
Description | Inauhzinisacell-permeableSIRT1inhibitorwithanIC50of0.7-2μMandreactivatesp53byinhibitingSIRT1deacetylationactivity. | ||
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Targets |
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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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