BI8622-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBI8622Cat.No.:HY-120929CASNo.:1875036-74-0分?式:C??H??N?O分?量:426.51作?靶點:E1/E2/E3Enzyme作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(293.08mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3446mL11.7231mL23.4461mL5mM0.4689mL2.3446mL4.6892mL10mM0.2345mL1.1723mL2.3446mL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%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.88mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.88mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.88mM);ClearsolutionBIOLOGICALACTIVITY?物活性BI8622?種泛素連接酶HUWE1特異性拮抗劑，IC50為3.1μM[1]。IC50&TargetIC50:3.1μM(HUWE1)[1]體外研究BI8622inducesHUWE1ectopicallyexpressestoabolishubiquitinationofMCL1withanIC50valueof6.8μMinHeLacells[1].BI8622suppressescolonyformationofLs174TcellswithestimatedIC50valueof8.4μM[1].BI8622(10μM;1-4days)treatmentretardspassageofLs174Tcellsthroughallphasesofthecellcycle,withtheeffectbeingstrongestforG1[1].BI8622(0-50μM;16hours)retardsthedegradationofMCL1inresponsetoUVirradiationbyinhibitingHUWE1inHeLacells[1].BI8622inhibitsMYC-dependenttransactivationincolorectalcancercells[1].CellCycleAnalysis[1]CellLine:Ls174TcellsConcentration:0μM,5μM,10μM,15μM,20μMIncubationTime:0-4daysResult:RetardedpassageofLs174Tcellsthroughallphasesofthecellcycle,withtheeffectbeingstrongestforG1.WesternBlotAnalysis[1]CellLine:HeLacellsConcentration:0μM,10μM,20μMIncubationTime:16hoursResult:RetardedthedegradationofMCL1inresponsetoUVirradiationbyinhibitingHUWE1inHeLacells.戶使?本產(chǎn)品發(fā)表的科研?獻?JClinInvest.2020Dec1;130(12):6301-6316.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?CellDeathDiffer.2020Dec;27(12):3273-3288.?ExpEyeRes.2022May13;220:109110.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PeterS,etal.Tumorcell-specificinhibitionofMYCfunctionusingsmallmoleculeinhibitorsoftheHUWE1ubiquitinligase.EMBOMolMed.2014Dec;6(12):1525-41.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl