K00546-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEK00546Cat.No.:HY-103647CASNo.:443798-47-8分?式:C??H??F?N?O?S?分?量:425.44作?靶點:CDK;VEGFR;GSK-3作?通路:CellCycle/DNADamage;ProteinTyrosineKinase/RTK;PI3K/Akt/mTOR;StemCell/Wnt儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(235.05mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3505mL11.7525mL23.5051mL5mM0.4701mL2.3505mL4.7010mL10mM0.2351mL1.1753mL2.3505mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性K00546?種有效的CDK1和CDK2抑制劑，對CDK1/cyclinB和CDK2/cyclinA的IC50分別為0.6nM和0.5nM。K00546也?種有效的CDC2樣激酶1(CLK1)和CLK3抑制劑，IC50分別為8.9nM和29.2nM。IC50&TargetCdk1/cyclinBcdk2/cyclinACLK1CLK30.6nM(IC50)0.5nM(IC50)8.9nM(IC50)29.2nM(IC50)1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEVEGF-R2GSK-332nM(IC50)140nM(IC50)體外研究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: