MHY1485-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMHY1485Cat.No.:HY-B0795CASNo.:326914-06-1分?式:C??H??N?O?分?量:387.39作?靶點(diǎn):mTOR;Autophagy作?通路:PI3K/Akt/mTOR;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗DMSO:7.69mg/mL(19.85mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic)(insoluble)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5814mL12.9069mL25.8138mL5mM0.5163mL2.5814mL5.1628mL10mM0.2581mL1.2907mL2.5814mL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；?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。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實(shí)驗請根據(jù)您的實(shí)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(shí)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(shí)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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥0.77mg/mL(1.99mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥0.77mg/mL(1.99mM);Clearsolution3.請依序添加每種溶劑：20%HP-β-CDinsalineSolubility:1mg/mL(2.58mM);Suspendedsolution;Needultrasonic4.請依序添加每種溶劑：50%PEG300>>50%salineSolubility:5mg/mL(12.91mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性MHY1485?種有效的細(xì)胞滲透性mTOR激活劑，靶向mTOR的ATP結(jié)構(gòu)域。MHY1485通過抑制?噬體和溶酶體之間的融合來抑制?噬(autophagy)。IC50&TargetmTORC1mTORC2Autophagy體外研究MHY1485(10μM;4hours)showsthatGCDC-inducedautophagicactivityisinhibitedbyupregulatingp-mTORexpressionanddownregulatingLC3andp62expressioninHCCcells[1].MHY1485(5μM;6hours)increasestheLC3II/LC3Iratioinadoseandtime-dependentlymannerduetopresumablyinhibitedLC3IIdegradationinratliverAc2Fcells[2].MHY1485(0.5-2μM;6hours)increasesthephosphorylationofmTORatser2448andupregulatesthelevelofphosphorylationof4E-BP1inadose-dependentlymannerinAc2Fcells[2].WesternBlotAnalysis[1]CellLine:HCCcellsConcentration:10μMIncubationTime:4hoursResult:Upregulatedp-mTORanddownregulatedLC3andp62expression.體內(nèi)研究MHY1485(intraperitonealinjection;10?mg/kg,2days)blockstheautophagysignalinginducedbyfollicle-stimulatinghormone(FSH).Itincreasesp-mTORandp-S6K1expressionlevels,whereasLC3expressionshowsnomarkedchangecomparedtothatinthecontrolgroup[3].AnimalModel:4-week-oldfemaleICRmice[3]Dosage:10?mg/kg,2daysAdministration:IntraperitonealinjectionResult:SuppressedtheautophagylevelfollowingFSHtreatment.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?JInfect.2019Sep;79(3):262-276.?BoneRes.2022Jun22;10(1):45.?RedoxBiol.2022Aug4;55:102426.?CancerLett.2020Jan28;469:481-489.?CellDeathDis.2022Jun20;13(6):557.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GaoL,etal.GlycochenodeoxycholatepromoteshepatocellularcarcinomainvasionandmigrationbyAMPK/mTORdependentautophagyactivation.CancerLett.2019Jul10;454:215-223.[2].ChoiYJ,etal.InhibitoryeffectofmTORactivatorMHY1485onautophagy:suppressionoflysosomalfusion.PLoSOne.2012;7(8):e43418.[3].ZhouJ,etal.Administrationoffollicle-stimulatinghormoneinducesautophagyviaupregulationofHIF-1αinmousegranulosacells.CellDeathDis.2017Aug17;8(8):e3001.McePdfHeightCaution:Producthasnotbee