Staurosporine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEStaurosporineCat.No.:HY-15141CASNo.:62996-74-1分⼦式:C₂₈H₂₆N₄O₃分⼦量:466.53作⽤靶点:PKC;PKA;Apoptosis;Bacterial;Fungal;Antibiotic作⽤通路:Epigenetics;TGF-beta/Smad;ProteinTyrosineKinase/RTK;StemCell/Wnt;Apoptosis;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months

-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(133.97mM;Needultrasonic)扫描⼆维码，H2O:<0.1mg/mL(insoluble)运⽤溶解⽅案计算器获得适合您实验体系的溶解⽅案MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1435mL10.7174mL21.4348mL5mM0.4287mL2.1435mL4.2870mL10mM0.2143mL1.0717mL2.1435mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶1.请依序添加每种溶剂：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.08mg/mL(4.46mM);Clearsolution此⽅案可获得≥2.08mg/mL(4.46mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述1/4www.MedChemEwww.MedChemE2.体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.46mM);Suspendedsolution;Needultrasonic此⽅案可获得2.08mg/mL(4.46mM)的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶3.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.08mg/mL(4.46mM);Clearsolution此⽅案可获得≥2.08mg/mL(4.46mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性Staurosporine⼀种有效，ATP竞争性的，⾮选择性蛋⽩激酶抑制剂，抑制PKC，PKA，c-Fgr，和Phosphorylasekinase的IC50分别为6nM，15nM，2nM，3nM。Staurosporine⼀个凋亡诱导剂。IC50&TargetPKCPKAc-FgrPhosphorylasekinase6nM(IC50)15nM(IC50)2nM(IC50)3nM(IC50)S6kinase(70kDa)v-Srccdc2TPK-IIB/Syk5nM(IC50)6nM(IC50)9nM(IC50)16nM(IC50)Ca2+/CaMPK-I1MLCKIREGF-R20nM(IC50)21nM(IC50)61nM(IC50)100nM(IC50)ERK-1CSKIGF-IRCK21500nM(IC50)2000nM(IC50)6150nM(IC50)19500nM(IC50)CK1163500nM(IC50)体外研究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].体内研究TheinhibitoryeffectofStaurosporineisstatisticallysignificantataroundWk10oftumorpromotion.Althoughstatisticallysignificantinhibitionisnotobtainedwith10ngofStaurosporineinlaterweeksoftheexperiment,adecreasingtendencyinthepercentagesoftumorbearingmiceandinaveragenumbersoftumorspermouseisapparent.Thus,StaurosporineslightlyinhibitstumorpromotionofTeleocidin,evenatthedoseatwhichStaurosporineitselfinducedtumors[3].Staurosponne(0.05and0.1mg/kgintraperitoneal)attenuates2/4www.MedChemEwww.MedChemEtheimpairedperlormanceofwatermazeandpassiveavoidancetasks,eventhoughthedrugadministrationbegan2weeksafterthelesion.Moreover,Staurosporine(0.1mg/kg)partiallyreversedthedecreaseofcholineacetyltransferaseactivityinthefronto-parietalcortexinducedbybasalforebrain-lesion.TheseresultssuggestthatStaurosporineattenuatesimpairmentoflearningthroughreversalofdamagetocholinergicneuronsinducedbybasalforebrain-lesion[4].PROTOCOLAnimalMice[3]Administration[3][4]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,andthe

passiveavoidancetaskiscarriedout4weeksaftertheBFlesion.TheratreceivedStaurosporineatdosesof0.01,0.03,0.1,and0.3mg/kg(i.p.,N=10ineachgroupfor2weeks)30mmpriortothewatermazetraining

sessionsandthepassiveavoidancetaskacquisitiontrial.InthegroupwhichisgivenStaurosporinefor4

weeks,thedrugisfirstgiven2weeksaftertheBF-lesion.Thewatermazetaskiscarriedout4weeksafter

theBF-lesion.Thepassiveavoidancetaskiscarriedout6weeksaftertheBF-lesion.Theratreceived

Staurosporineat0.05,0.1,and0.2mg/kg(i.p.,N=10ineachgroup)onceadayfor2weeksbeforetraining,

andfor2weeksafterthewatermazetrainingsessionsandthepassiveavoidancetaskacquisitiontrial.

Staurosporineissuspendedin0.3%ofsodiumcarboxymethylcellulose.Thevehicleisadministeredtothe

non-lesionedcontrolsandthelesionedcontrolsonthesamescheduleastheStaurosporine-treatedanimals.

MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Nature.2021Mar;591(7850):477-481.•Cell.2018Sep6;174(6):1477-1491.e19.•CellRes.2018Dec;28(12):1171-1185.•JAmChemSoc.2018Feb7;140(5):1863-1869.•SignalTransductTargetTher.2020Oct9;5(1):235.Seemorecustomervalidationsonwww.MedChemEREFERENCES3/4www.MedChemEwww.MedChemE[1].MeggioF,etal.Differentsusceptibilityofproteinkinasestostaurosporineinhibition.KineticstudiesandmolecularbasesfortheresistanceofproteinkinaseCK2.EurJBiochem.1995Nov15;234(1):317-22.[2].ChaeHJ,etal.Molecularmechanismofstaurosporine-inducedapoptosisinosteoblasts.PharmacolRes.2000Oct;42(4):373-81.[3].YoshizawaS,