Table 1.
In Vitro Potency of Rho-Associated Protein Kinase Inhibitors (nM)
| Compound | ROCK1 Ki | ROCK2 Ki | PKA Ki | PKCT Ki | MRCKA Ki | CAM2A Ki | PTM IC50 | HTM IC50 |
|---|---|---|---|---|---|---|---|---|
| Netarsudil | 1 | 1 | 5 | 92 | 129 | 5,312 | 79 | 16 |
| Netarsudil-M1 | 0.2 | 0.2 | 1 | 27 | 7 | 13,689 | 22 | 3 |
| AR-12286 | 2 | 2 | 69 | 9,322 | 28 | 5,855 | 924 | 818 |
| Y27632 | 22 | 41 | 21,006 | 413 | 485 | 16,863 | 9,970 | 1,738 |
| Fasudil | 76 | 47 | 216 | 3,162 | 5,983 | 3,162 | 10,060 | 3,942 |
Values represent the average of ≥3 replicate experiments.
CAM2A, calcium/calmodulin-dependent protein kinase 2A; HTM, human trabecular meshwork; IC50, half maximal inhibitory concentration; Ki, inhibition constant; MRCKA, myotonic dystrophy kinase-related CDC42-binding kinase A; PKA, protein kinase A; PKCT, protein kinase C, theta; PTM, porcine trabecular meshwork; ROCK1, Rho-associated protein kinase 1; ROCK2, Rho-associated protein kinase 2.