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- Order number: 7TMGRKCOMBO-IN
- Content: 2 x 5 mg
5 mg GRK2/3 Inhibitor (Cmpd 8h) + 5 mg GRK5/6 Inhibitor (Cmpd 18) Combo Pack
GRK2/3 Inhibitor (Cmpd 8h)
Compound 8h is a potent and selective inhibitor of GRK2 and GRK3.
CAS No.: 2592436-21-8
Molecular Weight: 332.36
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)
GRK5/6 Inhibitor (Cmpd 18)
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. Chemical Structure of GRK2/3 Inhibitor (Cmpd 8h) and GRK5/6 Inhibitor (Cmpd 18).
Figure 2. Inhibition of GRK-mediated β2 adrenergic receptor (β2) phosphorylation by GRK2/3 Inhibitor (Cmpd 8h). 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 GRK2/3 Inhibitor (Cmpd 8h) (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. 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 GRK2/3 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 4. Comparison of GRK2 inhibition of GRK-mediated β2 adrenergic receptor (β2) phosphorylation by GRK2/3 Inhibitor (Cmpd 8h) or Compound 101. HEK293 ΔGRK3/5/6 stably expressing the β2 were preincubated with increasing concentrations of the GRK2/3 Inhibitor (Cmpd 8h) or Compund 101 (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.
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
