Enpp-Carbonic-anhydrase-IN-1-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEnpp/Carbonicanhydrase-IN-1Cat.No.:HY-151916CASNo.:2883495-35-8分⼦式:C₂₃H₂₅NO₄S分⼦量:411.51作⽤靶点:Apoptosis;CarbonicAnhydrase;Phosphodiesterase(PDE)作⽤通路:Apoptosis;MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:100mg/mL(243.01mM;ultrasonicandwarmingandheatto50°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4301mL12.1504mL24.3007mL5mM0.4860mL2.4301mL4.8601mL10mM0.2430mL1.2150mL2.4301mL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(6.08mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:2.5mg/mL(6.08mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性Enpp/Carbonicanhydrase-IN-1(compound1e)⼀种有效的Enpp和carbonicanhydrase抑制剂，对NPP1、NPP2、NPP3、CA-II、CA-IX的IC50值分别1.36、1.35、3.00、0.88、1.02μM。Enpp/Carbonicanhydrase-IN-1对癌细胞具有抗增殖活性，对正常细胞具有低细胞毒性。Enpp/Carbonicanhydrase-IN-1诱导细胞凋亡(Apoptosis)[1]。IC50&TargetCAⅡCAⅨNPP1NPP20.88μM(IC50)1.02μM(IC50)1.36μM(IC50)1.35μM(IC50)NPP33.00μM(IC50)体外研究Enpp/Carbonicanhydrase-IN-1(compound1e)(0-100µM;)inhibitssomecancercellsgrowthwithIC50sof0.32,0.40,0.58,0.87,0.40,0.96µMforK-562,RPMI-8226,SR,COLO205,HT-29,SF-539cells,respectively[1].Enpp/Carbonicanhydrase-IN-1(0-2µM)showslowcytotoxicagainstnormalbreastepithelialcells(HME1)andnormalskinfibroblastcells(F180)withIC50sof>50μM[1].Enpp/Carbonicanhydrase-IN-1(0.32,0.64µM)inducesapoptosisinadose-dependentmanneratK-562cells[1].CellProliferationAssay[1]CellLine:K-562,RPMI-8226,SR,COLO205,HT-29,SF-539cellsConcentration:0-100µMIncubationTime:Result:InhibitedthecellgrowthwithIC50sof0.32,0.40,0.58,0.87,0.40,0.96µMforK-562,RPMI-8226,SR,COLO205,HT-29,SF-539cells,respectively.ApoptosisAnalysis[1]CellLine:K-562cellsConcentration:0.32,0.64µMIncubationTime:Result:Inducedapoptosisinadose-dependentmanner.REFERENCES[1].AfnanI.Shahin,etal.Designandsynthesisofnewadamantylderivativesaspromisingantiproliferativeagents.EuropeanJournalofMedicinalChemistry,2022.McePdfHeigtCaution:Producthasnotbeenfullyvalidatedformedicalapplications.hF