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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Y-27632二盐酸盐/HY-10583/2mg
商品详细Medchemexpress/Y-27632二盐酸盐/HY-10583/2mg
Medchemexpress/Y-27632二盐酸盐/HY-10583/2mg
Medchemexpress/Y-27632二盐酸盐/HY-10583/2mg
商品编号： HY-10583-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1100.00
美元价： 660.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
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商品介绍
Y-27632dihydrochlorideisanATP-competitiveinhibitorofROCK-IandROCK-II,withKiof220nMand300nMforROCK-IandROCK-II,respectively.
Description

Y-27632dihydrochlorideisanATP-competitiveinhibitorofROCK-IandROCK-II,withKiof220nMand300nMforROCK-IandROCK-II,respectively.

IC50&Target

Ki:220/300nM(ROCK-I/II)[1]

InVitro

Y-27632inhibitstheROCKfamilyofkinases100timesmorepotentlythanotherkinasesincludingproteinkinaseC,cAMP-dependentkinaseandmyosinlightchainkinase.Y-27632prolongsthelagtimeanddelaystheappearanceofBrdU-labeledcellsinaconcentration-dependentmanner,delaysofabout1and4harenoticedintheSwiss3T3cellstreatedwith10and100μMY-27632,respectively[1].Y-27632promotesneuronaldifferentiationofADIposetissue-derivedstemcells(ADSCs).Comparedto1.0and2.5μMY-27632inducedgroups,percentagesofneuroal-likecellsachievedapeakinthe5.0μMY-27632inducedgroup[2].

InVivo

Y-27632(5and10mg/kg)significantlyprolongstheonsettimeofmyoclonicjerkswhencomparewithsalinegroup.Y-27632(5and10mg/kg)significantlyprolongstheonsettimeofclonicconvulsionswhencomparewithsalinegroup[3].TreatmentwithDimethylnitrosamine(DMN)causesasignificantdecreaseinratbodyandliverweight(DMN-Sgroup)comparedwithcontrolanimals(S-Sgroup).OralY27632(30mg/kg)essentiallypreventsthisDMN-inducedratbodyandliverweightloss(DMN-Ygroup)[4].

References

  • [1].IshizakiT,etal.PharmacologicalpropertiesofY-27632,aspecificinhibitorofrho-associatedkinases.MolPharmacol.2000May;57(5):976-83.

    [2].XueZW,etal.Rho-associatedcoiledkinaseinhibitorY-27632promotesneuronal-likedifferentiationofadulthumanadiposetissue-derivedstemcells.ChinMedJ(Engl).2012Sep;125(18):3332-5.

    [3].InanS,etal.AntiepilepticeffectsoftwoRho-kinaseinhibitors,Y-27632andfasudil,inmice.BrJPharmacol.2008Sep;155(1):44-51.

    [4].TadaS,etal.AselectiveROCKinhibitor,Y27632,preventsdimethylnitrosamine-inducedhepaticfibrosisinrats.JHepatol.2001Apr;34(4):529-36.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM3.1225mL15.6123mL31.2246mL
5mM0.6245mL3.1225mL6.2449mL
10mM0.3122mL1.5612mL3.1225mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
KinaseAssay
[1]

RecombinantROCK-I,ROCK-II,PKN,orcitronkinaseisexpressedinHeLacellsasMyc-taggedproteinsbytransfectionusingLipofectamine,andisprecipitatedfromthecelllysatesbytheuseof9E10monoclonalanti-MycantibodycoupledtoGprotein-Sepharose.Recoveredimmunocomplexesareincubatedwithvariousconcentrationsof[32P]ATPand10mgofhistonetype2assubstratesintheabsenceorpresenceofvariousconcentrationsofeitherY-27632orY-30141at30°Cfor30mininatotalvolumeof30μLofthekinasebuffercontaining50mMHEPES-NaOH,pH7.4,10mMMgCl2,5mMMnCl2,0.02%Briji35,and2mMdithiothreitol.PKCaisincubatedwith5μM[32P]ATPand200μg/mLhistonetype2assubstratesintheabsenceorpresenceofvariousconcentrationsofeitherY-27632orY-30141at30°Cfor10mininakinasebuffercontaining50mMTris-HCl,pH7.5,0.5mMCaCl2,5mMmagnesiumacetate,25μg/mLphosphatidylserine,50ng/mL12-O-tetradecanoylphorbol-13-acetateand0.001%leupeptininatotalvolumeof30μL.Incubationisterminatedbytheadditionof10μLof43Laemmlisamplebuffer.Afterboilingfor5min,themixtureissubjectedtoSDS-polyacrylamidegelelectrophoresisona16%gel.ThegelisstainedwithCoomassieBrilliantBlue,andthendried.Thebandscorrespondingtohistonetype2areexcised,andtheradioactivityismeasured[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
[1]

