371962

H-89, Dihydrochloride

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

• Synonyme(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
• Formule empirique (notation de Hill): C₂₀H₂₀BrN₃O₂S
• Poids moléculaire : 446.36
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Essai: ≥99% (HPLC)
• Forme: liquid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Conditions d'expédition: wet ice
• Température de stockage: −20°C

Description

Description générale

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 (K_i = 48 nM). Inhibits other kinases at several fold higher concentrations: myosin light chain kinase (K_i = 28.3 µM), Ca²⁺/calmodulin-dependent protein kinase II (K_i = 29.7 µM), protein kinase C (K_i = 31.7 µM), casein kinase I (K_i = 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.

Actions biochimiques/physiologiques

Cell permeable: no

Primary Target
PKA

Product does not compete with ATP.

Reversible: no

Target K_i: 48 nM against protein kinase A

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Irritant (B)

Forme physique

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

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 10 - Combustible liquids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Point d'éclair (°C): 87 °C - closed cup - (Dimethylsulfoxide)