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InhibitorofRacfamilyGTPases.BlocksactivationbydirectbindingtoRac1,Rac1b,Rac2andRac3(KDvaluesare40,50,60and250nMrespectively).InhibitsRac,RasandTiam-inducedgrowthtransformationofNIH-3T3fibroblasts.Reducesβ-amyloidpeptideproductioninvivo.
SoldforresearchuseonlyunderlicensefromExonHitTherapeuticsS.A.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight581.47.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Desireetal(2005)RAC1inhibitiontargetsamyloidprecursorproteinprocessingbyγ-secretaseanddecreasesAβproductioninvitroandinvivo.J.Biol.Chem.28037516PMID:16150730
Shutesetal(2007)SpecificityandmechanismofactionofEHT1864,anovelsmallmoleculeinhibitorofracfamilysmallGTPases.J.Biol.Chem.28235666PMID:17932039
Onestoetal(2008)CharacterizationofEHT1864,anovelsmallmoleculeinhibitorofRacfamilysmallGTPases.MethodsEnzymol.439111PMID:18374160
Keywords:EHT1864,supplier,Rac-GEF,interaction,antioncogenic,G,Proteins,Small,transformation,Rac1,Rac1b,Rac2,Rac3,Ras,Tiam,inhibits,inhibitors,GTPases,EHT1864,G,Proteins,(Small),GTPase,G,Proteins,(Small),TocrisBioscience
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