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Merck
CN
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文件

371962

Sigma-Aldrich

H-89, Dihydrochloride

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

别名:

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

经验公式(希尔记法):
C20H20BrN3O2S
分子量:
446.36
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

检测方案

≥99% (HPLC)

形式

liquid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

运输

wet ice

储存温度

−20°C

一般描述

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.

生化/生理作用

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

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

外形

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

重悬

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

其他说明

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.

法律信息

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

WGK

WGK 1

闪点(°F)

188.6 °F

闪点(°C)

87 °C


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