UC2288-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEUC2288Cat.No.:HY-112780CASNo.:1394011-91-6分?式:C??H??ClF?N?O?分?量:481.82作?靶點:MDM-2/p53作?通路:Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:50mg/mL(103.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0755mL10.3773mL20.7546mL5mM0.4151mL2.0755mL4.1509mL10mM0.2075mL1.0377mL2.0755mL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?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)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(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%cornoilSolubility:≥2.08mg/mL(4.32mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性UC2288?種新型的、具有細胞通透性和?服活性的p21衰減試劑(對p21具有相對選擇性活性)，于索拉?尼(HY-10201)的結構合成。UC2288在不依賴p53的情況下下調p21mRNA的表達，降低p21蛋??平，對p21蛋?的穩(wěn)定性響很?。UC2288對VEGFR2和Raf激酶沒有抑制作?，即使在10μM。體外研究UC2288(0-10μM;24hours)decreasesp21proteinlevel,buthasnoeffectsonotherproteins[1].UC2288(0-10μM;24hours)decreasesp21mRNAexpressiontranscriptionallyorpost-transcriptionallybutindependentlyofp53[1].WesternBlotAnalysis[1]CellLine:HK2(normalkidney),786-O(RCC),Caki-1(RCC),ACHN(RCC)andHEY(ovariancancer)cellsConcentration:0μM;1μM;3μM;10μMIncubationTime:24hoursResult:Decreasedp21proteinexpression.RT-PCR[1]CellLine:p53-mutantRCCcellline786-OConcentration:10μMIncubationTime:24hoursResult:Decreasedp21mRNAindependentofp53expression.體內研究UC2888(oralgavage;15mg/kg;3timesaweek;4weeks)co-treatmentwithimetelstatsignificantlysuppressestumorgrowthanddoesnoteffectmiceweight[2].UC2288(intraperitonealinjection;10mg/kg;4timesin7days)attenuatesMPTP-inducedbehavioralimpairment,preventsactivationofMAPKpathwayintheMPTP-treatedmicebrain.MPTPtreatmentraisesTNF-α,IL-6andIL-1βlevelsinMPTPtreatedmicebrain,butUC2288signicantlydecreasesMPTP-inducedTNF-α,IL-6levels,butIL-1βisnotdecreasedinbrain[3].AnimalModel:Eight-weekold,athymicnude(NCrnu/nu)miceinjectedsubcutaneouslywithHCT116andACHNcancercells(2.5x106)[2]Dosage:15mg/kgAdministration:Oralgavage;3timesaweek;4weeks;co-treatmentwithimetelstatResult:Combinedtreatmentwithimetelstatsynergisticallyinhibitedtumorgrowthinmice.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:MPTP-inducedC57BL6Parkinson’sdiseasemicemodel[3]Dosage:10mg/kgAdministration:Intraperitonealinjection;4timesin7daysResult:AmelioratedMPTPinducedPDprogressionthroughinhibitionofneuroinammation.REFERENCES[1].HiromiIWettersten,etal.ANovelp21AttenuatorWhichIsStructurallyRelatedtoSorafenib.CancerBiolTher.2013Mar;14(3):278-85.[2].RomiGupta,etal.SynergistictumorsuppressionbycombinedinhibitionoftelomeraseandCDKN1A.ProcNatlAcadSciUSA.2014Jul29;111(30):E3062-71.[3].JunHyungIm,etal.p21inhibitorUC2288amelioratesMPTPinducedParkinson’sdiseaseprogressionthroughinhibitionofoxidativestressandneuroinammation.TranslationalMedicine.NeurobiologyofDiseaseMcePdfHeightCaution:Producthasnotbeen