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Medchemexpress/Staurosporine(Synonyms: Antibiotic AM-2282; STS; AM-2282)/HY-15141/2mg
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Medchemexpress/Staurosporine(Synonyms: Antibiotic AM-2282; STS; AM-2282)/HY-15141/2mg
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MedChemExp
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HY-15141-10mM*1mLinDMSO
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Staurosporineisaverypotentuniversalinhibitorofproteinkinasesbutshowinglittleselectivity,withIC50of6nM,15nM,2nM,and3nMforPKC,PKA,c-Fgr,andPhosphorylasekinase,respectively.

CustomerValidation

  • •CancerRes.2013Apr15;73(8):2574-86.
  • •ACSChemBiol.2017May19;12(5):1245-1256.
  • •SciRep.2015Aug3;5:12728.
  • •FutureMedChem.2017Jan;9(1):7-24.
  • •Neuroscience.2017Dec4;365:217-225.
  • •IntImmunopharmacol.2017Jun14;50:30-37.
  • •MedChemRes.09May2017.
Description

Staurosporineisaverypotentuniversalinhibitorofproteinkinasesbutshowinglittleselectivity,withIC50of6nM,15nM,2nM,and3nMforPKC,PKA,c-Fgr,andPhosphorylasekinase,respectively.

IC50&Target

IC50:6nM/15nM/2nM/3nM(PKC/PKA/c-Fgr/Phosphorylasekinase)[1]

InVitro

Staurosporine,widelyusedasaproteinkinaseC(PKC)inhibitorwithabroadspectrumofactivity,isanalkaloidisolatedfromtheculturebrothofStreptomycesstaurospores.MC3T3E-1osteoblasts,exposetoStaurosporine(100nM)for12h,releaseanamountofLDH(12.4±3.1%)thatissimilartothatreleasebythecontrolcells(10.0±2.4%),indicatingtherelativeabsenceoflyticdeath,whichoccursinnecrosis.Inaddition,treatmentwithStaurosporine(100nM)resultsinmorphologicalchanges,characteristicofapoptosis:abrightbluefluorescentcondensednucleiseenthroughafluorescencemicroscopeafterHoechst33258-staining,andareductionofcellvolume[2].

InVivo

TheinhibitoryeffectofStaurosporineisstatisticallysignificantataroundWk10oftumorpromotion.Althoughstatisticallysignificantinhibitionisnotobtainedwith10ngofStaurosporineinlaterweeksoftheexperiment,adecreasingtendencyinthepercentagesoftumorbearingmiceandinaveragenumbersoftumorspermouseisapparent.Thus,StaurosporineslightlyinhibitstumorpromotionofTeleocidin,evenatthedoseatwhichStaurosporineitselfinducedtumors[3].Staurosponne(0.05and0.1mg/kgintraperitoneal)attenuatestheimpairedperlormanceofwatermazeandpassiveavoidancetasks,eventhoughthedrugadmiNISTrationbegan2weeksafterthelesion.Moreover,Staurosporine(0.1mg/kg)partiallyreversedthedecreaseofcholineacetyltransferaseactivityinthefronto-parietalcortexinducedbybasalforebrain-lesion.TheseresultssuggestthatStaurosporineattenuatesimpairmentoflearningthroughreversalofdamagetocholinergicneuronsinducedbybasalforebrain-lesion[4].

References

  • [1].MeggioF,etal.Differentsusceptibilityofproteinkinasestostaurosporineinhibition.KineticstudiesandmolecularbasesfortheresistanceofproteinkinaseCK2.EurJBiochem.1995Nov15;234(1):317-22.

    [2].ChaeHJ,etal.Molecularmechanismofstaurosporine-inducedapoptosisinosteoblasts.PharmacolRes.2000Oct;42(4):373-81.

    [3].YoshizawaS,etal.Tumor-promotingactivityofstaurosporine,aproteinkinaseinhibitoronmouseskin.CancerRes.1990Aug15;50(16):4974-8.

    [4].NabeshimaT,etal.Staurosporinefacilitatesrecoveryfromthebasalforebrain-lesion-inducedimpairmentoflearninganddeficitofcholinergicneuroninrats.JPharmacolExpTher.1991May;257(2):562-6.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.1435mL10.7174mL21.4348mL
5mM0.4287mL2.1435mL4.2870mL
10mM0.2143mL1.0717mL2.1435mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[2]

