OSS-128167-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOSS_128167Cat.No.:HY-107454CASNo.:887686-02-4分?式:C??H??N?O?分?量:366.32作?靶點(diǎn):Sirtuin;HBV作?通路:CellCycle/DNADamage;Epigenetics;Anti-infection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:103.3mg/mL(281.99mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7299mL13.6493mL27.2985mL5mM0.5460mL2.7299mL5.4597mL10mM0.2730mL1.3649mL2.7299mL請根據(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?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.68mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.68mM);ClearsolutionBIOLOGICALACTIVITY?物活性O(shè)SS_128167?種有效的選擇性沉默調(diào)節(jié)蛋?6(SIRT6)抑制劑，對SIRT6，SIRT1和SIRT2的IC50分別為89μM，1578μM和751μM。OSS_128167具有抗HBV活性，可抑制HBV的轉(zhuǎn)錄和復(fù)制。OSS_128167具有抗癌，抗炎和抗病毒作?。IC50&TargetSIRT6SIRT2SIRT1HBV89μM(IC50)751μM(IC50)1578μM(IC50)體外研究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.體內(nèi)研究OSS_128167(50mg/kg;intraperitonealinjection;every4days;for12days;maleHBVtransgenicmice)treatmentmarkedlysuppressesthelevelofHBVDNAand3.5-KbRNAinHBVtransgenicmice[2].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:MaleHBVtransgenicmice(6-8-week-old)[2]Dosage:50mg/kgAdministration:Intraperitonealinjection;every4days;for12daysResult:ThelevelofHBVDNAand3.5-KbRNAweremarkedlysuppressedinHBVtransgenicmice.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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