Effects of kinase inhibitors on GRK2 and GRK5 activity
| Inhibitor | ||||||
|---|---|---|---|---|---|---|
| H-89 | H-85 | H-7 | KT5720 | ST | BisIX | |
| GRK2 | >1001-a | >>100 | >1000 | >>10 | >10 | 40 ± 5 |
| GRK5 | 40 ± 5 | >100 | >1000 | 10 ± 1 | 4 ± 1 | 12 ± 2 |
↵1-a 10−7 to 10−3 M final concentrations of inhibitors were tested for their ability to inhibit GRK2- or GRK5-mediated phosphorylation of rhodopsin as described inExperimental Procedures. Values reported are mean ± S.D. (micromolar concentrations) in which 50% inhibition was determined.
>, 20 to 40% inhibition observed at this (maximal) concentration.
>>, <20% inhibition observed.