V-11-0711-hydrochloride-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEV-11-0711hydrochlorideCat.No.:HY-120337A分⼦式:C₂₇H₃₆ClNO₃分⼦量:458.03作⽤靶点:CholineKinase;Apoptosis作⽤通路:NeuronalSignaling;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性V-11-0711(hydrochloride)⼀种强效且选择性的Chk-α抑制剂(IC50=20nM)。V-11-0711(hydrochloride)可显著降低PCho⽔平。V-11-0711(hydrochloride)可引起可逆性⽣长停滞。⾼浓度V-11-0711(hydrochloride)可诱导细胞凋亡(apoptosis)。V-11-0711(hydrochloride)可⽤于宫颈癌和三性乳腺癌的研究[1][2]。IC50&TargetChk-α20nMnM(IC50)体外研究V-11-0711(0.1-10μM,48h)(hydrochloride)reducesPCandGPClevelsinMDA-MB-231cellsandSUM149cells[2].V-11-0711(0.1-10μM,48h)(hydrochloride)doesnotreduceChk-αproteinlevelsinSUM149cellsatlowdoses,butreducesChk-αproteinlevelsbyapproximately50%athighdoses[2].V-11-0711(0.1-10μM,48h)(hydrochloride)significantlyreducesthelevelofPtdChoinSUM149cells,andincreasesfattyacidlevelsat10μM[2].V-11-0711(0.1-10μM,48h)(hydrochloride)increasesthenumberoflipiddropletsinSUM149cellsbyapproximately1.8timesat10μM[2].V-11-0711(0.1-10μM,48h)(hydrochloride)inducesapoptosisinSUM149cellsat10μM[2].WesternBlotAnalysis[2]CellLine:SUM149cells,MDA-MB-231cellsConcentration:0.1μM,1μM,10μMIncubationTime:48h1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:DidnotreduceChk-αproteinlevelsinSUM149cellsatlowdoses,butreducedChk-αproteinlevelsbyapproximately50%athighdoses.InMDA-MB-231,Chk-αproteinlevelsdidnotdecrease;infact,theyshowedaslightupwardtrend.REFERENCES[1].FalconSC,etal.Anon-catalyticroleofcholinekinasealphaisimportantinpromotingcancercellsurvival.Oncogenesis.2013;2(3):e38.[2].MoriN,etal.Cholinekinase-αproteinandphosphatidylcholinebutnotphosphocholinearerequiredforbreastcancercellsurvival.NMRBiomed.2015Dec;28(12):1697-706.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: