ProductDescription
MG-132isatriterpene,peptide-aldehydeproteasomeinhibitorderivedfromaChinesemedicinalplant.Itinhibits20Sproteasomeactivtybycovalentlybindingtotheactivesiteofthebetasubunitsandeffectivelyblockstheproteolyticactivityofthe26Sproteasomecomplex.Throughtheformationofreactiveoxygenspecies,MG-132inhibitstumorcellgrowthbyinducingcellcyclearrestandtriggeringapoptosis.[1]
MG-132wasfoundtoenhanceIL-6expressioninHUVEC.MG-132doesnotaffectIkBlevels,suggestingthatproteasomeinhibitiondoesnotinfluencetheNF-kBsystemwithoutanyagoNISTstimulation.Insimilarstudies,MG-132isbelievedtoinhibitthedegradationofphosphorylatedMEK1/2andactivatethedownstreamregionofthissignallingcascade.[2]
InNCIH2452andNCIH2052humanthoracicmalignantpleuralmesothelioma(MPM)celllines,itwasfoudthat0.5uMconcentrationsofMG-132causedsignificantapoptosisasevidencedbyDNAdamage,cleavageofPARPandcaspases3,7,and9.[3]
Technicalinformation:
| ChemicalFormula: | C26H41N3O5 | |
| CAS#: | 133407-82-6 | |
| MolecularWeight: | 475.62 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | benzyl(S)-4-methyl-1-((S)-4-methyl-1-((S)-4-methyl-1-oxopentan-2-ylamino)-1-oxopentan-2-ylamino)-1-oxopentan-2-ylcarbamate | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | MG-132,MG132,Z-LLL-CHO,MG132 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Guoetal.,MG132,aproteasomeinhibitor,inducesapoptosisintumorcells.AsiaPac.J.Oncol.2012,doi:10.1111/j.1743-7563.2012.01535.x |
| 2. | Shibataetal.,ProteasomeinhibitorMG-132enhancestheexpressionofinterleukin-6inhumanumbilicalveinendothelialcells:InvolvementofMAP/ERKkinase.Immunol.CellBiol.2002,80,226-230.PubmedID:12067409 |
| 3. | Yuanetal.,ProteasomeInhibitorMG132InducesApoptosisandInhibitsInvasionofHumanMalignantPleuralMesotheliomaCells.TranslationalOncol.2008,1(3),129-140.PubmedID:18795123 |
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