Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEML216Cat.No.:HY-12342CASNo.:1430213-30-1Synonyms:CID-49852229分?式:C??H?F?N?OS分?量:383.32作?靶點:DNA/RNASynthesis作?通路:CellCycle/DNADamage儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:20mg/mL(52.18mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6088mL13.0439mL26.0879mL5mM0.5218mL2.6088mL5.2176mL10mM0.2609mL1.3044mL2.6088mL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。-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>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2mg/mL(5.22mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性ML216(CID-49852229)?種有效，選擇性，細胞滲透性的BLM解旋酶抑制劑，對BLMfull-length和BLM636-1298的IC50分別為2.98μM和0.97μM。ML216以Ki為1.76μM來抑制BLM的ssDNA依賴性ATPase的活性。ML216具有抗腫瘤活性。IC50&TargetIC50:2.98μM(BLMfull-length)and0.97μM(BLM636-1298)[1]體外研究ML216(12.5-50μM;24-72hours;PSNG5andPSNG13cells)treatmentinhibitstheproliferationofPSNF5cellsinaconcentration-dependentmanner,butnotofPSNG13cells[1].ML216treatmentleadstoastatisticallysignificantincreaseinthefrequencyofsisterchromatidexchanges(SCEs)inPSNF5cells,butnotinPSNG13cells[1].ML216increasesthesensitivityofPSNF5cellstoaphidicolinbuthasnosensitizingeffectonisogenicPSNG13cellsdevoidofBLM[1].ML216inhibitsboththefulllengthWRN(IC50of5μM)andatruncatedWRN500-946(IC50of12.6μM),withtheformerbeing2.5-foldmoresensitivetoinhibition.BLMisalittlemoresensitivethanWRNtoinhibitionbyML216(1.7-foldbasedonIC50values).DespitethedetectableinhibitionofWRNbyML216,thiscompoundappearsselectiveforBLMinhumancells.ML216inhibitsproliferationofWRN+andWRN?cellsequallywell,andsimilarlysensitizedbothcelltypestoaphidicolin[1].CellProliferationAssay[1]CellLine:PSNG5andPSNG13cellsConcentration:12.5μMor50μMIncubationTime:24hours,48hours,72hoursResult:InhibitedtheproliferationofPSNF5cells,butnotofPSNG13cells,anddidsoinaconcentration-dependentmanner.體內研究AlthoughML216inhibitsunwindingbythesequence-relatedBLMandWRNhelicasessimilarlyinvitro,theapparentdependenceonBLMforML216toexertitsbiologicaleffectsinhumancellssuggestsBLMspecificityforthedrug’smechanismofactioninvivo.Aco-crystalstructureofBLMincomplexwithinhibitorwouldbeinformative.CellularcuesinvivomayinduceaspecificconformationofWRNthatmakesitresistanttoML216[2].戶使?本產品發表的科研?獻?AmJCancerRes.2021Apr15;11(4):1347-1368.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].NguyenGH,etal.AsmallmoleculeinhibitoroftheBLMhelicasemodulateschromosomestabilityinhumancells.ChemBiol.2013Jan24;20(1):55-62.[2].BanerjeeT,etal.AnewdevelopmentinDNArepairmodulation:discoveryofaBLMhelicaseinhibitor.CellCycle.2013Mar1;12(5):713-4.McePdfHeightCaution:Producthasnotbee