SPI-112-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESPI-112Cat.No.:HY-101964CASNo.:1051387-90-6分?式:C??H??FN?O?S分?量:468.46作?靶點(diǎn):Phosphatase作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(106.73mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1347mL10.6733mL21.3465mL5mM0.4269mL2.1347mL4.2693mL10mM0.2135mL1.0673mL2.1347mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性SPI-112?種有效的，選擇性和競(jìng)爭(zhēng)性的SHP2(PTPN11)抑制劑，對(duì)SHP2，蛋?酪氨酸磷酸酶(PTP)和PTP1B的IC50分別為1μM，18.3μM和14.5μM。IC50&TargetIC50:1μM(SHP2),18.3μM(PTP)and14.5μM(PTP1B)[2]體外研究SPI-112hasapolar-NO2oranegativelycharged-COOHgroupandhasnodetectablecellularactivity,1/2MasterofBioactiveMolecules—您?邊的抑制劑?師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;