HDAC1-IN-12-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHDAC1-IN-12Cat.No.:HY-181010分⼦式:C₂₃H₂₆FN₇O₃分⼦量:467.5作⽤靶点:HDAC;Parasite作⽤通路:CellCycle/DNADamage;Epigenetics;Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性HDAC1-IN-12⼀种恶性疟原⾍(Plasmodiumfalciparum)HDAC1(PfHDAC1)抑制剂，其对恶性疟原⾍的IC50为4.1nM。该抑制剂可抑制PfHDAC1，上调恶性疟原⾍(P.falciparum)寄⽣⾍中组蛋⽩H3的⼄酰化⽔平，下调疟疾⼊侵相关因的表达，并具有良好的安全性特征、改的理化性质和有效的体内抗疟活性。HDAC1-IN-12可⽤于疟疾研究[1]。体外研究HDAC1-IN-12(compound5ac)(72h)potentlyinhibitsP.falciparum3D7growthwithhighselectivityoverhumanHepG2andHEK293Tcells(IC50=4.1nMforP.falciparum3D7,1.5μMforHepG2,15μMforHEK293T)[1].HDAC1-IN-12(72h;6h)retainspotencyagainstmultidrug-resistantP.falciparumstrainsandinhibitsartemisinin-resistantring-stageparasites(IC50=3.9nMforGB4,6nMforCP286,5.3nMfor6267)[1].HDAC1-IN-12(5nM,50nM;3h)increasestheacetylationlevelofP.falciparumhistoneH3[1].HDAC1-IN-12(5-50nM;3h)downregulatesinvasion-relatedgenesandblocksP.falciparumegressanderythrocyteinvasion[1].体内研究HDAC1-IN-12(compound5ac)(30mg/kg;i.p.;daily;4days)exhibitsclearinvivoantimalarialefficacyinBALB/cmicePlasmodiumbergheiANKA-infectedmodel[1].AnimalModel:BALB/cmice(female,6–8weeksold)wereinoculatedwith105P.bergheiANKA\r\nparasite-infectederythrocytesviaintraperitonealinjection(i.p.)on\r\nday0.[1]Dosage:30mg/kgAdministration:i.p.;daily;4days1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Showednodetectableparasitemiauntilday11,withparasitemialevelsremainingmarkedlylowerthantheDMSOcontrolgroup.REFERENCES[1].NiH,etal.Discoveryofγ-TetrahydrocarbolineDerivativesasPlasmodiumfalciparumHistoneDeacetylaseInhibitorsforTreatmentofMalaria.JMedChem.2026Jan22;69(2):1434-1453.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400