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PARP&Proteasome

MG132 (133407-82-6)

MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 and 1.2 μM for the inhibition of proteasome and calpain, respectively…

Not Intended for Therapeutic Use. For research use only.

CAS: 133407-82-6 Category

MG132 (133407-82-6) Description:

MG132 is a specific, potent, reversible, and cell-permeable proteasome inhibitor (Ki = 4 nM) . It reduces the degradation of ubiquitin-conjugated proteins in mammalian cells and permeable strains of yeast by the 26S complex without affecting its ATPase or isopeptidase activities. MG132 activates c-Jun N-terminal kinase (JNK1), which initiates apoptosis. MG132 also inhibits NF-κB activation with an IC50 of 3 µM and prevents β-secretase cleavage. MG-132 induces MCPIP1 expression; induces C6 glioma cell apoptosis via oxidative stress; induces AIF nuclear translocation through down-regulation of ERK and Akt/mTOR pathway.

MG-132 displays >1000 times more activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of 20S proteasome with IC50 of 100 nM versus 110 μM. MG-132 also inhibits calpain with IC50 of 1.2 μM. MG-132 induces neurite outgrowth in PC12 cells at an optimal concentration of 20 nM, displaying 500 times more potency than ZLLal.

MG132 (133407-82-6) Specifications:

Product Name MG132
Synonyms MG-132; MG 132.
Chemical Name L-LeucinaMide, N-[(phenylMethoxy)carbonyl]-L-leucyl-N-[(1S)

-1-forMyl-3-Methylbutyl]-;MG 132 Calpain inhibitor IV-2; benzyl((S)-4-Methyl-1-(((S)-4-Methyl-1-(((S)-4-Methyl-1-oxopentan-2-yl)aMino)-1-oxopentan-2-yl)aMino)-1-oxopentan-2-yl)carbaMate;

Purity ≥98% (HPLC)
CAS Number 133407-82-6
Molecular Formula C26H41N3O5
Molecular Weight 475.63 g/mol
Monoisotopic Mass 475.305 g/mol
MDL number MFCD00674886
InChIKey TZYWCYJVHRLUCT-VABKMULXSA-N
InChi Code 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
SMILES O=C(OCC1=CC=CC=C1)N[[email protected]@H](CC(C)C)C(N[[email protected]@H](CC(C)C)C(N[[email protected]@H](CC(C)C)C=O)=O)=O
Form Powder
Color White
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0-4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life ≥ 2 years
Handling Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Provide appropriate exhaust ventilation at places where dust is formed
Application A proteasome and NF-κB inhibitor.

 


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RIDADR NONH for all modes of transport

References:

  • Sunkaria, Aditya; Bhardwaj, Supriya; Yadav, Aarti; Halder, Avishek; Sandhir, Rajat. Sulforaphane attenuates postnatal proteasome inhibition and improves spatial learning in adult mice. Journal of Nutritional Biochemistry 2018 vol. 51 p. 69 – 79.
  • Banerjee and Liefshitz (2001) Potential of the proteasome inhibitor MG-132 as an anticancer agent, alone and in combination. Anticancer Res. 21 3941 PMID: 11911275
  • Wang Y, Sun W, Du B, Miao X, Bai Y, Xin Y, Tan Y, Cui W, Liu B, Cui T, Epstein PN, Fu Y, Cai L. Therapeutic effect of MG-132 on diabetic cardiomyopathy is associated with its suppression of proteasomal activities: roles of Nrf2 and NF-κ Am J Physiol Heart Circ Physiol. 2013 Feb 15;304(4):H567-78. doi: 10.1152/ajpheart.00650.2012. Epub 2012 Dec 7. PubMed PMID: 23220333.
  • Luo, Dan; Dong, Xi-Wen; Yan, Bing; Liu, Mei; Xue, Tian-Hui; Liu, Hui; You, Jun-Hao; Li, Fang; Wang, Zi-Ling; Chen, Zhi-Nan. MG132 selectively upregulates MICB through the DNA damage response pathway in A549 cells – Molecular Medicine Reports 2019 vol. 19 # 1 p. 213 – 220.
  • Hosseini SM, Hajian M, Forouzanfar M, Ostadhosseini S, Moulavi F, Ghanaei HR, Gourbai H, Shahverdi AH, Vosough AD, Nasr-Esfahani MH. Chemically assisted somatic cell nuclear transfer without micromanipulator in the goat: effects of demecolcine, cytochalasin-B, and MG-132 on the efficiency of a manual method of oocyte enucleation using a pulled Pasteur pipette. Anim Reprod Sci. 2015 Jul;158:11-8. doi: 10.1016/j.anireprosci.2015.04.002. Epub 2015 Apr 15. PubMed PMID: 25956201.

1 review for MG132 (133407-82-6)

  1. Cofttek

    Never had such good experience before,The MG132 (133407-82-6) is high purity,also customer service is pretty nice !gotta try!!

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