Merck, 182200-5MG, βARK1 Inhibitor

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).
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
Preparation Note
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)