The βARK1 Inhibitor, also referenced under CAS 24269-96-3, controls the biological activity of βARK1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
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).
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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