MPT0G211-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMPT0G211Cat.No.:HY-123976CASNo.:2151853-97-1分?式:C??H??N?O?分?量:293.32作?靶點:HDAC作?通路:CellCycle/DNADamage;Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(340.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.4092mL17.0462mL34.0925mL5mM0.6818mL3.4092mL6.8185mL10mM0.3409mL1.7046mL3.4092mL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(fù)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(dāng)?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.52mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性MPT0G211?種?效、?服活性和選擇性的HDAC6抑制劑(IC50=0.291nM)。MPT0G211對HDAC6的選擇性其他HDAC亞型的1000倍。MPT0G211可以透過?腦屏障。MPT0G211改阿爾茨海默病模型中tau磷酸化和認(rèn)知缺陷。MPT0G211具有抗轉(zhuǎn)移和神經(jīng)保護(hù)作?。抗癌活性。IC50&TargetHDAC60.291μM(IC50)體外研究MPT0G211(0.1?μM;cellsweretransfectedwithpCAXAPP695andpRK5-EGFP-TauP301Lfor24?h)significantlyinhibitsthephosphorylationoftauSer396[1].MPT0G211inhibitsHDAC6/Hsp90bindingandcausessubsequentproteasomaldegradationofpolyubiquitinatedproteins[1].MPT0G211significantlydecreasesthephosphorylationoftaubyGSK3βinactivation[1].MPT0G211(0.1?μM;24hours)significantlyattenuatesthephosphorylationoftauSer396andSer404inbothcelllines(SH-SY5YandNeuro-2acellsweretransfectedfor24?hwithpCAXAPP695andpRK5-EGFP-TauP301L)[1].MPT0G211inhibitsMDA-MB-231andMCF-7cellsgrowth(GI50=16.19and5.6μM,respectively)[2].InAMLcells,MPT0G211potentiatedthecytotoxiceffectsofDOXObyimpairingDNArepairmachineryandactivatingBcl-2-associatedXprotein(BCL-XL)-dependentcellapoptosis[3].體內(nèi)研究MPT0G211(50?mg/kg;p.o.;dailyfor3months)significantlyamelioratesthespatialmemoryimpairment[1].MPT0G211(25?mg/kg;i.p.;qd;day73post-tumorinjection)reducesnumbersofnodulesandlungweights[2].MPT0G211treatmentnotonlydiminishestauphosphorylationbyinhibitionGSK3βactivitybutalsoenhancestheacetylationofHsp90,whichcausesthedownregulationofHDAC6/Hsp90bindingandfacilitatesproteasomaldegradationofpolyubiquitinatedp-tau[1].AnimalModel:Tripletransgenic(3×Tg-AD)mice(harboringAPPSweandtauP301Lmutanttransgenes[1]Dosage:50?mg/kgAdministration:P.o.;dailyfor3monthsResult:Significantlyamelioratedthespatialmemoryimpairment.AnimalModel:FemaleSCIDmice(bearingMDA-MB-231cells)[2]Dosage:25?mg/kgAdministration:I.p.;qd;day73post-tumorinjectionResult:Significantlyreducednumbersofnodulesandlungweights.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].FanSJ,HuangFI,etal.Thenovelhistonedeacetylase6inhibitor,MPT0G211,amelioratestauphosphorylationandcognitivedeficitsinanAlzheimer'sdiseasemodel.CellDeathDis.2018;9(6):655.Published2018May29.[2].HsiehYL,etal.Anti-metastaticactivityofMPT0G211,anovelHDAC6inhibitor,inhumanbreastcancercellsinvitroandinvivo.BiochimBiophysActaMolCellRes.2019;1866(6):992-1003.[3].TuHJ,etal.TheanticancereffectsofMPT0G211,anovelHDAC6inhibitor,combinedwithchemotherapeuticagentsinhumanacuteleukemiacells.ClinEpigenetics.2018;10(1):162.Published2018Dec29.McePdfHeightCaution:Product