CAY10746 is an inhibitor of Rho-associated kinase I (ROCK-I) and ROCK-II (IC50s = 14 and 3 nM, respectively).1It is selective for ROCK-I and ROCK-II over PKA (IC50= >10,000 nM) and over 387 recombinant human protein kinases in a panel of 394 kinases (IC50s = >10,000 nM for all) but does inhibit LIM kinase 2 (LIMK2), Aurora A, Aurora B, cGMP-dependent protein kinase 1α (PKG1α), and PKG1β (IC50s = 46, 1,072, 1,239, 517, and 660 nM, respectively). CAY10746 (0.1-10 μM) inhibits phosphorylation of the ROCK target protein MYPT1 in SH-SY5Y cells. It also inhibits migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 1 μM. CAY10746 (1 μM) protects isolated mouse retinal neurons from apoptosis and oxidative stress induced by high glucose in anin vitromodel of diabetic retinopathy. It also promotes high glucose-induced vessel regression in mouse retinal explants.

2247240-76-0

C26H23N3O5

457.48

CAY10746

DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years