Vorinostat-SAHA-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVorinostatCat.No.:HY-10221CASNo.:149647-78-9Synonyms:SAHA;Suberoylanilidehydroxamicacid分?式:C??H??N?O?分?量:264.32作?靶點(diǎn):HDAC;Autophagy;Mitophagy;Filovirus;Apoptosis;HPV作?通路:CellCycle/DNADamage;Epigenetics;Autophagy;Anti-infection;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥100mg/mL(378.33mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.7833mL18.9165mL37.8329mL5mM0.7567mL3.7833mL7.5666mL10mM0.3783mL1.8916mL3.7833mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.87mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.87mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.87mM);Clearsolution4.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.87mM);Clearsolution5.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.87mM);Clearsolution6.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.87mM);Clearsolution7.請(qǐng)依序添加每種溶劑：20%HP-β-CDinsalineSolubility:3.33mg/mL(12.60mM);Clearsolution;Needultrasonic8.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(9.46mM);Clearsolution9.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.46mM);ClearsolutionBIOLOGICALACTIVITY?物活性Vorinostat(SAHA)?種有效的，可?服的HDAC1，HDAC2，HDAC3(ClassI)，HDAC6和HDAC7(ClassII)和ClassIV(HDAC11)的抑制劑，對(duì)HDAC1/3的ID50值分別為10nM和20nM。Vorinostat可以誘導(dǎo)細(xì)胞凋亡(apoptosis)。Vorinostat還?種?類乳頭瘤病毒(HPV)-18DNA擴(kuò)增的有效抑制劑。IC50&TargetHDAC1HDAC3HDAC2HDAC710nM(ID50)20nM(ID50)HDAC11AutophagyMitophagy體外研究VorinostatefficientlysuppressesMES-SAcellgrowthatalowdosage(3μM)alreadyafter24hourstreatment.HDACsclassI(HDAC2and3)aswellasclassII(HDAC7)arepreferentiallyaffectedbythistreatment.Vorinostatsignificantlyincreasesp21WAF1expressionandapoptosisinMES-SAcells[1].VorinostatinhibitsSK-N-SHandSK-N-Be(2)CwiththeIC25valuesof1μMand0.5μM,respectively[2].VorinostatisaneffectiveinhibitorofHPV-18DNAamplification,reducesoncoproteinsE6andE7activitiesandtriggersapoptosisinHPV-infected,differentiatedcells[7].體內(nèi)研究Vorinostat(50mg/kg/day)reducestumorgrowthbymorethan50%innudemiceinjectedwith5×106MES-SAcells[1].PROTOCOL2/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellAssay[1]CelllysatesarepreparedbyusingRIPAbuffer(25mMTris-HClpH7.6,150mMNaCl,1%NP-40,1%sodiumdeoxycholate,0.1%SDS),andtheproteinconcentrationisdeterminedbyBio-RadDCProteinAssay.ProteinlysatesareseparatedbySDSandtransferredtonitrocellulosemembrane.Followingantibodiesanddilutionsareused:rabbitantiHDAC1(1μg/mL);rabbitantiHDAC2(1μg/mL);rabbitantiHDAC3(9μg/mL);rabbitantiHDAC7(3μg/mL);mouseantip21WAF1(0.5μg/mL).Assecondaryantibodies,therabbitanti-mouseandswineanti-rabbitHRP-coupledantibodiesatafinalconcentrationof1μg/mL.Anovernightincubationat4°Cisusedforallprimaryantibodies,followedbywashingand2-hoursincubationatRTwithsecondaryantibodies.Specificproteinbandsarevisualizedbyenhancedchemiluminescenceassay.Todemonstrateequalloadingofproteinsamplesallwesternblotsareprobedforβ-tubulin.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalTwelveweeksoldmalemice(n=14)areanesthetizedwithIsofluranand5×106MES-SAcellsareinjectedAdministration[1]subcutaneouslyintotherightflankoftheanimal.Micefromacontrolgroupreceivesplacebocontaining300μLofemptyHOP-β-CD(2-hydroxypropyl-β-cyclodextrin)vesicles.AnothergroupofmicereceivesvorinostatdissolvedinHOP-β-CDataconcentrationof50mg/kg/day.Both,emptyvesiclesandvorinostatareadministeredintraperitoneally,startingontheday4aftertheinjectionofMES-SAtumorcells.Micebodyweightandtumorsize(w2×l×0.52;measuredbycaliper)areestimatedtwiceaweek.Allmicearetreatedfor21daysandafterwardssacrificedbycervicaldislocation.Eachtumorisisolatedasawholeanddifferenttumorparametersaredetermined.Finally,tumorslicesarecryopreservedandformalinfixed(4%)forfurtheranalyses.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?MilMedRes.2022Sep27;9(1):54.?NatCommun.2021Mar3;12(1):1407.?NatCommun.2017Dec20;8(1):2207.?JExpMed.2022Jan3;219(1):e20210789.?ActaPharmSinB.21July2021.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HrzenjakAetal.Histonedeacetylaseinhibitorvorinostatsuppressesthegrowthofuterinesarcomasinvitroandinvivo.MolCancer.2010Mar4;9:49.[2].LautzTB,etal.TheeffectofvorinostatonthedevelopmentofresistancetoNSC123127inneuroblastoma.PLoSOne.2012;7(7):e40816.[3].RichonVM,etal.Aclassofhybridpolarinducersoftransformedcelldifferentiationinhibitshistonedeacetylases.ProcNatlAcadSciUSA.1998Mar17;95(6):3003-7.[4].XuWS,etal.Histonedeacetylaseinhibitors:molecularmechanismsofaction.Oncogene.2007Aug13;26(37):5541-52.[5].Pérez-Ca?amásA,etal.Sphingomyelin-inducedinhibitionoftheplasmamembranecalciumATPasecausesneurodegenerationintype