Pifithrin-μ-PFTμ-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPifithrin-μCat.No.:HY-10940CASNo.:64984-31-2Synonyms:PFTμ;2-Phenylethynesulfonamide分?式:C?H?NO?S分?量:181.21作?靶點(diǎn):MDM-2/p53;HSP;Autophagy作?通路:Apoptosis;CellCycle/DNADamage;MetabolicEnzyme/Protease;Autophagy儲(chǔ)存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥108mg/mL(595.99mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM5.5185mL27.5923mL55.1846mL5mM1.1037mL5.5185mL11.0369mL10mM0.5518mL2.7592mL5.5185mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(11.48mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(11.48mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(11.48mM);ClearsolutionBIOLOGICALACTIVITY?物活性Pifithrin-μ?種p53和HSP70的抑制劑，具有抗腫瘤和神經(jīng)保護(hù)作?。IC50&TargetHSP70MDM-2/p53體外研究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].體內(nèi)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?邊的抑制劑?師www.MedChemEtumorvolume.Tumorvolumeisdeterminedas0.5×length×width2.Tumorsamplesarecollectedandfixedin10%neutralbufferedformalin.Hematoxylinandeosinstainingandimmunohistochemistryforhistologicalanalysisoftumorsamplesaremeasured[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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