DNMDP-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDNMDPCat.No.:HY-W028690CASNo.:328104-79-6分⼦式:C₁₅H₂₀N₄O₃分⼦量:304.34作⽤靶点:Phosphodiesterase(PDE)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:50mg/mL(164.29mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2858mL16.4290mL32.8580mL5mM0.6572mL3.2858mL6.5716mL10mM0.3286mL1.6429mL3.2858mL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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.21mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性DNMDP⼀种PDE3A抑制剂，⼀种⾼效、选择性的肿瘤细胞毒药物。DNMDP与PDE3A结合促进PDE3A与Schlafen12(SLFN12)之间的相互作⽤。DNMDP具有明显的细胞选择性细胞毒性。体外研究DNMDP(0-1000μM;48hours)showsclearcell-selectivecytotoxicity[1].HeLacellsundergoapoptosisuponDNMDPtreatment,indicatesbycaspaseactivitydetectedbyacaspase-sensitiveluciferaseassayandbypolyADPribosepolymerase(PARP)cleavage.Ataconcentrationof100nM,DNMDPspecificallyinhibitsbothPDE3AandPDE3B,weaklyinhibitsPDE10,andhadlittleornodetectableeffectonotherphosphodiesterases[1].CellViabilityAssay[1]CellLine:NCI-H1563,NCI-H2122,HeLa,A549,MCF7,andPC3cellsConcentration:0-1000μMIncubationTime:48hoursResult:ShowedanEC50between10and100nMfortwoadditionallungadenocarcinomacelllines,NCI-H1563andNCI-H2122,andforHeLacervicalcarcinomacells,butanEC50greaterthan1µMforA549,MCF7,andPC3cells.REFERENCES[1].deWaalL,etal.Identificationofcancer-cytotoxicmodulatorsofPDE3Abypredictivechemogenomics.NatChemBiol.2016Feb;12(2):102-8.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel