Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJQKD82trihydrochlorideCat.No.:HY-138691ASynonyms:JADA82trihydrochloride;PCK82trihydrochloride分?式:C??H??Cl?N?O?分?量:610.01作?靶點:HistoneDemethylase作?通路:Epigenetics儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數據體外實驗DMSO:50mg/mL(81.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.6393mL8.1966mL16.3932mL5mM0.3279mL1.6393mL3.2786mL10mM0.1639mL0.8197mL1.6393mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，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:≥2.5mg/mL(4.10mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.10mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.10mM);ClearsolutionBIOLOGICALACTIVITY?物活性JQKD82(JADA82)trihydrochloride?種細胞通透性和選擇性KDM5抑制劑。JQKD82trihydrochloride增加H3K4me3，可?于多發性?髓瘤的研究。體外研究JQKD82(0.3μM;24hours)trihydrochloridecausesanincreaseintheglobalH3K4me3levelofMM.1Scells[1].JQKD82(0.1-10μM;day1-day5)trihydrochlorideinhibitsthegrowthofMM.1Scellsinadose-andtime-dependentmanner.JQKD82trihydrochlorideispotentatelicitinggrowthsuppressioninMM.1Scells(IC50=0.42μM)[1].JQKD82(1μM;24hours)trihydrochlorideinducesG1cell-cyclearrestby48hoursinMM.1SandMOLP-8cells[1].體內研究JQKD82(50-75mg/kg;i.p.;twiceadayfor3weeks)trihydrochloridehasanti-multiplemyelomaactivity[1].JQKD82trihydrochloridedisplaysanincreaseinH3K4me3levelsandresultsinadramaticreductionofMYCimmuno-staininginvivo[1].AnimalModel:Six-week-oldfemaleNOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ(NSG)mice(bearingMOLP-8TurboGFP-Luccells)[1]Dosage:50mg/kg,75mg/kgAdministration:i.p.;twiceadayfor3weeksResult:Significantlyreducedtumorburden.REFERENCES[1].JunQi,etal.Histonedemethylase5inhibitorsandusesthereof.WO2020033377A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr