SKLB325-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESKLB325Cat.No.:HY-139782分⼦式:C₁₂H₁₂N₄O₂分⼦量:244.25作⽤靶点:HistoneDemethylase;Apoptosis作⽤通路:Epigenetics;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:20.83mg/mL(85.28mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.0942mL20.4708mL40.9417mL5mM0.8188mL4.0942mL8.1883mL10mM0.4094mL2.0471mL4.0942mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(8.52mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(8.52mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性SKLB325⼀种JMJD6抑制剂，其结合亲和⼒(KD)值为0.755μM，IC50值为0.7797μM。SKLB325在体内外对巢癌具有抗肿瘤作⽤。SKLB325诱导细胞凋亡(apoptosis)[1]。SKLB325在肾细胞癌(RCC)中表现出显的抗肿瘤功效[2]。体外研究SKLB325suppressesovariancancergrowththroughinhibitionofproliferationandinductionofapoptosisandcelldeath,andinhibitingangiogenesismayplayasignificantroleininhibitingtumorgrowth[1].SKLB325(0.25-16ꢀμM;for24-72ꢀh)hassignificantinhibitoryeffectsontheinvitroproliferationofovariancancercells.Furthermore,themosteffectiveconcentrationatwhichJMJD6inhibitedSKOV3cellgrowthis4ꢀμM,andtheoptimaldurationofactionis72ꢀh[1].SKLB325upregulatestheexpressionofp53anditsdownstreameffectorsatboththemRNAandproteinlevelsinvitro[1].CellProliferationAssay[1]CellLine:SKOV3,ES2,A2780sandCP70cellsConcentration:0,0.25,0.5,1,2,4,8,and16ꢀμMIncubationTime:24ꢀh,48ꢀh,and72ꢀhResult:WithincreasingSKLB325concentration,theinhibitoryeffectalsoincreased,exhibitingasignificantdose-responserelationship.Therewasasignificantdifferencebetweenthedruggroupacrossdifferentdosesandthecontrolgroup.WesternBlotAnalysis[1]CellLine:SKOV3,ES2andA2780scellsConcentration:4ꢀμMIncubationTime:72ꢀhoursResult:p53,p21,andPUMAproteinlevelsweresignificantlyupregulatedinSKOV3,ES2andA2780scells.体内研究SKLB325(10ꢀmg/kg)hasantitumoractivitiesinanintraperitonealxenograftmodel.SKLB325significantlyprolongsthesurvivaloftumor-bearingmicewithoutobvioussideeffects.SKLB325treatmentprotocolswereeffectiveinsuppressingSKOV3,ES2,CP70,andA2780stumorgrowthinnudemice[1].AnimalModel:FemaleathymicBALB/cnudemice[1]Dosage:10ꢀmg/kgAdministration:I.p.injectionseverythreedaysforeightdosestotal2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Theaverageweightofintraperitonealtumornoduleswas1.56ꢀ±ꢀ0.70,1.04ꢀ±ꢀ0.62,and0.14ꢀ±ꢀ0.11ꢀginthecontrol,vehicleandSKLB325groups,respectively.Tumorweightwassignificantlyreducedby91and86%intheSKLB325groupscomparedtothecontrolandvehiclegroups,respectively.REFERENCES[1].HengZheng,etal.Jumonjidomain-containing6(JMJD6)identifiedasapotentialtherapeutictargetinovariancancer.SignalTransductTargetTher.2019Jul26;4:24.[2].ChuanjieZhang,etal.EpigenomescreeninghighlightsthatJMJD6confersanepigeneticvulnerabilityandmediatessunitinibsensitivityinrenalcellcarcinoma.ClinTranslMed.2021Feb;11(2):e328.McePdfHeightCaution:Product