Pifithrin-μ-PFTμ-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPifithrin-μCat.No.:HY-10940CASNo.:64984-31-2Synonyms:PFTμ;2-Phenylethynesulfonamide分⼦式:C₈H₇NO₂S分⼦量:181.21作⽤靶点:MDM-2/p53;HSP;Autophagy作⽤通路:Apoptosis;CellCycle/DNADamage;MetabolicEnzyme/Protease;Autophagy储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:≥108mg/mL(595.99mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM5.5185mL27.5923mL55.1846mL5mM1.1037mL5.5185mL11.0369mL10mM0.5518mL2.7592mL5.5185mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(11.48mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(11.48mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(11.48mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Pifithrin-μ⼀种p53和HSP70的抑制剂，具有抗肿瘤和神经保护作⽤。IC50&TargetHSP70MDM-2/p53体外研究Pifithrin-μ(10μM)isap53inhibitor,whichinhibitsp53bindingtomitochondriabyreducingitsaffinitytoantiapoptoticproteinsBcl-xLandBcl-2buthasnoeffectonp53-dependenttransactivation,activityofcaspases2,8,9and10inacell-freesystem,orNF-κB-dependenttranscription[1].Pifithrin-μ(PES)time-anddose-dependentlyreducesviabilityinA549cells,withIC50sof44.9and25.7µMat24hand48h.Pifithrin-μ(20μM)suppressesthecellmigration,inducescellcyclearrestandcellapoptosisinA549andH460cells.Pifithrin-μ(10or20µM)inhibitsactivitiesofAKT,ERK,andHsp70inA549andH460cells.Pifithrin-μ(20µM)sensitizesA549andH460celllinestoTRAIL-inducedcellproliferationinhibitionandapoptosis[2].体内研究Pifithrin-μ(40mg/kg,i.p.)showsnoprotectiveeffectagainstdosesofradiationthatcausegastrointestinalsyndromeinmice[1].Pifithrin-μ(PES,10mg/kg)showsantitumoreffectinmicebearingA549cells[2].Pifithrin-μexhibitsneuroprotectiveeffectwiththeP53-inhibitorpifithrin-μaftercardiacarrestinarodentmodel[3].PROTOCOLCellAssay[2]ThecellviabilityisdeterminedbytheCellCountingKit-8assay.Briefly,A549andH460cellsareincubatedin96-wellplatesatadensityof5×103per100µLofculturemediumovernight.AftertreatedwithindicatedconcentrationofPifithrin-μfor24and48h,10µLoftetrazoliumsubstrateareaddedtoeachwelloftheplate.Afterincubationat37°Cfor1h,theabsorbanceisrecordedatawavelengthof450nmusingamicroplatereader.Eachexperimentisdeterminedintriplicateandrepeatedatleastthreetimes[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[2]Administration[2]A549cells(1×107)aresuspendedinMatrigelandinoculatedsubcutaneouslyintothemice.TwelvemicebearingevidenttumorsarearbitrarilyassignedtoPBScontrolgroupandPifithrin-μtreatmentgroups(sixmicepergroup).Whentumorsreachasizeof-5×5mm2,micearetreatedwitheitherasingleofintraperitonealinjectionofPifithrin-μ(20mg/kg)orPBSeverytwodays.After3-weektreatment,miceareeuthanizedwithcarbondioxide.Tumorburdensareevaluatedbymeasuringbodyweight,tumorweight,and2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEtumorvolume.Tumorvolumeisdeterminedas0.5×length×width2.Tumorsamplesarecollectedandfixedin10%neutralbufferedformalin.Hematoxylinandeosinstainingandimmunohistochemistryforhistologicalanalysisoftumorsamplesaremeasured[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Theranostics.2019Jan1;9(2):554-572.•BiomedPharmacother.2022Jan5;147:112604.•ColloidsSurfBBiointerfaces.2July2022,112686.•Patent.US20180263995A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].StromE,etal.Small-moleculeinhibitorofp53bindingtomitochondriaprotectsmicefromgammaradiation.NatChemBiol.2006Sep;2(9):474-9.Epub2006Jul23.[2].ZhouY,etal.Pifithrin-μisefficaciousagainstnon-smallcelllungcancerviainhibitionofheatshockprotein70.OncolRep.2017Jan;37(1):313-322.[3].GlasM,etal.NeuroprotectionwiththeP53-InhibitorPifithrin-μafterCardiacArrestinaRodentModel