ST13-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEST13Cat.No.:HY-179654CASNo.:1013620-98-8分⼦式:C₂₁H₁₈N₂O₃分⼦量:346.38作⽤靶点:HDAC;Apoptosis作⽤通路:CellCycle/DNADamage;Epigenetics;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性ST13⼀种邻羟苯胺类化合物，选择性、慢速且紧密结合的HDAC1和HDAC2抑制剂，其IC50值分别为23nM和49nM。ST13对HDAC3(IC50=4.30μM)和HDAC6(IC50>10μM)的抑制作⽤较弱。ST13的诱导契合机制通过两步过程进⾏：⾸先，酶和抑制剂快速形成碰撞复合物(EI)，然后缓慢转化为稳定的复合物E*I。ST13可诱导癌细胞凋亡(apoptosis)。ST13可⽤于⿊⾊素瘤和三性乳腺癌的研究。IC50&TargetHDAC1HDAC2HDAC3HDAC623nM(IC50)49nM(IC50)4300nM(IC50)>10μM(IC50)体外研究ST13(72-120h)exhibitstime-dependentantiproliferativeactivityincancercelllines,withEC50valuesdecreasingfrom2.77µM(72h)to0.311µM(120h)inMV-3cells.InMDA-MB-231,EC50valuesdecreasedfrom4.87µM(72h)to0.087µM(120h)[1].ST13(10µM;48h)significantlyinducesapoptosisinMDA-MB-231cells[1].ST13(5μM,24-72h)showsasubstantialincreaseinacetylatedhistoneH3inMV-3cells[1].InMV-3cells,MDA-MB-231cells,nontumorigeniccelllineHEK293andhematologicalcancercelllineMM.1S,ST13(18h)exhibitsaninhibitoryeffectagainstHDACs,withEC50valuesof0.311μM,0.577μM,0.333μMand0.637μM,respectively[1].ST17(0.040µM,0.072µM;10min)isalight-activatableprodrugofST13withpotentHDAC1/HDAC2inhibitionuponUVirradiation[1].ApoptosisAnalysis[1]CellLine:MDA-MB-2311/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:10µMIncubationTime:48hResult:InducedapoptosisinMDA-MB-231cells.WesternBlotAnalysis[1]CellLine:MV-3cellsConcentration:5µMIncubationTime:24h,48h,72hResult:OnlyledtohyperacetylationofhistoneH3,indicatingselectivitytowardclassIHDACsandtheabsenceofHDAC6inhibitioninacellularenvironment.REFERENCES[1].HoninI,etal.Ortho-Hydroxyanilides:Slow-Acting,SelectiveHistoneDeacetylase1/2InhibitorsSuitableforPhotocagingApplications.ACSPharmacolTranslSci.2025;8(12):4385-4398.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.