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.

• Synonyme(s) : βARK1 Inhibitor, β-Adrenergic Receptor Kinase1 Inhibitor, GRK2 Inhibitor, Methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate
• Formule empirique (notation de Hill): C₁₂H₉NO₆
• Numéro CAS: 24269-96-3
• Poids moléculaire : 263.20
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥97% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow to orange
• Solubilité: DMSO: 5 mg/mL; methanol: soluble
• Conditions d'expédition: ambient
• Température de stockage: −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+
• Clé InChI: YDJPHSNZGRVPCK-NSCUHMNNSA-N

Description

Description générale

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).

Actions biochimiques/physiologiques

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)

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable