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Beschreibung

Category: Inhibitors, Protein Kinase Inhibitors and Activators, Pharmaceuticals, Intermediates and Fine Chemicals /// Appearance: White to Off-White Solid /// Application Notes: ROCK Inhibitor. A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK: Ki=1.6nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki=630nM for PKA 9.27 mMfor PKC, and 10.1mM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50=2.5nM) in NT-2 cells. /// References: Ikenoya, M., et al.: J. Neurochem., 81, 9 (2002), Sasaki, Y., et al.: Pharmacol. Ther., 93, 225 (2002)