N-[2-((p-Bromocinnamyl)amino)ethyl]-5-isoquinolinesulfonamide, 2HCl Off-white solid. PACKAGED UNDER INERT GAS. A cell-permeable, selective, and potent inhibitor of protein kinase A (Ki = 48 nM). Inhibits other kinases only at much higher concentrations: CaM kinase II (Ki = 29.7 µM), casein kinase I (Ki = 38.3 µM), myosin light chain kinase (Ki = 28.3 µM), protein kinase C (Ki = 31.7 µM), and ROCK-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, GEFII, or Epac (exchange protein directly activated by cAMP). Enhances radiation-induced apoptosis in the human cell line BM 13674. Purity: ≥99% by HPLC. CAS 127243-85-0. Ref.: Leemhuis, J., et al. 2002. J. Pharmacol. Exp. Ther. 300, 1000. Davies, S.P., et al. 2000. Biochem. J. 351, 95. Kawasaki, H., et al. 1998. Science 282, 2275. de Rooij, J., et al. 1998. Nature 396, 474. Findik, D., et al. 1995. J. Cell. Biochem. 57, 12. Geilen, C.C. 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. Not available for sale in Japan. |