371962

H-89, Dihydrochloride

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

• Synonym(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
• Empirical Formula (Hill Notation): C₂₀H₂₀BrN₃O₂S
• Molecular Weight: 446.36
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥99% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

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.

Biochem/physiol Actions

Cell permeable: no

Primary Target
PKA

Product does not compete with ATP.

Reversible: no

Target K_i: 48 nM against protein kinase A

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

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).

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 1
• Flash Point(F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Flash Point(C): 87 °C - closed cup - (Dimethylsulfoxide)