SPI-112-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESPI-112Cat.No.:HY-101964CASNo.:1051387-90-6分⼦式:C₂₂H₁₇FN₄O₅S分⼦量:468.46作⽤靶点:Phosphatase作⽤通路:MetabolicEnzyme/Protease储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:50mg/mL(106.73mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1347mL10.6733mL21.3465mL5mM0.4269mL2.1347mL4.2693mL10mM0.2135mL1.0673mL2.1347mL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(protectfromlight)。-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。BIOLOGICALACTIVITY⽣物活性SPI-112⼀种有效的，选择性和竞争性的SHP2(PTPN11)抑制剂，对SHP2，蛋⽩酪氨酸磷酸酶(PTP)和PTP1B的IC50分别为1μM，18.3μM和14.5μM。IC50&TargetIC50:1μM(SHP2),18.3μM(PTP)and14.5μM(PTP1B)[2]体外研究SPI-112hasapolar-NO2oranegativelycharged-COOHgroupandhasnodetectablecellularactivity,1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEsuggestingthatSPI-112isnotcellpermeable[1].Insurfaceplasmonresonance(SPR)bindingassay,SPI-112displaysa1:1stoichiometricbindingkineticstoSHP2withakineticconstantKDof1.30µM.EnzymekineticdataobtainedwithSPI-112arebestfittedwiththecompetitiveinhibitionmodel(Kiof0.8µM),suggestingthatSPI-112interactswiththecatalyticsiteofSHP2[1].REFERENCES[1].ChenL,etal.InhibitionofcellularShp2activitybyamethylesteranalogofSPI-112.BiochemPharmacol.2010Sep15;80(6):801-10.[2].LawrenceHR,etal.InhibitorsofSrchomology-2domaincontainingproteintyrosinephosphatase-2(Shp2)basedonoxindolescaffolds.JMedChem.2008Aug28;51(16):4948-56.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;