182200

βARK1 Inhibitor

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.

• Synonym(s): βARK1 Inhibitor, β-Adrenergic Receptor Kinase1 Inhibitor, GRK2 Inhibitor, Methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate
• Empirical Formula (Hill Notation): C₁₂H₉NO₆
• CAS Number: 24269-96-3
• Molecular Weight: 263.20
• MDL number: MFCD00099039
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 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
• SMILES string: [N+](=O)([O-])c1[o]c(cc1)\C=C\c2[o]c(cc2)C(=O)OC
• 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

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).

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)

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable