
Description | BAI1isadirectallostericinhibitorofBAXwithadissociationconstant(Kd)of15.0±4μM. |
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Invitro | BAXactivationinhibitor1(BAI1)demonstratesinhibitionoftBID-inducedBAX-mediatedmembranepermeABIlizationinadosedependentmannerwithanIC50of3.3μM.BAI1bindstomonomericBAXatanovelallostericsite.BAI1isapotentinhibitorofBAXconformationalactivationandoligomerizationinsolution,notbydirectcompetitionwiththeactivator,butratherthroughanallostericmechanismthatfavorstheinactiveBAX.Moreover,BAI1inhibitedBAXmembraneassociationandtranslocationinducedeitherbytBID(IC50=5±1μΜ)orBIMSAHB(IC50=2±1μΜ)inadosedependentmannerandwithasimilarIC50toBAX-mediatedLiposomalrelease.BAI1selectivelyinhibitsBAX-dependentcelldeath[1]. |
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