Seclidemstat-SP-2577-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESeclidemstatCat.No.:HY-103713CASNo.:1423715-37-0Synonyms:SP-2577分?式:C??H??ClN?O?S分?量:450.94作?靶點:HistoneDemethylase作?通路:Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(110.88mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2176mL11.0879mL22.1759mL5mM0.4435mL2.2176mL4.4352mL10mM0.2218mL1.1088mL2.2176mL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?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)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(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：0.5%CMC-Na/salinewater1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:10mg/mL(22.18mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：1.6%DMA>>5%Ethanol>>45%PEG400>>48.4%PBSSolubility:2mg/mL(4.44mM);Clearsolution;Needultrasonicandwarmingandheatto60°C3.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.61mM);ClearsolutionBIOLOGICALACTIVITY?物活性Seclidemstat?種有效的?競爭性可逆KDM1A(LSD1)抑制劑(Ki=31nM,IC50)。Seclidemstat促進SWI/SNF復合物突變巢癌的抗腫瘤免疫，并抑制病毒產(chǎn)?、病毒DNA復制和晚期因表達。Seclidemstat可?于尤??瘤的研究。IC50&TargetKi:31nM(LSD1)[1]IC50:13nM(LSD1)[1]體外研究Seclidemstat(72hours)inhibitsSWI/SNF-mutation-dependenttumorcellproliferationwithIC50rangingfrom0.013to2.819μM(COV434,BIN67,SCCOHT-1,TOV21G,SKOV3,A427,H522,A549,H1299,G401,G402,HCC15cells)[2].Seclidemstat(72hours)promotesendogenousretroviruses(ERVs)expressionandactivationofIFNβpathwayinSCCOHTcelllines(SCCOHT-1,BIN67,andCOV434cells)[2].Seclidemstat(3μM)promotesPD-L1expressioninSCCOHTCOV434pIND20BRG1-2.7cellline[2].戶使?本產(chǎn)品發(fā)表的科研?獻?NatCellBiol.2022Feb17.?ACSPharmacolTranslSci.November12,2021.?bioRxiv.2020May.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DaiXJ,etal.ReversibleLysineSpecificDemethylase1(LSD1)Inhibitors:APromisingWrenchtoImpairLSD1[publishedcorrectionappearsinJMedChem.2021May13;64(9):6410-6411].JMedChem.2021;64(5):2466-2488.[2].SoldiR,etal.ThenovelreversibleLSD1inhibitorSP-2577promotesanti-tumorimmunityinSWItch/Sucrose-NonFermentable(SWI/SNF)complexmutatedovariancancer.PLoSOne.2020;15(7):e0235705.Published2020Jul10.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio