ML-792-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEML-792Cat.No.:HY-108702CASNo.:1644342-14-2分?式:C??H??BrN?O?S分?量:551.41作?靶點(diǎn):E1/E2/E3Enzyme作?通路:MetabolicEnzyme/Protease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(181.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8135mL9.0677mL18.1353mL5mM0.3627mL1.8135mL3.6271mL10mM0.1814mL0.9068mL1.8135mL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、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(3.77mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.77mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.77mM);ClearsolutionBIOLOGICALACTIVITY?物活性ML-792?種特異性的?泛素樣修飾物(SUMO)活化酶(SAE)抑制劑。ML-792有效選擇性抑制SAE/SUMO1和SAE/SUMO2，IC50分別為3和11nM。ML-792微弱抑制NAE/NEDD8和UAE/ubiquitin，IC50分別為32μM和>100μM[1]。IC50&TargetIC50:3nM(SAE/SUMO1),11nM(SAE/SUMO2)[1]體外研究ML-792(0.0007-5μM;4hours)inhibitsSAEandSUMO-pathwayactivitiesinHCT116cells[1].ML-792(0.001-10μM;72hours)inhibitscellproliferationanddecreasescancercellviabilityinMDA-MB-468,MDA-MB-231,HCT116,Colo-205,andA375[1].CellViabilityAssay[1]CellLine:HumanbreastcancercellsMDA-MB-468andMDA-MB-231;humancoloncarcinomacellsHCT116andColo-205;humanmelanomacelllineA375Concentration:0.001,0.01,0.1,1,10μMIncubationTime:72hoursResult:Demonstratedadose-dependentviabilityeffectwithEC50valuesof0.06μMinMDA-MB-468cellsto0.45μMinA375cells.WesternBlotAnalysis[1]CellLine:HCT116cellsConcentration:0,0.0007,0.002,0.007,0.02,0.06,0.19,0.56,1.7,5μMIncubationTime:4hoursResult:Revealedadose-dependentdecreaseintheSAEandUBC9thioesterlevels.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?MolCell.2020Jul2;79(1):54-67.e7.?NatCommun.2022Nov11;13(1):6840.?NatCommun.2022Sep29;13(1):5726.?NatCommun.2022Sep3;13(1):5204.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?CellRep.2022Mar22;38(12):110534.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HeX,etal.ProbingtherolesofSUMOylationincancercellbiologybyusingaselectiveSAEinhibitor.NatChemBiol.2017Nov;13(11):1164-1171.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl