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文件名称:Ruboxistaurin-Standard-LY333531-Standard-生命科学试剂-MCE.pdf
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文档摘要

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Inhibitors?ScreeningLibraries?Proteins

www.MedChemE

Ruboxistaurin(Standard)

Cat.No.:HY-10195R

CASNo.:169939-94-0

Synonyms:LY333531(Standard)

分?式:C??H??N?O?

分?量:468.55

作?靶点:PKC

作?通路:Epigenetics;TGF-beta/Smad

储存?式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

?物活性Ruboxistaurin(Standard)是Ruboxistaurin的分析标准品。本产品?于研究及分析应?。Ruboxistaurin

(LY333531)是?种具有?服活性,选择性PKCbeta抑制剂(Ki=2nM),Ruboxistaurin表现出ATP依赖的竞争

性抑制PKCbetaI,其IC50为4.7nM。Ruboxistaurin对PKCbetaII的IC50为5.9nM[1][2]。

IC50TargetIC50:4.7nMand5.9nM(PKCβ),Ki:2nM(PKCβ)[1]

REFERENCES

[1].JirousekMR,etal.(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H,13H-dibenzo[e,k]pyrrolo[3,4-

h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione(LY333531)andrelatedanalogues:isozymeselectiveinhibitorsofproteinkinaseC

beta.JMedChem.1996;39(14):2664-2671.

[2].Ruboxistaurin:LY333531.DrugsRD.2007;8(3):193-199.

[3].KuntT,etal.Thebeta-specificproteinkinaseCinhibitorruboxist