High-affinityinhibitorofE3ubiquitinligaseVHL(Kd =80-90nM).BlocksinteractionbetweenVHLandHIF-αdownstreamofHIF-αhydroxylation,initiatinghypoxicresponse.Resultsintime-andconcentration-dependentaccumulationofhydroxylatedHIF-α,andupregulatesmRNAandproteinlevelsofHIFtargetgenes.Cellpermeable.
Application
High-affinityinhibitorofVHL
ProductInformation
Purity: >98%
MW: 523.65
Formula: C27H33N5O4S
CASNo. 2097381-85-4
PhysicalState: Lyophilizedwhitepowder
Quantity: 5mg;10mg;25mg
Solubility: 50mg/mLinDMSO;50mg/mLinEthanol
Storage: Storedesiccatedassuppliedat-20°Cforupto3years.Storesolutionsat-80°Cforupto6monthsor-20°Cforupto1month.
Documents
References
1. Frost etal (2015)PotentandselectivechemicalprobeofhypoxicsignallingdownstreamofHIF-αhydroxylationviaVHLinhibition.Nat.Commun. 7 13312PMID: 27811928
2. Soares etal (2018)Group-basedoptimizationofpotentandcell-activeinhibitorsofthevonHippel-Lindau(VHL)E3ubiquitinligase:structure-activityrelationshipsleADIngtothechemicalprobe(2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3J.Med.Chem. 61 599PMID: 28853884
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那糖酵解中依赖NAD的酶不是要在线粒体内反应?
蛋白酶分布广泛,主要存在于人和动物消化道中,而消化道通过口与肛门与外界相通,属于外环境或外界环境
(溶菌酶、凝血酶原等)分布在内环境
(消化)酶分布在消化道

