Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemETubulin/LSD1-IN-1Cat.No.:HY-176283分子式:C??H??N?O?S?分子量:644.81作用靶點(diǎn):Microtubule/Tubulin;HistoneDemethylase;Apoptosis;Wee1;Bcl-2Family;Caspase作用通路:CellCycle/DNADamage;Cytoskeleton;Epigenetics;Apoptosis儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Tubulin/LSD1-IN-1是一種有效的微管蛋白聚合和LSD1(IC50=1.72μM)雙重抑制劑。Tubulin/LSD1-IN-1對癌細(xì)胞系有廣譜抗增殖活性。Tubulin/LSD1-IN-1通過靶向秋水仙堿結(jié)合位點(diǎn)抑制微管蛋白聚合，從而破壞胃癌細(xì)胞中的微管網(wǎng)絡(luò)。Tubulin/LSD1-IN-1可提高H3K4me1/2和H3K9me2/3的甲基化水平，從而實(shí)現(xiàn)表觀遺傳調(diào)控。Tubulin/LSD1-IN-1誘導(dǎo)G2/M期阻滯、促進(jìn)細(xì)胞凋亡(Apoptosis)，有效地抑制胃癌細(xì)胞的集落形成[1]。IC50&TargetCaspase-3Caspase-7體外研究Tubulin/LSD1-IN-1(CompoundL-6)(10-60nM,12-48h)hasadose-andtime-dependentinhibitoryeffectonMGC-803andHGC-27cells,inhibitsthelong-termproliferationofgastriccancercells,andhaslowtoxicitytoGES-1cells[1].Tubulin/LSD1-IN-1(48h)hasanIC50oflessthan100nMagainstvariouscancercells(IC50:MGC-803=33nM,HGC-27=49nM,HTC-116=38nM,KYSE-450=48nM)[1].Tubulin/LSD1-IN-1(10-60nM,24-48h)regulatesthecellcycleinMGC-803andHGC-27cells,inhibitsmicrotubulepolymerization,andarrestscellsintheG2/Mphase[1].Tubulin/LSD1-IN-1(20-60nM,48h)inducessignificantmorphologicalchangesandapoptosisinMGC-803andHGC-27cells[1].Tubulin/LSD1-IN-1(10-60nM,48h)caneffectivelysuppressesthedemethylationoftheH3K4me1/2andH3K9me2/3inMGC-803andHGC-27cells[1].CellViabilityAssay[1]CellLine:MGC-803cells,HGC-27cells,GES-1cells1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEConcentration:10nM,20nM,30nM,40nM,60nMIncubationTime:12h,24h,36h,48hResult:Graduallyinhibitedcellviabilitytolessthan50%at48hoursinMGC-803andHGC-27cells.HadanIC50of300nMforGES-1cells.CellCycleAnalysis[1]CellLine:MGC-803cells,HGC-27cellsConcentration:10nM,20nM,30nM,40nM,60nMIncubationTime:24hResult:IncreasedsignificantlytheproportionofcellsintheG2/Mphase(MGC-803:increasedfrom26.04%to66.88%;HGC-27:increasedfrom43.77%to56.23%).ApoptosisAnalysis[1]CellLine:MGC-803cells,HGC-27cellsConcentration:20nM,30nM,40nM,60nMIncubationTime:48hResult:Causedcellsizereduction,nuclearfragmentation,andincreasedcelldeath.Showedapoptoticratesofcellstreatedwith40nMand60nMas73.0%(MGC-803cells)and42.66%(HGC-27cells),respectively.Immunofluorescence[1]CellLine:MGC-803cells,HGC-27cellsConcentration:20nM,30nM,40nM,60nMIncubationTime:24hResult:Causedthemicrotubulenetworktofragmentandaccumulateintheperinuclearregion,consistentwiththeactionofcolchicine.WesternBlotAnalysis[1]CellLine:MGC-803cells,HGC-27cellsConcentration:10nM,20nM,30nM,40nM,60nMIncubationTime:48h2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEResult:DownregulatedCyclinA1/2,CyclinB1,p-CDC2(Thr14/161),andWee1amongthecellcycle-relatedproteins;andupregulatedp-HistoneH3.UpregulatedcleavedCaspase-3/7andcleavedPARPamongapoptosis-relatedproteins;downregulatedBcl-2.REFERENCESJianweiJi,etal.Discoveryofnovel1,2,3-triazolearylamidederivativesbearingdithiocarbamatemoietyasdualinhibitorsoftubulinandLSD1withpotentanticanceractivity.EurJMedChem.2025Oct15.296:117879.McePdfHeightCaution:Producthasnotbee