MC3T3E-1cells(2×106cells/group)aretreatedwith100nMStaurosporineforvarioustimeperiodsandlysedinalysisbuffer(EBbuffer:1%TritonX-100,10mMTris,pH7.6,50mMNaCl,1mg/mLAprotinin,5mMEDTA,50mMNaF,0.1%2-mercaptoethanol,and100μMsodiumorthovanadate).Thelysateofthecellsissubjectedtocentrifugationat12000gat4°Cfor30min.Solublefractioniscollectedandincubatedwithanti-JNK1antibodies.Afterincubationonicefor3h,100μLofa10%solutionofformalin-fixedStaphylococcusaureusisaddedtotheanti-JNK1immunoprecipitatesandfurtherincubatedonicefor1h.TheabsorbedimmunecomplexiswashedtwicewithEBbufferandPANbuffer(10mMPIPESbuffer,pH7.0,1%aprotinin,100mMNaCl).Theimmunecomplexismixedwith2μgofGST-c-JunNT1-79proteinsasasubstratein30μLofthereactionbuffercontaining2μMcoldATP,2mMDTT,20mMMgCl2,2μCi[γ33-P]-ATP,and20mMTris-HCl,pH7.5at30°Cfor20min.Thereactionisterminatedbyadding15μLof3×SDS-PAGEsamplebufferandboilingat98°Cfor5min.Theproteinsareseparatedon12%SDS-PAGEandtransferredontoanitrocellulosemembraneviathesemi-dryelectrotransfersystem.Themembraneisimmunoblottedwithrabbitanti-JNK1antibodiesandhorserADIshpeoxidaseconjugatedanti-rabbitantibodiestovisualizethesignalsmeasuredbyanenhancedchemiluminescencesystem.Thegelisdriedunderavacuum,andthephosphotransferaseactivityisvisualizedbyautoradiographyandquantifiedbyaPhosphoImageranalyzer[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[3][4]

StaurosporineissUSPendedin0.3%ofsodiumcarboxymethylcellulose(Rat)[4].

Mice[3]
FemaleCD-Imiceareused.VariousamountsofStaurosporinein10μLofacetoneareappliedtotheearsof8-wk-oldCD-Imice.Theextentofirritationisexpressedastheminimumdoseofthecompoundcausingirritation.InductionofHOCinMouseSkinStaurosporinein0.1mLofacetoneisappliedtotheskinofthebacksofCD-Imice,andacrudeenzymeextractisobtainedfromtheskin18hlater.HDCactivityisexpressedaspmolofCO2releasedpermgofproteinperlhofincubation.InductionofODCinMouseSkinStaurosporinein0.2mLofacetoneisappliedtotheskinofthebacksofCD-Imice.After4h,acrudeenzymeextractispreparedfromtheepidermis,anditsODCactivityismeasured.EnzymeactivityisexpressedasnmolofCO2permgofproteinper30minofincubation.
Rats[4]
MaleKblWistarrats(weighing270to310g)areused.InthegroupwhichisgivenStaurosporinefor2weeks,thewatermazetaskandStaurosporineadministrationarestarted2weeksaftertheBF-lesion,andthepassiveavoidancetaskiscarriedout4weeksaftertheBFlesion.TheratreceivedStaurosporineatdosesof0.01,0.03,0.1,and0.3mg/kg(i.p.,N=10ineachgroupfor2weeks)30mmpriortothewatermazetrainingsessionsandthepassiveavoidancetaskacquisitiontrial.InthegroupwhichisgivenStaurosporinefor4weeks,thedrugisfirstgiven2weeksaftertheBF-lesion.Thewatermazetaskiscarriedout4weeksaftertheBF-lesion.Thepassiveavoidancetaskiscarriedout6weeksaftertheBF-lesion.TheratreceivedStaurosporineat0.05,0.1,and0.2mg/kg(i.p.,N=10ineachgroup)onceadayfor2weeksbeforetraining,andfor2weeksafterthewatermazetrainingsessionsandthepassiveavoidancetaskacquisitiontrial.Staurosporineissuspendedin0.3%ofsodiumcarboxymethylcellulose.Thevehicleisadministeredtothenon-lesionedcontrolsandthelesionedcontrolsonthesamescheduleastheStaurosporine-treatedanimals.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].MeggioF,etal.Differentsusceptibilityofproteinkinasestostaurosporineinhibition.KineticstudiesandmolecularbasesfortheresistanceofproteinkinaseCK2.EurJBiochem.1995Nov15;234(1):317-22.

    [2].ChaeHJ,etal.Molecularmechanismofstaurosporine-inducedapoptosisinosteoblasts.PharmacolRes.2000Oct;42(4):373-81.

    [3].YoshizawaS,etal.Tumor-promotingactivityofstaurosporine,aproteinkinaseinhibitoronmouseskin.CancerRes.1990Aug15;50(16):4974-8.

    [4].NabeshimaT,etal.Staurosporinefacilitatesrecoveryfromthebasalforebrain-lesion-inducedimpairmentoflearninganddeficitofcholinergicneuroninrats.JPharmacolExpTher.1991May;257(2):562-6.

MolecularWeight

466.53

Formula

C₂₈H₂₆N₄O₃

CASNo.

62996-74-1

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥31mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.98%

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