MolecularWeight: | 332.36 |
Formula: | C17H16N8 |
Purity: | ≥98% |
CAS#: | 1216665-49-4 |
Solubility: | DMSOupto100mM |
ChemicalName: | N2-(1H-benzo[d]imidazol-6-yl)-N4-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine |
Storage: | Powder:4oC1year.DMSO:4oC3month;-20oC1year. |
APY29isahighlypotentandselectivesmallmoleculemodulatorofIRE1α.Underendoplasmicreticulumstress,unfoldedproteinaccumulationleadstoactivationoftheendoplasmicreticulumtransmembranekinase/endoRNase(RNase)IRE1α.IRE1αoligomerizes,autophosphorylatesandinitiatessplicingofXBP1mRNA,thustriggeringtheunfoldedproteinresponse(UPR).Interestingly,APY29occupiesIRE1α"skinaseATP-bindingsitetoactivateRNase-mediatedXBP1mRNAsplicingevenwithoutupstreamendoplasmicreticulumstress.Itdose-dependentlyreducesIRE1αkinaseautophosphorylationinvitrowithIC50~0.28µM.AsdysregulationoftheUPRhasbeenimplicatedinavarietyofcelldegenerativeandneoplasticdisorders,smallmoleculemodulatorsofIRE1α,suchasAPY29,serveasusefultoolstounderstandtheUPR"sroleinpathophysiologyandtodevelopdrugsforendoplasmicreticulumstress-relateddiseases.
HowtoUse:
Invitro:APY29wasusedat2-20µMinvitroandincellularassays.
Invivo:n/a
Reference:
- 1.WangL,etal.DivergentallostericcontroloftheIRE1αendoribonucleaseusingkinaseinhibitors.(2012)NatChemBiol.8(12):982-9.
- 2.KorennykhAV,etal.Theunfoldedproteinresponsesignalsthroughhigh-orderassemblyofIre1.(2009)Nature.457(7230):687-93.
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