Valproic-acid-sodium-salt-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEValproicacidsodiumsaltCat.No.:HY-10585ACASNo.:1069-66-5分⼦式:C₈H₁₅NaO₂分⼦量:166.19作⽤靶点:HDAC;Autophagy;Mitophagy;HIV;Notch作⽤通路:CellCycle/DNADamage;Epigenetics;Autophagy;Anti-infection;NeuronalSignaling;StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months

-20°C1month溶解性数据体外实验H2O:≥48mg/mL(288.83mM)扫描⼆维码，*"≥"meanssoluble,butsaturationunknown.运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM6.0172mL30.0860mL60.1721mL5mM1.2034mL6.0172mL12.0344mL10mM0.6017mL3.0086mL6.0172mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性Valproicacidsodiumsalt(SodiumValproate)⼀种HDAC抑制剂，IC50值为0.5-2mM，抑制HDAC1的活性，(IC50，400μM)，同时可诱导HDAC2的降解。Valproicacidsodiumsalt激活Notch1信号并抑制⼩细胞肺癌(SCLC)细胞的增殖。Valproicacidsodiumsalt可⽤于癫痫、双相情感障碍和偏头痛等的研究。IC50&TargetHDAC1HDACHDAC2Autophagy400μM(IC50)0.5-2mM(IC50)1/4www.MedChemEwww.MedChemEMitophagy体外研究Valproicacidsodiumsalt(SodiumValproate)inhibitsthegrowthdose-andtime-dependentlywithanIC50ofappr10and4mMat24and72h,respectively.Valproicacidsodiumsaltsignificantlyattenuatestheactivitiesoftotal,cytosolandnuclearHDACs.Valproicacidsodiumsaltincreasestheformofacetylatedhistone3inHeLacells.Valproicacidsodiumsalt(1-3mM)inducesaG1phasearrest,while10mMValproicacidsodiumsaltsignificantlyinducesaG2/MphasearrestofcellcycleinHeLacells.Inaddition,Valproicacidsodiumsaltincreasesthepercentageofsub-G1cellsinHeLacellsinadose-dependentmannerat24h[1].ValproicacidsodiumsaltinhibitsthemRNAandproteinexpressionofVEGF,VEGFR2andbFGF.ValproicacidsodiumsaltinhibitstheproteinexpressionofHDAC1,increaseshistoneH3acetylation,andenhancestheaccumulationofhyperacetylatedhistoneH3onVEGFpromoters[2].ValproicacidsodiumsalttreatmentresultsinincreasedlevelsofphosphorylatedAMPK/ACCinprimarymousehepatocytes.PhosphorylationofACCfollowingValproicacidsodiumsalttreatmentisAMPK-dependent.ValproicacidsodiumsaltinhibitsthedeacetylaseactivityofbothmouselivernuclearextractsandhumanrecombinantHDAC1whileofthemetabolitesofValproicacid,only2-ene-Valproicacidand4-ene-Valproicaciddiminishdeacetylaseactivity[4].体内研究Valproicacidsodiumsalt(SodiumValproate;500mg/kg,i.p.)inhibitsthetumorgrowthandangiogenesisinthemicetransplantedwithKasumi-1cells.TheIRrateintheValproicacidsodiumsaltgroupis57.25%attheendoftheexperiment[2].Valproicacidsodiumsalt(350mg/kg,i.p.)demonstratesmoresocialinvestigationandplayfightingthancontrolanimals[3].PROTOCOLKinaseAssay[1]Theactivityofcaspase-3,-8and-9isassessedusingthecaspase-3,-8and-9colorimetricassaykits,respectively.Inbrief,1×106cellsina60-mmculturedishareincubatedwith10mMValproicacidfor24h.ThecellsarethenwashedinPBSandsuspendedin5volumesoflysisbufferprovidedwiththekit.ProteinconcentrationsaredeterminedusingtheBradfordmethod.Supernatantscontaining50μgtotalproteinareusedtodeterminecaspase-3,-8and-9activities.Thesupernatantsareaddedtoeachwellin96-wellmicrotiterplateswithDEVD-pNA,IETD-pNAorLEHD-pNAascaspase-3,-8and-9substratesandtheplatesareincubatedat37°Cfor1h.Theopticaldensityofeachwellismeasuredat405nmusingamicroplatereader.Theactivityofcaspase-3,-8and-9isexpressedinarbitraryabsorbanceunits.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.CellAssay[1]Inbrief,5×105cellsareseededin96-wellmicrotiterplatesforMTTassays.AfterexposuretothedesignateddosesofValproicacidfortheindicatedtimes,MTTsolution[20mL:2mg/mLinphosphate-bufferedsaline(PBS)]isaddedtoeachwellofthe96-wellplates.Theplatesareadditionallyincubatedfor3hat37°C.Mediumiswithdrawnfromtheplatesbypipettingand200mLDMSOisaddedtoeachwelltosolubilizetheformazancrystals.Theopticaldensityismeasuredat570nmusingamicroplatereader.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalSplenectomiesareperformedontheBALB/cnudemice.Oneweekafterthesplenectomies,themicereceiv2/4www.MedChemEwww.MedChemEAdministration[2]wholebodyirradiationwith137Csatadoseof4Gy.At48-72hpost-irradiation,themicearesubcutaneouslyimplantedwithKasumi-1cells(2×107cells/mousewith0.15-0.2mL)intherightaxillaryregion.ThemicearerandomLyassignedtotwogroups,theValproicacid(n=6)andcontrol(n=6)groups.Whenthetumorsareappr200mm3insizeatappr10dayspost-implantation,0.2mLValproicacid(500mg/kgbodyweight)or0.2mLsalineisinjectedintraperitoneallyeveryday.Valproicacidisdissolvedinsalineataconcentrationof25mg/mL.Thelongestdiameter(a)andtheshortestdiameter(b)ofthetumoraremeasuredeverythreedays,andthetumorvolume(TV)iscalculatedaccordingtothefollowingformula:TV=1/2×a×b2.Followingtwoweeksofinjections,themicearesacrificedbycervicaldislocationandthetumormassesareremovedforthefollowingexperiments.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Biomaterials.2018Dec6;193:30-46.•Oncogene.2021Mar12.•SciTotalEnviron.2021,147014.•ActaPharmacolSin.2020Jun17.•SciRep.2020Sep16;10(1):15201.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HanBR,etal.ValproicacidinhibitsthegrowthofHeLacervicalcancercellsviacaspase-dependentapoptosis.OncolRep.2013Dec;30(6):2999-3005.[2].ZhangZH,etal.ValproicacidinhibitstumorangiogenesisinmicetransplantedwithKasumi1leukemiacells.MolMedRep.2013Nov28.[3].CohenOS,etal.Acuteprenatalexposuretoamoderatedoseofvalproicacidincreasessocialbehaviorandaltersgeneexpressioninrats.IntJDevNeurosci.2013Dec;31(8):740-50.[4].AveryLB,etal.ValproicAcidIsaNovelActivatorofAMP-ActivatedProteinKinaseandDecreasesLiverMass,HepaticFatAccumu