DMU2139-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDMU2139Cat.No.:HY-101285CASNo.:1821143-80-9分⼦式:C₁₉H₁₅NO₂分⼦量:289.33作⽤靶点:CytochromeP450作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:77.5mg/mL(267.86mM;Needultrasonic)Ethanol:5mg/mL(17.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4563mL17.2813mL34.5626mL5mM0.6913mL3.4563mL6.9125mL10mM0.3456mL1.7281mL3.4563mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.58mg/mL(8.92mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.58mg/mL(8.92mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性DMU2139有效的特异性细胞⾊素P4501B1(CYP1B1)的抑制剂，其对CYP1B1和CYP1A1的IC50值分别为9nM，795nM。IC50&TargetCYP1B1CYP1A19nM(IC50)795nM(IC50)体外研究DMU2139(6j)shows88and133-foldselectivityforCYP1B1overCYP1A1andCYP1A2.InthepresenceofDMU2139,theEC50isreversedbackto8.3μMfrom61μM(seeninCYP1B1-expressingcellswithoutanyinhibitor).TheEC50value,inthepresenceofDMU2139,resemblestheEC50ofcisplatin,8.7μM,incellstransfectedwiththeemptyplasmidwhichhasnoCYP1B1geneandthereforecannotexpressCYP1B1protein[1].REFERENCES[1].HorleyNJ,etal.DiscoveryandcharacterizationofnovelCYP1B1inhibitorsbasedonheterocyclicchalcones:OvercomingcisplatinresistanceinCYP1B1-overexpressinglines.EurJMedChem.2017Mar31;129:159-174.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8