Y-27632isdissolvedinwaterandstored[1].

HeLacellsareplatedatadensityof3×104cellsper3.5-cmdish.ThecellsareculturedinDMEMcontaining10%FBSinthepresenceof10mMThymidinefor16h.AfterthecellsarewashedwithDMEMcontaining10%FBS,theyareculturedforanadditional8h,andthen40ng/mLofNocodazoleisadded.After11.5hoftheNocodazoletreatment,variousconcentrationsofY-27632(0-300μM),Y-30141,orvehicleisaddedandthecellsareincubatedforanother30min[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[3][4]

Y-27632isdissolvedin0.9%NaCl(saline)(Mice)[3].
Y-27632isdissolvedinsaline(finalconcentration2%)(Rat)[4].

Mice[3]
Male,inbredSwissalbinomice(2-3monthsold)weighing25-30gareused.Miceareinjectedwithasub-convulsivedoseofPTZ(35mg/kg,i.p.)(onMondays,WednesdaysandFridays)ofeachweekforatotalof11injections.AftereachPTZinjection,miceareobservedfor30minandtheoccurrenceofconvulsiveactivityisrecorded.After30min,themicearetheninjectedwitheitherFasudil(25mg/kg,i.p.)orY-27632(5mg/kg,i.p.)andreturnedtotheirhomecagesuntilthenextinjection.ControlmiceforFasudilandY-27632receivessaline.
Rat[4]
MaleWistarKindArats(200-250g)areused.DMN(1g/mL)isdilutedtentimeswithsaline(finalconcentration1%)and10mg/kgperdayofDMNisinjectedintraperitoneally(i.p.)onthefirst3daysofeachweekfor4weeks.Y27632isgivenorallyonceperdayatadoseof30mg/kgfor4weeksstartingonthedayofthefirstinjectionofDMN.Thedoseof30mg/kgcorrectshypertensioninseveralratmodelswithouttoxicity.Twentyratsarerandomizedintofourexperimentalgroups(n=5ineachgroup)asfollows:(1)S-S(injectionofsalinei.p.andoraladministrationofsaline);(2)S-Y(injectionofsalinei.p.andoraladministrationofY27632);(3)DMN-S(DMNi.p.andoraladministrationofsaline);(4)DMN-Y(DMNi.p.andoraladministrationofY27632).Theratsareweighedeveryweek.Theyaresacrificedattheendofthefourthweekandtheliverisexcised.Inaddition,abloodsampleistakenimmediatelybeforetheratsaresacrificed.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].IshizakiT,etal.PharmacologicalpropertiesofY-27632,aspecificinhibitorofrho-associatedkinases.MolPharmacol.2000May;57(5):976-83.

    [2].XueZW,etal.Rho-associatedcoiledkinaseinhibitorY-27632promotesneuronal-likedifferentiationofadulthumanadiposetissue-derivedstemcells.ChinMedJ(Engl).2012Sep;125(18):3332-5.

    [3].InanS,etal.AntiepilepticeffectsoftwoRho-kinaseinhibitors,Y-27632andfasudil,inmice.BrJPharmacol.2008Sep;155(1):44-51.

    [4].TadaS,etal.AselectiveROCKinhibitor,Y27632,preventsdimethylnitrosamine-inducedhepaticfibrosisinrats.JHepatol.2001Apr;34(4):529-36.

MolecularWeight

320.26

Formula

C₁₄H₂₃Cl₂N₃O

CASNo.

129830-38-2

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥32mg/mL

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

Purity:98.53%