Prices plus VAT plus shipping costs
Ready to ship today,
Delivery time appr. 5-8 days
- Order number: 7TMGRK56-IN
- Content: 5 mg
Compound 18 is a potent and selective inhibitor for GRK5 and GRK6.
CAS No.: 2677786-61-5
Molecular Weight: 438.91
Amount: 5 mg
Solubility: 1 mg/ml in DMSO or Methanol
Storage: - 20°C, Protected from light (in Solution: -80°C, 6 months; -20°C, 1 month; protected from light)
| IC50 (µM) | ||||
| GRK2 | GRK3 | GRK5 | GRK6 | |
| Cmpd 8h | 2.1 | 3.2 | >30 | >30 |
| Cmpd 18 | >30 | >30 | 11.2 | 8.5 |
| Cmpd 19 | >30 | >30 | 1.5 | 1,1 |
Figure 1. Inhibition of GRK-mediated β2 adrenergic receptor (β2) phosphorylation by GRK5/6 Inhibitor (Cmpd 18). HEK293 ΔGRK3/5/6 (GRK2) or ΔGRK2/5/6 (GRK3) or ΔGRK2/3/6 (GRK5) or ΔGRK2/3/5 (GRK6) stably expressing the β2 were preincubated with increasing concentrations of the GRK5/6 Inhibitor (Cmpd 18) (30 min, 37°C) prior to treatment with 10 µM isoproterenol (ISO) (30 min, 37°C). Receptor phosphorylation was assessed using the 7TM phosphorylation assay and data were normalized to 10 µM ISO without inhibitor.
Figure 2. Comparison of GRK5 inhibition of GRK-mediated β2 adrenergic receptor (β2) phosphorylation by GRK5/6 Inhibitor (Cmpd 18) or GRK5/6 Inhibitor 2 (Cmpd 19). HEK293 ΔGRK2/3/6 stably expressing the β2 were preincubated with increasing concentrations of the GRK5/6 Inhibitor (Cmpd 18) or GRK5/6 Inhibitor 2 (Cmpd 19) (30 min, 37°C) prior to treatment with 10 µM isoproterenol (ISO) (30 min, 37°C). Receptor phosphorylation was assessed using the 7TM phosphorylation assay and data were normalized to 10 µM ISO without inhibitor.
Figure 3. Comparison of GRK6 inhibition of GRK-mediated β2 adrenergic receptor (β2) phosphorylation by GRK2/3 Inhibitor (Cmpd 8h) or GRK5/6 Inhibitor 2 (Cmpd 19). HEK293 ΔGRK2/3/5 stably expressing the β2 were preincubated with increasing concentrations of the GRK5/6 Inhibitor (Cmpd 18) or GRK5/6 Inhibitor 2 (Cmpd 19) (30 min, 37°C) prior to treatment with 10 µM isoproterenol (ISO) (30 min, 37°C). Receptor phosphorylation was assessed using the 7TM phosphorylation assay and data were normalized to 10 µM ISO without inhibitor.
Figure 4. Chemical Structure of GRK5/6 Inhibitor (Cmpd 18).
Nina K Blum, Manuela C Kiefer, Angelika Decker, Laura Klement, Edda S F Matthees, Verena Weitzel, Falko Nagel, Babu Joseph, Julia Drube, David Uehling, Carsten Hoffmann, Stefan Schulz. Cell-based and isoform-selective G protein-coupled receptor kinase assays for comprehensive inhibitor evaluation Commun Biol 2026 Jan 16. doi: 10.1038/s42003-026-09568-0. PMID: 41545717
