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
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About This Item
Empirical Formula (Hill Notation):
C12H9NO6
CAS Number:
Molecular Weight:
263.20
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
Quality Level
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
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)
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)
Storage Class
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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