Pular para o conteúdo
Merck
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Documentos Principais

371962

Sigma-Aldrich

H-89, Dihydrochloride

InSolution 10 mM, ≥99%, reversible ATP-competitive inhibitor of protein kinase A

Sinônimo(s):

InSolution H-89, Dihydrochloride, N-[2-(( p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor III, N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl, PKA Inhibitor III

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About This Item

Fórmula empírica (Notação de Hill):
C20H20BrN3O2S
Peso molecular:
446.36
Código UNSPSC:
12352200
NACRES:
NA.77

Nível de qualidade

Ensaio

≥99% (HPLC)

Formulário

liquid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

Condições de expedição

wet ice

temperatura de armazenamento

−20°C

Descrição geral

A solution of H-89, Dihydrochloride (Cat. No. 371963) in anhydrous DMSO. H-89 is a cell-permeable selective and potent inhibitor of protein kinase A (Ki = 48 nM). Inhibits other kinases at several fold higher concentrations: myosin light chain kinase (Ki = 28.3 µM), Ca2+/calmodulin-dependent protein kinase II (Ki = 29.7 µM), protein kinase C (Ki = 31.7 µM), casein kinase I (Ki = 38.3 µM), and Rho Kinase II (IC50 = 270 nM). May be used to discriminate between the effects of PKA and cAMP-regulated guanine-nucleotide-exchange factors (GEFs), such as GEFI or Epac (exchange protein directly activated by cAMP) and GEFII. Reported to induce neurite formation in NG 108-15 cells (~1 µM) by blocking the action of Rho kinase II.

Ações bioquímicas/fisiológicas

Cell permeable: no
Primary Target
PKA
Product does not compete with ATP.
Reversible: no
Target Ki: 48 nM against protein kinase A

Embalagem

Packaged under inert gas

Advertência

Toxicity: Irritant (B)

forma física

A 10 mM (1 mg/193 µl) solution of H-89, 2HCl (Cat. No. 371963) in DMSO.

Reconstituição

Following initial thaw, aliquot and freeze (-20°C).

Outras notas

Leemhuis, J., et al. 2002. J. Pharmacol. Exp. Ther.300, 1000.
Davies, S.P. et al. 2000. Biochem. J.351, 95.
de Rooij, J., et al. 1998. Nature.396, 474.
Kawasaki, H., et al. 1998. Science.282, 2275.
Findik, D., et al. 1995. J. Cell. Biochem.57, 12.
Hidaka, H., and Kobayashi, R. 1992. Annu. Rev. Pharmacol. Toxicol.32, 377.
Geilen, C.C., et al. 1992. FEBS Lett.309, 381.
Chijiwa, T., et al. 1990. J. Biol. Chem.265, 5267.
Combest, W.L., et al. 1988. J. Neurochem.51, 1581.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Código de classe de armazenamento

10 - Combustible liquids

Classe de risco de água (WGK)

WGK 1

Ponto de fulgor (°F)

188.6 °F - closed cup - (Dimethylsulfoxide)

Ponto de fulgor (°C)

87 °C - closed cup - (Dimethylsulfoxide)


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