Description General description A selective inhibitor of β-adrenergic receptor kinase 1 (βARK1) (IC50 = 126 µM). Displays no inhibitory activity against protein kinase A (PKA). Identified from a group of existing compounds (not previously demonstrated to inhibit βARK1) using a two-step rational drug design protocol that included molecular modeling and comparative docking studies. Represents the first inhibitor that distinguishes between βARK1 and PKA, an enzyme with a similar adenine binding pocket. May be useful in the study of mechanisms involved in congestive heart failure where elevated levels of βARK1 desensitize agonist-bound β2-adrenergic receptors. A selective inhibitor of βARK1 (β-Adrenergic Receptor Kinase 1) (IC50 = 126 µM). Has no inhibitory activity against protein kinase A (PKA). Packaging 5 mg in Plastic ampoule Biochem/physiol Actions Cell permeable: no Primary Target βARK1 (β-Adrenergic Receptor Kinase 1) Product does not compete with ATP. Reversible: no Target IC50: 126 µM against βARK1 (β-Adrenergic Receptor Kinase 1) Packaging Packaged under inert gas Warning Toxicity: Standard Handling (A) Reconstitution Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. Other Notes Iino, M., et al. 2002. J. Med. Chem.45, 2150.