MedKoo Biosciences/P22077/406569/500mg

P22077isapotentandselectiveubiquitin-specificprotease7(USP7)inhibitor.P22077potentlyinducesapoptosisinNBcellswithanintactUSP7-HDM2-p53axisbutnotinNBcellswithmutantp53orwithouthumanhomologofMDM2(HDM2)expression.P22077alsosignificantlyaugmentedthecytotoxiceffectsofdoxorubicin(Dox)andetoposide(VP-16)inNBcellswithanintactUSP7-HDM2-p53axis.Moreover,P22077wasfoundtobeabletosensitizechemoresistantLA-N-6NBcellstochemotherapy.InaninvivoorthotopicNBmousemodel,P22077significantlyinhibitedthexenograftgrowthofthreeNBcelllines.USP7-specificinhibitorslikeP22077mayservenotonlyasastand-alonetherapybutalsoasaneffectiveadjuncttocurrentchemotherapeuticregimensfortreatingNBwithanintactUSP7-HDM2-p53axis.

MedKooCat#:406569
Name:P22077
CAS#:1247819-59-5
ChemicalFormula:C12H7F2NO3S2
ExactMass:314.98354
MolecularWeight:315.31
ElementalAnalysis:C,45.71;H,2.24;F,12.05;N,4.44;O,15.22;S,20.34

Synonym:P22077;P-22077;P22077.

IUPAC/ChemicalName:1-(5-((2,4-difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone

InChiKey:RMAMGGNACJHXHO-UHFFFAOYSA-N

InChiCode:InChI=1S/C12H7F2NO3S2/c1-6(16)11-5-9(15(17)18)12(20-11)19-10-3-2-7(13)4-8(10)14/h2-5H,1H3

SMILESCode:CC(C1=CC([N+]([O-])=O)=C(SC2=CC=C(F)C=C2F)S1)=O

TechnicalData

Appearance:

Solidpowder

Purity:

>98%(orrefertotheCertificateofAnalysis)

ShippingCondition:

Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:

Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:

SolubleinDMSO,notinwater

ShelfLife:

>2yearsifstoredproperly

DrugFormulation:

ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:

0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:

293490

AdditionalInformation

References

1:FanYH,ChengJ,VasudevanSA,DouJ,ZhangH,PatelRH,MaIT,RojasY,ZhaoY,YuY,ZhangH,ShohetJM,NuchternJG,KimES,YangJ.USP7inhibitorP22077inhibitsneuroblastomagrowthviainducingp53-mediatedapoptosis.CellDeathDis.2013Oct17;4:e867.doi:10.1038/cddis.2013.400.PubMedPMID:24136231;PubMedCentralPMCID:PMC3920959.

2:DarA,ShibataE,DuttaA.DeubiquitinationofTip60byUSP7determinestheactivityofthep53-dependentapoptoticpathway.MolCellBiol.2013Aug;33(16):3309-20.doi:10.1128/MCB.00358-13.Epub2013Jun17.PubMedPMID:23775119;PubMedCentralPMCID:PMC3753911.

3:AltunM,KramerHB,WillemsLI,McDermottJL,LeachCA,GoldenbergSJ,KumarKG,KonietznyR,FischerR,KoganE,MackeenMM,McGouranJ,KhoronenkovaSV,ParsonsJL,DianovGL,NicholsonB,KesslerBM.Activity-basedchemicalproteomicsacceleratesinhibitordevelopmentfordeubiquitylatingenzymes.ChemBiol.2011Nov23;18(11):1401-12.doi:10.1016/j.chembiol.2011.08.018.PubMedPMID:22118674.

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MedKoo Biosciences/P22077/406569/500mg

TechnicalData

AdditionalInformation

References