Purvalanol-A-NG-60-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPurvalanolACat.No.:HY-18299ACASNo.:212844-53-6Synonyms:NG-60分?式:C??H??ClN?O分?量:388.89作?靶點:CDK;Autophagy;Apoptosis作?通路:CellCycle/DNADamage;Autophagy;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥50mg/mL(128.57mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5714mL12.8571mL25.7142mL5mM0.5143mL2.5714mL5.1428mL10mM0.2571mL1.2857mL2.5714mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.43mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.43mM);ClearsolutionBIOLOGICALACTIVITY?物活性PurvalanolA?種有效的CDK抑制劑，對cdc2-cyclinB，cdc2-cyclinB，cdk2-cyclinE，cdk4-cyclinD1和cdk5-p35的IC50值分別為4，70，35，850和75nM。IC50&Targetcdc2-cyclinBcdk2-cyclinEcdk2-cyclinAcdk4-cyclinD14nM(IC50)35nM(IC50)70nM(IC50)850nM(IC50)cdk5-p35erk175nM(IC50)9000nM(IC50)體外研究PurvalanolAinhibitscdc28(S.cerevisiae)anderk1withIC50sof80and9000nM.PurvalanolAshowsinhibitoryactivitiesagainsttheNCIpanelof60humantumorcelllines,withaverageGI50of2μM;twocelllinesshowan-20-foldincreaseinsensitivitytopurvalanolA:theKM12coloncancercelllinewithaGI50of76nMandtheNCI-H522non–smallcelllungcancercelllinewithaGI50of347nM[1].PurvalanolAisa2.5-foldmorepotentinhibitorofCDK2,butalsoinhibitsDYRK1Apotentlyandanumberofotherproteinkinasesinthelowmicromolarrange.PurvalanolAinhibitsMKK1,MAPK2/ERK2,JNK/SAPK1cwithIC50sof80,26,84μM[2].PurvalanolAselectivelyinhibitsthephosphorylationofcellularproteins.PurvalanolApreventstheincreasesofthecontentsofcyclinsDandEduringserum-inducedG1phaseprogression.PurvalanolAdoesnotinhibittranscriptionundercell-freeconditions[3].戶使?本產(chǎn)品發(fā)表的科研?獻?EMBORep.2022Apr11;e53932.?iScience.2019May31;15:291-306.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GrayNS,etal.Exploitingchemicallibraries,structure,andgenomicsinthesearchforkinaseinhibitors.Science.1998Jul24;281(5376):533-8.[2].BainJ,etal.Thespecificitiesofproteinkinaseinhibitors:anupdate.BiochemJ.2003Apr1;371(Pt1):199-204.[3].VillerbuN,etal.CellulareffectsofpurvalanolA:aspecificinhibitorofcyclin-dependentkinaseactivities.IntJCancer.2002Feb20;97(6):761-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform