MRT00033659-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEMRT00033659Cat.No.:HY-117857CASNo.:1401731-54-1分⼦式:C₁₅H₁₄N₄O分⼦量:266.3作⽤靶点:CaseinKinase;CheckpointKinase(Chk);MDM-2/p53作⽤通路:CellCycle/DNADamage;StemCell/Wnt;Apoptosis储存⽅式:Powder-20°C3years4°C2years*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:83.33mg/mL(312.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7552mL18.7758mL37.5516mL5mM0.7510mL3.7552mL7.5103mL10mM0.3755mL1.8776mL3.7552mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥4.17mg/mL(15.66mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥4.17mg/mL(15.66mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥4.17mg/mL(15.66mM);Clearsolution1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性MRT00033659⼀种有效的⼴谱激酶抑制剂，抑制CK1(对CK1δ：IC50=0.9µM)和CHK1(IC50=0.23µM)。MRT00033659⼀种吡唑并吡啶类似物，可以诱导p53途径活化和E2F-1不稳定。IC50&TargetCKIδChk10.9μM(IC50)0.23μM(IC50)体外研究MRT00033659(5-40µM;48hours)issufficienttosignificantlyreducecellnumberof5µM[1].MRT00033659(1-80µM;48hours)inducessubstantialcelldeathfrom5µM[1].MRT00033659(0.2-80µM;48hours)inducesarobustandsustainedstabilisationofp53,MDM2andp21proteins,aswellasE2F-1destabilisationfrom0.2µMto5µM[1].MRT00033659doesnotinhibitp38αMAPK[1].CellViabilityAssay[1]CellLine:A375cellsConcentration:5,20,40µMIncubationTime:48hoursResult:Significantlyreducedcellnumberof5µM.ApoptosisAnalysis[1]CellLine:A375cellsConcentration:1,5,10,20,40,80µMIncubationTime:48hoursResult:Inducedsubstantialcelldeathfrom5µM.WesternBlotAnalysis[1]CellLine:A375cellsConcentration:0.2,1,5,10,20,40,80µMIncubationTime:48hoursResult:Inducedarobustandsustainedstabilisationofp53,MDM2andp21proteins,aswellasE2F-1destabilisationfrom0.2µMto5µM.REFERENCES2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].HuartAS,etal.ACaseinkinase1/Checkpointkinase1pyrazolo-pyridineproteinkinaseinhibitorasnovelactivatorofthep53pathway.BioorgMedChemLett.2013Oct15;23(20):5578-85.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.