KN-93-phosphate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKN-93phosphateCat.No.:HY-15465BCASNo.:1913269-12-1分⼦式:C₂₆H₃₂ClN₂O₈PS分⼦量:599.03作⽤靶点:CaMK;Autophagy作⽤通路:NeuronalSignaling;Autophagy储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:100mg/mL(166.94mM;Needultrasonic)H2O:50mg/mL(83.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6694mL8.3468mL16.6937mL5mM0.3339mL1.6694mL3.3387mL10mM0.1669mL0.8347mL1.6694mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:≥10mg/mL(16.69mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥10mg/mL(16.69mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥10mg/mL(16.69mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性KN-93钙离⼦/钙调蛋⽩依赖激酶II（CaMKII）抑制剂，能竞争性阻断钙调蛋⽩与对应激酶的结合，Ki为370nM。IC50&TargetKi:370nM(CaMK-II)体外研究After2daysofKN-93treatment,95%ofcellsarearrestedinG1.G1arrestisreversible;1dayafterKN-93release,apeakofcellshadprogressedintoSandG2-M.KN-93alsoblockscellgrowthstimulatedbybasicfibroblastgrowthfactor,platelet-derivedgrowthfactor-BB,andepidermalgrowthfactorinNIH3T3fibroblasts[1].KN-93inhibitstheH+,K+-ATPaseactivitybutstronglydissipatestheprotongradientformedinthegastricmembranevesiclesandreducesthevolumeofluminalspace[2].KN-93(0.5μM)preventsincreasedLVdevelopedpressureduringactionpotentialprolongationandearlyafterdepolarizations.Ca2+-independentCaMkinaseactivityisincreasedduringearlyafterdepolarizationsandthisincreaseispreventedbyKN-93[3].户使⽤本产品发表的科研⽂献•Cell.2022Jun23;185(13):2354-2369.e17.•NatCommun.2022Jul22;13(1):4255.•CellSyst.2018Apr25;6(4):424-443.e7.•RedoxBiol.October2021,102115.•SciTotalEnviron.2020Feb10;703:134702.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TombesRM,etal.G1cellcyclearrestandapoptosisareinducedinNIH3T3cellsbyKN-93,aninhibitorofCaMK-II(themultifunctionalCa2+/CaMkinase).CellGrowthDiffer.1995Sep;6(9):1063-70.[2].MamiyaN,etal.InhibitionofacidsecretioningastricparietalcellsbytheCa2+/calmodulin-dependentproteinkinaseIIinhibitorKN-93.BiochemBiophysResCommun.1993Sep15;195(2):608-15.[3].AndersonME,etal.KN-93,aninhibitorofmultifunctionalCa++/calmodulin-dependentproteinkinase,decreasesearlyafterdepolarizationsinrabbitheart.JPharmacolExpTher.1998Dec;287(3):996-1006.[4].LiJ,etal.CurcuminAttenuatesRetinalVascularLeakagebyInhibitingCalcium/Calmodulin-DependentProteinKinaseIIActivityinStreptozotocin-InducedDiabetes.CellPhysiolBiochem.2016;39(3):1196-208.McePdfHeihtCaution:Producthasnotbeenfully