OSS-128167-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOSS_128167Cat.No.:HY-107454CASNo.:887686-02-4分⼦式:C₁₉H₁₄N₂O₆分⼦量:366.32作⽤靶点:Sirtuin;HBV作⽤通路:CellCycle/DNADamage;Epigenetics;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:103.3mg/mL(281.99mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7299mL13.6493mL27.2985mL5mM0.5460mL2.7299mL5.4597mL10mM0.2730mL1.3649mL2.7299mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.68mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.68mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性OSS_128167⼀种有效的选择性沉默调节蛋⽩6(SIRT6)抑制剂，对SIRT6，SIRT1和SIRT2的IC50分别为89μM，1578μM和751μM。OSS_128167具有抗HBV活性，可抑制HBV的转录和复制。OSS_128167具有抗癌，抗炎和抗病毒作⽤。IC50&TargetSIRT6SIRT2SIRT1HBV89μM(IC50)751μM(IC50)1578μM(IC50)体外研究OSS_128167(Compound9;100µM;0-24hours;BxPC3cells)treatmentincreasesH3K9acetylation.AndalsoincreasesGLUT-1expressioninBxPC-3cells[1].OSS_128167(Compound9)effectivelybluntsphorbolmyristateacetate(PMA)-inducedTNF-αsecretioninculturedBxPC-3cells.OSS_128167increasesglucoseuptakeincells[1].OSS_128167(100µM;96hours;HepG2.2.15andHepG2-NTCPcells)treatmentsignificantlydecreaseSHBVcoreDNAand3.5-KbRNAlevels.OSS_128167treatmentalsoinhibitshepatitisBsurfaceantigen(HBsAg)andhepatitisBenvelopeantigen(HBeAg)secretions,aswellasHBsAgexpressionincelllysates[2].OSS_128167(200μM)induceschemosensitizationinprimarymultiplemyeloma(MM)cells(NCI-H929),aswellasinmelphalan-resistant(LR-5)anddoxorubicin-resistant(Dox40)MMcelllines[3].WesternBlotAnalysis[1]CellLine:BxPC3cellsConcentration:100µMIncubationTime:0hours,2hours,6hours,18hours,24hoursResult:IncreasedH3K9acetylation.RT-PCR[2]CellLine:HepG2.2.15andHepG2-sodiumtaurocholatecotransportingpolypeptide(NTCP)cellsConcentration:100µMIncubationTime:96hoursResult:SignificantlydecreasedHBVcoreDNAand3.5-KbRNAlevels.体内研究OSS_128167(50mg/kg;intraperitonealinjection;every4days;for12days;maleHBVtransgenicmice)treatmentmarkedlysuppressesthelevelofHBVDNAand3.5-KbRNAinHBVtransgenicmice[2].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:MaleHBVtransgenicmice(6-8-week-old)[2]Dosage:50mg/kgAdministration:Intraperitonealinjection;every4days;for12daysResult:ThelevelofHBVDNAand3.5-KbRNAweremarkedlysuppressedinHBVtransgenicmice.户使⽤本产品发表的科研⽂献•CellBiosci.2021Dec14;11(1):210.•ActaPharmacolSin.2020Dec;41(12):1557-1567.•Phytomedicine.2022Jun13;104:154276.•iScience.2020Aug21;23(8):101431.•FrontPharmacol.2020Mar18;11:264.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ParentiMD,etal.DiscoveryofnovelandselectiveSIRT6inhibitors.JMedChem.2014Jun12;57(11):4796-804.[2].CeaM,etal.EvidenceforaroleofthehistonedeacetylaseSIRT6inDNAdamageresponseofmultiplemyelomacells.Blood.2016Mar3;127(9):1138-50.[3].JiangH,etal.SIRT6Inhibitor,OSS_128167RestrictsHepatitisBVirusTranscriptionandReplicationThroughTargetingTranscriptionFactorPeroxisomeProliferator-ActivatedReceptorsα.FrontPharmacol.2019Oct25;10:1270.McePdfHeightCaution