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371962

Sigma-Aldrich

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

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About This Item

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

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

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 (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.

Biochem/physiol Actions

Cell permeable: no
Primary Target
PKA
Product does not compete with ATP.
Reversible: no
Target Ki: 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

wgk_germany

WGK 1

flash_point_f

188.6 °F

flash_point_c

87 °C

Certificates of Analysis (COA)

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