CAY10746

CAY10746 is an inhibitor of Rho-associated kinase I (ROCK1) and ROCK2 (IC50s = 14 and 3 nM, respectively). It is selective for ROCK1 and ROCK2 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 1alpha (PKG1alpha), and PKG1beta (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 an in vitro model of diabetic retinopathy. It also promotes high glucose-induced vessel regression in mouse retinal explants.Formal Name: 4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]-benzamide. CAS Number: 2247240-76-0. Molecular Formula: C26H23N3O5. Formula Weight: 457.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. lambdamax: 239, 247, 305 nm. SMILES: CN(C)C1=CC=C(C(NC2=CC=CC(NC(COC3=CC(OC=CC4=O)=C4C=C3)=O)=C2)=O)C=C1. InChi Code: InChI=1S/C26H23N3O5/c1-29(2)20-8-6-17(7-9-20)26(32)28-19-5-3-4-18(14-19)27-25(31)16-34-21-10-11-22-23(30)12-13-33-24(22)15-21/h3-15H,16H2,1-2H3,(H,27,31)(H,28,32). InChi Key: WVGDUQVQWLHVEA-UHFFFAOYSA-N.