 out of 5 by 2.
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| See 42 Citations
Synonym: Carbobenzoxy-L-leucyl-L-leucyl-L-leucinal
Application: A proteasome and NF-κB inhibitor
CAS Number: 133407-82-6
Purity: >98%
Molecular Weight: 475.62
Molecular Formula: C26H41N3O5
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

Ordering Information

PRODUCT NAME CATALOG # UNIT PRICE QTY FAVORITES
MG-132 [Z-Leu- Leu-Leu-CHO] sc-201270 5 mg $78.00
MG-132 [Z-Leu- Leu-Leu-CHO] sc-201270A 25 mg $295.00

MG-132 [Z-Leu-Leu-Leu-CHO] is a proteasome inhibitor, used as a tool for perturbing the proteasome-regulated degradation of intracellular proteins. These proteins processed by the proteasome are involved in inflammatory processes and cell cycle regulation, presenting broad relevance for aldehydic proteasome inhibitors of this type. MG-132 suppresses NF-κB activation (at 10 μM) by preventing IκB degradation (IC50=3 μM), which blocks the transcription factor from providing chemoresistance to cancer cells. It is also an an inhibitor of calpain. MG-132 [Z-Leu-Leu-Leu-CHO] is an inhibitor of 26S Proteasome and an activator of JNK1, c-Jun and c-Fos.


References

1. Lee, D.H. and Goldberg, A.L. 1998. Trends Cell Biol. 8: 397-403. PMID: 9789328
2. Arlt, A., et al. 2001. Oncogene. 20: 859-868. PMID: 11314019
3. Elliott, P.J., et al. 2003. J. Mol. Med. 81: 235-245. PMID: 12700891
4. Vivier, M., et al. 2008. J. Med. Chem. 51: 1043-1047. PMID: 18237109
5. Ye, X. et al. 2014. PLoS Pathog. 10(4): e1004070. PMID: 24722419

Physical State :
Solid
Sequence :
Z-Leu-Leu-Leu-CHO
Solubility :
Soluble in DMSO (25 mg/ml), 100% ethanol (25 mg/ml), chloroform:methanol solution (95:5) (10 mg/ml), water (<1 mg/ml), and DMF (~25 mg/ml).
Storage :
Store at -20° C
Melting Point :
96-99° C
Boiling Point :
~682.0° C at 760 mmHg (Predicted)
Density :
~1.1 g/cm3 (Predicted)
Refractive Index :
n20D 1.51
IC50 :
NF-κB activation: IC50 = 3 µM; Suc-LLVY-AMC cleaving activity of proteasome: IC50 = 0.85 µM; Z-LLL-AMC cleaving activity of proteasome: IC50 = 0.1 µM; calpain: IC50 = 1.2 µM; IκBα degradation: IC50 = 3 µM
Ki Data :
proteasome: Ki= 4 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
OH2824610
PubChem CID :
462382
MDL Number :
MFCD00674886
SMILES :
CC(C)C[C@@H](C=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)OCC1=CC=CC=C1

Download SDS (MSDS)

Certificate of Analysis

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MG-132 [Z-Leu-Leu-Leu-CHO] Product Citations

See how others have used MG-132 [Z-Leu-Leu-Leu-CHO]. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 42 total

PMID: # 27151455
Kim, SJ. et al. 2016. Activated Rac1 regulates the degradation of IκBα and the nuclear translocation of STAT3-NFκB complexes in starved cancer cells. Exp. Mol. Med.. 48: e231.

PMID: # 26728942
Guo, Z. et al. 2016. DCAF1 controls T-cell function via p53-dependent and -independent mechanisms. Nat Commun. 7: 10307.

PMID: # 25622294
Silva, GM. et al. 2015. K63 polyubiquitination is a new modulator of the oxidative stress response. Nat. Struct. Mol. Biol.. 22: 116-23.

PMID: # 26554417
Zhuang, T. et al. 2015. p21-activated kinase group II small compound inhibitor GNE-2861 perturbs estrogen receptor alpha signaling and restores tamoxifen-sensitivity in breast cancer cells. Oncotarget. 6: 43853-68.

PMID: # 25996284
Sieprath, T. et al. 2015. Sustained accumulation of prelamin A and depletion of lamin A/C both cause oxidative stress and mitochondrial dysfunction but induce different cell fates. Nucleus (Austin, Tex.). 6: 236-46.

PMID: # 26231201
Liu, Y. et al. 2015. A novel effect of thalidomide and its analogs: suppression of cereblon ubiquitination enhances ubiquitin ligase function. FASEB J.. 29: 4829-39.

PMID: # 25691063
Jha, H.C. et al. 2015. EBNA3C regulates p53 through induction of Aurora kinase B. Oncotarget. 6: 5788-803.

PMID: # 26183205
Liu, Y. et al. 2015. Transcription factor IKZF1 is degraded during the apoptosis of multiple myeloma cells induced by kinase inhibition. FEBS Lett.. 589: 2233-40.

PMID: # 25500897
Fiebiger, BM. et al. 2015. Polyubiquitination of lysine-48 is an essential but indirect signal for MHC class I antigen processing. European journal of immunology. 45: 716-27.

PMID: # 25043125
Yu, HJ. et al. 2015. Inhibition of myeloid cell leukemia-1: Association with sorafenib-induced apoptosis in human mucoepidermoid carcinoma cells and tumor xenograft. Head Neck. 37: 1326-35.

Citations 1 to 10 of 42 total

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. MG-132 [Z-Leu-Leu-Leu-CHO], sc-201270, is a crystalline solid.
Answered by: Chemical Support 4
Date published: 2017-03-15
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Rated 5 out of 5 by from Good quality Good quality, worked well in cell culture studies.
Date published: 2015-10-16
Rated 5 out of 5 by from Ye Ye, X. et al. (PubMed 24722419) used MG-132 [Z-Leu-Leu-Leu-CHO], a potent, reversible and selective proteasome inhibitor, to confirm the involvement of ubiquitin-proteasome pathway in miR-21 mediated desmin degradation. MG-132 eliminated the effect of miR-21 on desmin downregulation, indicating that miR-21 promotes desmin degradation through the ubiquitin-proteasome pathway. -SCBT Publication Review
Date published: 2015-06-18
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