K00546-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEK00546Cat.No.:HY-103647CASNo.:443798-47-8分⼦式:C₁₅H₁₃F₂N₇O₂S₂分⼦量:425.44作⽤靶点:CDK;VEGFR;GSK-3作⽤通路:CellCycle/DNADamage;ProteinTyrosineKinase/RTK;PI3K/Akt/mTOR;StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(235.05mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3505mL11.7525mL23.5051mL5mM0.4701mL2.3505mL4.7010mL10mM0.2351mL1.1753mL2.3505mL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，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性K00546⼀种有效的CDK1和CDK2抑制剂，对CDK1/cyclinB和CDK2/cyclinA的IC50分别为0.6nM和0.5nM。K00546也⼀种有效的CDC2样激酶1(CLK1)和CLK3抑制剂，IC50分别为8.9nM和29.2nM。IC50&TargetCdk1/cyclinBcdk2/cyclinACLK1CLK30.6nM(IC50)0.5nM(IC50)8.9nM(IC50)29.2nM(IC50)1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEVEGF-R2GSK-332nM(IC50)140nM(IC50)体外研究K00546bindstotheSLKATP-bindingsiteformingthreehydrogenbondswiththekinasehingeresiduesE109andC111.ThesulphamoylmoietyofK00546alsointeractswiththemainchainofL40[1].K00546(compound3n)alsoinhibitsPKA,caseinkinase-1,MAPkinase(ERK-2),calmodulinkinase,VEGF-R2,GSK-3andPDGF-RβwithIC50valuesof5.2μM,2.8μM,1.0μM,8.9μM,0.032μM,0.14μMand1.6μM,respectively[2].REFERENCES[1].AshleyCWPike,etal.Activationsegmentdimerization:amechanismforkinaseautophosphorylationofnon-consensussites.EMBOJ.2008Feb20;27(4):704-14.[2].OlegFedorov,etal.SpecificCLKinhibitorsfromanovelchemotypeforregulationofalternativesplicing.ChemBiol.2011Jan28;18(1):67-76.[3].RonghuiLin,etal.1-Acyl-1H-[1,2,4]triazole-3,5-diamineanaloguesasnovelandpotentanticancercyclin-dependentkinaseinhibitors:synthesisandevaluationofbiologicalactivities.JMedChem.2005Jun30;48(13):4208-11.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: