?ARK1 INHIBITOR 1PC X 5MG

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

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

Molecular Weight: 263.20. Empirical Formula: C₁₂H₉NO₆. Quality Level: 100. Assay: ≥. 97% (HPLC). form: solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: yellow to orange. solubility: DMSO: 5 . mg/mL, methanol: soluble. shipped in: ambient. storage temp.: −. 20°C. InChI: 1S/C12H9NO6/c1-17-12(14)10-6-4-8(18-10)2-3-9-5-7-11(19-9)13(15)16/h2-7H,1H3/b3-2+. InChI key: YDJPHSNZGRVPCK-NSCUHMNNSA-N. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.