Laccaic-acid-A-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELaccaicacidACat.No.:HY-124326CASNo.:15979-35-8分⼦式:C₂₆H₁₉NO₁₂分⼦量:537.43作⽤靶点:DNAMethyltransferase作⽤通路:Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性LaccaicacidA⼀种⼝服有效的DNA甲转移酶1(Dnmt1)的DNA竞争型抑制剂(Ki=310nM;IC50=650nM)。LaccaicacidA⽐SG-1027(HY-13962)对Dnmt1的抑制效⼒更强。LaccaicacidA与Phenethylisothiocyanate联合对结直肠癌有强协同作⽤。IC50&TargetDNMT1DNMT1650nM(IC50)310nM(Ki)体外研究LaccaicacidA(200μM)alterstheexpressionofmethylatedgenesinMCF-7breastcancercellssynergisticallywith0.5μMDecitabine(HY-A0004)[1][1].LaccaicacidA(0.01-100μM;24h,48h,and72h)inhibitshumancoloncarcinomaHT29growthwithanIC50valueof6.08μMfor72h-treatment[2].LaccaicacidA(6.08μM)inducescellapoptosisandarrestscellcycleatsub-G1phaseinHT29[2].体内研究LaccaicacidA(50mg/kg,100mg/kg,and200mg/kg;p.o.;oncedailyfor21d)improvesthecoloncarcinomamodelinrats[2].AnimalModel:HealthySpragueDawleyrats[2]Dosage:50mg/kg,100mg/kg,and200mg/kgAdministration:Oralgavage;oncedailyfor21daysResult:SignificantlyreducedthetissuelevelsofDnmt1,HDAC1,andcytokinesIL-6andTNF-1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEalphaat200mg/kgdose.REFERENCES[1].FaganRL,etal.LaccaicacidAisadirect,DNA-competitiveinhibitorofDNAmethyltransferase1.JBiolChem.2013Aug16;288(33):23858-67.[2].GuptaR,etal.PotentantitumoractivityofLaccaicacidandPhenethylisothiocyanatecombinationincolorectalcancerviadualinhibitionofDNAmethyltransferase-1andHistonedeacetylase-1.ToxicolApplPharmacol.2019Aug15;377:114631.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-379