ProductDescription
YO-01027(Dibenzazepine,DBZ)isadipeptidicg-secretaseinhibitorwithIC50of2.6and2.9nMforAPPLandNotch,respectively.YO-01027targetsthePresenilinfragment.IncreasingconcentrationsofYO-01027admiNISTeredtoAPPl-orNotch-expressingcellsleadstotheprogressiveaccumulationofAPPLC-terminalfragmentsandadecreaseinNICDproductioninadose-dependentmanner.[1]
Inaninvitromodelofhumancornealandconjunctivalepithelialcelldifferentation,YO-01027impairedMUC16biosynthesisinaconcentration-dependentmanner.[2]
Inoncologymodels,YO-01027preferentiallyinhibitedNotchandsignificantlydecreasedMCF7tumorsandincreasedlatencycomparedwithcontrolmice.[3]
Technicalinformation:
| ChemicalFormula: | C26H23F2N3O3 | |
| CAS#: | 209984-56-5 | |
| MolecularWeight: | 463.48 | |
| Purity: | >98% | |
| Appearance: | White | |
| ChemicalName: | 7-(S)-[N"(3,5-difluorophenylacetyl)-L-alaninyl]amino-5-methyl-5,7-dihydro-6H-dibenz[b,d]azepin-6-one | |
| Solubility: | Upto100mMinDMSO | |
| Synonyms: | YO-01027,YO01027,Dibenzazepine,DeshydroxyLY411575 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Grothetal.,PharmacologicalAnalysisofDrosophilamelanogasterg-SecretasewithRespecttoDifferentialProteolysisofNotchandAPP.Mol.Pharmacol.2010,77(4),567-574.PubmedID:20064975 |
| 2. | Xiongetal.,NotchSignalingModulatesMUC16BiosynthesisinanInVitroModelofHumanCornealandConjunctivalEpithelialCellDifferentiation.Invest.Ophthalmol.Vis.Sci.2011,52(8),5641-5646.PubmedID:21508102 |
| 3. | Harrisonetal.,RegulationofBreastCancerStemCellActivitybySignalingthroughtheNotch4Receptor.CancerRes.,2010,70,709-718.PubmedID:20068161 |
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