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Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENicotinamideHydrochlorideCat.No.:HY-B0150ACASNo.:25334-23-0Synonyms:NiacinamideHydrochloride;NicotinicacidamideHydrochloride分?式:C?H?ClN?O分?量:158.59作?靶點(diǎn):Sirtuin;EndogenousMetabolite作?通路:CellCycle/DNADamage;Epigenetics;MetabolicEnzyme/Protease儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性NicotinamideHydrochloride維?素B3或煙酸的?種形式,可抑制SIRT2的體外活性,其EC50值為2μM。NicotinamideHydrochloride可抑制90%的??素瘤細(xì)胞數(shù)量,并增加細(xì)胞內(nèi)NAD+、ATP、ROS?平。NicotinamideHydrochloride抑制??素瘤??的腫瘤?長(zhǎng)并提??存率,可?于??素瘤等?膚癌相關(guān)的研究[1]。IC50&TargetHumanEndogenousMetaboliteSIRT22μM(EC50)體外研究NicotinamideHydrochloride(0-50mM,24/48h)reducescellnumberinatime-dependentanddose-dependentmannerinA375andSK-MEL-28cells[1].NicotinamideHydrochloride(10-50mM,24h)makesA375cellsundergoaccumulationinG1phase,reductioninSphase,andincreaseinthesub-G1(apoptosis)phase[1].NicotinamideHydrochloride(1-50mM,6h)increasesNAD+,ATPandROSlevelsinA375andSK-MEL-28cells[1].NicotinamideHydrochloride(0.01-20mM,1h)inhibitspurifiedSIRT2enzymaticactivityinvitrowithanEC50of2μM[1].CellViabilityAssay[1]CellLine:A375,SK-MEL-28,mouseB16-F10cellConcentration:0,1,20,50mMIncubationTime:24h,48h1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Reducedcellnumberinadose-dependentmannerwithastronginhibitoryeffectat20mMandanalmostcompleteeffectat50mM.CellCycleAnalysis[1]CellLine:A375,SK-MEL-28Concentration:10,20,50mMIncubationTime:24hResult:ArrestedA375cellsinG1phase.體內(nèi)研究NicotinamideHydrochloride(Intraperitonealinjection,1500and1800mg/Kg,5daysperweek)inhibitstumorgrowthinmurinemetastaticmelanomamodel[1].NicotinamideHydrochloride(Intraperitonealinjection,1800mg/Kg,onceaday,murinemetastaticmelanomamodel)affectsIFN-γ(akeymediatorofcell-mediatedanti-tumorimmunity),increasestheplasmalevelsofeotaxinandIL-5,reducestheplasmalevelsofIL-3,IL-12,RANTESandIL-10[1].AnimalModel:C57BL/6mice(subcutaneousinjectedwithB16-F10cells)[1]Dosage:1000,1500,1800mg/Kg.Administration:Intraperitonealinjection,5daysperweek(followedby2-dayrest)oronceaday.Result:Inhibitedtumorgrowthat1500and1800mg/Kg,andhadnoeffectonthebodyweight.IncreasedthefrequencyofIFN-γproducingcellsandmodulatedtheproteinlevelsofcytokinesandchemokinesintheplasmaoftumor-bearingmice.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellStemCell.2022Sep1;29(9):1366-1381.e9.?NatCommun.2021Sep20;12(1):5548.?NatCommun.2021Jul9;12(1):4227.?Autophagy.2020Oct;16(10):1823-1837.?Theranostics.2019Apr13;9(9):2424-2438.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].[1]FrancescaScatozza,etal.Nicotinamideinhibitsmelanomainvitroandinvivo.JExpClinCancerRes.2020Oct7;39(1):211.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidate

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