Laccaic-acid-A-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELaccaicacidACat.No.:HY-124326CASNo.:15979-35-8分?式:C??H??NO??分?量:537.43作?靶點(diǎn):DNAMethyltransferase作?通路:Epigenetics儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性LaccaicacidA?種?服有效的DNA甲轉(zhuǎn)移酶1(Dnmt1)的DNA競(jìng)爭(zhēng)型抑制劑(Ki=310nM;IC50=650nM)。LaccaicacidA?SG-1027(HY-13962)對(duì)Dnmt1的抑制效?更強(qiáng)。LaccaicacidA與Phenethylisothiocyanate聯(lián)合對(duì)結(jié)直腸癌有強(qiáng)協(xié)同作?。IC50&TargetDNMT1DNMT1650nM(IC50)310nM(Ki)體外研究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].體內(nèi)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?邊的抑制劑?師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