Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECMPD101Cat.No.:HY-103045CASNo.:865608-11-3分?式:C??H??F?N?O分?量:466.46作?靶點(diǎn):PKC;ROCK作?通路:Epigenetics;TGF-beta/Smad;CellCycle/DNADamage;Cytoskeleton;StemCell/Wnt儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(535.95mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1438mL10.7190mL21.4381mL5mM0.4288mL2.1438mL4.2876mL10mM0.2144mL1.0719mL2.1438mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.46mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.46mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.46mM);ClearsolutionBIOLOGICALACTIVITY?物活性CMPD101?種?效、?選擇性、膜透性的GRK2/3?分?抑制劑，IC50分別為18nM和5.4nM。CMPD101針對(duì)GRK1、GRK5ROCK-2和PKCα的選擇性較?，IC50值分別為3.1μM，2.3μM，1.4μM和8.1μM。CMPD101可?于?衰疾病的研究。IC50&TargetGRK2GRK3PKCαROCK218nM(IC50)5.4nM(IC50)8.1μM(IC50)1.4μM(IC50)體外研究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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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