371962

H-89, Dihydrochloride

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

• 別名: 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
• 実験式（ヒル表記法）: C₂₀H₂₀BrN₃O₂S
• 分子量: 446.36
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥99% (HPLC)
• フォーム: liquid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 輸送温度: wet ice
• 保管温度: −20°C

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: no

Primary Target
PKA

Product does not compete with ATP.

Reversible: no

Target K_i: 48 nM against protein kinase A

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

物理的形状

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

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 10 - Combustible liquids
• WGK: WGK 1
• 引火点(°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• 引火点(℃): 87 °C - closed cup - (Dimethylsulfoxide)