CMPD101-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECMPD101Cat.No.:HY-103045CASNo.:865608-11-3分⼦式:C₂₄H₂₁F₃N₆O分⼦量:466.46作⽤靶点:PKC;ROCK作⽤通路:Epigenetics;TGF-beta/Smad;CellCycle/DNADamage;Cytoskeleton;StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(535.95mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1438mL10.7190mL21.4381mL5mM0.4288mL2.1438mL4.2876mL10mM0.2144mL1.0719mL2.1438mL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。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.46mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.46mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.46mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CMPD101⼀种⾼效、⾼选择性、膜透性的GRK2/3⼩分⼦抑制剂，IC50分别为18nM和5.4nM。CMPD101针对GRK1、GRK5ROCK-2和PKCα的选择性较⼩，IC50值分别为3.1μM，2.3μM，1.4μM和8.1μM。CMPD101可⽤于⼼衰疾病的研究。IC50&TargetGRK2GRK3PKCαROCK218nM(IC50)5.4nM(IC50)8.1μM(IC50)1.4μM(IC50)体外研究CMPD101(100μM;pre-20mins)inhibittheinternalizationofβ2AR,remarkablydecreasestheisoproterenol-inducedformationofclathrin-coatedvesiclesandtheβ2AR-GFPfusionproteinremainedontheplasmamembraneinHEK-B2cellline[1].CMPD101(3-30μM;pre-30minutes)producedarobustphosphorylationofSer375,whichispartiallyinhibitedbypretreatmentofcellsfor30minuteswith3μMCmpd101andfullyblockedbypretreatmentwith30μMCmpd101.ItalsoinhibitsphosphorylationofMOPratThr370,Thr376,andThr379residues[2].CMPD101(3-30μM;pre-30minutes)doesnotaffecttheDAMGO-inducedincreaseinERK1/2andElk-1phosphorylation,at30μM,thiscompoundproducesasmallincreaseinbasalERK1/2phosphorylationinHEK293cellsexpressingHA-MOPrs[2].WesternBlotAnalysis[2]CellLine:HEK293cellsstablyexpressingHA-taggedratMOPrConcentration:3μM,30μMIncubationTime:Pre-30minutesResult:SurpressedSer375expressioncompletelyatahighdose.WesternBlotAnalysis[2]CellLine:HEK293cellsstablyexpressingHA-taggedratMOPrConcentration:3μM,30μMIncubationTime:Pre-30minutesResult:HadnoeffectonDAMGO-inducedp-ERK1/2andp-Elk-1expression.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•JExpClinCancerRes.2020Jun9;39(1):107.•IntJMolSci.2022,23(16),8903.•Biomolecules.2022,12(3),426.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].OkawaT,etal.Design,Synthesis,andEvaluationoftheHighlySelectiveandPotentG-Protein-CoupledReceptorKinase2(GRK2)InhibitorforthePotentialTreatmentofHeartFailure.JMedChem.2017Aug24;60(16):6942-6990.[2].YuQ,etal.InhibitionofprostaticsmoothmusclecontractionbytheinhibitorofGprotein-coupledreceptorkinase2/3,CMPD101.EurJPharmacol.2018Jul15;831:9-19.McePdfHeightCaution:Producthasnotbeenf