Geldanamycin-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEGeldanamycinCat.No.:HY-15230CASNo.:30562-34-6分?式:C??H??N?O?分?量:560.64作?靶點:HSP;Bacterial;InfluenzaVirus;Antibiotic作?通路:CellCycle/DNADamage;MetabolicEnzyme/Protease;Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥24mg/mL(42.81mM)掃描?維碼，H2O:<0.1mg/mL(insoluble)運?溶解?案計算器*"≥"meanssoluble,butsaturationunknown.獲得適合您實驗體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7837mL8.9184mL17.8368mL5mM0.3567mL1.7837mL3.5674mL10mM0.1784mL0.8918mL1.7837mL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備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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%DMSO40%PEG3005%Tween-8045%salineSolubility:2.17mg/mL(3.87mM);Suspendedsolution;Needultrasonic此?案可獲得2.17mg/mL(3.87mM)的均勻懸濁液，懸濁液可?于?服和腹腔注射。以1mL?作液為例，取100μL21.7mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。1/3www.MedChemEwww.MedChemE2.請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:2.17mg/mL(3.87mM);Suspendedsolution;Needultrasonic此?案可獲得2.17mg/mL(3.87mM)的均勻懸濁液，懸濁液可?于?服和腹腔注射。以1mL?作液為例，取100μL21.7mg/mL的澄DMSO儲備液加到900μL20%的SBE-β-CD?理鹽??溶液中，混合均勻。BIOLOGICALACTIVITY?物活性GeldanamycinHsp90抑制劑，具有抗許多?蘭?陽性和?些?蘭?性細(xì)的活性。Geldanamycin還具有抗流感病毒H5N1的活性。IC50&TargetHSP901.2μM(Kd)體外研究Geldanamycinsignificantlydelaysandreducesviperinexpression,indicatingthatIRF3isinvolvedinviperininductioninRAW264.7cells[1].Geldanamycin(GA),abenzoquinoneansamycin,protectedagainstneuronalinjuryinducedbyoxygen-glucosedeprivation(OGD)/zVADtreatmentinculturedprimaryneurons.Moreimportantly,GeldanamycindecreasesRIP1proteinlevelinatimeandconcentration-dependentmanner.GeldanamycinalsodecreasestheHsp90proteinlevel,whichcausesinstabilityofRIP1protein,resultingindecreasedRIP1proteinlevelbutnotRIP1mRNAlevelafterGeldanamycintreatment[2].Geldanamycin(GA)isidentifiedasthefirstnaturalproductinhibitorofHsp90thatbindstotheN-terminalATPasedomainofHsp90toinhibititschaperonefunction,andsignificantlyinducestumorcelldeathviaanapoptoticmechanism[3].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NucleicAcidsRes.2020Aug20;48(14):7944-7957.?CellSyst.2018Apr25;6(4):424-443.e7.?JCellBiochem.2019Sep;120(9):16254-16263.?JCellBiochem.2018Oct10.?MolImmunol.2020Nov;127:230-237.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].TangHB,etal.ViperininhibitsrabiesvirusreplicationviareducedcholesterolandsphingomyelinandisregulatedupstreambyTLR4.SciRep.2016Jul26;6:30529[2].ChenWW,etal.RIP1mediatestheprotectionofGeldanamycinonneuronalinjuryinducedbyoxygen-glucosedeprivationcombinedwithzVADinprimarycorticalneurons.JNeurochem.2012Jan;120(1):70-7.[3].LinZ,etal.17-ABAG,anovelGeldanamycinderivative,inhibitsLNCaP-cellproliferationthroughheatshockprotein90inhibition.IntJMolMed.2015Aug;36(2):424-32.[4].RoeSM,etal.StructuralbasisforinhibitionoftheHsp90molecularchaperonebytheantitumorantibioticsradicicolandgeldanamycin.J2/3www.MedChemEwww.MedChemEMedChem.1999Jan28;42(2):260-6.[5].WangC,etal.GeldanamycinReducesAcuteRespiratoryDistressSyndromeandPromotestheSurvivalofMiceInfectedwiththeHighlyVirulentH5N1InfluenzaVirus.FrontCellInfectMicrobiol.2017Jun15;7:267.McePdfHeight關(guān)注MCE中國公眾號，

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