SKL2001-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESKL2001Cat.No.:HY-101085CASNo.:909089-13-0分⼦式:C₁₄H₁₄N₄O₃分⼦量:286.29作⽤靶点:Wnt;β-catenin作⽤通路:StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥96.66mg/mL(337.63mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4930mL17.4648mL34.9296mL5mM0.6986mL3.4930mL6.9859mL10mM0.3493mL1.7465mL3.4930mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(8.73mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.73mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性SKL2001Wnt/β-catenin信号通路的激动剂，具有抗肿瘤活性。SKL2001通过破坏Axin/β-catenin相互作⽤，稳定细胞内β-catenin。IC50&TargetWnt/β-catenin[1]体外研究SKL2001isanagonistoftheWnt/β-cateninpathway,andalsoupregulatestheexpressionofAxin2,adownstreamtargetoftheWnt/β-cateninpathway,butshowsnoeffectonNF-κB,p53reporteractivityandGSK-3βactivity.SKL2001causesosteoblastdifferentiation(20and40μM)andsuppressespreadipocytedifferentiation(5,10,and30μM)viatheactivationoftheWnt/β-cateninpathway.SKL2001(5,10,and30μM)stabilizesintracellularβ-cateninin3T3-L1cells[1].SKL2001(40μM)significantlyinhibitstheproliferationofHCT116spheroidsindependentlyofcytotoxicityandtheinhibitionisreversible;SKL2001cuasescellcyclearrestinHCT116spheroids.SKL2001(40μM)enhancesround-shapespheroidformationandE-cadherinexpression[2].PROTOCOLCellAssay[1]ST2cellsareculturedonglasschamberslidesandthentreatedwithDMSOorSKL2001for15h.Aftertreatment,thecellsarewashedwithPBS,fixedwith4%formaldehyde,permeabilizedin0.3%TritonX-100,andblockedin4%bovineserumalbuminfor1h.Thecellsarestainedwithanti-β-cateninantibodyandthenanalyzedbyconfocalmicroscopyusingamicroscope[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•JAdvRes.26November2021.•ExpMolMed.2022Sep1.•CellDeathDis.2020Aug18;11(8):644.•BiomedPharmacother.2020Sep;129:110414.•BiomedPharmacother.2019May16;116:108974.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GwakJ,etal.Smallmolecule-baseddisruptionoftheAxin/β-cateninproteincomplexregulatesmesenchymalstemcelldifferentiation.ellRes.2012Jan;22(1):237-47.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].OhashiW,etal.SKL2001suppressescoloncancerspheroidgrowththroughregulationoftheE-cadherin/β-Catenincomplex.BiochemBiophysResCommun.2017Nov25;493(3):1342-1348.McePdfHeightCaution:Producthasnotbeenfullyvalid