βARK1 Inhibitor

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).

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)

Packaged under inert gas

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Iino, M., et al. 2002. J. Med. Chem.45, 2150.

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

Toxicity: Standard Handling (A)