G-quadruplex-ligand-4-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEG-quadruplexligand4Cat.No.:HY-179480分⼦式:C₂₅H₃₀N₄O₂分⼦量:418.53作⽤靶点:DrugDerivative;G-quadruplex;Apoptosis;Telomerase;Ras;Bcl-2Family作⽤通路:Others;CellCycle/DNADamage;Apoptosis;GPCR/GProtein;MAPK/ERKPathway储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性G-quadruplexligand4⼀种⾊原酮衍⽣物，也⼀种⼈端粒酶逆转录酶hTERTG4配体。G-quadruplexligand4会下调hTERT的表达，并对三性乳腺癌(TNBC)细胞系表现出显著的细胞毒性。G-quadruplexligand4可导致S/G2期细胞周期停滞并诱导细胞凋亡(apoptosis)。G-quadruplexligand4会下调hTERT、KRAS和BCL-2的表达。G-quadruplexligand4可⽤于三性乳腺癌的研究。IC50&TargetBcl-2K-RAS体外研究G-quadruplexligand4(Compound17)(72h)inhibitscellviabilityinMDA-MB-231,HCC-1806,MCF-7andHEK-293withIC50valuesof2.5,2.7,5.5and3.3μM[1].G-quadruplexligand4(2.5-10μM;72h)causesG2/SphasecellcyclearrestandinducesapoptosisinMDA-MB-231cells[1].G-quadruplexligand4(2.5-10μM;24h)downregulatestheexpressionofhTERT,KRAS,andBCL-2inMDA-MB-231cells[1].ApoptosisAnalysis[1]CellLine:MDA-MB-231cellsConcentration:2.5μM,5μM,10μMIncubationTime:72hResult:Showedincreasingproportionsofearly-apoptotic(4.9%,9.5%,28.8%)andlate-apoptoticcells(12.1%,17.4%,30.0%)atdifferentconcentrations.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellCycleAnalysis[1]CellLine:MDA-MB-231cellsConcentration:2.5μM,5μM,10μMIncubationTime:72hResult:IncreasedtheproportionofcellsintheSphase(17.5%,23.9%,29.0%)andG2phase(11.1%,16.1%,23.7%).RealTimeqPCR[1]CellLine:MDA-MB-231cellsConcentration:2.5μM,5μM,10μMIncubationTime:24hResult:ShowedsignificantreductionsinmRNAlevelswithKRAS(21-23%),BCL-2(25-30%),andhTERT(40-56%);\rwhereastheexpressionofHRASandc-MYCremainedunchanged.REFERENCES[1].MockPY,etal.Explorationofchromenone-basedligandsasDNAG-quadruplextargetsintriple-negativebreastcancer.BioorgChem.2025;166:109150.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te