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Selleckchem/Inauhzin/S6744

DescriptionInauhzinisacell-permeableSIRT1inhibitorwithanIC50of0.7-2μMandreactivatesp53byinhibitingSIRT1deacetylationactivity.
Targets
SIRT1[2]()p53[1]()
Invitro

Inauhzin(INZ)isapotentp53activatorandmediatesp53-dependentcytotoxicity.INZinhibitscellproliferationbytriggeringbothapoptosisandsenescenceinp53-containningcells,thoughitpredominantlyinducesp53-dependentapoptosis.INZisabletopreventp53fromMDM2-mediatedubiquitylationandproteasomaldegradationandprotectsp53withouteitherdirectlyinhibitingMDM2activitytowardsp53orinterferingwithMDMX/MDM2–p53interaction.INZinducesacetylationofp53,butnottubulin,incells[1].Inauhzinisa(sub)micromolarSIRT1iselectiveoverSIRT2/3[2].

Invivo

Inauhzin(INZ)hasgoodtumourtissuepenetrationandisabletoinhibittumourgrowthbyinducingp53[1].

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