Quisinostat-dihydrochloride-JNJ-26481585-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEQuisinostatdihydrochlorideCat.No.:HY-15433ACASNo.:875320-31-3Synonyms:JNJ-26481585dihydrochloride分⼦式:C₂₁H₂₈Cl₂N₆O₂分⼦量:467.39作⽤靶点:HDAC;Apoptosis;Autophagy作⽤通路:CellCycle/DNADamage;Epigenetics;Apoptosis;Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:41.67mg/mL(89.15mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1395mL10.6977mL21.3954mL5mM0.4279mL2.1395mL4.2791mL10mM0.2140mL1.0698mL2.1395mLBIOLOGICALACTIVITY⽣物活性Quisinostatdihydrochloride(JNJ-26481585dihydrochloride)⼀种有⼝服活性，⾼效的pan-HDAC抑制剂，对HDAC1，HDAC2，HDAC4，HDAC10，HDAC11的IC50值分别为0.11nM，0.33nM，0.64nM，0.46nM和0.37nM。Quisinostatdihydrochloride具有⼴泛的抗肿瘤活性[1]。IC50&TargetHDAC1HDAC2HDAC11HDAC100.11nM(IC50)0.33nM(IC50)0.37nM(IC50)0.46nM(IC50)HDAC5HDAC8HDAC3HDAC93.69nM(IC50)4.26nM(IC50)4.86nM(IC50)32.1nM(IC50)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEHDAC6HDAC776.8nM(IC50)119nM(IC50)体外研究JNJ-26481585inhibitsHDACisozymesinvitro[1].JNJ-26481585(30-1000nM;24hours)isapotentpan-HDACinhibitorintumorcells[1].JNJ-26481585hasbroadspectrumantiproliferativeactivityagainstsolidandhematologiccancercelllinesandinducesapoptosis[1].WesternBlotAnalysis[1]CellLine:HumanA2780ovariancarcinomacellsConcentration:30nM,100nM,300nM,1000nMIncubationTime:24hoursResult:InducedH3andH4acetylationatconcentrationsaslowas30to100nM.体内研究JNJ-26481585(40mg/kg;p.o.;oncedaily,for3days)asapotentHDAC1inhibitorp21waf1,cip1ZsGreentumorsinvivo[1].JNJ-26481585inducescontinuousH3acetylationintumortissueinvivo[1].JNJ-26481585(10mg/kg;oncedaily;i.p.;for14days)stronglyinhibitsthegrowthoflargepre-establishedHCT116colonxenografts[1].AnimalModel:NMRInudemice,withHCT116coloncarcinomacellsxenografts[1]Dosage:10mg/kgAdministration:Intraperitonealinjection,oncedaily,for14daysResult:Stronglyinhibitedthegrowthoflargepre-establishedHCT116colonxenografts.户使⽤本产品发表的科研⽂献•Theranostics.2019Jan30;9(4):1096-1114.•ExpHematolOncol.2019Nov15;8:30.•ToxicolApplPharmacol.2021Jan1;410:115363.•TheFacultyForChemieAndPharmazie,Albert-ludwigs-universityOfFreiburg.2019Dec.•Patent.US20180263995A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ArtsJ,etal.JNJ-26481585,anovel"second-generation"oralhistonedeacetylaseinhibitor,showsbroad-spectrumpreclinical2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEantitumoralactivity.ClinCancerRes.2009Nov15;15(22):6841-51.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala