Medchemexpress/H-89 dihydrochloride(Synonyms: Protein kinase inhibitor H-89 dihydrochloride)/HY-15979A/100mg,MCE,,MCE,MedChemExp,MedChemExpress,+,,Array.Array.Array蚂蚁淘厂家直采.

产品名称：Medchemexpress/H-89 dihydrochloride(Synonyms: Protein kinase inhibitor H-89 dihydrochloride)/HY-15979A/100mg

产品编号：HY-15979A-10mM*1mLinDMSO

市场价：¥1480.00

场地：美国(厂家直采)

产品分类：生化试剂>生物分子>小分子>

联系QQ：1570468124

电话号码：4000-520-616

邮箱： info@ebiomall.com

美元价：$74.00

品牌： MCE

公司：Medchemexpress

公司分类：

商品介绍

H-89(dihydrochloride)isapotentinhibitorofcyclicAMP-dependentproteinkinase(proteinkinaseA)withIC₅₀of48nMandhasweakinhibitiononPKG,PKC,CaseinKinase,andotherskinases.

Description	H-89(dihydrochloride)isapotentinhibitorofcyclicAMP-dependentproteinkinase(proteinkinaseA)withIC₅₀of48nMandhasweakinhibitiononPKG,PKC,CaseinKinase,andotherskinases.
IC₅₀&Target	IC50:48nM(proteinkinaseA)
InVitro	H-89inhibitsproteinkinaseA,incompetitivefashionagainstATP.H-89causesadose-dependentinhibitionoftheforskolin-inducedproteinphosphorylation,withnodecreaseinintracellularcyclicAMPlevelsinPC12Dcells.H-89significantlyinhibitstheforskolin-inducedneuriteoutgrowthfromPC12Dcells.H-89(30μM)inhibitssignificantlycAMP-dependenthistoneIIbphosphorylationactivityinPC12Dcelllysates^[1].H-89(1-2μM)significantlyslowsthereprimingrateinratskinnedfibres,mostlikelyduetoitdeleteriouslyaffectingtheT-systempotential.H-89(10-100μM)inhibitsnetCa²⁺uptakebytheSRandaffectestheCa²⁺-sensitivityofthecontractileapparatusinratskinnedfibres^[2].
InVivo	H-89(0.2mg/100g,i.p.)significantlyincreasesseizurelatencyandthresholdinPTZ-treatedanimals.H-89(0.05,0.2mg/100g,i.p.)preventstheepileptogenicactivityofbucladesine(300nM)withsignificantincreaseofseizurelatencyandseizurethreshold^[3].
References	[1].ChijiwaT,etal.Inhibitionofforskolin-inducedneuriteoutgrowthandproteinphosphorylationbyanewlysynthesizedselectiveinhibitorofcyclicAMP-dependentproteinkinase,N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide(H-89),ofPC12D [2].BlazevR,etal.EffectsofthePKAinhibitorH-89onexcitation-contractioncouplinginskinnedandintactskeletalmusclefibres.JMuscleResCellMotil.2001;22(3):277-86. [3].Hosseini-ZareMS,etal.EffectsofpentoxifyllineandH-89onepileptogenicactivityofbucladesineinpentylenetetrazol-treatedmice.EurJPharmacol.2011Nov30;670(2-3):464-70.

PreparingStockSolutions

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	1.9257mL	9.6287mL	19.2574mL
5mM	0.3851mL	1.9257mL	3.8515mL
10mM	0.1926mL	0.9629mL	1.9257mL

Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.

KinaseAssay
^[1]

Kinaseactivitiesareassayedat30°Cfor2-5minbymeasuringthetransferof³²Pfrom[γ-³²P]ATPtosubstrates.Thereactionisterminatedbyadding1mLof20%trichloroaceticacid,followingtheadditionof100μgofbovineserumalbuminasacarrierprotein.Thesampleiscentrifugedat3000rpmfor10min,thepelletisresUSPendedin5%trichloroaceticacidsolution,thefinalpelletisdissolvedin1mLof1NNaOHandtherADIoactivityismeasuredinaliquidscintillationcounter.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

CellAssay
^[1]

After48hinculture,PCl2Dcellsareculturedintestmediumcontaining30μMH-89for1handthenexposedtofreshmediumthatcontainedboth10μMforskolinand30μMH-89.Cellsarescrapedoffwitharubberpolicemanandsonicatedinthepresenceof0.5mLof6%trichloroaceticacid.Toextracttrichloroaceticacid,2mLofpetroleumetherisadded,thepreparationmixedandcentrifugedat3000rpmfor10min.Afteraspirationoftheupperlayer,theresiduesamplesolutionisusedfordetermination.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
^[1]

H-89isdissolvedinDMSOanddistilledwater(10%).

Malealbinomiceweighing20-25gareobtained.Pentoxifylline(25,50,100mg/kg),bucladesine(50,100,300nM/mouse)andH-89(0.05,0.1,0.2mg/100g)areadministeredintraperitoneally(i.p.)30minbeforeintravenous(i.v.)infusionofPTZ.Incombinationgroups,thefirstandsecondcomponentsareinjected45and30minbeforePTZinfusion.Inallgroups,therespectivecontrolanimalsreceiveanappropriatevolumeofvehicle.Forthei.v.infusion,theneedleisinsertedintothelateraltailvein,fixedtothetailveinbyanarrowpieceofadhesivetape,andtheanimalisallowedtomovefreely.PTZsolutionisinfusedataconcentrationrateof1mL/min.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

[1].ChijiwaT,etal.Inhibitionofforskolin-inducedneuriteoutgrowthandproteinphosphorylationbyanewlysynthesizedselectiveinhibitorofcyclicAMP-dependentproteinkinase,N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide(H-89),ofPC12D
[2].BlazevR,etal.EffectsofthePKAinhibitorH-89onexcitation-contractioncouplinginskinnedandintactskeletalmusclefibres.JMuscleResCellMotil.2001;22(3):277-86.
[3].Hosseini-ZareMS,etal.EffectsofpentoxifyllineandH-89onepileptogenicactivityofbucladesineinpentylenetetrazol-treatedmice.EurJPharmacol.2011Nov30;670(2-3):464-70.

MolecularWeight

519.28

Formula

C₂₀H₂₂BrCl₂N₃O₂S

CASNo.

130964-39-5

Storage

Powder	-20°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥50mg/mL

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

Purity:98.94%

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