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Selleckchem/T-3775440 HCl/S8438

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S8438

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DescriptionT-3775440HClisanirreversIBLeLSD1inhibitorthatishighlyselectiveforLSD1relativetoothermonoamineoxidases(e.g.,MAO-AandMAO-B),withanIC50valueof2.1nmol/L.TargetsLSD1[1]()2.1nMInvitroT-3775440treatmentenforcestransdifferentiationoferythroid/megakaryocyticlineagesintogranulomonocytic-likelineagecells.T-3775440disruptstheinteractionbetweenLSD1andgrowthfactor-independent1B(GFI1B),atranscriptionfactorcriticalforthedifferentiationprocessesoferythroidandmegakaryocyticlineagecells.48-hourT-3775440treatmentinducescell-cyclearrestandapoptosisinAEL(TF-1a,HEL92.1.7)andAMKLcelllines(CMK11-5,M07e).T-3775440treatmentincreasestheG1andsub-G1phasepopulationsinTF-1aandCMK11-5cells[1].AssayMethodsTestIndexPMIDWesternblotp27/cPARP;PubMed:27903753MolCancerTherTF-1aandCMK11-5cellsweretreatedwiththeindicatedconcentrationofT-3775440for24or48hours.Treatedcellsweresubsequentlyharvestedandlysedtopreparetotallysates.Immunoblottinganalyseswereperformedtodeterminetheexpressionlevelsofp27,cleavedPARP,andβ-actininthecelllysates.27903753GrowthinhibitionassayIC50;PubMed:27903753MolCancerTherInvitroproliferationassayof27leukemiacelllines.CellsweretreatedwithT-3775440for3days.Redbars,AELcelllines;greenbars,AMKLcelllines;andbluebars,T-ALLcelllines.27903753InvivoT-3775440exertstumorgrowthsuppressionininvivomousexenograftmodelsofAML.Inmice,T-3775440treatmentresultsinatransientreductioninplatelets,followedbyasignificantrebound.ThereisnoobviouseffectonredbloodcellcountsfollowingasingleadmiNISTration.T-3775440alsoexhibitspotentantitumoreffectsinanadditionalAELmodelofHEL92.1.7andanAMKLmodelofCMK11-5,possessingprofoundanti-AELandanti-AMKLactivity[1].

Selleck Chemicals是世界领先的高性能的生命科学产品供应商之一，主要致力于提供MAPK和PI3K/Akt/mTOR等上百个信号通路的高特异性小分子抑制剂。Selleck 产品线补充非常及时，可以提供行业内最新的抑制剂类产品。同时Selleck也是专业的高通量筛选抑制剂分子库、API、天然产物和多肽供应商。